Olmesartan liposome solid preparation

A technology of azilsartan medoxomil and liposome preparation, applied in the field of medicine, can solve the problems of poor stability and encapsulation efficiency of liposomes, and solve the problems of poor stability and encapsulation efficiency and long retention time. , significant curative effect

Inactive Publication Date: 2011-08-03
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The azilsartan medoxomil liposome provided by the invention has high encapsulation efficiency, good stability and high bioavailability, can solve the tech

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] The preparation of embodiment 1 azilsartan medoxomil liposome tablet

[0062] prescription:

[0063]

[0064] Preparation Process

[0065] (a) 40g azilsartan medoxomil, 200g dioleoylphosphatidylcholine, 96g cholesterol, 80g sodium glycocholate and 52g soybean sterol are dissolved in 1200ml of mixed solvent of ethanol and n-hexane with a volume ratio of 1:2 , mix well, and remove the organic solvent under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0066] (b) Add citric acid-sodium citrate buffer solution with a pH of 6.0, shake and stir for 30 minutes at a speed of 500r / min to completely hydrate the phospholipid membrane, and emulsify with a high-speed tissue masher for 10 minutes , rotate at 5000r / min, and filter through a microporous membrane with a pore size of 0.45 μm to obtain a liposome suspension.

[0067] (c) Spray drying the above liposome suspension to prepare azilsartan medoxomil liposome powder.

[0068] (d) Azil...

Embodiment 2

[0075] The preparation of embodiment 2 azilsartan medoxomil liposome tablet

[0076] prescription:

[0077]

[0078] Preparation Process

[0079] (a) 80g azilsartan medoxomil, 240g dioleoylphosphatidylcholine, 64g cholesterol, 80g sodium glycocholate and 40g soybean sterol are dissolved in 1300ml of mixed solvent of ethanol and n-hexane with a volume ratio of 1:2 , mix well, and remove the organic solvent under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0080] (b) Add citric acid-sodium citrate buffer solution with a pH of 6.0, shake and stir for 30 minutes at a speed of 1000r / min to completely hydrate the phospholipid membrane, and homogenize and emulsify for 15 minutes with a tissue masher , rotate at 10000r / min, and filter through a microporous membrane with a pore size of 0.45 μm to obtain a liposome suspension.

[0081] (c) Spray drying the above liposome suspension to prepare azilsartan medoxomil liposome powder.

[0082] (d...

Embodiment 3

[0089] The preparation of embodiment 3 azilsartan medoxomil liposome tablet

[0090] prescription:

[0091]

[0092]

[0093] Preparation Process

[0094] (a) 40g azilsartan medoxomil, 320g dioleoylphosphatidylcholine, 160g cholesterol, 120g sodium glycocholate and 80g soybean sterol are dissolved in 3000ml of ethanol and n-hexane with a volume ratio of 1:2 , mix well, and remove the organic solvent under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0095] (b) Add citric acid-sodium citrate buffer solution with a pH of 6.0, shake and stir for 30 minutes at a speed of 700r / min to completely hydrate the phospholipid membrane, and emulsify for 12 minutes at high speed with a tissue masher , with a rotation speed of 8000r / min, and filtered through a microporous membrane with a pore size of 0.45 μm to obtain a liposome suspension.

[0096] (c) Spray drying the above liposome suspension to prepare azilsartan medoxomil liposome powder. ...

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Abstract

The invention discloses an olmesartan liposome solid preparation prepared by the following raw and supplementary material components in parts by weight: 1 part of olmesartan, 2.5-14 parts of dioleoyl-phosphatidylcholine, 0.5-6 parts of cholesterol, 0.8-10 parts of sodium glycyl-cholate, 0.2-5 parts of soy sterol and 2-20 parts of pharmaceutically acceptable carriers or excipients. The liposome solid preparation provided by the invention has high entrapment rate, even grain size, long medicament retention time in blood circulation, simple equipment, easiness in operation, improved product quality of the preparation and lessened toxic and side effects and is suitable for industrial production.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to an azilsartan medoxomil liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Azilsartan medoxomil, in the form of potassium salt in pharmaceutical preparations, the chemical name is (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl -2-Ethoxy-1-{[2'-(5-oxo-4,5 dihydro-1,2,4-oxadiazol-3 base)biphenyl-4-yl]methyl}- 1H-Benzimidazole-7-carboxylic acid monopotassium salt, molecular formula C 30 h 23 KN 4 o 8 , the molecular weight is 606.62, and the structural formula is: [0003] [0004] On February 25, 2011, Japan's Takeda Pharmaceutical Company announced that the U.S. Food and Drug Administration (FDA) had approved the angiotensin II receptor blocker Edarbi (azilsartan medoxomil) for the treatment of hypertension in adults. The drug is taken orally, once a day, either alone or in combination with other ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/20A61K31/4245A61K47/28A61P9/12
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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