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Polymorphic substance of atorvastatin semi-strontium salt as well as preparation method and application of polymorphic substance as HMG-CoA (Hydroxy Methylglutaryl Coenzyme A) enzyme inhibitor

一种多晶型物、阿伐他汀的技术，应用在HMG-CoA酶抑制剂领域，能够解决水溶性低等问题，达到控制血胆固醇、避免钙的摄入的效果

Inactive Publication Date: 2013-03-20
TIANJIN HEMAY BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Atorvastatin hemi-calcium salt trihydrate has low water solubility and its oral bioavailability is only 12%

Method used

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  • Polymorphic substance of atorvastatin semi-strontium salt as well as preparation method and application of polymorphic substance as HMG-CoA (Hydroxy Methylglutaryl Coenzyme A) enzyme inhibitor
  • Polymorphic substance of atorvastatin semi-strontium salt as well as preparation method and application of polymorphic substance as HMG-CoA (Hydroxy Methylglutaryl Coenzyme A) enzyme inhibitor
  • Polymorphic substance of atorvastatin semi-strontium salt as well as preparation method and application of polymorphic substance as HMG-CoA (Hydroxy Methylglutaryl Coenzyme A) enzyme inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Add the aqueous solution of strontium nitrate (1.83g) to the aqueous solution of atorvastatin sodium (10g) at room temperature, stir at room temperature until solid is precipitated, collect the solid by suction filtration, wash the filter cake with 100mL water, put the filter cake into a vacuum drying oven (40 °C) after drying, the polymorph HA of atorvastatin hemistrontium salt was obtained. MP: decomposes at 202-212°C, the content of strontium determined by atomic emission spectrometry is 6.7%, MS: 557 (M-1). Water solubility: 0.7mg / mL.

Embodiment 2

[0044] Dissolve 5 g of atorvastatin ammonium in THF, add an aqueous solution of strontium acetate (1.75 g) at room temperature, stir at room temperature until a solid precipitates, collect the solid by suction filtration, wash the filter cake with 50 mL of water, put the filter cake into a vacuum drying oven (40 ℃) to obtain atorvastatin hemistrontium salt after drying. MP: decomposed at 201-205°C, and the content of strontium was determined to be 6.6% by atomic emission spectrometry.

Embodiment 3

[0046] Add a methanol solution of strontium methanesulfonate (1.2g) to a methanol solution of atorvastatin sodium (5g) at room temperature, stir at room temperature until a solid precipitates, collect the solid by suction filtration, wash the filter cake with 40mL of water, put the filter cake in a vacuum After drying in a drying oven (40°C), atorvastatin hemistrontium salt was obtained. MP: decomposed at 203-206°C, and the content of strontium was determined to be 6.7% by atomic emission spectrometry.

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Abstract

The invention discloses a polymorphic substance HB of an atorvastatin semi-strontium salt shown as a formula (I) or a solvate of the polymorphic substance HB. The polymorphic substance HB of a compound shown as the formula (I) or the solvate of the polymorphic substance HB, disclosed by the invention and used as a better selection of a drug belonging to an HMG-CoA (Hydroxy Methylglutaryl Coenzyme A) enzyme inhibitor, is provided for hypercalcemia patients. By using the polymorphic substance HB of the compound shown as the formula (I) or the solvate of the polymorphic substance as the drug belonging to the HMG-CoA enzyme inhibitor, the aim of controlling blood cholesterol can be achieved, extra calium intake can be avoided, and therefore, the polymorphic substance HB or the solvate thereof is the optical selection of such patients.

Description

technical field [0001] The invention discloses atorvastatin semi-strontium salt polymorph, its preparation method and application as HMG-CoA enzyme inhibitor. Background of the invention [0002] The mechanism of action of statins to reduce low-density lipoprotein in the body has been clarified. The enzyme HMG-CoA converts HMG to mevalonate, which is the decisive step in the biosynthesis of cholesterol in the liver. Very low-density lipoprotein (VLDL) moves cholesterol and triglycerides from the liver to outer cells. VLDL is broken down by external cells to release fatty acids. The VLDL will then be converted to intermediate-density lipoprotein (IDL), which can be transferred or converted to LDL by low-density lipoprotein (LDL) receptors. Lowering cholesterol levels increases the number of LDL receptors and correspondingly reduces the amount of LDL converted from IDL. By inhibiting the HMG-CoA enzyme, statins can effectively block the synthesis of cholesterol in the live...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/34A61K31/40A61P3/06A61P19/10
Inventor 张和胜
Owner TIANJIN HEMAY BIO TECH CO LTD
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