CN101559059B - Pharmaceutical composition containing amiloride hydrochloride and preparation method thereof - Google Patents
Pharmaceutical composition containing amiloride hydrochloride and preparation method thereof Download PDFInfo
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- CN101559059B CN101559059B CN 200810104134 CN200810104134A CN101559059B CN 101559059 B CN101559059 B CN 101559059B CN 200810104134 CN200810104134 CN 200810104134 CN 200810104134 A CN200810104134 A CN 200810104134A CN 101559059 B CN101559059 B CN 101559059B
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- amiloride hydrochloride
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Abstract
The invention discloses a pharmaceutical composition containing amiloride hydrochloride and a preparation method thereof. The composition is prepared by melting the amiloride hydrochloride, poloxamer and polyvinylpyrrolidon. After other proper pharmaceutic adjuvants are added, the pharmaceutical composition can be prepared into capsules, tablets, granules and the like.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition that contains amiloride hydrochloride and preparation method thereof, also contain poloxamer and polyvinylpyrrolidone in this pharmaceutical composition.
Background technology
Amiloride hydrochloride has good guarantor's potassium row sodium function, and alternative acts on the cell inner membrance of renal tubules, can block sodium and get in the cell, thereby reduce lumen wall negative potential, makes K
+, H
+Drainage is obstructed and is shown guarantor K
+Effect.
Amiloride hydrochloride is oral after gastrointestinal absorption.Effect is 6～9 hours the half-life, and single oral onset time is 2 hours, and the serum-concentration peak time is 3-4 hour, and effectively the persistent period is 6～10 hours, and about 50% drains from urine with the prototype medicine, and 40% discharged with feces in 72 hours.
Because amiloride hydrochloride does not influence blood fat, blood glucose metabolism, no kidney decreases and protects the potassium diuresis, and its effect is strong, and rapid-action, dosage is little, and prospect is very wide.List marketing at present tablet only arranged, the clinical treatment edema disease that is mainly used in also can be used for the auxiliary treatment of intractable hypokalemia.
The amiloride hydrochloride bitter in the mouth, slightly soluble in water, its disintegration of tablet time is long, and dissolution and dissolution rate are low, absorption difference, bioavailability is low, has influenced the performance of amiloride hydrochloride therapeutical effect.
CN 1582937A discloses a kind of amiloride hydrochloride drop pill and preparation method thereof.This invention is processed the amiloride hydrochloride drop pill through superfine communication technique and dropping pill formulation technology.
The present invention adopts solid dispersion technology, and has added suitable adjuvant and prepared a kind of pharmaceutical composition that contains amiloride hydrochloride.It is poor that said composition has effectively solved amiloride hydrochloride solid preparation dissolution, the problem that bioavailability is low.
Summary of the invention
It is poor that pharmaceutical composition of the present invention is intended to solve amiloride hydrochloride solid preparation dissolution, the problem that bioavailability is low.
A kind of pharmaceutical composition that contains amiloride hydrochloride of the present invention has wherein also added pharmaceutic adjuvant poloxamer and polyvinylpyrrolidone.
Pharmaceutical composition of the present invention, wherein the ratio of amiloride hydrochloride and poloxamer (weight) is 1: 1～1: 9.
Pharmaceutical composition of the present invention, wherein the ratio of amiloride hydrochloride and poloxamer (weight) is 1: 2～1: 6.
Pharmaceutical composition of the present invention, wherein the ratio of amiloride hydrochloride and polyvinylpyrrolidone (weight) is 1: 0.1～1: 4.
Pharmaceutical composition of the present invention, wherein the ratio of amiloride hydrochloride and polyvinylpyrrolidone (weight) is 1: 0.5～1: 2.
Pharmaceutical composition of the present invention, the wherein preferred PVP-K30 of polyvinylpyrrolidone.
Pharmaceutical composition of the present invention is through its preparation of following method:
(1) amiloride hydrochloride and poloxamer are heated to fusion in 70 ℃ of water-baths, constantly stir, medicine is well dispersed in the carrier;
(2) rapid cooling curing takes out in 60 ℃ of drying under reduced pressure 4h;
(3) pulverize, cross 80 mesh sieves;
(4) add polyvinylpyrrolidone, mix promptly getting.
Pharmaceutical composition of the present invention, it can be prepared as capsule, tablet or granule.
The specific embodiment
Below in conjunction with embodiment the present invention is done further detailed description, but be not limited to following embodiment.Following " weight " is the amount of 1000 dosage units.
Embodiment 1
Composition weight
Amiloride hydrochloride 2.5g
Poloxamer 2.5g
PVP-K30 1.25g
Mannitol 80g
Microcrystalline Cellulose 63g
Magnesium stearate 0.75g
Total 150g
Method for preparing:
(1) amiloride hydrochloride and poloxamer are heated to fusion in 70 ℃ of water-baths, constantly stir, medicine is well dispersed in the carrier;
(2) rapid cooling curing takes out in 60 ℃ of drying under reduced pressure 4h;
(3) pulverize, cross 80 mesh sieves;
(4) add polyvinylpyrrolidone, mix promptly getting pharmaceutical composition.
(5) adding recipe quantity mannitol and microcrystalline Cellulose get mixture I in pharmaceutical composition;
(6) adding wetting agent water is an amount of among the mixture I, and the system soft material is crossed 18 mesh sieves and granulated;
After (7) 60 ℃ of dryings, cross 24 mesh sieve granulate;
(8) take by weighing magnesium stearate and dried granule mixing gets mixtures II;
(9) mixtures II is filled to capsule No. 2, gets final product.
Embodiment 2
Composition weight
Amiloride hydrochloride 2.5g
Poloxamer 22.5g
PVP-K30 10g
Starch 24.25g
Lactose 40g
Microcrystalline Cellulose 50g
Magnesium stearate 0.75g
Total 150g
Method for preparing:
(1) amiloride hydrochloride and poloxamer are heated to fusion in 70 ℃ of water-baths, constantly stir, medicine is well dispersed in the carrier;
(2) rapid cooling curing takes out in 60 ℃ of drying under reduced pressure 4h;
(3) pulverize, cross 80 mesh sieves;
(4) add polyvinylpyrrolidone, mix promptly getting pharmaceutical composition.
(5) in pharmaceutical composition, add recipe quantity starch, lactose and microcrystalline Cellulose get mixture I;
(6) adding wetting agent water is an amount of among the mixture I, and the system soft material is crossed 24 mesh sieves and granulated;
After (7) 60 ℃ of dryings, cross 30 mesh sieve granulate;
(8) take by weighing magnesium stearate by recipe quantity and dried granule mixing gets mixtures II;
(9) with mixtures II tabletting on tablet machine, get final product.
Embodiment 3
Composition weight
Amiloride hydrochloride 2.5g
Poloxamer 10g
PVP-K30 5g
Lactose 97.5g
Microcrystalline Cellulose 135g
Sucrose 250g
Method for preparing:
(1) amiloride hydrochloride and poloxamer are heated to fusion in 70 ℃ of water-baths, constantly stir, medicine is well dispersed in the carrier;
(2) rapid cooling curing takes out in 60 ℃ of drying under reduced pressure 4h;
(3) pulverize, cross 80 mesh sieves;
(4) add polyvinylpyrrolidone, mix promptly getting pharmaceutical composition.
(5) in pharmaceutical composition, add recipe quantity lactose, sucrose and microcrystalline Cellulose and get mixture I;
(6) adding wetting agent water is an amount of among the mixture I, and the system soft material is crossed 16 mesh sieves and granulated;
After (7) 60 ℃ of dryings, cross 20 mesh sieve granulate, packing gets final product.
The mensuration of pharmaceutical composition dissolubility
Assay method with reference to Chinese Pharmacopoeia version dissolubility in 2005; Measured the pharmaceutical composition (in the preparation of the ratio among the embodiment 3) of method preparation of the present invention and the dissolubility of corresponding proportion physical mixture, the result shows that the dissolubility of pharmaceutical composition is 3.9 times of physical mixture.This shows that the pharmaceutical composition for preparing through fusion method can improve the dissolubility of amiloride hydrochloride, thereby the curative effect that can guarantee amiloride hydrochloride can be brought into play effectively.
Claims (1)
1. granule that contains amiloride hydrochloride is characterized in that:
(1) amiloride hydrochloride and the poloxamer with recipe quantity is heated to fusion in 70 ℃ of water-baths, constantly stirs, and medicine is well dispersed in the carrier;
(2) rapid cooling curing takes out in 60 ℃ of drying under reduced pressure 4h;
(3) pulverize, cross 80 mesh sieves;
(4) add polyvinylpyrrolidone 5g, mix promptly getting granule;
(5) in granule, add recipe quantity lactose, sucrose and microcrystalline Cellulose and get mixture I;
(6) adding wetting agent water is an amount of in mixture I, and the system soft material is crossed 16 mesh sieves and granulated;
After (7) 60 ℃ of dryings, cross 20 mesh sieve granulate, packing gets final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200810104134 CN101559059B (en) | 2008-04-16 | 2008-04-16 | Pharmaceutical composition containing amiloride hydrochloride and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200810104134 CN101559059B (en) | 2008-04-16 | 2008-04-16 | Pharmaceutical composition containing amiloride hydrochloride and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101559059A CN101559059A (en) | 2009-10-21 |
| CN101559059B true CN101559059B (en) | 2012-12-05 |
Family
ID=41218150
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200810104134 Active CN101559059B (en) | 2008-04-16 | 2008-04-16 | Pharmaceutical composition containing amiloride hydrochloride and preparation method thereof |
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| Country | Link |
|---|---|
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102406785B (en) * | 2010-09-25 | 2013-07-31 | 吉林省利华制药有限公司 | Guyuling tablet pharmaceutical composition and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1173817A (en) * | 1995-10-26 | 1998-02-18 | 巴克·诺顿药物有限公司 | Method, compsns and kits for increasing the oral bioavilability of pharmaceuticalagents |
| CN1582937A (en) * | 2004-05-21 | 2005-02-23 | 南昌弘益科技有限公司 | Amiloride hydrochloride drops and their preparation |
| CN1695738A (en) * | 2005-04-04 | 2005-11-16 | 广州市施柏医药科技有限公司 | Compsn. of medication for treating high blood pressure |
| CN1901888A (en) * | 2003-12-01 | 2007-01-24 | 生命周斯药物公司 | Pharmaceutical compositions comprising lercanidipine |
-
2008
- 2008-04-16 CN CN 200810104134 patent/CN101559059B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1173817A (en) * | 1995-10-26 | 1998-02-18 | 巴克·诺顿药物有限公司 | Method, compsns and kits for increasing the oral bioavilability of pharmaceuticalagents |
| CN1901888A (en) * | 2003-12-01 | 2007-01-24 | 生命周斯药物公司 | Pharmaceutical compositions comprising lercanidipine |
| CN1582937A (en) * | 2004-05-21 | 2005-02-23 | 南昌弘益科技有限公司 | Amiloride hydrochloride drops and their preparation |
| CN1695738A (en) * | 2005-04-04 | 2005-11-16 | 广州市施柏医药科技有限公司 | Compsn. of medication for treating high blood pressure |
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| Publication number | Publication date |
|---|---|
| CN101559059A (en) | 2009-10-21 |
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