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Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination

A technology of liposome preparation and hydrochlorothiazide, which is applied in the field of medicine, can solve the problems of liposome stability and poor encapsulation efficiency, and achieve the effects of excellent dissolution, high stability and high bioavailability

Inactive Publication Date: 2013-09-25
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The present inventor has studied carefully for a long time, and through a large number of screening experiments, finally screened the combination of these three materials of soybean lecithin, octadecylamine and cholesterol acetyl ester, found the combination of these three materials unexpectedly, solved the problem of The technical problems of liposome stability and poor encapsulation efficiency have obtained unexpected formulation effects, thus providing liposomes with good quality

Method used

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  • Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination
  • Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination
  • Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Example 1 Preparation of Benazepril / Hydrochlorothiazide Liposomal Tablets

[0085] The raw and auxiliary materials used in the prescription (1000 tablets) are as follows:

[0086]

[0087] Preparation Process

[0088] (1) 250g soybean lecithin, 100g octadecylamine and 25g cholesterol acetyl ester are dissolved in the mixed solvent of acetonitrile and dichloromethane that the volume ratio of 1000ml is 2: 3, obtain lipid solution;

[0089] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 55° C. to form a uniform lipid film;

[0090] (3) Disperse 5 g of benazepril hydrochloride and 6.25 g of hydrochlorothiazide in 500 ml of water, add them to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0091] (4) Place the above-mentioned suspension in an ultr...

Embodiment 2

[0096] Example 2 Preparation of Benazepril / Hydrochlorothiazide Liposomal Tablets

[0097] The raw and auxiliary materials used in the prescription (1000 tablets) are as follows:

[0098]

[0099] Preparation Process

[0100] (1) 700g soybean lecithin, 350g octadecylamine and 200g cholesterol acetyl ester are dissolved in the mixed solvent of acetonitrile and dichloromethane that 2000ml volume ratio is 2: 3, obtain lipid solution;

[0101] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 45° C. to form a uniform lipid film;

[0102] (3) Disperse 5 g of benazepril hydrochloride and 6.25 g of hydrochlorothiazide in 500 ml of water, add them to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0103] (4) Place the above-mentioned suspension in an ultrasonic...

Embodiment 3

[0108] Example 3 Preparation of Benazepril / Hydrochlorothiazide Liposomal Tablets

[0109] The raw and auxiliary materials used in the prescription (1000 tablets) are as follows:

[0110]

[0111] Preparation Process

[0112] (1) 600g soybean lecithin, 300g octadecylamine and 80g cholesterol acetyl ester are dissolved in the mixed solvent of acetonitrile and dichloromethane that 1500ml volume ratio is 2: 3, obtain lipid solution;

[0113] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 50° C. to form a uniform lipid film;

[0114] (3) Disperse 10 g of benazepril hydrochloride and 12.5 g of hydrochlorothiazide in 600 ml of water, add them to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0115] (4) Place the above-mentioned suspension in an ultrasonic...

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Abstract

The invention discloses a liposome solid preparation of benazepril / hydrochlorothiazide and a preparation method thereof. The liposome solid preparation is prepared mainly by the liposome made of 1 portion of hydrochloric acid benazepril, 1.25 portions of hydrochlorothiazide, 50-200 portions of soya bean lecithin, 20-100 portions of octadecylamine and 5-60 portions of cholesterol acetyl lipide measured based on weight, the benazepril / hydrochlorothiazide liposome, and the other excipients typically used in pharmacy. According to the invention, the product quality of the preparation is improved, the toxic and side effects are reduced, the stability, dissolution and bioavailability of the medicine are greatly improved, and a stable and enduring function and remarkable therapeutic effects are achieved.

Description

technical field [0001] The invention relates to a compound preparation of benazepril / hydrochlorothiazide, in particular to a solid preparation of a pharmaceutical composition of benazepril / hydrochlorothiazide and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the diseases with the highest morbidity and mortality in the world today. They are the leading cause of death and the number one killer of health. The incidence of cardiovascular system diseases in my country is basically the same as that in the world, showing an upward trend year by year. From the 7th cause of death in the 1960s to the 1st, 3 million people die from cardiovascular and cerebrovascular diseases every year, and 10 million people become disabled due to cardiovascular and cerebrovascular diseases. Almost every cardiovascular and cerebrovascular patient has clinical symptoms of elevated blood pres...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/20A61K9/48A61K31/55A61K47/28A61K47/24A61K47/18A61P9/12A61P9/00A61K31/549
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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