CN1568990A - Dripping pills of cyproheptadine hydrochloride and its preparation method - Google Patents
Dripping pills of cyproheptadine hydrochloride and its preparation method Download PDFInfo
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- CN1568990A CN1568990A CNA2004100444460A CN200410044446A CN1568990A CN 1568990 A CN1568990 A CN 1568990A CN A2004100444460 A CNA2004100444460 A CN A2004100444460A CN 200410044446 A CN200410044446 A CN 200410044446A CN 1568990 A CN1568990 A CN 1568990A
- Authority
- CN
- China
- Prior art keywords
- cyproheptadine hydrochloride
- coolant
- preparation
- polyethylene glycol
- cyproheptadine
- 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
- 229960003596 cyproheptadine hydrochloride Drugs 0.000 title claims abstract description 28
- ZPMVNZLARAEGHB-UHFFFAOYSA-N cyproheptadine hydrochloride (anhydrous) Chemical compound Cl.C1CN(C)CCC1=C1C2=CC=CC=C2C=CC2=CC=CC=C21 ZPMVNZLARAEGHB-UHFFFAOYSA-N 0.000 title claims abstract description 28
- 239000006187 pill Substances 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 title claims description 13
- 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
- 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
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 239000011159 matrix material Substances 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
- 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
- 238000000034 method Methods 0.000 abstract description 11
- 238000004519 manufacturing process Methods 0.000 abstract description 4
- 208000019505 Deglutition disease Diseases 0.000 abstract description 3
- 239000003814 drug Substances 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 3
- 239000002671 adjuvant 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
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 208000010668 atopic eczema 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
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 1
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical compound OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- 206010012434 Dermatitis allergic Diseases 0.000 description 1
- 206010012442 Dermatitis contact Diseases 0.000 description 1
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 description 1
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 208000024780 Urticaria Diseases 0.000 description 1
- 208000001407 Vascular Headaches Diseases 0.000 description 1
- 208000002029 allergic contact dermatitis Diseases 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 230000001705 anti-serotonergic effect Effects 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 201000008937 atopic dermatitis Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000019636 bitter flavor Nutrition 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229960003291 chlorphenamine Drugs 0.000 description 1
- 230000003153 cholinolytic effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000000994 depressogenic effect Effects 0.000 description 1
- 230000036267 drug metabolism Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 229940097043 glucuronic acid Drugs 0.000 description 1
- 239000000938 histamine H1 antagonist Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 206010027599 migraine Diseases 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
- 229960003910 promethazine Drugs 0.000 description 1
- 230000008085 renal dysfunction Effects 0.000 description 1
- 206010039083 rhinitis Diseases 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a cyproheptadine hydrochloride drop pill prepared through ultramicro disintegration and drop pills manufacturing technique, 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 cyproheptadine hydrochloride drop pill and preparation method thereof.
Background technology
Cyproheptadine hydrochloride is H
1Receptor antagonist, effect is strong than chlorphenamine, promethazine, and antiserotonergic effect and cholinolytic effect light, moderate are arranged, so its energy blocking 5-hydroxytryptamine to the effect of blood vessel, intestinal and other smooth muscle, can be used as the depressant of vascular headache.
The cyproheptadine hydrochloride oral absorption is better, about 8 hours of acting duration.Product in the body after most of drug metabolism combines with glucuronic acid, mainly by urine excretion, still has a small amount of original shape medicine and metabolite to be discharged by feces.The elimination speed of renal dysfunction person medicine slows down.List marketing at present tablet only arranged, clinically be used for urticaria, eczema, allergic dermatitis and contact dermatitis, skin pruritus, rhinitis, migraine, asthma etc. as antihistaminic.
The cyproheptadine hydrochloride mildly bitter flavor, slightly soluble in water, its disintegration of tablet time is longer, 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 cyproheptadine hydrochloride therapeutical effect.
The present invention makes the cyproheptadine hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of cyproheptadin hydrochloride tablet, and the therapeutical effect of cyproheptadine hydrochloride is given full play to.
Summary of the invention
The cyproheptadine 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 cyproheptadine hydrochloride 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.
The chemical name of cyproheptadine hydrochloride is 1-methyl-4-(5H-dibenzo [a, d] cycloheptatriene-5-subunit) piperidine hydrochlorate sesquialter hydrate among the present invention, and molecular formula is C
21H
21NHcl1 H
2O, molecular weight are 350.89, and structural formula is
Hcl, 1 H
2O.
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 cyproheptadin hydrochloride tablet disintegration time testing result: 56 minutes
Three, example 1 sample disintegrate (molten loosing) time detecting result: 2 minutes
Four, example 2 sample disintegrates (molten loosing) time detecting result: 3 minutes
Five, example 3 sample disintegrates (molten loosing) time detecting result: 2 minutes
Six, example 4 sample disintegrates (molten loosing) time detecting result: 5 minutes
Seven, example 5 sample disintegrates (molten loosing) time detecting result: 8 minutes
Eight, example 6 sample disintegrates (molten loosing) time detecting result: 8 minutes
The specific embodiment
One, example 1
Prescription:
Cyproheptadine hydrochloride 2g
Polyethylene glycol 6000 18g
Make 1000
Method for making: the cyproheptadine 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:
Cyproheptadine hydrochloride 2g
Macrogol 4000 18g
Make 1000
Method for making: the cyproheptadine 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:
Cyproheptadine hydrochloride 2g
Polyethylene glycol 6000 12g
Macrogol 4000 6g
Make 1000
Method for making: the cyproheptadine hydrochloride 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:
Cyproheptadine hydrochloride 2g
Glyceryl monostearate 18g
Make 1000
Method for making: the cyproheptadine 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:
Cyproheptadine hydrochloride 2g
Polyethylene glycol 6000 12g
Poloxamer 6g
Make 1000
Method for making: the cyproheptadine 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:
Cyproheptadine hydrochloride 2g
Glyceryl monostearate 16g
Poloxamer 2g
Make 1000
Method for making: get the mixing fine powders that cyproheptadine 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. cyproheptadine hydrochloride drop pill and preparation method thereof is characterized in that: the cyproheptadine 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 chemical name of the described cyproheptadine hydrochloride of claim 1 is 1-methyl-4-(5H-dibenzo [a, d] cycloheptatriene-5-subunit) piperidine hydrochlorate sesquialter hydrate, and molecular formula is C
21H
21NHcl1 H
2O, molecular weight are 350.89, and structural formula is
Hcl, 1 H
2O.
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 |
|---|---|---|---|
| CNA2004100444460A CN1568990A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of cyproheptadine hydrochloride and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100444460A CN1568990A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of cyproheptadine hydrochloride and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1568990A true CN1568990A (en) | 2005-01-26 |
Family
ID=34481896
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2004100444460A Pending CN1568990A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of cyproheptadine hydrochloride and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1568990A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111643462A (en) * | 2020-06-24 | 2020-09-11 | 上海复旦复华药业有限公司 | Formula and process for producing cyproheptadine hydrochloride tablets with high curative effect |
| WO2022188898A3 (en) * | 2021-12-04 | 2022-11-03 | 中国农业科学院兰州兽医研究所 | Use of cyproheptadine hydrochloride compound in preparation of drug for preventing or treating african swine fever |
-
2004
- 2004-05-13 CN CNA2004100444460A patent/CN1568990A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111643462A (en) * | 2020-06-24 | 2020-09-11 | 上海复旦复华药业有限公司 | Formula and process for producing cyproheptadine hydrochloride tablets with high curative effect |
| WO2022188898A3 (en) * | 2021-12-04 | 2022-11-03 | 中国农业科学院兰州兽医研究所 | Use of cyproheptadine hydrochloride compound in preparation of drug for preventing or treating african swine fever |
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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 |