CN1602860A - Dripping pills of clemastine fumarate and its preparation method - Google Patents
Dripping pills of clemastine fumarate and its preparation method Download PDFInfo
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- CN1602860A CN1602860A CNA2004100553379A CN200410055337A CN1602860A CN 1602860 A CN1602860 A CN 1602860A CN A2004100553379 A CNA2004100553379 A CN A2004100553379A CN 200410055337 A CN200410055337 A CN 200410055337A CN 1602860 A CN1602860 A CN 1602860A
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- clemastine fumarate
- coolant
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- polyethylene glycol
- dissolution
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Abstract
The invention uses super micro shattering and drop pills producing the technology to produce fenfluramine drop pills, reaching the purposes such as increasing speed, and dissolution of disintegration, increasing the medicine stability, reducing the dose of auxiliary materials and decreasing cost, with rapid effect and convenient use. It can be buccal as well as deglutition, has remarkable conformity, and is especially suitable for children, older man, sicker in bed or with difficulty of swallowing.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically clemastine fumarate drop pill and preparation method thereof.
Background technology
Clemastine fumarate is H
1Receptor antagonist can suppress the permeability of blood capillary, can be antipruritic rapidly, still have cholinolytic and sedation.
Clemastine fumarate is oral to be absorbed rapidly through digestive tract, the onset in back 30 minutes of taking medicine, and blood drug level reached the peak in 2～5 hours, acted on sustainable 12 hours, and it is more to be distributed in internal organs such as liver, kidney, lung, spleen.t
1/2Be 21 hours, in liver, be metabolized to Dan Jihua, two methylate, or combine, mainly by draining in urine and the feces, can appear in the milk on a small quantity with metabolite and a small amount of original shape medicament forms with glucuronic acid.List marketing at present tablet, clinical allergic rhinitis, urticaria and other anaphylaxis dermatosis of being mainly used in only arranged.
The clemastine fumarate mildly bitter flavor, soluble,very slightly in water, its disintegration of tablet time is long, dissolution and dissolution rate are low, absorption difference, and bioavailability is low, 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 clemastine fumarate therapeutical effect.
The present invention makes the clemastine fumarate drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of clemastine fumarate sheet, and the therapeutical effect of clemastine fumarate is given full play to.
Summary of the invention
The clemastine fumarate drop pill 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, 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 clemastine fumarate fine powder of 1 weight portion through micronizing is added in 5～30 weight portion molten matrix, fully mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
The chemical name of clemastine fumarate is [R-(R among the present invention
*, R
*)]-1-methyl-2-[2-[1-(4-chlorphenyl)-1-benzene ethyoxyl] ethyl]-pyrrolidine (E)-2-butylene diacid salt, molecular formula is C
21H
26CLNOC
4H
4O
4, molecular weight is 459.97, 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 second methods of Chinese Pharmacopoeia version in 2000), [get citric acid-hydrate 1.0g with Chinese holly edge acid buffer (pH4.0), add water 1000ml and make dissolving, hydro-oxidation sodium solution (3 → 10) 22.0ml and hydrochloric acid 8.8ml, add the water mixing, make the solution of 2000ml, regulate pH value to 4.0, promptly] 500ml is a solution, rotating speed is that per minute 50 changes, and operation in accordance with the law is through 10,20,30, in the time of 40 minutes, get solution 50ml, get reference substance solution (it is an amount of to get the clemastine fumarate reference substance, and solubilizer is diluted to the concentration near need testing solution) 50ml and solvent 50ml simultaneously, put in the separatory funnel respectively.Each methylate orange solution (is got methyl orange indicator solution 20ml, thin up is to 100ml) 10ml, chloroform 20ml, jolting 10 minutes, tell chloroform layer, filter, get subsequent filtrate respectively, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 B), wavelength place at 420nm measures trap, calculates stripping quantity.
Two, commercially available clemastine fumarate sheet testing result
1. disintegration time: 59 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 31.2 41.3 61.4 72.5
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 63.6 98.4 97.3 99.6
Four, example 2 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 58.9 96.7 99.0 99.8
Five, example 3 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 67.3 98.9 97.2 98.6
Six, example 4 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 56.4 92.3 99.5 98.0
Seven, example 5 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 61.4 94.6 98.7 95.2
Eight, example 6 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 52.3 93.4 98.6 96.5
The specific embodiment
One, example 1
Prescription:
Clemastine fumarate 1.34g
Polyethylene glycol 6000 20g
Make 1000
Method for making: the clemastine fumarate 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:
Clemastine fumarate 1.34g
Macrogol 4000 20g
Make 1000
Method for making: the clemastine fumarate 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:
Clemastine fumarate 1.34g
Polyethylene glycol 6000 10g
Macrogol 4000 10g
Make 1000
Method for making: the clemastine fumarate 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:
Clemastine fumarate 1.34g
Glyceryl monostearate 20g
Make 1000
Method for making: the clemastine fumarate 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:
Clemastine fumarate 1.34g
Polyethylene glycol 6000 15g
Poloxamer 5g
Make 1000
Method for making: the clemastine fumarate 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:
Clemastine fumarate 1.34g
Glyceryl monostearate 20g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that clemastine fumarate 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. clemastine fumarate drop pill and preparation method thereof is characterized in that: the clemastine fumarate fine powder of 1 weight portion through micronizing is added in 5～30 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 clemastine fumarate of claim 1 is [R-(R
*, R
*)]-1-methyl-2-[2-[1-(4-chlorphenyl)-1-benzene ethyoxyl] ethyl]-pyrrolidine (E)-2-butylene diacid salt, structural formula is
, molecular formula is C
21H
26CLNOC
4H
4O
4, molecular weight is 459.97.
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 |
|---|---|---|---|
| CNA2004100553379A CN1602860A (en) | 2004-08-23 | 2004-08-23 | Dripping pills of clemastine fumarate and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100553379A CN1602860A (en) | 2004-08-23 | 2004-08-23 | Dripping pills of clemastine fumarate and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1602860A true CN1602860A (en) | 2005-04-06 |
Family
ID=34666169
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2004100553379A Pending CN1602860A (en) | 2004-08-23 | 2004-08-23 | Dripping pills of clemastine fumarate and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1602860A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102816101A (en) * | 2012-08-21 | 2012-12-12 | 江苏恒祥化工有限责任公司 | Synthesis method of (S)-N-methyl-2 chloro-ethyl-pyrrolidine |
| CN111920805A (en) * | 2020-08-14 | 2020-11-13 | 济南市儿童医院 | Application of clemastine fumarate in preparation of methicillin-resistant staphylococcus aureus |
-
2004
- 2004-08-23 CN CNA2004100553379A patent/CN1602860A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102816101A (en) * | 2012-08-21 | 2012-12-12 | 江苏恒祥化工有限责任公司 | Synthesis method of (S)-N-methyl-2 chloro-ethyl-pyrrolidine |
| CN111920805A (en) * | 2020-08-14 | 2020-11-13 | 济南市儿童医院 | Application of clemastine fumarate in preparation of methicillin-resistant staphylococcus aureus |
| CN111920805B (en) * | 2020-08-14 | 2021-11-19 | 山东省妇幼保健院 | Application of clemastine fumarate in preparation of methicillin-resistant staphylococcus aureus |
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| WD01 | Invention patent application deemed withdrawn after publication |