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Amlodipine/benazepril medicament composition liposome solid preparation

A technology of amlodipine and liposome, which is applied in the field of medicine, can solve the problems of low bioavailability, long dissolution time, and influence on the therapeutic effect, and achieve high bioavailability, excellent dissolution, and good sustained-release effect Effect

Inactive Publication Date: 2013-05-29
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are amlodipine and benazepril ordinary compressed tablets in the domestic marketed drugs, but these dosage forms have the following problems: due to reasons such as preparation technology, most oral preparations of drugs have long dissolution time and dissolution low drug efficacy, poor absorption, frequent doses, uncontrollable drug release, hepatoenteric first-pass effect, and low bioavailability, which affect the efficacy of the drug and directly affect the therapeutic effect, so its bioavailability is low
[0017] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Amlodipine/benazepril medicament composition liposome solid preparation
  • Amlodipine/benazepril medicament composition liposome solid preparation
  • Amlodipine/benazepril medicament composition liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Example 1 Amlodipine / Benazepril Liposomal Tablets

[0091]

[0092] Adopt the following production process to prepare amlodipine / benazepril liposome tablet:

[0093] (1) Accurately weigh 5g amlodipine besylate, 10g benazepril hydrochloride, 300g phosphatidylethanolamine, 150g dioleoylphosphatidylglycerol, 450g cholesterol, 60g sodium deoxycholate, dissolve in 1000ml volume ratio of In a 2:1 mixed solvent of tert-butanol and methanol, stir to dissolve;

[0094] (2) Place the above solution in an eggplant-shaped bottle, remove tert-butanol and methanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0095] (3) Add 1000ml of acetate buffer solution with a pH value of 6.5 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0096] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in a -20°C ...

Embodiment 2

[0100] Example 2 Amlodipine / Benazepril Liposomal Tablets

[0101]

[0102] Adopt following production process to prepare amlodipine / benazepril liposomal tablet:

[0103] (1) Accurately weigh 2.5g amlodipine besylate, 10g benazepril hydrochloride, 300g phosphatidylethanolamine, 150g dioleoylphosphatidylglycerol, 450g cholesterol, 60g sodium deoxycholate, dissolve in 1000ml volume ratio In a 2:1 mixed solvent of tert-butanol and methanol, stir to dissolve it;

[0104] (2) Place the above solution in an eggplant-shaped bottle, remove tert-butanol and methanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0105] (3) Add 1000ml of acetate buffer solution with a pH value of 6.5 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0106] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in a -20°C r...

Embodiment 3

[0110] Example 3 Amlodipine / Benazepril Liposomal Tablets

[0111]

[0112] Adopt following production process to prepare amlodipine / benazepril liposomal tablet:

[0113] (1) Accurately weigh 5g amlodipine besylate, 10g benazepril hydrochloride, 700g phosphatidylethanolamine, 350g dioleoylphosphatidylglycerol, 525g cholesterol, 200g sodium deoxycholate and dissolve them in 1200ml with a volume ratio of 2 : 1 in a mixed solvent of tert-butanol and methanol, stirred to dissolve;

[0114] (2) Place the above solution in an eggplant-shaped bottle, remove tert-butanol and methanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0115] (3) Add 1200ml of acetate buffer solution with a pH value of 6.5 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0116] (4) Filter the above solution with a 0.45 μm microporous membrane, place the fi...

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PUM

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Abstract

The invention discloses an amlodipine / benazepril medicament composition liposome solid preparation and a preparation method thereof. The liposome is prepared by combining active components of benzenesulfonic acid amlodipine, benzepril hydrochloride and specific combination of phosphatidyl ethanolamine, dioleoyl phosphatidylglycerol, cholesterol and deoxysodium cholate, so that the stability, dissolution and bioavailability of the medicament are greatly improved, and the effect is stable and durable, and the curative effect is obvious. By utilizing the amlodipine / benazepril medicament composition liposome solid preparation, the quality of the product is improved, and the toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a novel solid preparation of amlodipine / benazepril combination, in particular to a liposome solid preparation of amlodipine / benazepril combination 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 pressure and needs...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/55A61K31/4422A61K9/127A61K9/20A61K47/24A61K47/28A61P9/00
Inventor 杨明贵刘斌
Owner HAINAN MEILAN SMITH KLINE PHARMA
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