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Losartan potassium liposome solid preparation

A technology for losartan potassium ester and solid preparation, which is applied in the field of medicine and achieves the effects of improving stability, high encapsulation efficiency and simple preparation process

Inactive Publication Date: 2012-07-18
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Losartan potassium liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Losartan Potassium Liposome Tablets

[0053] Prescription (1000 tablets)

[0054]

[0055] Preparation Process:

[0056] (1) 50g of losartan potassium, 48g of phosphatidylinositol, 16g of dimyristoyl lecithin and 28g of cholesterol are dissolved in 300ml of absolute ethanol, stirred and dissolved to obtain a lipid solution;

[0057] (2) Pour the above-mentioned lipid solution into a pear-shaped bottle, remove absolute ethanol by rotary evaporation in a constant temperature water bath at 40-50°C, and form a uniform lipid film on the bottle wall;

[0058] (3) Pour 400ml of phosphate buffer solution with a pH of 5.0 into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in the buffer solution for dissolving, to obtain a liposome suspension;

[0059] (4) Filter the above suspension with a filter membrane with a pore size of 0.45 μm, collect the filtrate, freeze the filtrate in a refrigerator at -20°C for 10-24 hours, free...

Embodiment 2

[0067] Example 2 losartan potassium liposomal tablets

[0068] Prescription (1000 tablets)

[0069]

[0070] Preparation Process:

[0071] (1) 100g of losartan potassium, 42g of phosphatidylinositol, 14g of dimyristoyl lecithin and 16g of cholesterol are dissolved in 600ml of absolute ethanol, stirred and dissolved to obtain a lipid solution;

[0072] (2) Pour the above-mentioned lipid solution into a pear-shaped bottle, remove absolute ethanol by rotary evaporation in a constant temperature water bath at 40-50°C, and form a uniform lipid film on the bottle wall;

[0073] (3) Pour 800ml of phosphate buffer solution with a pH of 5.0 into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in the buffer solution for dissolving, to obtain a liposome suspension;

[0074] (4) Filter the above suspension with a filter membrane with a pore size of 0.45 μm, collect the filtrate, freeze the filtrate in a refrigerator at -20°C for 10-24 hours, fr...

Embodiment 3

[0082] Example 3 Losartan Potassium Liposome Capsules

[0083] Prescription (1000 capsules)

[0084]

[0085] Preparation Process:

[0086] (1) 100g of losartan potassium, 60g of phosphatidylinositol, 20g of dimyristoyl lecithin and 40g of cholesterol are dissolved in 600ml of absolute ethanol, stirred and dissolved to obtain a lipid solution;

[0087] (2) Pour the above-mentioned lipid solution into a pear-shaped bottle, remove absolute ethanol by rotary evaporation in a constant temperature water bath at 40-50°C, and form a uniform lipid film on the bottle wall;

[0088] (3) Pour 800ml of phosphate buffer solution with a pH of 5.0 into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in the buffer solution for dissolving, to obtain a liposome suspension;

[0089] (4) Filter the above suspension with a filter membrane with a pore size of 0.45 μm, collect the filtrate, freeze the filtrate in a refrigerator at -20°C for 10-24 hours, f...

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Abstract

The invention discloses a losartan potassium liposome solid preparation and a preparation method thereof. Excellent quality of losartan potassium liposome is prepared by selecting specific weight proportions of losartan potassium, phosphatidylinositol, dimyristoyl lecithin and cholesterol, and then the losartan potassium liposome is prepared into a solid preparation by a general preparation method. Compared with the existing preparation, the liposome solid preparation provided by the invention has a high encapsulating rate and a uniform grain size, the medicine is maintained in blood circulation for a long time, apparently the stability and the bioavailability of the preparation product are improved, the quality of the preparation product is improved, and toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a new solid preparation of losartan potassium, in particular to a solid preparation of losartan potassium liposome and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Hypertension is one of the most common cardiovascular diseases in the world today and the leading cause of death and disability in adults. Due to the improvement of people's living standards and the increasingly tense job competition, the number of people suffering from high blood pressure has greatly increased. The prevalence of hypertension in my country has increased significantly. According to statistics from my country, my country has become the country with the most serious hazards of hypertension in the world. Hypertension can cause damage to the heart, brain, kidney and other organs, seriously threatening human health and life. [0003] Sartan drugs are first-line antihypertensive drugs, with a br...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4178A61K47/28A61K47/24A61P9/12
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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