CN1528295A - Indapamide drop pill and preparing method thereof - Google Patents
Indapamide drop pill and preparing method thereof Download PDFInfo
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- CN1528295A CN1528295A CNA2003101009363A CN200310100936A CN1528295A CN 1528295 A CN1528295 A CN 1528295A CN A2003101009363 A CNA2003101009363 A CN A2003101009363A CN 200310100936 A CN200310100936 A CN 200310100936A CN 1528295 A CN1528295 A CN 1528295A
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- indapamide
- coolant
- pill
- polyethylene glycol
- drop pill
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Abstract
The present invention utilizes ultramicropulverization and dripping pill preparation production process to make indapamide 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 and ministration. 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 indapamide drop pill and preparation method thereof.
Background technology
Indapamide is a kind of sulfonamides diuretic, plays a role by water of absorption again and the electrolyte that suppresses distal renal tubular cortex dilution section.Hypotensive effect is not bright, and its diuresis can not be explained hypotensive effect, may be the interior stream of calcium of regulating vascular smooth muscle cell, stimulates prostate PGE
2With prostaglandin PGI
2Synthetic, lower the hypersensitivity of blood vessel, thereby suppress vasoconstriction, influence little or nothing to cardiac output, heart rate and the rhythm of the heart during blood pressure lowering the blood vessel pressor amine, life-time service seldom influences glomerular filtration rate or renal blood flow, does not influence the metabolism of blood fat and carbohydrate.
The indapamide oral absorption is fast, and bioavailability reaches 93% and complete, the influence of unable to take food thing, and plasma protein binding rate is 71%～79%, also combines with the elastoser of vascular smooth muscle.Reached the peak hypotensive effect after the single oral dose in about 24 hours; Reach the peak effect about 8-12 week of multiple dosing, effect was kept for 8 weeks, and the half-life is 14-18 hour, at the liver intracellular metabolite, produce 19 kinds of metabolites, about 70% through renal excretion, wherein 7% is original shape, and 23% through the gastrointestinal tract discharge, and renal failure person's pharmacokinetic parameter is provided with change.The clinical hypertension that is used for the treatment of.
The indapamide odorless, tasteless, almost insoluble in water, its 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 indapamide therapeutical effect.
The present invention makes the indapamide drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of indapamide sheet, and the therapeutical effect of indapamide is given full play to.
Summary of the invention
The indapamide 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 indapamide fine powder of 1 weight portion through micronizing is added in 5～20 weight portion molten matrix, abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
The chemical name of indapamide among the present invention (Indapamide) is N-(2-methyl-2,3-dihydro-1H-indyl)-3-sulfamoyl-4-chloro-Benzoylamide, and molecular formula is C
16H
16ClN
3O
3S, molecular weight are 365.83, 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), 900ml is a solvent with alcohol-water (5: 895), rotating speed is that per minute 75 changes, and operation in accordance with the law is in the time of 10,20,30,40,50 minutes, get solution 10ml, filter, get filtrate, measure trap at the wavelength place of 242nm according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A); Precision takes by weighing the indapamide reference substance 25mg that is dried to constant weight through 105 ℃ in addition, puts in the 50ml measuring bottle, adds dissolve with ethanol and is diluted to scale, shake up, precision is measured 10ml, puts in the 100ml measuring bottle, thin up is to scale, shake up, precision is measured 5ml, puts in the 100ml measuring bottle, thin up is to scale, shake up, measure, calculate stripping quantity with method.
Two, commercially available indapamide sheet testing result
1. disintegration time: 68 minutes
2. dissolution rate:
Time (minute) 10 20 30 40 50
Dissolution (%) 23.4 37.6 51.2 60.5 71.2
Three, example 1 sample detection result
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40 50
Dissolution (%) 43.6 68.4 92.5 99.7 98.6
Four, example 2 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate:
Time (minute) 10 20 30 40 50
Dissolution (%) 38.4 57.2 90.3 98.6 97.1
Five, example 3 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40 50
Dissolution (%) 43.6 67.5 89.6 98.9 101.2
Six, example 4 sample detection results
1. the molten diffusing time: 9 minutes
2. dissolution rate:
Time (minute) 10 20 30 40 50
Dissolution (%) 35.3 59.2 87.5 97.6 98.4
Seven, example 5 sample detection results
1. the molten diffusing time: 7 minutes
2. dissolution rate:
Time (minute) 10 20 30 40 50
Dissolution (%) 41.3 62.5 84.6 98.7 99.0
Eight, example 6 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate
Time (minute) 10 20 30 40 50
Dissolution (%) 32.1 58.6 79.4 95.3 98.1
The specific embodiment
One, example 1
Prescription:
Indapamide 2.5g
Polyethylene glycol 6000 18g
Make 1000
Method for making: the indapamide 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:
Indapamide 2.5g
Macrogol 4000 18g
Make 1000
Method for making: the indapamide 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:
Indapamide 2.5g
Polyethylene glycol 6000 8g
Macrogol 4000 10g
Make 1000
Method for making: the indapamide 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:
Indapamide 2.5g
Glyceryl monostearate 18g
Make 1000
Method for making: the indapamide 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:
Indapamide 2.5g
Polyethylene glycol 6000 13g
Poloxamer 5g
Make 1000
Method for making: the indapamide 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:
Indapamide 2.5g
Glyceryl monostearate 16g
Poloxamer 2g
Make 1000
Method for making: get the mixing fine powders that indapamide 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. indapamide drop pill and preparation method thereof is characterized in that: the indapamide fine powder of 1 weight portion through micronizing is added in 5～20 weight portion molten matrix, and abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the molecular formula of the described indapamide Indapamide of claim 1 is C
16H
16ClN
3O
3S, molecular weight are 365.83, 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 |
|---|---|---|---|
| CNA2003101009363A CN1528295A (en) | 2003-10-06 | 2003-10-06 | Indapamide drop pill and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2003101009363A CN1528295A (en) | 2003-10-06 | 2003-10-06 | Indapamide drop pill and preparing method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1528295A true CN1528295A (en) | 2004-09-15 |
Family
ID=34304120
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2003101009363A Pending CN1528295A (en) | 2003-10-06 | 2003-10-06 | Indapamide drop pill and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1528295A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100339076C (en) * | 2004-07-09 | 2007-09-26 | 天津美伦医药集团有限公司 | Indapamide dripping pills, and its prepn. method |
-
2003
- 2003-10-06 CN CNA2003101009363A patent/CN1528295A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100339076C (en) * | 2004-07-09 | 2007-09-26 | 天津美伦医药集团有限公司 | Indapamide dripping pills, and its prepn. method |
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| WD01 | Invention patent application deemed withdrawn after publication |