CN1528320A - Acetyl rhizoma gastrodiae extract drop pill and preparing method thereof - Google Patents
Acetyl rhizoma gastrodiae extract drop pill and preparing method thereof Download PDFInfo
- Publication number
- CN1528320A CN1528320A CNA031433367A CN03143336A CN1528320A CN 1528320 A CN1528320 A CN 1528320A CN A031433367 A CNA031433367 A CN A031433367A CN 03143336 A CN03143336 A CN 03143336A CN 1528320 A CN1528320 A CN 1528320A
- Authority
- CN
- China
- Prior art keywords
- acegastrodine
- coolant
- drop pill
- polyethylene glycol
- preparation
- 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.)
- Pending
Links
- 239000006187 pill Substances 0.000 title claims abstract description 17
- 238000000034 method Methods 0.000 title description 12
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 title 1
- HGUDVDQXCUHOED-YMQHIKHWSA-N [(2r,3r,4s,5r,6s)-3,4,5-triacetyloxy-6-[4-(hydroxymethyl)phenoxy]oxan-2-yl]methyl acetate Chemical compound CC(=O)O[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(=O)C)O[C@H]1OC1=CC=C(CO)C=C1 HGUDVDQXCUHOED-YMQHIKHWSA-N 0.000 claims description 27
- 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
- 238000002360 preparation method Methods 0.000 claims description 12
- 238000001035 drying Methods 0.000 claims description 8
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 8
- 239000000843 powder Substances 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
- 239000000126 substance 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
- 238000004519 manufacturing process Methods 0.000 abstract description 4
- 230000001225 therapeutic effect Effects 0.000 abstract description 3
- 238000004090 dissolution Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 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
- 238000004891 communication Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 206010019233 Headaches Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 230000003727 cerebral blood flow Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 208000001286 intracranial vasospasm Diseases 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 230000002557 soporific effect Effects 0.000 description 1
- 230000002936 tranquilizing effect Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention utilizes ultramicropulverization and dripping pill production process to produce acelylgastrodin dripping pills, and can attain the goal of raising disintegration and dissolution speed, quickly obtain therapeutic effect, raising stability of medicine, reducing dose of auxiliary material, reducing production cost and convenient administration, and its compliance property is good.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically acegastrodine drop pill and preparation method thereof.
Background technology
Acegastrodine can strengthen corticocerebral process of inhibition, presents the brain wave type that maincenter suppresses, and has maincenter tranquilizing soporific effect, and has analgesic activity; But the cerebral blood flow increasing amount is also alleviated cerebral vasospasm; And electrocardiogram, blood pressure there is not obvious influence.List marketing at present tablet only arranged, clinically be used for calmness, sleep peacefully and the cardiovascular nervous headache.
The acegastrodine odorless, bitter in the mouth, insoluble in water, its disintegration of tablet time is long, absorption difference, bioavailability is low, and the supplementary product consumption ratio is big, child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, have influenced the performance of acegastrodine therapeutical effect.
The present invention makes the acegastrodine drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of acegastrodine sheet, and the therapeutical effect of acegastrodine is given full play to.
Summary of the invention
The acegastrodine drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, steady quality, the pill volume is little, and is easy to carry and use, and 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 acegastrodine 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.
Among the present invention the chemical name of acegastrodine be 4-methylol benzene-2 ', 3 ', 4 ', 6 '-four-O-acetyl-β-D-pyranglucoside, molecular formula is C
21H
26O
11, molecular weight is 454.42, structural formula is:
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
Disintegrate (molten loosing) time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000).
Two, commercially available acegastrodine sheet disintegration time testing result: 57 minutes
Three, example 1 sample disintegrate (molten loosing) time detecting result: 4 minutes
Four, example 2 sample disintegrates (molten loosing) time detecting result: 5 minutes
Five, example 3 sample disintegrates (molten loosing) time detecting result: 6 minutes
Six, example 4 sample disintegrates (molten loosing) time detecting result: 12 minutes
Seven, example 5 sample disintegrates (molten loosing) time detecting result: 13 minutes
Eight, example 6 sample disintegrates (molten loosing) time detecting result: 16 minutes
The specific embodiment
One, example 1
Prescription:
Acegastrodine 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the acegastrodine 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:
Acegastrodine 5g
Macrogol 4000 15g
Make 1000
Method for making: the acegastrodine 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:
Acegastrodine 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the acegastrodine 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:
Acegastrodine 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the acegastrodine 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:
Acegastrodine 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the acegastrodine 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:
Acegastrodine 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that acegastrodine 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 (4)
1. acegastrodine drop pill and preparation method thereof is characterized in that: the acegastrodine 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.
The chemical name of the described acegastrodine of claim 1 be 4-methylol benzene-2 ', 3 ', 4 ', 6 '-four-O-acetyl-β-D-pyranglucoside, molecular formula is C
21H
26O
11, molecular weight is 454.42, structural formula is:
3. 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.
4. 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 |
|---|---|---|---|
| CNA031433367A CN1528320A (en) | 2003-09-27 | 2003-09-27 | Acetyl rhizoma gastrodiae extract drop pill and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031433367A CN1528320A (en) | 2003-09-27 | 2003-09-27 | Acetyl rhizoma gastrodiae extract drop pill and preparing method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1528320A true CN1528320A (en) | 2004-09-15 |
Family
ID=34286560
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031433367A Pending CN1528320A (en) | 2003-09-27 | 2003-09-27 | Acetyl rhizoma gastrodiae extract drop pill and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1528320A (en) |
-
2003
- 2003-09-27 CN CNA031433367A patent/CN1528320A/en active Pending
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| 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 |