CN1546026A - Dripping pills of perhexiline maleate and its preparation - Google Patents
Dripping pills of perhexiline maleate and its preparation Download PDFInfo
- Publication number
- CN1546026A CN1546026A CNA2003101219200A CN200310121920A CN1546026A CN 1546026 A CN1546026 A CN 1546026A CN A2003101219200 A CNA2003101219200 A CN A2003101219200A CN 200310121920 A CN200310121920 A CN 200310121920A CN 1546026 A CN1546026 A CN 1546026A
- Authority
- CN
- China
- Prior art keywords
- perhexiline
- perhexiline maleate
- maleate
- preparation
- coolant
- 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
- JDZOTSLZMQDFLG-BTJKTKAUSA-N (z)-but-2-enedioic acid;2-(2,2-dicyclohexylethyl)piperidine Chemical compound OC(=O)\C=C/C(O)=O.C1CCCNC1CC(C1CCCCC1)C1CCCCC1 JDZOTSLZMQDFLG-BTJKTKAUSA-N 0.000 title claims description 30
- 229960004803 perhexiline maleate Drugs 0.000 title claims description 30
- 238000002360 preparation method Methods 0.000 title claims description 13
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims abstract description 3
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims abstract 2
- 229960000989 perhexiline Drugs 0.000 claims abstract 2
- CYXKNKQEMFBLER-UHFFFAOYSA-N perhexiline Chemical compound C1CCCNC1CC(C1CCCCC1)C1CCCCC1 CYXKNKQEMFBLER-UHFFFAOYSA-N 0.000 claims abstract 2
- 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
- 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
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 6
- 235000013870 dimethyl polysiloxane Nutrition 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
- 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
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- -1 liquid paraffin 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
- 238000004519 manufacturing process Methods 0.000 abstract description 4
- 208000019505 Deglutition disease Diseases 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 abstract 1
- 239000002671 adjuvant Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000011976 maleic acid Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 description 10
- 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
- 206010002383 Angina Pectoris Diseases 0.000 description 2
- 206010003119 arrhythmia Diseases 0.000 description 2
- 230000006793 arrhythmia Effects 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
- 230000001225 therapeutic effect Effects 0.000 description 2
- 208000009079 Bronchial Spasm Diseases 0.000 description 1
- 208000014181 Bronchial disease Diseases 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 description 1
- 239000000006 Nitroglycerin Substances 0.000 description 1
- 208000004880 Polyuria Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000000621 bronchi Anatomy 0.000 description 1
- 239000003218 coronary vasodilator agent Substances 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000035619 diuresis Effects 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229960003711 glyceryl trinitrate Drugs 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 210000005240 left ventricle Anatomy 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000002107 myocardial effect Effects 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to a maleic acid perhexiline drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically perhexiline maleate drop pill and preparation method thereof.
Background technology
Perhexiline maleate has the expansion coronary vasodilator, increases coronary flow, reduces the left ventricle load, reduces the effect of myocardial oxygen consumption.Arrhythmia is arranged, the effect of diuresis and expansion bronchus.To patient, can reduce the angina pectoris attacks number of times and reduce the nitroglycerin consumption with heart failure and bronchospasm.
Perhexiline maleate is drawn from gastrointestinal tract and is received, and slowly after the metabolism, drains from urine and feces.Half-life (t
1/2) scope is 3～12 days.Clinical angina pectoris, the arrhythmia of being used for.
Perhexiline maleate sheet disintegration time is long, absorption difference, and bioavailability is 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 perhexiline maleate therapeutical effect.
The present invention makes the perhexiline maleate drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of perhexiline maleate sheet, and the therapeutical effect of perhexiline maleate is given full play to.
Summary of the invention
The perhexiline maleate 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, 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 has working condition and production equipment is simple, production cost is low, compares the advantage that supplementary product consumption reduces with tablet, has 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 perhexiline maleate 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 perhexiline maleate among the present invention (Perhexiline Maleate) is 2-(2, a 2-dicyclohexyl ethyl) piperidines maleate, and molecular formula is C
23H
39NO
4, molecular weight is 393.57, 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 perhexiline maleate sheet disintegration time testing result: 58 minutes
Three, example 1 sample disintegrate (molten loosing) time detecting result: 3 minutes
Four, example 2 sample disintegrates (molten loosing) time detecting result: 2 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: 5 minutes
Eight, example 6 sample disintegrates (molten loosing) time detecting result: 9 minutes
The specific embodiment
One, example 1
Prescription:
Perhexiline maleate 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the perhexiline maleate 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:
Perhexiline maleate 5g
Macrogol 4000 15g
Make 1000
Method for making: the perhexiline maleate 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:
Perhexiline maleate 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the perhexiline maleate 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:
Perhexiline maleate 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the perhexiline maleate 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:
Perhexiline maleate 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the perhexiline maleate 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:
Perhexiline maleate 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that perhexiline maleate 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. perhexiline maleate drop pill and preparation method thereof is characterized in that: the perhexiline maleate 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 perhexiline maleate Perhexiline of claim 1 Maleate is C
23H
39NO
4, molecular weight is 393.57, 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 |
|---|---|---|---|
| CNA2003101219200A CN1546026A (en) | 2003-12-08 | 2003-12-08 | Dripping pills of perhexiline maleate and its preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101219200A CN1546026A (en) | 2003-12-08 | 2003-12-08 | Dripping pills of perhexiline maleate and its preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1546026A true CN1546026A (en) | 2004-11-17 |
Family
ID=34338571
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2003101219200A Pending CN1546026A (en) | 2003-12-08 | 2003-12-08 | Dripping pills of perhexiline maleate and its preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1546026A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101194904B (en) * | 2006-12-08 | 2011-08-10 | 天津天士力制药股份有限公司 | Dropping pills containing perhexiline maleic acid and method for preparing the same |
-
2003
- 2003-12-08 CN CNA2003101219200A patent/CN1546026A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101194904B (en) * | 2006-12-08 | 2011-08-10 | 天津天士力制药股份有限公司 | Dropping pills containing perhexiline maleic acid and method for preparing the same |
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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 |