Unlock instant, AI-driven research and patent intelligence for your innovation.

Solid preparation of aliskiren-valsartan pharmaceutical composition liposome

A technology of aliskiren valsa and solid preparations, applied in the field of medicine, can solve the problems of uncontrollable drug release speed and drug release process, unsatisfactory long-term stability of drugs, unfavorable long-term storage, etc., to improve bioavailability, reduce Toxic and side effects, the effect of improving the curative effect

Inactive Publication Date: 2014-02-26
HAINAN MEILAN SMITH KLINE PHARMA
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Although the above-mentioned Aliskiren-valsartan tablet has been prepared by screening specific auxiliary materials, it has certain advantages, but the long-term stability of the medicine is not ideal, it is not conducive to long-term storage, and the drug release rate and the drug release process cannot be controlled, so it will give Clinical use brings hidden dangers

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Solid preparation of aliskiren-valsartan pharmaceutical composition liposome
  • Solid preparation of aliskiren-valsartan pharmaceutical composition liposome
  • Solid preparation of aliskiren-valsartan pharmaceutical composition liposome

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0066] On the other hand, the present invention provides the preparation method of Aliskiren valsartan pharmaceutical composition liposome, the method comprises the following steps:

[0067] (a) Aliskiren, valsartan, egg yolk lecithin, soybean phosphatidylglycerol, cholesterol and Tween 80 are dissolved in an organic solvent, mixed evenly, and the organic solvent is removed under reduced pressure on a rotary thin film evaporator to obtain a lipid membrane;

[0068] (b) Add the buffer solution, shake and stir for 45 minutes at a speed of 800r / min to completely hydrate the phospholipid film. Use a tissue masher for high-speed homogeneous emulsification for 5-15 minutes at a speed of 8000r / min. Filter through a pore filter to obtain a liposome suspension;

[0069] (c) Spray-drying the above liposome suspension to prepare Aliskiren valsartan liposome powder.

[0070] In a preferred embodiment of the liposome preparation method of Aliskiren valsartan pharmaceutical composition of...

Embodiment 1

[0111] Example 1 Preparation of Aliskiren Valsartan Pharmaceutical Composition Liposome Tablets

[0112] The raw materials used are as follows:

[0113]

[0114] The following production process was used to prepare Aliskiren-Valsartan pharmaceutical composition liposome tablets:

[0115] (1) Dissolve 150g of aliskiren, 160g of valsartan, 300g of egg yolk lecithin, 100g of soybean phosphatidylglycerol, 300g of cholesterol, and 50g of Tween 80 in 5000ml of isopropanol, mix well, and place on a rotary thin-film evaporator Isopropanol was removed under reduced pressure to obtain a lipid film;

[0116] (2) Add 5000ml of phosphate buffer with pH value of 7.0, shake and stir for 45 minutes, and the rotation speed is 800r / min to completely hydrate the phospholipid membrane, and use a tissue masher to homogenize and emulsify at high speed for 5 minutes at a rotation speed of 8000r / min. min, filter with 0.45μm microporous membrane to prepare liposome suspension;

[0117] (3) abo...

Embodiment 2

[0121] Example 2 Preparation of Aliskiren Valsartan Pharmaceutical Composition Liposome Tablets

[0122] The raw materials used are as follows:

[0123]

[0124] Aliskiren-valsartan liposomal tablets were prepared by the following production process:

[0125] (1) Dissolve 150g of aliskiren, 160g of valsartan, 800g of egg yolk lecithin, 50g of soybean phosphatidylglycerol, 400g of cholesterol, and 200g of Tween 80 in 8000ml of isopropanol, mix well, and place on a rotary thin-film evaporator Isopropanol was removed under reduced pressure to obtain a lipid film;

[0126] (2) Add 8000 ml of phosphate buffer with pH value of 7.0, shake and stir for 45 minutes, and the rotating speed is 800 r / min to completely hydrate the phospholipid membrane, and use a tissue masher for high-speed homogeneous emulsification for 15 minutes, and the rotating speed is 8000 r / min. , filtered with a 0.45 μm microporous membrane to obtain a liposome suspension;

[0127] (3) above-mentioned lipo...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a solid preparation of aliskiren-valsartan pharmaceutical composition liposome, and a method for preparing the same. Aliskiren-valsartan pharmaceutical composition liposome with excellent quality is prepared by selecting and using aliskiren, valsartan, egg lecithin, soybean phosphatidylglycerol, cholesterol, and tween 80 of a specific weight ratio. The solid preparation is prepared from the aliskiren-valsartan pharmaceutical composition liposome by using a common preparation method. The liposome solid preparation provided by the invention has a high entrapment rate, can be released stably at an expected speed, has a uniform particle size, and has long medicament retention time in blood circulation. The preparation method has simple equipment, is easy to operate, improves product quality, reduces toxic and side effects, and is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a liposome solid preparation of an aliskiren-valsartan pharmaceutical composition, which belongs to the technical field of medicine. Background technique [0002] Aliskiren, chemical name is (2S,4S,5S,7S)-5-nitro-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl yl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide, molecular formula: C 30 H 53 N 3 O 6 , molecular weight 551.76, structural formula: [0003] [0004] Aliskiren is a new class of antihypertensive drugs that has been on the market for more than ten years. It is an oral and effective non-peptide renin inhibitor that acts on the renin-angiotensin-aldosterone system (RAS). The first drug with a novel pharmacological mechanism of action launched in the field. This product was first approved for listing in the United States in March 2007, and has now been listed in more than 40 countries and regions aro...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/127A61K31/41A61K47/34A61P9/12A61K31/165
Inventor 马明杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA