CN1561977A - Chlorpronaline hydrochloride dripping pill and its preparing method - Google Patents
Chlorpronaline hydrochloride dripping pill and its preparing method Download PDFInfo
- Publication number
- CN1561977A CN1561977A CN 200410030364 CN200410030364A CN1561977A CN 1561977 A CN1561977 A CN 1561977A CN 200410030364 CN200410030364 CN 200410030364 CN 200410030364 A CN200410030364 A CN 200410030364A CN 1561977 A CN1561977 A CN 1561977A
- Authority
- CN
- China
- Prior art keywords
- clorprenaline hydrochloride
- coolant
- hydrochloride
- clorprenaline
- polyethylene glycol
- 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
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 title description 11
- SSMSBSWKLKKXGG-UHFFFAOYSA-N 1-(2-chlorophenyl)-2-isopropylaminoethanol Chemical compound CC(C)NCC(O)C1=CC=CC=C1Cl SSMSBSWKLKKXGG-UHFFFAOYSA-N 0.000 claims description 29
- 229950011462 clorprenaline Drugs 0.000 claims description 29
- 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
- 239000000758 substrate Substances 0.000 claims description 7
- 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
- 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
- -1 liquid paraffin Substances 0.000 claims description 3
- 239000011159 matrix material Substances 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
- 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
- 238000010298 pulverizing process Methods 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 description 4
- 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
- 230000000694 effects Effects 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 description 2
- 208000019505 Deglutition disease Diseases 0.000 description 2
- 206010006451 bronchitis Diseases 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229940039009 isoproterenol Drugs 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 206010006458 Bronchitis chronic Diseases 0.000 description 1
- 206010048610 Cardiotoxicity Diseases 0.000 description 1
- 206010014561 Emphysema Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- WVDDGKGOMKODPV-UHFFFAOYSA-N benzyl alcohol Substances OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 1
- 210000000621 bronchi Anatomy 0.000 description 1
- 231100000259 cardiotoxicity Toxicity 0.000 description 1
- 230000007681 cardiovascular toxicity Effects 0.000 description 1
- 208000007451 chronic bronchitis Diseases 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000000916 dilatatory effect Effects 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 208000030603 inherited susceptibility to asthma Diseases 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
- 230000009325 pulmonary function Effects 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
A dripping pill of chorprenaline hydrochloride is prepared through superfine pulverizing and conventional steps for preparing dripping pills.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically clorprenaline hydrochloride drop pill and preparation method thereof.
Background technology
Clorprenaline hydrochloride is the beta 2 receptor agonist, and bronchus is had tangible dilating effect, the effect of relievining asthma than isoproterenol slightly a little less than, but cardiac toxicity is obviously reduced, only be 1/3～1/10 of isoproterenol to the excitation of heart.
Coming into force in the oral back of clorprenaline hydrochloride in 15～30 minutes, reached ceiling effect in about 1 hour, and effect was kept 4-6 hour.
List marketing at present the clorprenaline hydrochloride sheet only arranged, the clinical bronchial asthma, asthmatic bronchitis, chronic bronchitis of being used for merges emphysema, can relieving asthma and improves pulmonary function.
The clorprenaline hydrochloride bitter in the mouth, easily molten in water, but 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 clorprenaline hydrochloride therapeutical effect.
The present invention makes the clorprenaline hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of clorprenaline hydrochloride sheet, and the therapeutical effect of clorprenaline hydrochloride is given full play to.
Summary of the invention
The clorprenaline hydrochloride 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 clorprenaline hydrochloride 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 clorprenaline hydrochloride is α-[[(1-Methylethyl) amino] methyl]-2-chloro-benzyl alcohol hydrochloride among the present invention, and molecular formula is C
11H
16ClNOHCl, molecular weight are 250.17, and 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 X of Chinese Pharmacopoeia version in 2000 A).
Two, commercially available clorprenaline hydrochloride sheet disintegration time testing result: 49 minutes
Three, example 1 sample disintegrate (molten loosing) time detecting result: 4 minutes
Four, example 2 sample disintegrates (molten loosing) time detecting result: 3 minutes
Five, example 3 sample disintegrates (molten loosing) time detecting result: 3 minutes
Six, example 4 sample disintegrates (molten loosing) time detecting result: 6 minutes
Seven, example 5 sample disintegrates (molten loosing) time detecting result: 8 minutes
Eight, example 6 sample disintegrates (molten loosing) time detecting result: 10 minutes
The specific embodiment
One, example 1
Prescription:
Clorprenaline hydrochloride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the clorprenaline hydrochloride 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:
Clorprenaline hydrochloride 5g
Macrogol 4000 15g
Make 1000
Method for making: the clorprenaline hydrochloride 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:
Clorprenaline hydrochloride 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the clorprenaline hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added to fused Macrogol 4000 and polyethylene glycol 6000 closes in the substrate, stirs evenly, and be coolant with the dimethicone, the dropping preparation method pill, drying, promptly.
Four, example 4
Prescription:
Clorprenaline hydrochloride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the clorprenaline hydrochloride 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:
Clorprenaline hydrochloride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the clorprenaline hydrochloride 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:
Clorprenaline hydrochloride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that clorprenaline hydrochloride 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. clorprenaline hydrochloride drop pill and preparation method thereof is characterized in that: the clorprenaline hydrochloride 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 molecular formula of the described clorprenaline hydrochloride of claim 1 is C
11H
16ClNOHCl, molecular weight are 250.17, and structural formula is
HCl.
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 |
|---|---|---|---|
| CN 200410030364 CN1561977A (en) | 2004-03-29 | 2004-03-29 | Chlorpronaline hydrochloride dripping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410030364 CN1561977A (en) | 2004-03-29 | 2004-03-29 | Chlorpronaline hydrochloride dripping pill and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1561977A true CN1561977A (en) | 2005-01-12 |
Family
ID=34481091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410030364 Pending CN1561977A (en) | 2004-03-29 | 2004-03-29 | Chlorpronaline hydrochloride dripping pill and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1561977A (en) |
-
2004
- 2004-03-29 CN CN 200410030364 patent/CN1561977A/en active Pending
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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 |