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Olmesartan ester liposome solid preparation

A technology of olmesartan medoxomil and olmesartan medoxomil, which is applied in the directions of liposome delivery, pill delivery, medical preparations of inactive ingredients, etc., can solve the problem of low bioavailability, long dissolution time, and many medication times and other problems, to achieve the effect of high bioavailability, good sustained release effect and excellent dissolution.

Inactive Publication Date: 2013-04-17
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Olmesartan medoxomil common compressed tablet is arranged in domestic and foreign marketed medicine at present, but this dosage form has the following problems: due to reasons such as preparation technology, the oral preparation of most medicines all exists long dissolving time after taking, dissolution rate is low, Poor absorption, many times of taking medicine, uncontrollable drug release, low bioavailability and other problems, which affect the efficacy of the drug and directly affect the therapeutic effect, so its bioavailability is low
[0013] Olmesartan medoxomil liposome and solid preparation thereof designed for oral application are not disclosed in the prior art

Method used

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  • Olmesartan ester liposome solid preparation
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  • Olmesartan ester liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1 Olmesartan Medoxomil Liposome Tablets

[0073] The raw and auxiliary materials used are as follows:

[0074]

[0075] Adopt the following production process to prepare Olmesartan Medoxomil liposome tablet:

[0076] (1) Accurately weigh 20g olmesartan medoxomil, 200g phosphatidylinositol, 100g distearoylphosphatidylglycerol, 50g cholesterol succinate, 40g Tween 80, dissolve in 1000ml methanol and In the acetone mixed solvent, stir to make it dissolve;

[0077] (2) Put the above solution in an eggplant-shaped bottle, remove methanol and acetone under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the wall of the bottle;

[0078] (3) Add 1000ml of acetate buffer solution with a pH value of 6.0 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;

[0079] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in a ...

Embodiment 2

[0083] Example 2 Olmesartan Medoxomil Liposome Tablets

[0084] The raw and auxiliary materials used are as follows:

[0085]

[0086] Adopt the following production process to prepare Olmesartan Medoxomil liposome tablet:

[0087] (1) Accurately weigh 20g olmesartan medoxomil, 400g phosphatidylinositol, 200g distearoylphosphatidylglycerol, 300g cholesterol succinate, 40g Tween 80, dissolve in 2000ml methanol and In the acetone mixed solvent, stir to make it dissolve;

[0088] (2) Put the above solution in an eggplant-shaped bottle, remove methanol and acetone under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the wall of the bottle;

[0089] (3) Add 2000ml of acetate buffer solution with a pH value of 6.0 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;

[0090] (4) Filter the above solution with a 0.45 μm microporous membrane, place the filtrate in a...

Embodiment 3

[0094] Example 3 Olmesartan Medoxomil Liposome Tablets

[0095] The raw and auxiliary materials used are as follows:

[0096]

[0097] Adopt following production process to prepare Olmesartan Medoxomil liposomal tablet:

[0098] (1) Accurately weigh 40g olmesartan medoxomil, 800g phosphatidylinositol, 400g distearoylphosphatidylglycerol, 600g cholesterol succinate, 80g Tween 80 and dissolve in 3000ml methanol and acetone with a volume ratio of 2:1 In the mixed solvent, stir to dissolve it;

[0099] (2) Put the above solution in an eggplant-shaped bottle, remove methanol and acetone under reduced pressure in a water bath at 45°C, and form a uniform transparent film on the wall of the bottle;

[0100] (3) Add 3000ml of acetate buffer solution with a pH value of 6.0 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;

[0101] (4) Filter the above solution with a 0.45 μm microporous membrane, p...

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Abstract

The invention discloses an olmesartan ester liposome solid preparation and a preparation method thereof. Active ingredient-olmesartan ester, particularly-combined phosphatidyl inositol, di-stearoyl phosphatidyl glycerol, cholesterol succinate and tween 80 are prepared into liposome, the stability, the dissolution rate and the bioavailability of the preparation is greatly increased, the action is stable and lasting, and the curative effect is significant. The product quality of the preparation is increased, and the toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a new preparation of olmesartan medoxomil, in particular to olmesartan medoxomil liposome and its solid preparation and preparation method, and belongs to the technical field of medicine. Background technique [0002] Hypertension is one of the most common and important cardiovascular diseases in clinical practice. According to a recent report by the International Society of Hypertension, there are about 1 billion people in the world suffering from high blood pressure or high blood pressure, which is equivalent to 26.4% of the adult population. With the continuous improvement of people's living standards, the prevalence of hypertension in my country is also increasing year by year. According to the epidemiological statistics of hypertension, the prevalence of hypertension among adults in my country has risen from 5.1% in 1959 to 11.68% at present. On the one hand, hypertension can be a clinical manifestation caused by differe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/127A61K31/4178A61K47/34A61P9/12A61K47/26
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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