Pravastatin sodium liposome solid preparation

Abstract

The invention discloses a pravastatin sodium liposome preparation. The pravastatin sodium liposome is mainly prepared from 1 weight part of pravastatin sodium, 3 to 10 weight parts of glycerol monoacetate, 1.5 to 6 weight parts of poloxamer 188 and 0.05 to 5 weight parts of sodium deoxycholate. The invention further discloses a pravastatin sodium liposome solid preparation. The solid preparation is prepared from the pravastatin sodium liposome preparation and other pharmaceutically common excipients. The product quality of the preparation is improved and the toxic or side effects are reduced.

Description

technical field [0001] The invention relates to a new solid preparation of pravastatin, in particular to a pravastatin sodium liposome solid preparation such as a tablet and a capsule, and belongs to the field of pharmaceutical preparations. Background technique [0002] Pravastatin sodium, chemical name: {1S-[1a(bs*,ds*), 2a, 6a, 8b(R*), 8aa]}-1,2,6,7,8,8a-hexahydro -b, d, 6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-1-naphthalene heptanoic acid monosodium salt, the molecular formula is C23H35NaO7, the molecular weight is 446.52, and the structural formula is : [0003] [0004] Pravastatin was developed by Sankyo Corporation of Japan, and was first launched in Japan in 1989 under the trade name "Mebele", followed by pravastatin sodium produced by Bristol-Myers Squibb under the trade name "Puragu". Pravastatin sodium is a competitive inhibitor of 3-hydroxy 3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), which is the rate-limiting enzyme in the initial stag...

AI Technical Summary

Problems solved by technology

[0006] Chinese patent CN02809354.2 discloses a stable pharmaceutical preparation of pravastatin, which improves the pH value environment by adding sodium stearyl fumarate, but sodium stearyl fumarate is hydrophobic, slow onset, and difficult to achieve in a short time The required pH environment still has a certain impact on the stability and bioavailability of pravastatin

[0007] Chinese patent CN02151239.6 discloses a pravastatin preparation using amino acid and its amino acid salt as a stabilizer. The pH value of the aqueous suspension is 6.0-8.9, and the alkalinity is low, which also cannot provide a sufficient stable environment.

[0008] Chinese patent CN101732267A and the listed preparation "Pulagu" have added magnesium oxide as a stabilizer, and magnesium oxide can be used as an osmotic laxative and magnesium supplement clinically, so the adverse reactions caused by excessive application of magnesium oxide are also It is clear

The prepared liposome also has higher auxiliary material content and less main drug content; the external size of the pharmaceutical composition made from liposomes is too large, and is also not suitable for varieties with higher main drug content.

Images