CN1493288A - Hanfangchin A drip pill and its preparation method - Google Patents
Hanfangchin A drip pill and its preparation method Download PDFInfo
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- CN1493288A CN1493288A CNA031576680A CN03157668A CN1493288A CN 1493288 A CN1493288 A CN 1493288A CN A031576680 A CNA031576680 A CN A031576680A CN 03157668 A CN03157668 A CN 03157668A CN 1493288 A CN1493288 A CN 1493288A
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- retrandrine
- preparation
- coolant
- polyethylene glycol
- pill
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Abstract
A dripping pill of fanchinin and its superfine pulverizing process for preparing it are disclosed. Its advantages are high dissolving and disintegrating speed, high stripping percentage, quickly taking its effect and low cost.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically retrandrine drop pill and preparation method thereof.
Background technology
Retrandrine (Tetrandrine) is for extracting a kind of alkaloid that obtains in the root of menispermaceae plant powder Radix Stephaniae Tetrandrae (stone Bufo siccus) StcphaniaTctrandra Smoorc.Retrandrine plays analgesic activity by reducing peroxide release and cytophagous activity; Can also increase chemotherapeutics gathering in tumor cell by suppressing tumor drug resistance cell surface P-glycoprotein overexpression function, strengthen the sensitivity of tumor cell chemotherapeutics.
Retrandrine can make loose, the degraded of silicosis collagen fiber, and lipid reduces, and micro-tubular structure disappears, depolymerization, and precollagen transforms and is obstructed, and occurs new cell in the gap.
Retrandrine mainly is distributed in histoorgans such as liver, lung, kidney after absorbing.Internal metabolism becomes two-compartment model, and major part exists with original shape, and the small part metabolic conversion is retrandrine-N-oxide isomer and N-2-demethyl retrandrine, half-life (t in the body
1/2) be 90 minutes, clearance rate (CL) is 38.6Lkg
-1H
-1
List marketing at present retrandrine coated tablet and Film coated tablets, clinical rheumatalgia, arthralgia, the neuralgia of being used for arranged.Be used for pulmonary carcinoma with low dose radiation merging; Also be used for simple silicosis I, II, III phase and each phase quartz lung.
Water insoluble, the odorless of retrandrine, it is little sweet to distinguish the flavor of.Retrandrine sheet disintegration time is long, and dissolution and dissolution rate are 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 retrandrine therapeutical effect.
The present invention makes the retrandrine drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of retrandrine sheet, and the therapeutical effect of retrandrine is given full play to.
Summary of the invention
The retrandrine 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 retrandrine 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.
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 first methods of Chinese Pharmacopoeia version in 2000), with 0.1mol/L hydrochloric acid solution 600ml is solvent, and rotating speed is that per minute 100 changes, operation in accordance with the law, in the time of 5,10,20,30 and 45 minutes, get solution and filter, get subsequent filtrate, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), wavelength place at 280nm measures trap, presses C
38H
42N
2O
6Absorptance (E
1cm 1%) be 111 calculating stripping quantities.
Two, commercially available retrandrine sheet testing result
1. disintegration time: 45 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 20.3 31.5 52.3 69.2 82.5
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 61.4 85.6 97.8 99.2 99.6
Four, example 2 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 65.3 82.5 93.6 97.8 98.4
Five, example 3 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 65.6 83.2 95.4 98.5 99.6
Six, example 4 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 58.4 79.2 93.5 98.7 97.6
Seven, example 5 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 60.3 79.2 95.6 96.7 98.2
Eight, example 6 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 63.5 82.4 93.5 97.6 99.1
The specific embodiment
One, example 1
Prescription:
Retrandrine 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the retrandrine 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:
Retrandrine 5g
Macrogol 4000 15g
Make 1000
Method for making: the retrandrine 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:
Retrandrine 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the retrandrine 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:
Retrandrine 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the retrandrine 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:
Retrandrine 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the retrandrine 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:
Retrandrine 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that retrandrine 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 (3)
1. retrandrine drop pill and preparation method thereof is characterized in that: the retrandrine 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 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.
3. 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 |
|---|---|---|---|
| CNA031576680A CN1493288A (en) | 2003-09-06 | 2003-09-06 | Hanfangchin A drip pill and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031576680A CN1493288A (en) | 2003-09-06 | 2003-09-06 | Hanfangchin A drip pill and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1493288A true CN1493288A (en) | 2004-05-05 |
Family
ID=34240895
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031576680A Pending CN1493288A (en) | 2003-09-06 | 2003-09-06 | Hanfangchin A drip pill and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1493288A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108904500A (en) * | 2018-08-13 | 2018-11-30 | 河北工业大学 | Bis ether bond type BBI is inhibiting application and drug in Kv10.1 ion channel activity |
-
2003
- 2003-09-06 CN CNA031576680A patent/CN1493288A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108904500A (en) * | 2018-08-13 | 2018-11-30 | 河北工业大学 | Bis ether bond type BBI is inhibiting application and drug in Kv10.1 ion channel activity |
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| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |