CN1568987A - Dripping pills of paroxetine hydrochloride and its preparation method - Google Patents
Dripping pills of paroxetine hydrochloride and its preparation method Download PDFInfo
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- CN1568987A CN1568987A CNA2004100444390A CN200410044439A CN1568987A CN 1568987 A CN1568987 A CN 1568987A CN A2004100444390 A CNA2004100444390 A CN A2004100444390A CN 200410044439 A CN200410044439 A CN 200410044439A CN 1568987 A CN1568987 A CN 1568987A
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- paroxetine hydrochloride
- coolant
- preparation
- polyethylene glycol
- drop pill
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- Plural Heterocyclic Compounds (AREA)
Abstract
The invention relates to an Paroxetine Hydrochloride drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. oral or swallow administration, 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 paroxetine hydrochloride drop pill and preparation method thereof.
Background technology
Paroxetine hydrochloride is a selectivity nervus centralis serotonin reuptake inhibitor, can make that 5-hydroxy tryptamine concentration increases in the synaptic space, the performance antidepressant effect.A little less than other mediator effects, less to the unify influence of cardiovascular system of autonomic nerve system.
The oral easy absorption of paroxetine hydrochloride is not subjected to the influence of antiacid medicine or food, and oral 30mg, peak reaching time of blood concentration are 6.3 hours, and peak concentration is 17.6 μ g/ml, T
1/2Be 24 hours, apparent volume of distribution is 3-28L/kg.Plasma protein binding rate is 95%.7-14 reaches Cpss in day, and is distributed to each histoorgan rapidly.At liver metabolism, about 2% is discharged by urine with original shape, and all the other are discharged from urine with metabolite form, and fraction is from defecate.List marketing at present tablet only arranged, the clinical depression that is used for also can be treated obsession, panic disorder or social anxiety disorder.
The paroxetine hydrochloride disintegration of tablet time is long, and dissolution and dissolution rate are low, absorption difference, bioavailability is low, and the supplementary product consumption ratio is big, and child, old people, bed patient and dysphagia patients are taken inconvenience, compliance is poor, has influenced the performance of paroxetine hydrochloride therapeutical effect.
The present invention makes the paroxetine hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of paroxetine hydrochloride sheet, and the therapeutical effect of paroxetine hydrochloride is given full play to.
Summary of the invention
The paroxetine hydrochloride 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, 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, 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 paroxetine 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 paroxetine hydrochloride is (-)-anti--4-(4-fluorophenyl)-3-[[3 among the present invention, 4-(methylenedioxy group) phenoxy group] methyl]-piperidine hydrochlorate, molecular formula is C
19H
20NO
3FHcl, molecular weight are 365.84, 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
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), 1000ml is a solvent with hydrochloric acid solution (9 → 1000), rotating speed is that per minute 50 changes, operation in the time of 10,20,30,40 minutes, is got solution 20ml in accordance with the law, filter, get subsequent filtrate as need testing solution.Precision takes by weighing the about 23mg of paroxetine hydrochloride reference substance in addition, puts in the 100ml measuring bottle, adds above-mentioned solvent dilution to scale, shakes up, in contrast product solution.Measuring according to high performance liquid chromatography (two appendix VD of Chinese Pharmacopoeia version in 2000), is filler with the cyano group bonded silica gel; (get phosphatase 24 .9g with phosphate buffer, add water 800ml and make dissolving, regulate pH value to 6.0, be diluted with water to 1000ml again with the 0.1mol/L sodium hydroxide solution)-acetonitrile (1: 1) is a mobile phase, the detection wavelength is 295nm, and number of theoretical plate must not calculate by the paroxetine hydrochloride peak and is lower than 2000.Precision is measured each 20 μ l of above-mentioned two kinds of solution respectively, injects chromatograph of liquid respectively, and the record chromatogram is pressed external standard method with the calculated by peak area stripping quantity.
Two, commercially available paroxetine hydrochloride sheet testing result
1. disintegration time: 49 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 27.6 51.3 68.9 84.2
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 49.7 86.5 99.8 100.4
Four, example 2 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 53.6 91.2 99.6 99.3
Five, example 3 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 47.6 88.4 98.8 97.2
Six, example 4 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 41.3 79.6 95.4 98.7
Seven, example 5 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 42.5 89.4 93.6 99.2
Eight, example 6 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 55.4 86.6 99.7 98.0
The specific embodiment
One, example 1
Prescription:
Paroxetine hydrochloride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the paroxetine 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:
Paroxetine hydrochloride 5g
Macrogol 4000 15g
Make 1000
Method for making: the paroxetine 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:
Paroxetine hydrochloride 5g
Polyethylene glycol 6000 10g
Macrogol 4000 5g
Make 1000
Method for making: the paroxetine 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:
Paroxetine hydrochloride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the paroxetine 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:
Paroxetine hydrochloride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the paroxetine 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:
Paroxetine hydrochloride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that paroxetine 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. paroxetine hydrochloride drop pill and preparation method thereof is characterized in that: the paroxetine 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 paroxetine hydrochloride of claim 1 is (-)-anti--4-(4-fluorophenyl)-3-[[3,4-(methylenedioxy group) phenoxy group] methyl]-piperidine hydrochlorate, molecular formula is C
19H
20NO
3FHcl, molecular weight are 365.84, and 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 |
|---|---|---|---|
| CNA2004100444390A CN1568987A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of paroxetine hydrochloride and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100444390A CN1568987A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of paroxetine hydrochloride and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1568987A true CN1568987A (en) | 2005-01-26 |
Family
ID=34481889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2004100444390A Pending CN1568987A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of paroxetine hydrochloride and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1568987A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102302453A (en) * | 2011-09-14 | 2012-01-04 | 海南美大制药有限公司 | Paroxetine hydrochloride liposome solid preparation |
| CN110833533A (en) * | 2018-08-18 | 2020-02-25 | 郑州泰丰制药有限公司 | Preparation method of paroxetine hydrochloride enteric sustained-release dropping pill |
-
2004
- 2004-05-13 CN CNA2004100444390A patent/CN1568987A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102302453A (en) * | 2011-09-14 | 2012-01-04 | 海南美大制药有限公司 | Paroxetine hydrochloride liposome solid preparation |
| CN102302453B (en) * | 2011-09-14 | 2012-11-21 | 海南美大制药有限公司 | Paroxetine hydrochloride liposome solid preparation |
| CN110833533A (en) * | 2018-08-18 | 2020-02-25 | 郑州泰丰制药有限公司 | Preparation method of paroxetine hydrochloride enteric sustained-release dropping pill |
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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 |