CN1493288A - Hanfangchin A drip pill and its preparation method - Google Patents
Hanfangchin A drip pill and its preparation method Download PDFInfo
- Publication number
- CN1493288A CN1493288A CNA031576680A CN03157668A CN1493288A CN 1493288 A CN1493288 A CN 1493288A CN A031576680 A CNA031576680 A CN A031576680A CN 03157668 A CN03157668 A CN 03157668A CN 1493288 A CN1493288 A CN 1493288A
- Authority
- CN
- China
- Prior art keywords
- retrandrine
- preparation
- coolant
- polyethylene glycol
- pill
- 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.)
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Links
- 239000006187 pill Substances 0.000 title claims abstract description 16
- 238000002360 preparation method Methods 0.000 title claims description 13
- WVTKBKWTSCPRNU-KYJUHHDHSA-N (+)-Tetrandrine Chemical compound C([C@H]1C=2C=C(C(=CC=2CCN1C)OC)O1)C(C=C2)=CC=C2OC(=C2)C(OC)=CC=C2C[C@@H]2N(C)CCC3=CC(OC)=C(OC)C1=C23 WVTKBKWTSCPRNU-KYJUHHDHSA-N 0.000 title description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 12
- 239000002826 coolant Substances 0.000 claims description 12
- 239000000843 powder Substances 0.000 claims description 9
- 238000001035 drying Methods 0.000 claims description 8
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 8
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 6
- 229940008099 dimethicone Drugs 0.000 claims description 6
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 6
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 claims description 6
- 229960000502 poloxamer Drugs 0.000 claims description 6
- 229920001983 poloxamer Polymers 0.000 claims description 6
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 6
- 239000000758 substrate Substances 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- 239000011159 matrix material Substances 0.000 claims description 4
- IQXJCCZJOIKIAD-UHFFFAOYSA-N 1-(2-methoxyethoxy)hexadecane Chemical compound CCCCCCCCCCCCCCCCOCCOC IQXJCCZJOIKIAD-UHFFFAOYSA-N 0.000 claims description 2
- 239000001828 Gelatine Substances 0.000 claims description 2
- 241000238631 Hexapoda Species 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 230000001476 alcoholic effect Effects 0.000 claims description 2
- 229950009789 cetomacrogol 1000 Drugs 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 claims description 2
- 235000011187 glycerol Nutrition 0.000 claims description 2
- 229960005150 glycerol Drugs 0.000 claims description 2
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 claims description 2
- 229940057995 liquid paraffin Drugs 0.000 claims description 2
- -1 liquid paraffin Substances 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
- 229940093430 polyethylene glycol 1500 Drugs 0.000 claims description 2
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims description 2
- 229940080350 sodium stearate Drugs 0.000 claims description 2
- 239000008117 stearic acid 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
- 239000001993 wax Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 238000010298 pulverizing process Methods 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 description 19
- 238000000034 method Methods 0.000 description 11
- 238000001514 detection method Methods 0.000 description 6
- 229940075507 glyceryl monostearate Drugs 0.000 description 4
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 238000005516 engineering process Methods 0.000 description 3
- 208000019505 Deglutition disease Diseases 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 201000010001 Silicosis Diseases 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- 102100033350 ATP-dependent translocase ABCB1 Human genes 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 241000269417 Bufo Species 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 108010047230 Member 1 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 description 1
- 241000218164 Menispermaceae Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 239000007941 film coated tablet Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 150000002978 peroxides Chemical class 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000010453 quartz Substances 0.000 description 1
- WVTKBKWTSCPRNU-UHFFFAOYSA-N rac-Tetrandrin Natural products O1C(C(=CC=2CCN3C)OC)=CC=2C3CC(C=C2)=CC=C2OC(=C2)C(OC)=CC=C2CC2N(C)CCC3=CC(OC)=C(OC)C1=C23 WVTKBKWTSCPRNU-UHFFFAOYSA-N 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicon dioxide Inorganic materials O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000004575 stone Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
A dripping pill of fanchinin and its superfine pulverizing process for preparing it are disclosed. Its advantages are high dissolving and disintegrating speed, high stripping percentage, quickly taking its effect and low cost.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically retrandrine drop pill and preparation method thereof.
Background technology
Retrandrine (Tetrandrine) is for extracting a kind of alkaloid that obtains in the root of menispermaceae plant powder Radix Stephaniae Tetrandrae (stone Bufo siccus) StcphaniaTctrandra Smoorc.Retrandrine plays analgesic activity by reducing peroxide release and cytophagous activity; Can also increase chemotherapeutics gathering in tumor cell by suppressing tumor drug resistance cell surface P-glycoprotein overexpression function, strengthen the sensitivity of tumor cell chemotherapeutics.
Retrandrine can make loose, the degraded of silicosis collagen fiber, and lipid reduces, and micro-tubular structure disappears, depolymerization, and precollagen transforms and is obstructed, and occurs new cell in the gap.
Retrandrine mainly is distributed in histoorgans such as liver, lung, kidney after absorbing.Internal metabolism becomes two-compartment model, and major part exists with original shape, and the small part metabolic conversion is retrandrine-N-oxide isomer and N-2-demethyl retrandrine, half-life (t in the body
1/2) be 90 minutes, clearance rate (CL) is 38.6Lkg
-1H
-1
List marketing at present retrandrine coated tablet and Film coated tablets, clinical rheumatalgia, arthralgia, the neuralgia of being used for arranged.Be used for pulmonary carcinoma with low dose radiation merging; Also be used for simple silicosis I, II, III phase and each phase quartz lung.
Water insoluble, the odorless of retrandrine, it is little sweet to distinguish the flavor of.Retrandrine sheet disintegration time is long, and dissolution and dissolution rate are low, and the supplementary product consumption ratio is big, and child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, has influenced the performance of retrandrine therapeutical effect.
The present invention makes the retrandrine drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of retrandrine sheet, and the therapeutical effect of retrandrine is given full play to.
Summary of the invention
The retrandrine drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, dissolution and dissolution rate improve, steady quality, the pill volume is little, both can swallow also can buccal, easy to carry and use, onset is rapid, compliance is good, be particularly suitable for the characteristics that child, old people, bed patient and dysphagia patients are taken, but also have working condition and production equipment is simple, production cost is low, compare the advantage that supplementary product consumption reduces with tablet, demonstrated fully the new drug research exploitation spirit that people-oriented.
For achieving the above object, the present invention by the following technical solutions: the retrandrine fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
Substrate among the present invention includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
Coolant among the present invention includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Below through detecting to beneficial effect of the present invention as directed
One, detects index and method
1. disintegrate (molten loosing) time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000).
2. dissolution rate: sample thief, according to dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2000), with 0.1mol/L hydrochloric acid solution 600ml is solvent, and rotating speed is that per minute 100 changes, operation in accordance with the law, in the time of 5,10,20,30 and 45 minutes, get solution and filter, get subsequent filtrate, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), wavelength place at 280nm measures trap, presses C
38H
42N
2O
6Absorptance (E
1cm 1%) be 111 calculating stripping quantities.
Two, commercially available retrandrine sheet testing result
1. disintegration time: 45 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 20.3 31.5 52.3 69.2 82.5
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 61.4 85.6 97.8 99.2 99.6
Four, example 2 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 65.3 82.5 93.6 97.8 98.4
Five, example 3 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 65.6 83.2 95.4 98.5 99.6
Six, example 4 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 58.4 79.2 93.5 98.7 97.6
Seven, example 5 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 60.3 79.2 95.6 96.7 98.2
Eight, example 6 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 63.5 82.4 93.5 97.6 99.1
The specific embodiment
One, example 1
Prescription:
Retrandrine 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the retrandrine fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused polyethylene glycol 6000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Two, example 2
Prescription:
Retrandrine 5g
Macrogol 4000 15g
Make 1000
Method for making: the retrandrine fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused Macrogol 4000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Three, example 3
Prescription:
Retrandrine 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the retrandrine fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused Macrogol 4000 and the polyethylene glycol 6000 mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Four, example 4
Prescription:
Retrandrine 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the retrandrine fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused glyceryl monostearate substrate, and mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Five, example 5
Prescription:
Retrandrine 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the retrandrine fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused polyethylene glycol 6000 and the poloxamer mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Six, example 6
Prescription:
Retrandrine 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that retrandrine and poloxamer cross 200 mesh sieves through micronizing and be added in the fused glyceryl monostearate substrate, mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Claims (3)
1. retrandrine drop pill and preparation method thereof is characterized in that: the retrandrine fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, fully mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the described substrate of claim 1 includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
3. the described coolant of claim 1 includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031576680A CN1493288A (en) | 2003-09-06 | 2003-09-06 | Hanfangchin A drip pill and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031576680A CN1493288A (en) | 2003-09-06 | 2003-09-06 | Hanfangchin A drip pill and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1493288A true CN1493288A (en) | 2004-05-05 |
Family
ID=34240895
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031576680A Pending CN1493288A (en) | 2003-09-06 | 2003-09-06 | Hanfangchin A drip pill and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1493288A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108904500A (en) * | 2018-08-13 | 2018-11-30 | 河北工业大学 | Bis ether bond type BBI is inhibiting application and drug in Kv10.1 ion channel activity |
-
2003
- 2003-09-06 CN CNA031576680A patent/CN1493288A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108904500A (en) * | 2018-08-13 | 2018-11-30 | 河北工业大学 | Bis ether bond type BBI is inhibiting application and drug in Kv10.1 ion channel activity |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |