CN1528296A - Pilocarpine nitrate drop pill and preparing method thereof - Google Patents
Pilocarpine nitrate drop pill and preparing method thereof Download PDFInfo
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- CN1528296A CN1528296A CNA2003101009378A CN200310100937A CN1528296A CN 1528296 A CN1528296 A CN 1528296A CN A2003101009378 A CNA2003101009378 A CN A2003101009378A CN 200310100937 A CN200310100937 A CN 200310100937A CN 1528296 A CN1528296 A CN 1528296A
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- pilocarpine nitrate
- pilocarpine
- coolant
- nitrate
- pill
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Abstract
The present invention utilizes ultramicropulverization and dripping pill preparation production process to make pilocarpine nitrate dripping pills, and can attain the goal of raising disintegration and dissolution speed, quickly obtaining therapeutic effect, raising stability of medicine, reducing dose of auxiliary material, reducing production cost and convenient administration. Said pill not only can be sucked, but also can be swallowed, and its compliance property is good.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically pilocarpine nitrate drop pill and preparation method thereof.
Background technology
Pilocarpine nitrate is anti-xerostomia disease medicine, chance light is perishable, 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 pilocarpine nitrate therapeutical effect.
The present invention makes the pilocarpine nitrate drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of determination of pilocarpine nitrate tablets, and the therapeutical effect of pilocarpine nitrate is given full play to.
Summary of the invention
The pilocarpine nitrate 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 child, the old people, the characteristics that 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 pilocarpine nitrate fine powder of 1 weight portion through micronizing is added in 5～20 weight portion molten matrix, fully mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
The molecular formula of pilocarpine nitrate among the present invention (Pilocarpine Nitrate) is C
11H
16N
2O
2HNO
3
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 water 500ml is solvent, rotating speed is that per minute 100 changes, drop into 2 (2) in each commentaries on classics basket and operate in accordance with the law, in the time of 5,10,20,30,45 minutes, get solution 10ml, filter, get subsequent filtrate as need testing solution.It is an amount of that other gets the pilocarpine reference substance, and accurate the title decides, and makes the solution that every 1ml contains 8 μ g approximately, product solution in contrast with water dissolution and dilution.According to high performance liquid chromatography (two appendix VD of Chinese Pharmacopoeia version in 2000), with octadecylsilane chemically bonded silica is filler, after being dissolved in water into 600ml (pH 4.5) with sodium acetate 2.94g and spirit of vinegar 38.4ml, adding the solution that methanol 400ml makes is mobile phase; The detection wavelength is 230nm.Number of theoretical plate is pressed the pilocarpine peak and is calculated and should not hang down 1000.
Precision is measured need testing solution and each 10 μ l of reference substance solution, and the inhalant liquid chromatography writes down chromatogram respectively, calculates stripping quantity by external standard method.
Two, commercially available determination of pilocarpine nitrate tablets testing result
1. disintegration time: 37 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 25.4 35.6 58.3 81.2 90.4
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 47.5 79.6 93.4 100.7 99.6
Four, example 2 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 43.5 72.3 89.4 98.6 99.7
Five, example 3 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 51.2 79.6 97.8 101.6 100.3
Six, example 4 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 38.5 67.2 81.3 94.6 98.7
Seven, example 5 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 40.6 58.9 79.3 95.4 99.7
Eight, example 6 sample detection results
1. the molten diffusing time: 9 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 45.4 67.2 85.3 98.6 97.8
The specific embodiment
One, example 1
Prescription:
Pilocarpine nitrate 2g
Polyethylene glycol 6000 18g
Make 1000
Method for making: the pilocarpine nitrate 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:
Pilocarpine nitrate 2g
Macrogol 4000 18g
Make 1000
Method for making: the pilocarpine nitrate 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:
Pilocarpine nitrate 2g
Polyethylene glycol 6000 5g
Macrogol 4000 13g
Make 1000
Method for making: the pilocarpine nitrate 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:
Pilocarpine nitrate 2g
Glyceryl monostearate 18g
Make 1000
Method for making: the pilocarpine nitrate 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:
Pilocarpine nitrate 2g
Polyethylene glycol 6000 13g
Poloxamer 5g
Make 1000
Method for making: the pilocarpine nitrate 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:
Pilocarpine nitrate 2g
Glyceryl monostearate 15g
Poloxamer 3g
Make 1000
Method for making: get the mixing fine powders that pilocarpine nitrate 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. pilocarpine nitrate drop pill and preparation method thereof is characterized in that: the pilocarpine nitrate fine powder of 1 weight portion through micronizing is added in 5～20 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 pilocarpine nitrate Pilocarpine of claim 1 Nitrate is C
11H
16N
2O
2HNO
3
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 |
|---|---|---|---|
| CNA2003101009378A CN1528296A (en) | 2003-10-06 | 2003-10-06 | Pilocarpine nitrate drop pill and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101009378A CN1528296A (en) | 2003-10-06 | 2003-10-06 | Pilocarpine nitrate drop pill and preparing method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1528296A true CN1528296A (en) | 2004-09-15 |
Family
ID=34304121
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2003101009378A Pending CN1528296A (en) | 2003-10-06 | 2003-10-06 | Pilocarpine nitrate drop pill and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1528296A (en) |
-
2003
- 2003-10-06 CN CNA2003101009378A patent/CN1528296A/en active Pending
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