CN1526382A - Sertraline hydrochloride dripping pills and the prepn - Google Patents
Sertraline hydrochloride dripping pills and the prepn Download PDFInfo
- Publication number
- CN1526382A CN1526382A CNA031595553A CN03159555A CN1526382A CN 1526382 A CN1526382 A CN 1526382A CN A031595553 A CNA031595553 A CN A031595553A CN 03159555 A CN03159555 A CN 03159555A CN 1526382 A CN1526382 A CN 1526382A
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- CN
- China
- Prior art keywords
- sertraline hydrochloride
- coolant
- polyethylene glycol
- preparation
- dissolution
- Prior art date
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention is Sertraline hydrochloride dripping pill prepared through superfine crushing and dripping pill producing process. The Sertraline hydrochloride dripping pill has raised disintegrating and dissolving speed, high digestion rate and digestion degree, fast acting, high stability, reduced supplementary material consumption, low production cost and easy carrying about and taking. It may be sucked in mouth or swallowed, has excellent conformity and is especially suitable for children, the aged and other patients with dysphagia.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically sertraline hydrochloride drop pill and preparation method thereof.
Background technology
Sertraline hydrochloride is the reuptake of the alternative central nervous system of inhibition to 5-hydroxy tryptamine, and 5-hydroxy tryptamine concentration increases in the synaptic space thereby make, the performance antidepressant effect.
The oral easy absorption of sertraline hydrochloride, peak reaching time of blood concentration is 6-10 hour, t
1/2Be about 26 hours, the 4-7 day of taking medicine can reach stabilised blood concentration.Plasma protein binding rate is 97%, and at liver metabolism, metabolite is the N-Desmethylsertraline, and activity is 1/10 of female medicine, is mainly discharged by urine.List marketing at present tablet only arranged, the clinical depression that is used for also can be used for treating obsession.
Sertraline hydrochloride sheet disintegration 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 sertraline hydrochloride therapeutical effect.
The present invention makes the sertraline hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of sertraline hydrochloride sheet, and the therapeutical effect of sertraline hydrochloride is given full play to.
Summary of the invention
The sertraline 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 sertraline 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.
Sertraline hydrochloride among the present invention (Sertraline Hydrochloride) chemical name is (1s-cis)-4-(3, the 4-Dichlorobenzene base)-1,2,3,4-tetrahydrochysene-N-methyl isophthalic acid-naphthylamine hydrochloride, and molecular formula is C
17H
17NCl
2HCl, molecular weight are 342.70, 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), (get glacial acetic acid 2.8ml with sodium-acetate buffer, add water to 1000ml, regulating pH to 4.5 with 50% sodium hydroxide solution) 900ml is solvent, Revolution Per Minute 75 changes, operation in accordance with the law, through 5,10,20, in the time of 30 and 45 minutes, it is an amount of to get solution, filter, get subsequent filtrate, according to high performance liquid chromatography (two appendix VD of Chinese Pharmacopoeia version in 2000) as need testing solution, with octadecylsilane chemically bonded silica is filler, with acetonitrile-methanol-buffer (0.045mol/L acetum and 0.025mol/L triethylamine solution mixed in equal amounts) (40: 40: 20) is mobile phase, and the detection wavelength is 267nm, and number of theoretical plate calculates by the sertraline hydrochloride peak should be not less than 1200.It is an amount of that in addition precision takes by weighing the sertraline hydrochloride reference substance, with the mobile phase dissolving and quantitatively dilution make the solution product solution in contrast that contains 0.1mg among every 1ml.Precision is measured need testing solution and each 20 μ l of reference substance solution, injects chromatograph of liquid respectively, and by external standard method, with calculated by peak area, the result multiply by 0.8949, calculates stripping quantity.
Two, commercially available sertraline hydrochloride sheet testing result
1. disintegration time: 54 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 21.6 35.4 42.5 67.8 81.3
Three, example 1 sample detection result
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 52.4 79.6 92.5 98.6 97.4
Four, example 2 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 53.7 75.2 88.3 98.6 97.8
Five, example 3 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 54.5 85.2 98.7 97.5 99.2
Six, example 4 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 49.3 78.6 89.2 98.4 100.6
Seven, example 5 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 45.3 72.5 86.4 97.2 98.6
Eight, example 6 sample detection results
1. the molten diffusing time: 15 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 49.6 67.5 86.3 98.4 98.7
The specific embodiment
One, example 1
Prescription:
Sertraline hydrochloride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the sertraline 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:
Sertraline hydrochloride 5g
Macrogol 4000 15g
Make 1000
Method for making: the sertraline 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:
Sertraline hydrochloride 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the sertraline 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:
Sertraline hydrochloride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the sertraline 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:
Sertraline hydrochloride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the sertraline 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:
Sertraline hydrochloride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that sertraline 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. sertraline hydrochloride drop pill and preparation method thereof is characterized in that: the sertraline 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 sertraline hydrochloride of claim 1 is C
17H
17NCl
2HCl, molecular weight are 342.70, 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 |
|---|---|---|---|
| CNA031595553A CN1526382A (en) | 2003-09-23 | 2003-09-23 | Sertraline hydrochloride dripping pills and the prepn |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031595553A CN1526382A (en) | 2003-09-23 | 2003-09-23 | Sertraline hydrochloride dripping pills and the prepn |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1526382A true CN1526382A (en) | 2004-09-08 |
Family
ID=34287330
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031595553A Pending CN1526382A (en) | 2003-09-23 | 2003-09-23 | Sertraline hydrochloride dripping pills and the prepn |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1526382A (en) |
-
2003
- 2003-09-23 CN CNA031595553A patent/CN1526382A/en active Pending
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| 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 |