Solid preparation containing rosuvastain calcium liposome

A technology of rosuvastatin calcium and liposome preparations, which is applied in the field of medicine, can solve the problems that the pharmaceutical composition does not meet the storage period requirements, the difficulty in preparing products, and the reduction of bioavailability, so as to protect vascular endothelial cells and microvascular system, reducing the size of myocardial infarction, and enhancing the effect of targeting

Inactive Publication Date: 2011-04-27
HAINAN MEIDA PHARMA
View PDF5 Cites 21 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Rosuvastatin calcium also has defects. For example, it is easily degraded in a higher temperature or higher humidity environment, and the main products formed are (3R, 5S) lactone degradation products and oxidation products, which makes the preparation of products difficult to operate, and The prepared pharmaceutical composition does not meet the storage period requirements
However, the addition of a large amount of alkaline agent is not conducive to the formulation of the pharmaceutical composition. After entering the body, the alkaline agent may also cause a variety of unexpected side effects, and may even lead to a decrease in bioavailability.

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 containing rosuvastain calcium liposome
  • Solid preparation containing rosuvastain calcium liposome
  • Solid preparation containing rosuvastain calcium liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Implementation Example 1 Preparation of Rosuvastatin Calcium Liposome

[0055] Prescription Rosuvastatin Calcium 100g

[0056] Soy Lecithin 800g

[0057] Cholesterol 300g

[0058] Tween 80 50g

[0059] Sodium deoxycholate 100g

[0060] Preparation Process

[0061] (1) Dissolve 100g rosuvastatin calcium, 800g soybean lecithin, 300g cholesterol, 50g Tween 80 and 100g sodium deoxycholate in 5000ml methanol, mix well, remove methanol under reduced pressure on a rotary thin film evaporator, Prepare phospholipid film;

[0062] (2) Add 2500ml of phosphoric acid-sodium dihydrogen phosphate buffer solution with pH = 4.5, stir to completely hydrate the phospholipid membrane, then homogeneously emulsify with a tissue grinder for 20min at a speed of 12000r / min, mix the solution evenly, and keep warm at 50°C Under ultrasonic treatment for 60 minutes, the liposome suspension was obtained;

[0063] (3) Spray-dry the suspension obtained in the ...

Embodiment 2

[0070] Example 2 Preparation of Rosuvastatin Calcium Liposome

[0071] Prescription: Rosuvastatin Calcium 200g

[0072] Soy Lecithin 5000g

[0073] Cholesterol 2000g

[0074] Tween 80 2400g

[0075] Sodium deoxycholate 2000g

[0076] Preparation Process

[0077] (1) 200g rosuvastatin calcium, 5000g soybean lecithin, 2000g cholesterol, 2400g Tween 80 and 2000g sodium deoxycholate were dissolved in 40000ml methanol, mixed uniformly, and decompressed on a rotary thin film evaporator to remove methanol, Prepare phospholipid film;

[0078] (2) Add 20000ml of citric acid-sodium citrate buffer solution with pH = 6.0, stir to completely hydrate the phospholipid membrane, then homogeneously emulsify for 10min with a tissue grinder at a speed of 15000r / min, mix the solution evenly, and keep warm for 70 Ultrasound at ℃ for 40 minutes to prepare liposome suspension;

[0079] (3) Spray-dry the suspension obtained in the above step (2) to prepare rosuvasta...

Embodiment 3

[0091] Example 3 Preparation of Rosuvastatin Calcium Liposome Particles

[0092] Prescription (1000 bags)

[0093] Rosuvastatin calcium liposome (calculated as rosuvastatin calcium) 10g

[0094] Starch 80g

[0095] Dextrin 35g

[0096] Sucrose 50g

[0097] Aspartame 1.5g

[0098] Hypromellose 1.2g

[0099] Strawberry essence 1.5g

[0100] Preparation Process

[0101] (1) Pulverize the liposome containing 10g rosuvastatin calcium, cross 80 mesh sieves, and set aside;

[0102] (2) Take by weighing 80g starch, 35g dextrin, 50g sucrose and 1.5g aspartame, cross 80 mesh sieves, mix and set aside;

[0103] (3) Mix the above raw and auxiliary materials evenly, then mix evenly with 1.5g strawberry essence, add 60ml of 2% hypromellose 20% ethanol solution to make soft material, pass through a 20 mesh sieve to granulate, dry at 60°C, 18 mesh Sieve whole grains, set aside;

[0104] (4) Divide the dried granules to prepare rosuvastatin...

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 containing rosuvastain calcium liposome and particularly relates to the solid preparation containing rosuvastain calcium liposome and a preparation method thereof. The rosuvastain calcium liposome mainly comprises 1 part of rosuvastain calcium, 2-25 parts of soyabean lecithin, 0.5-10 parts of cholesterol, 0.5-12 parts of tween 80 and 0.05-10 parts of sodium desoxycholate. The rosuvastain calcium solid preparation prepared from the liposome not only increases the dissolution, but also improves the stability and the bioavilability. The quality of preparation products is improved and the toxic or side effects are reduced.

Description

technical field [0001] The invention relates to a rosuvastatin calcium liposome solid preparation and a preparation method thereof, in particular to an amorphous rosuvastatin calcium liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cardiovascular disease is a kind of disease that seriously endangers human health. In recent years, its morbidity and mortality have remained high all over the world, and it is currently the number one killer of human beings. According to the statistics of the World Health Organization, about 15 million people die of cardiovascular and cerebrovascular diseases in the world every year. With the improvement of people's living standards in my country, the growth of the elderly population (the elderly population over 60 years old has accounted for 10.7% of the national population at present, reaching as many as 130 million). With the accelerated pace of life, eati...

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 Applications(China)
IPC IPC(8): A61K9/127A61K9/00A61K9/16A61K9/20A61K31/505A61K31/685A61P9/00
Inventor 陶灵刚
Owner HAINAN MEIDA PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap