CN1322851C - Tripterygium total terpenoids drop pill and its preparation method - Google Patents
Tripterygium total terpenoids drop pill and its preparation method Download PDFInfo
- Publication number
- CN1322851C CN1322851C CNB2004100971577A CN200410097157A CN1322851C CN 1322851 C CN1322851 C CN 1322851C CN B2004100971577 A CNB2004100971577 A CN B2004100971577A CN 200410097157 A CN200410097157 A CN 200410097157A CN 1322851 C CN1322851 C CN 1322851C
- Authority
- CN
- China
- Prior art keywords
- drop pill
- medicine
- polyethylene glycol
- dry powder
- radix tripterygii
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 239000006187 pill Substances 0.000 title claims abstract description 59
- 241000545405 Tripterygium Species 0.000 title claims abstract description 38
- 150000003505 terpenes Chemical class 0.000 title claims abstract description 38
- 238000002360 preparation method Methods 0.000 title abstract description 39
- 239000000203 mixture Substances 0.000 claims abstract description 16
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 11
- 239000002202 Polyethylene glycol Substances 0.000 claims description 82
- 229920001223 polyethylene glycol Polymers 0.000 claims description 82
- 239000000758 substrate Substances 0.000 claims description 40
- 229920002472 Starch Polymers 0.000 claims description 35
- 239000008107 starch Substances 0.000 claims description 35
- 235000019698 starch Nutrition 0.000 claims description 35
- -1 polyoxyethylene stearate Polymers 0.000 claims description 33
- 150000002148 esters Chemical class 0.000 claims description 31
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 30
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 30
- 239000011734 sodium Substances 0.000 claims description 30
- 229910052708 sodium Inorganic materials 0.000 claims description 30
- 239000000284 extract Substances 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- 238000010438 heat treatment Methods 0.000 claims description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 5
- 150000002596 lactones Chemical class 0.000 claims description 5
- 239000000839 emulsion Substances 0.000 claims description 4
- 239000000725 suspension Substances 0.000 claims description 4
- 238000005303 weighing Methods 0.000 claims description 4
- 239000002994 raw material Substances 0.000 claims description 3
- 238000003756 stirring Methods 0.000 claims description 3
- 238000001816 cooling Methods 0.000 claims description 2
- 230000006837 decompression Effects 0.000 claims description 2
- 229940057995 liquid paraffin Drugs 0.000 claims description 2
- 239000003208 petroleum Substances 0.000 claims description 2
- 238000004064 recycling Methods 0.000 claims description 2
- 238000010992 reflux Methods 0.000 claims description 2
- 229920002545 silicone oil Polymers 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 235000015112 vegetable and seed oil Nutrition 0.000 claims description 2
- 239000008158 vegetable oil Substances 0.000 claims description 2
- 235000019441 ethanol Nutrition 0.000 claims 3
- 238000007493 shaping process Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 101
- 230000000694 effects Effects 0.000 abstract description 15
- 208000002193 Pain Diseases 0.000 abstract description 5
- 208000025747 Rheumatic disease Diseases 0.000 abstract 2
- 230000004913 activation Effects 0.000 abstract 1
- 230000007547 defect Effects 0.000 abstract 1
- 230000008030 elimination Effects 0.000 abstract 1
- 238000003379 elimination reaction Methods 0.000 abstract 1
- 210000003205 muscle Anatomy 0.000 abstract 1
- 231100000614 poison Toxicity 0.000 abstract 1
- 230000007096 poisonous effect Effects 0.000 abstract 1
- 210000002435 tendon Anatomy 0.000 abstract 1
- 239000000843 powder Substances 0.000 description 72
- 239000011159 matrix material Substances 0.000 description 52
- 239000000470 constituent Substances 0.000 description 38
- 229920000858 Cyclodextrin Polymers 0.000 description 28
- 239000001116 FEMA 4028 Substances 0.000 description 28
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 28
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 28
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 28
- 229960004853 betadex Drugs 0.000 description 28
- 229920001983 poloxamer Polymers 0.000 description 28
- 229960000502 poloxamer Drugs 0.000 description 28
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 16
- 238000012360 testing method Methods 0.000 description 16
- 229940079593 drug Drugs 0.000 description 14
- 238000002474 experimental method Methods 0.000 description 13
- 239000004615 ingredient Substances 0.000 description 13
- 239000008194 pharmaceutical composition Substances 0.000 description 13
- 239000000969 carrier Substances 0.000 description 9
- 238000005516 engineering process Methods 0.000 description 9
- 238000009472 formulation Methods 0.000 description 9
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 9
- 239000001828 Gelatine Substances 0.000 description 8
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 8
- 239000004141 Sodium laurylsulphate Substances 0.000 description 8
- 235000021355 Stearic acid Nutrition 0.000 description 8
- 229920000159 gelatin Polymers 0.000 description 8
- 235000019322 gelatine Nutrition 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 8
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 8
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 8
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 description 8
- 239000008117 stearic acid Substances 0.000 description 8
- 201000010099 disease Diseases 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 239000004353 Polyethylene glycol 8000 Substances 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 6
- 208000006820 Arthralgia Diseases 0.000 description 5
- 206010063659 Aversion Diseases 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 210000003414 extremity Anatomy 0.000 description 5
- 230000009545 invasion Effects 0.000 description 5
- 210000003127 knee Anatomy 0.000 description 5
- 206010039073 rheumatoid arthritis Diseases 0.000 description 5
- 235000015424 sodium Nutrition 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 230000008961 swelling Effects 0.000 description 4
- 229920001353 Dextrin Polymers 0.000 description 3
- 239000004375 Dextrin Substances 0.000 description 3
- 235000019425 dextrin Nutrition 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 239000000428 dust Substances 0.000 description 3
- 238000010579 first pass effect Methods 0.000 description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000002131 composite material Substances 0.000 description 2
- 238000009833 condensation Methods 0.000 description 2
- 230000005494 condensation Effects 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 230000000857 drug effect Effects 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 235000015250 liver sausages Nutrition 0.000 description 2
- 239000000741 silica gel Substances 0.000 description 2
- 229910002027 silica gel Inorganic materials 0.000 description 2
- 239000007962 solid dispersion Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 238000012795 verification Methods 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- 206010070840 Gastrointestinal tract irritation Diseases 0.000 description 1
- 102000000340 Glucosyltransferases Human genes 0.000 description 1
- 108010055629 Glucosyltransferases Proteins 0.000 description 1
- 241001640034 Heteropterys Species 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 229920002701 Polyoxyl 40 Stearate Polymers 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 239000007941 film coated tablet Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 235000001727 glucose Nutrition 0.000 description 1
- 125000002791 glucosyl group Chemical class C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 238000009413 insulation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 230000029052 metamorphosis Effects 0.000 description 1
- 239000004531 microgranule Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- FDRCDNZGSXJAFP-UHFFFAOYSA-M sodium chloroacetate Chemical compound [Na+].[O-]C(=O)CCl FDRCDNZGSXJAFP-UHFFFAOYSA-M 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a medicinal composition for treating rheumatic diseases, which has the action of wind elimination, humidity removal, muscle and tendon relaxation, channel and collateral activation, detumescence and pain relief. The aim of the medicinal composition is to overcome the defects of the existing oral medical agent used for treating rheumatic diseases and provide a tripterygium total terpenoids drop pill as the oral agent medical composition, which has the advantages of high biological utilization rate, quick medicine release, quick medicine effect, small poisonous and side effect, high medicine content, small and accurate taking dosage, convenient taking, low price and outing portability. The tripterygium total terpenoids drop pill referred in the present invention is prepared by combining a preparation process of drop pills on the basis of a preparation process of tripterygium total terpenoids tablets with a traditional Chinese medicine set prescription.
Description
Technical field
The present invention relates to a kind of expelling wind and removing dampness that has, the Shujin Lip river of living, the reducing swelling and alleviating pain effect is used for the treatment of the cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis is seen the pharmaceutical composition that above-mentioned symptom person is arranged, and particularly based on Chinese traditional patent formulation tripterygium total terpenoids sheet, changes a social system a kind of drug composition oral dropping pill formulation that forms through dosage form.
Background technology
The tripterygium total terpenoids sheet that is prepared from according to the prescription that provides among the national drug standards WS-10715 (ZD-0715)-2002 and preparation method, it is a kind of expelling wind and removing dampness that has, Shujin Lip river alive, the reducing swelling and alleviating pain effect is used for the treatment of the cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis sees above-mentioned symptom person's oral Chinese medicine preparation, through clinical verification, steady quality, determined curative effect is clinical and family is used for the treatment of the common drug preparation of above disease.
Below be the contained partial content of this drug standard:
Prescription: Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol) 20mg, starch 75g, dextrin 75g, sucrose 4g, micropowder silica gel 0.75g;
Method for making: get Radix Tripterygii Wilfordii extract, behind dextrin, starch, the abundant mixing of micropowder silica gel, add 40% syrup, make granule, drying, tabletting, the bag film-coat, promptly.
Be explained as follows for this product in the appended description:
Nomenclature of drug: tripterygium total terpenoids sheet;
Main component: Radix Tripterygii Wilfordii extract;
Character: this product is a Film coated tablets, removes film-coat and shows brown;
Function cures mainly: expelling wind and removing dampness, Shujin Lip river alive, reducing swelling and alleviating pain.Be used for cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis is seen above-mentioned symptom person;
Usage and dosage: oral, one time 2,3 times on the one.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, conventional peroral dosage form as tablet, capsule etc., because the technology of granulation is arranged, therefore can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
Summary of the invention
Purpose of the present invention is to replenish the existing cold-damp invasion and attack that are used for the treatment of, the arthralgia that obstruction of collaterals by blood stasis causes, and joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; The deficiency of rheumatoid arthritis sees above-mentioned symptom person's oral drug preparation, a kind of bioavailability height is provided, release fast, quick produce effects, toxic and side effects is littler, and medicament contg height, taking dose is little, and taking dose is accurate, taking convenience, cheap, and be convenient to the drug composition oral preparation tripterygium total terpenoids drop pill of going out to carry.
Tripterygium total terpenoids drop pill involved in the present invention determines that through a large amount of experiment sievings based on the preparation technology of Chinese traditional patent formulation tripterygium total terpenoids sheet, process is adjusted part technology, and cooperates drop pill preparation technology to be prepared from.Be prepared by the following technical solutions, can obtain tripterygium total terpenoids drop pill involved in the present invention:
[preparation method]
1. be unit with g or kg, calculate, get 1 part of Radix Tripterygii Wilfordii extract according to weight, standby;
2. substrate---Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), one or more the mixture in pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning---with g or kg is unit, Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol): substrate=1: 1～1: 9;
4. according to the given ratio of prescription, accurately take by weighing medicine dry powder and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing medicine dry powder and substrate and/or emulsion and/or suspension;
5. adopt homemade or general drop pill machine (as the TZDW-1 type drop pill machine of Changzheng Tianmin High Science ﹠ Technology Co., Ltd., Beijing's production), and the temperature control system of adjustment drop pill machine, make the water dropper temperature heating of drop pill machine and remain on (50～90) ℃, the temperature cooling of condensing agent also remains on (40～-5) ℃;
6. treating that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively is in above the 2nd step during desired state of temperature, to contain in the fused solution and/or emulsion and/or suspension of medicine dry powder and substrate, under the temperature conditions close, make evenly through fully stirring with the water dropper temperature, insulation, place in the water dropper jar of drop pill machine, splash in the condensing agent by water dropper;
Condensing agent can be any one in liquid paraffin, methyl-silicone oil, the vegetable oil;
7. will shrink the drop pill taking-up of molding by the outlet of drop pill machine, remove the surface condensation agent, be drying to obtain.
[appendix: a kind of preparation method of Radix Tripterygii Wilfordii extract]
Get the Radix Tripterygii Wilfordii root and rhizome, be cut into the thick decoction pieces of 3～5mm, with 85% ethanol (5,4,4 times of amounts) reflux, extract, 3 times, each 4 hours, the extracting solution decompression recycling ethanol is to thick paste shape (relative density 1.25～1.30,60 ℃), dry below 60 ℃, dry extract is pulverized, and takes off ester, removal of solvent under reduced pressure with No. 90 petroleum ether, dry below 60 ℃, promptly.
Given here is according to the preparation method of a kind of Chinese medicine dry powder comparatively commonly used, its processing step adjustment is formed again.Similarly method is a lot, is not limited to this a kind of method during actual enforcement.
Beneficial effect
The tripterygium total terpenoids sheet that is prepared from according to the prescription that provides among the national drug standards WS-10715 (ZD-0715)-2002 and preparation method, it is a kind of expelling wind and removing dampness that has, Shujin Lip river alive, the reducing swelling and alleviating pain effect is used for the treatment of the cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis sees above-mentioned symptom person's oral Chinese medicine preparation, through clinical verification, steady quality, determined curative effect is clinical and family is used for the treatment of the common drug preparation of above disease.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, conventional peroral dosage form as tablet, capsule etc., because the technology of granulation is arranged, therefore can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
Tripterygium total terpenoids drop pill involved in the present invention is compared with the tripterygium total terpenoids sheet has following beneficial effect:
1. tripterygium total terpenoids drop pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the dry powder that contains the Radix Tripterygii Wilfordii extract active component, make medicine be molecule, colloid or microcrystalline state and be scattered in the substrate, the total surface area of medicine increases; and substrate is hydrophilic; medicine is had wetting action, can make that medicine is rapidly molten to loose into microgranule or solution, thereby make the dissolving of medicine and absorb and accelerate; thereby improved bioavailability, brought into play efficient, quick-acting effects etc.
Compare with the administering mode of tripterygium total terpenoids sheet, exist essential distinction.Utilize the drop pill of solid dispersion technology preparation, can adopt oral and sublingual administration, effective ingredient is fully contacted with mucomembranous surface, absorb, directly enter blood circulation by mucomembranous epithelial cell.Because active constituents of medicine directly enters blood circulation without gastrointestinal tract and liver, avoided first pass effect effectively, also avoided gastrointestinal irritation, thereby thereby it is rapid to make that tripterygium total terpenoids drop pill involved in the present invention has an onset, the bioavailability height, characteristics such as side effect is little, and medication is convenient.
2. tripterygium total terpenoids drop pill involved in the present invention contacts promptly with saliva and to dissolve rapidly, and is absorbed by oral mucosa, and is not only rapid-action, and the influence of not taken food, and promptly all can containing take after meal ante cibum.
3. tripterygium total terpenoids drop pill involved in the present invention mixes the dry powder that contains active constituents of medicine mutually with molten matrix, splashes in the not miscible condensed fluid and makes.Therefore, the stability of drug height, not facile hydrolysis, oxidation, and the operation be under liquid state, to carry out, no dust pollution is not subject to the influence of crystal formation, thereby has guaranteed the quality of medicine, has increased stability.
In sum, make tripterygium total terpenoids drop pill involved in the present invention have the advantage of triple effect (quick-acting, efficient, long-acting), three little (taking dose is little, toxicity is little, side effect little), five convenience (convenient for production, store convenience, convenient transportation, easy to carry, easy to use).
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of tripterygium total terpenoids drop pill of the present invention.
First group: the test of single-matrix
1. the ratio that provides according to [preparation method] 1 takes by weighing the raw material of Chinese medicine of some, and it is standby to make the dry powder that contains the Radix Tripterygii Wilfordii extract active component earlier according to [appendix: a kind of preparation method of Radix Tripterygii Wilfordii extract] joint again;
2. substrate: Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning---with g or kg is unit, Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol): substrate=1: 1～1: 9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the tripterygium total terpenoids drop pill of various different sizes.
[result of the test]
Test 1: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 1 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, according to 1: 1 ratio, the dry powder that will contain active constituents of medicine respectively with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 3 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, according to 1: 3 ratio, the dry powder that will contain active constituents of medicine respectively with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 9 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, according to 1: 9 ratio, the dry powder that will contain active constituents of medicine respectively with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. the ratio that provides according to [preparation method] 1 takes by weighing the raw material of Chinese medicine of some, and it is standby to make the dry powder that contains the Radix Tripterygii Wilfordii extract active component earlier according to [appendix: a kind of preparation method of Chinese medicine dry powder] joint again;
2. substrate:
2.1 Polyethylene Glycol---English name Macrogol,
2.2 polyoxyethylene stearate 40 esters---English name Polyoxyl (40) Stearate,
Molecular formula is with C
17H
35COO (CH
2CH
2O)
nH represents that n is about 40,
2.3 poloxamer---English name Poloxamer, polyoxyethylene poly-oxygen propylene aether,
Molecular formula HO (C
2H
4O)
a(C
3H
6O)
b(C
2H
4O)
cH,
The sodium salt of the starch carboxymethyl ester that 2.4 carboxymethyl starch sodium---English name Carboxymethylstach Sodium, starch generates with the monoxone effect under alkali condition,
2.5 betacyclodextrin---English name Betacyclodextrin, molecular formula C
6H
10O
5, this product is that ring dextrin glucosyl transferase acts on 7 glucoses that starch generates with α-1, the bonded cyclic oligosaccharide of 4-glycosidic bond;
3. (with g or kg is unit to proportioning, by weight)
3.1 the ratio of composite interstitial substance---polyoxyethylene stearate 40 esters: Polyethylene Glycol or poloxamer: Polyethylene Glycol or carboxymethyl starch sodium: Polyethylene Glycol or betacyclodextrin: Polyethylene Glycol=1: 1～1: 10,
3.2 Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol): mixed-matrix weight and=1: 1～1: 9;
4. be prepared according to [preparation method] again, promptly can make the tripterygium total terpenoids drop pill of various different sizes.
[result of the test]
Test 4: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 4.
Test 5: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 5.
Test 6: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 6.
Test 7: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 7.
Test 8: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 8.
Test 9: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 9.
Test 10: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 10.
Test 11: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 11.
Test 12: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, the dry powder that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 12.
The group practices of table 1 medicine dry powder and single-matrix
(medicine dry powder: substrate=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | 50.0 | 67 | ＜30 | ＞10 | + |
| Polyethylene Glycol 4000 | 50.0 | 71 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 6000 | 50.0 | 81 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 8000 | 50.0 | 80 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 10000 | 50.0 | 85 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 50.0 | 84 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 75 | ＜30 | ＞10 | ++ |
| Betacyclodextrin | 50.0 | 73 | ＜30 | ＞10 | ++ |
| Poloxamer | 50.0 | 72 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 71 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 50.0 | 69 | ＜30 | ＞10 | ++ |
| Stearic acid | 50.0 | 59 | ＜30 | ＞10 | ++ |
| Sodium stearate | 50.0 | 54 | ＜30 | ＞10 | +++ |
| Glycerin gelatine | 50.0 | 57 | ＜30 | ＞10 | +++ |
| Lac | 50.0 | 54 | ＞30 | ＞10 | +++ |
The group practices of table 2 medicine dry powder and single-matrix
(medicine dry powder: substrate=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | 25.0 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 25.0 | 82 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 25.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 25.0 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 92 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 25.0 | 85 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 25.0 | 82 | ＜30 | ＜10 | ++ |
| Poloxamer | 25.0 | 85 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 25.0 | 83 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 25.0 | 77 | ＜30 | ＞10 | ++ |
| Stearic acid | 25.0 | 72 | ＞30 | ＞10 | ++ |
| Sodium stearate | 25.0 | 73 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 25.0 | 68 | ＞30 | ＞10 | +++ |
| Lac | 25.0 | 70 | ＞30 | ＞10 | +++ |
The group practices of table 3 medicine dry powder and different substrates
(medicine dry powder: substrate=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | 10.0 | 84 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 87 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 10.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 10.0 | 94 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 10.0 | 88 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 10.0 | 89 | ＜30 | ＜10 | ++ |
| Poloxamer | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 10.0 | 82 | ＜30 | ＞10 | +++ |
| Sodium lauryl sulphate | 10.0 | 84 | ＜30 | ＞10 | +++ |
| Stearic acid | 10.0 | 81 | ＞30 | ＞10 | +++ |
| Sodium stearate | 10.0 | 82 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 10.0 | 76 | ＞30 | ＞10 | +++ |
| Lac | l0.0 | 76 | ＞30 | ＞10 | +++ |
The group practices of table 4 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | 50 | 81 | ＜30 | ＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 50 | 82 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 79 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 71 | ＜30 | ＞10 | + |
The group practices of table 5 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | 25 | 87 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 25 | 88 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | 86 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 25 | 85 | ＜30 | ＞10 | ++ |
The group practices of table 6 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | 10 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 10 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 10 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 10 | 88 | ＜30 | ＜10 | +++ |
The group practices of table 7 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 50 | 86 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 50 | 85 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 50 | 84 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 50 | 85 | ＜30 | ＞10 | ++ |
The group practices of table 8 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 25 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 25 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 25 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 25 | 87 | ＜30 | ＜10 | ++ |
The group practices of table 9 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 10 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 10 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 10 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 10 | 91 | ＜30 | ＜10 | +++ |
The group practices of table 10 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | 50 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 50 | 89 | ＜30 | ＜10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 50 | 88 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 50 | 87 | ＜30 | ＞10 | ++ |
The group practices of table 11 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | 25 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 25 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 25 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 25 | 93 | ＜30 | ＜1 | +++ |
The group practices of table 12 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | 10 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 10 | 93 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 10 | 92 | ＜30 | ＜10 | +++ |
1. can be seen by the result in the table: when the ratio of medicine dry powder and substrate was 1: 1, its rounding rate, the ball method of double differences was different and index such as hardness is all undesirable, and dissolve scattered time limit influenced not obvious.
2. when the ratio of medicine dry powder and substrate is 1: 3, the rounding rate, the ball method of double differences is different and index such as hardness slightly all begins to enter preferable state.
3. when the ratio of medicine dry powder and substrate is 1: 9, though the rounding rate, the ball method of double differences is different and index such as hardness has raising, and is not obvious.
4. the general effect of composite interstitial substance is better than single-matrix.
5. the hardness method for expressing in the subordinate list adopts drop pill is placed on the glass plate, press...withes one's finger it, observes its metamorphosis."+" expression flicking promptly is out of shape, " ++ " expression distortion of firmly pressing, and " +++" expression is indeformable by it.
Claims (2)
1. a tripterygium total terpenoids drop pill that is used for the treatment of rheumatism is a raw material with the Radix Tripterygii Wilfordii extract, is prepared from a certain proportion of pharmaceutically suitable carrier, it is characterized in that:
1.1 described Radix Tripterygii Wilfordii extract obtains by following method: get the Radix Tripterygii Wilfordii root and rhizome, be cut into the thick decoction pieces of 3～5mm, use 85% ethanol, be respectively 5,4,4 times of amounts, reflux, extract, 3 times, each 4 hours, 60 ℃ of decompression recycling ethanols of extracting solution were to the thick paste shape of relative density 1.25～1.30, dry below 60 ℃, dry extract is pulverized, and takes off ester, removal of solvent under reduced pressure with No. 90 petroleum ether, dry below 60 ℃, promptly;
1.2 described substrate is the mixture of Polyethylene Glycol and polyoxyethylene stearate 40 esters or carboxymethyl starch sodium; According to the weight portion meter, polyoxyethylene stearate 40 esters or carboxymethyl starch sodium and ratio be 1: 1～1: 10, in Radix Tripterygii Wilfordii lactone alcohol, the ratio of Radix Tripterygii Wilfordii extract and substrate is 1: 3;
1.3, accurately take by weighing Radix Tripterygii Wilfordii extract and substrate according to aforementioned proportion, be placed in the heating container heating while stirring, standby until the fused solution that obtains containing Radix Tripterygii Wilfordii extract and substrate and/or emulsion and/or suspension;
1.4 adjust the temperature control system of drop pill machine, make the water dropper temperature heating of drop pill machine and remain on 50 ℃～90 ℃, the temperature cooling of condensing agent also remains on-5 ℃～40 ℃;
1.5 when treating that the temperature of dropping-pill machine head and condensing agent reaches the said temperature state respectively, fused solution and/or the emulsion and/or the suspension that will contain Radix Tripterygii Wilfordii extract and substrate, place in the water dropper jar of drop pill machine, splash in the condensing agent by water dropper and shrink shaping promptly.
2. tripterygium total terpenoids drop pill as claimed in claim 1 is characterized in that: described condensing agent be methyl-silicone oil or/and liquid paraffin or/and vegetable oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100971577A CN1322851C (en) | 2004-12-13 | 2004-12-13 | Tripterygium total terpenoids drop pill and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100971577A CN1322851C (en) | 2004-12-13 | 2004-12-13 | Tripterygium total terpenoids drop pill and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1634507A CN1634507A (en) | 2005-07-06 |
| CN1322851C true CN1322851C (en) | 2007-06-27 |
Family
ID=34847916
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100971577A Expired - Fee Related CN1322851C (en) | 2004-12-13 | 2004-12-13 | Tripterygium total terpenoids drop pill and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1322851C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147766B (en) * | 2015-10-26 | 2019-08-06 | 苏州麦迪仙医药科技有限公司 | A kind of pharmaceutical composition and its preparation method and application for treating rheumatoid arthritis |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1471945A (en) * | 2002-07-30 | 2004-02-04 | 中国人民解放军海军医学研究所 | Tripterygium wilfordii dropping pills for treating autoimmune diseases |
-
2004
- 2004-12-13 CN CNB2004100971577A patent/CN1322851C/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1471945A (en) * | 2002-07-30 | 2004-02-04 | 中国人民解放军海军医学研究所 | Tripterygium wilfordii dropping pills for treating autoimmune diseases |
Non-Patent Citations (1)
| Title |
|---|
| 国家中成药标准汇编经络肢体脑系分册 国家药品监督管理局，457-458 2002 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1634507A (en) | 2005-07-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN100358562C (en) | Tendril-leaved fritillary bulb loquat drop pills and preparation method thereof | |
| CN1322851C (en) | Tripterygium total terpenoids drop pill and its preparation method | |
| CN100348170C (en) | Yitongshu drop pill for treating pain and its preparation method | |
| CN100348169C (en) | Saussurea involucrata drop pill and its preparation method | |
| CN100364506C (en) | Drop pills preparation in use for treating bronchitis and preparation method | |
| CN100367934C (en) | Yin-nourishing lung-heat clearing drop pills | |
| CN100382786C (en) | Bastard feverfew throat clearing drip pill and its preparation method | |
| CN100453072C (en) | Banlangen dripping pills and preparation method thereof | |
| CN100358496C (en) | 'Xingnaojing' dripping pills for treating cephalitis and hepatic coma and preparation process thereof | |
| CN100348215C (en) | Kaihoujian drip pill for treating throat disease and its preparation method | |
| CN1297255C (en) | Dripping pills for treating high blood fat and its preparing method | |
| CN100367937C (en) | Throat dripping pill for clearing away heat and toxic material and its preparing method | |
| CN100367938C (en) | Sihuang intense heat purging dripping pill and its preparing method | |
| CN100364513C (en) | Gansu dripping pill for treating hepatitis and preparation method thereof | |
| CN100348174C (en) | Oral drop pill in use for clearing away heat and toxic material, relieving inflammation and alleviating pain, and preparation method | |
| CN1315462C (en) | Throat clearing drip pill and its preparation method | |
| CN100348177C (en) | Two kinds of oral drip pills for treating tracheitis and its preparation method | |
| CN100348175C (en) | Bistort drop pill and preparation method | |
| CN1325044C (en) | Drop pills for treating apoplexy diseases and preparation method thereof | |
| CN101269108A (en) | Tripterygium wilfordii total terpene sustained-release dropping pill and preparation method thereof | |
| CN100542515C (en) | Polygala dripping pills and preparation method thereof | |
| CN100364509C (en) | Compound drop pills of dahurian rhododendron leaf and preparation method | |
| CN100348171C (en) | Yujin drop pill for clearing away the heat-evil and expelling superficial evils and its preparation method | |
| CN1315470C (en) | Compound liver-benefiting dropping pill for treating hepatitis and its preparing method | |
| CN1315468C (en) | Liver-benefiting dropping pill prepared from total neterosides of swertia mileensis, and its preparing method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20070627 Termination date: 20100113 |