CN1493296A - Hemsleya amabilis drip pill and its preparation method - Google Patents
Hemsleya amabilis drip pill and its preparation method Download PDFInfo
- Publication number
- CN1493296A CN1493296A CNA031591973A CN03159197A CN1493296A CN 1493296 A CN1493296 A CN 1493296A CN A031591973 A CNA031591973 A CN A031591973A CN 03159197 A CN03159197 A CN 03159197A CN 1493296 A CN1493296 A CN 1493296A
- Authority
- CN
- China
- Prior art keywords
- hemsleyadin
- coolant
- preparation
- polyethylene glycol
- dissolution
- 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 19
- 238000002360 preparation method Methods 0.000 title claims description 16
- 241000465412 Hemsleya amabilis Species 0.000 title 1
- 239000002826 coolant Substances 0.000 claims description 15
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 12
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 12
- 238000001035 drying Methods 0.000 claims description 11
- 239000000843 powder Substances 0.000 claims description 11
- 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 10
- 229940008099 dimethicone Drugs 0.000 claims description 9
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 9
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 9
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 9
- 239000000758 substrate Substances 0.000 claims description 8
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 6
- 229960000502 poloxamer Drugs 0.000 claims description 6
- 229920001983 poloxamer Polymers 0.000 claims description 6
- 239000011159 matrix material Substances 0.000 claims description 5
- 238000002156 mixing Methods 0.000 claims description 5
- 239000000203 mixture Substances 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
- 241000196324 Embryophyta Species 0.000 claims description 3
- 241001529246 Platymiscium Species 0.000 claims description 3
- 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 25
- 238000000034 method Methods 0.000 description 14
- 238000001514 detection method Methods 0.000 description 9
- 239000000243 solution Substances 0.000 description 8
- 238000003756 stirring Methods 0.000 description 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 229940075507 glyceryl monostearate Drugs 0.000 description 4
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 4
- 238000005516 engineering process Methods 0.000 description 3
- 239000000047 product Substances 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
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 208000004429 Bacillary Dysentery Diseases 0.000 description 1
- 208000004232 Enteritis Diseases 0.000 description 1
- 206010017915 Gastroenteritis shigella Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 206010001093 acute tonsillitis Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 201000005113 shigellosis Diseases 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003440 toxic substance Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
A dripping pill of hemsleyadine 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 high stability and low cost.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically drop pills of hemsleyadin and preparation method thereof.
Background technology
Hemsleyadin (Hemsleyadinum) based on the hemsleyadin first, has heat-clearing and toxic substances removing, the effect of anti-inflammation for the hemsleyadin first extracted in the cucurbitaceous plant Radix Hemsleyae Macrospermae platymiscium and the mixture of hemsleyadin second.Clinical bacillary dysentery, enteritis, bronchitis, the acute tonsillitis of being used for.
Existing market is sold has only hemsleyadine tablet, not only dosage form is single, and because hemsleyadin is water insoluble, hydrophobicity is strong, make the disintegration time of hemsleyadine tablet long, dissolution and dissolution rate are low, absorption difference, and bioavailability is low, supplementary product consumption is big, child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, have influenced the performance of hemsleyadin therapeutical effect.
The present invention makes the drop pills of hemsleyadin agent by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of hemsleyadine tablet, and the therapeutical effect of hemsleyadin is given full play to.
Summary of the invention
The drop pills of hemsleyadin 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, with tablet and compare the advantage that supplementary product consumption reduces, 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 hemsleyadin 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.
Hemsleyadin is the hemsleyadin first extracted in the cucurbitaceous plant Radix Hemsleyae Macrospermae platymiscium and the mixture of hemsleyadin second among the present invention, based on the hemsleyadin first.The molecular formula of hemsleyadin first is C
32H
50O
8, molecular weight is 562.74, structural formula is:
The molecular formula of hemsleyadin second is C
30H
48O
7, molecular weight is 520.71, 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
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), 600ml is a solvent with hydrochloric acid solution (9 → 1000), in the time of 5,10,20,30 and 45 minutes, get solution, filter, subsequent filtrate is as need testing solution.It is an amount of that other gets hemsleyadin first reference substance, with above-mentioned dissolve with hydrochloric acid solution and dilution, product solution in contrast.Get above-mentioned two kinds of solution,, measure trap, calculate stripping quantity at 525nm wavelength place according to spectrophotography (Chinese Pharmacopoeia two appendix VI A in 2000).
Two, commercially available hemsleyadine tablet testing result
1. disintegration time: 54 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 18.6 31.2 50.3 67.9 76.3
Three, example 1 sample detection result
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 53.4 71.2 89.5 98.6 99.7
Four, example 2 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 50.2 70.3 89.6 98.9 99.4
Five, example 3 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 48.3 69.2 89.5 98.6 99.5
Six, example 4 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 58.6 80.3 95.6 98.7 98.2
Seven, example 5 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 45.3 59.6 78.2 95.7 97.8
Eight, example 6 sample detection results
1. the molten diffusing time: 9 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 45.3 61.2 78.9 93.5 98.7
Nine, example 7 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 52.3 73.5 92.6 99.7 100.8
Ten, example 8 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 58.9 83.6 96.7 99.8 99.2
11, example 9 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 55.1 78.3 94.5 98.2 99.7
The specific embodiment
One, example 1
Prescription:
Hemsleyadin 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the hemsleyadin 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:
Hemsleyadin 5g
Macrogol 4000 15g
Make 1000
Method for making: the hemsleyadin 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:
Hemsleyadin 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the hemsleyadin 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:
Hemsleyadin 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the hemsleyadin 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:
Hemsleyadin 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the hemsleyadin 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:
Hemsleyadin 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that hemsleyadin 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.
Seven, example 7
Prescription:
Hemsleyadin 2g
Polyethylene glycol 6000 18g
Make 1000
Method for making: the hemsleyadin 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.
Eight, example 8
Prescription:
Hemsleyadin 2g
Macrogol 4000 18g
Make 1000
Method for making: the hemsleyadin 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.
Nine, example 9
Prescription:
Hemsleyadin 2g
Polyethylene glycol 6000 6g
Macrogol 4000 12g
Make 1000
Method for making: the hemsleyadin 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.
Claims (4)
1. drop pills of hemsleyadin and preparation method thereof is characterized in that: the hemsleyadin fine powder of 1 weight portion through micronizing is added in 1~10 weight portion molten matrix, and abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the described hemsleyadin of claim 1 is the hemsleyadin first extracted in the cucurbitaceous plant Radix Hemsleyae Macrospermae platymiscium and the mixture of hemsleyadin second, based on the hemsleyadin first.The molecular formula of hemsleyadin first is C
32H
50O
8, molecular weight is 562.74, structural formula is:
The molecular formula of hemsleyadin second is C
30H
48O
7, molecular weight is 520.71, 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 |
---|---|---|---|
CNA031591973A CN1493296A (en) | 2003-09-10 | 2003-09-10 | Hemsleya amabilis drip pill and its preparation method |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNA031591973A CN1493296A (en) | 2003-09-10 | 2003-09-10 | Hemsleya amabilis drip pill and its preparation method |
Publications (1)
Publication Number | Publication Date |
---|---|
CN1493296A true CN1493296A (en) | 2004-05-05 |
Family
ID=34240933
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNA031591973A Pending CN1493296A (en) | 2003-09-10 | 2003-09-10 | Hemsleya amabilis drip pill and its preparation method |
Country Status (1)
Country | Link |
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CN (1) | CN1493296A (en) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1927251B (en) * | 2005-09-09 | 2010-10-13 | 天津瑞普生物技术股份有限公司 | Medicament for animals with heat clearing and detoxicating functions and preparing method thereof |
CN1872075B (en) * | 2005-06-01 | 2010-11-03 | 天津天士力制药股份有限公司 | Drop pills of hemsleyadin, and preparation method |
CN101422466B (en) * | 2006-05-19 | 2010-12-29 | 樊献俄 | Use of cucurbitacin in preparing medicine for treating cancer |
CN101829121B (en) * | 2007-02-13 | 2011-06-22 | 昆明四创药业有限公司 | Hemsleyadin sustained-release preparation |
-
2003
- 2003-09-10 CN CNA031591973A patent/CN1493296A/en active Pending
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1872075B (en) * | 2005-06-01 | 2010-11-03 | 天津天士力制药股份有限公司 | Drop pills of hemsleyadin, and preparation method |
CN1927251B (en) * | 2005-09-09 | 2010-10-13 | 天津瑞普生物技术股份有限公司 | Medicament for animals with heat clearing and detoxicating functions and preparing method thereof |
CN101422466B (en) * | 2006-05-19 | 2010-12-29 | 樊献俄 | Use of cucurbitacin in preparing medicine for treating cancer |
CN101829121B (en) * | 2007-02-13 | 2011-06-22 | 昆明四创药业有限公司 | Hemsleyadin sustained-release preparation |
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C06 | Publication | ||
PB01 | Publication | ||
C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
WD01 | Invention patent application deemed withdrawn after publication |