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

Novel pravastatin lactone crystal form

A technology of pravastatin lactone and polymorphism, which is applied to medical preparations containing active ingredients, metabolic diseases, cardiovascular system diseases, etc., and can solve the problem of pravastatin lactone purification, crystal form and preparation method. And other issues

Inactive Publication Date: 2009-01-21
LIVZON NEW NORTH RIVER PHARMA +1
View PDF11 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This kind of preparation method is described in patent US6750366, US6696599, US2004259216, US2005153422 etc., described in the patent US2004167352, US2005215636 etc. in the separation and purification method of pravastatin sodium in the fermented liquid, in patent US6740775, US6790984, US20052828370, 7CN A1) etc. have described the crystal form of multiple pravastatin sodium and preparation method thereof, but do not see the report of purification, crystal form and preparation method of pravastatin lactone

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
  • Novel pravastatin lactone crystal form
  • Novel pravastatin lactone crystal form
  • Novel pravastatin lactone crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1: Preparation of type A polycrystal

[0038] Dissolve 4.0 g of pravastatin in 20 mL of acetone, and stir at 30° C. for 0.5 h. 10 mL of petroleum ether was added to the mixture and stirred at 48 °C for 1 h. The mixture was cooled to room temperature, left standing for 3 h, and the suspension was filtered to obtain pravastatin lactone crystals, which were put into an oven and kept at 50° C. for 12 h to obtain pravastatin lactone type A. The crystal form is characterized by the X-ray powder diffraction pattern shown in Figure 1 .

Embodiment 2

[0039] Embodiment 2: the preparation of type A polycrystal

[0040] Dissolve 10.0 g of pravastatin in 50 mL of acetone, and stir at 30° C. for 0.5 h. 20 mL of petroleum ether was added to the solution, and stirring was continued at 45 °C for 1 h. The mixture was cooled to room temperature, left for 3 hours, filtered, and the obtained crystals were placed in an oven at 50° C. for 12 hours to obtain pravastatin lactone type A. Form A is characterized by the X-ray powder diffraction pattern shown in Figure 1 of the accompanying drawings.

Embodiment 3

[0041] Embodiment 3: the preparation of B type polycrystal

[0042] Dissolve 5.0 g of pravastatin lactone in 10 mL of a mixed solvent of ethanol and water at a volume ratio of 1:1, heat the suspension to 50° C., and stir until the pravastatin lactone is completely dissolved. Add 60 mL of acetonitrile to this mixture, raise the temperature to 77°C, and stir for 1 h. The obtained suspension was filtered, the filter cake was washed once with acetonitrile, and dried naturally to obtain pravastatin lactone type B. Form B is characterized by the X-ray powder diffraction pattern shown in Figure 2 of the accompanying drawings.

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 relates to novel crystal forms of a lactone of Pravastatin. The novel crystal form is called polymorph A, B, C, D and E. Additionally, the invention also relates to the methods for preparing the novel crystal forms and the drug compositions containing the crystal forms.

Description

technical field [0001] The invention relates to crystal forms of pravastatin lactone, a preparation method thereof and pharmaceutical compositions containing these crystal forms. Background technique [0002] The present invention relates to a crystal form of pravastatin lactone. [0003] The known chemical name of pravastatin lactone is 2-methylbutanoic acid-1,2,3,7,8,8α-hexahydro-3-hydroxy-7-methyl-8-[2-(tetrahydro -4-hydroxy-6-oxo-2H-pyranyl-2)ethyl]-1-naphthol ester, pravastatin lactone has the following structural formula: [0004] [0005] Pravastatin is an HMG-CoA reductase inhibitor used for the treatment of hyperlipidemia and atherosclerosis. It is the carboxylic acid form of pravastatin lactone after opening of the lactone ring. Vastatin exists as an active open acid salt structure and has high water solubility. It mainly acts on the liver, and its ability to inhibit cholesterol synthesis in the liver is 400-1200 times higher than that in surrounding tissues. ...

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): C07D309/30A61K31/366A61P9/10A61P3/06
Inventor 李晶张雷于秀凤邱科先杨亚勇
Owner LIVZON NEW NORTH RIVER PHARMA