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Medicinal atorvastatin calcium composition capsules for treating coronary heart disease

A technology of atorvastatin calcium and composition, applied in the field of medicine, can solve the problems of high water content of sulfobutyl-β-cyclodextrin, degradation of atorvastatin calcium, low bioavailability and the like, and achieve water and impurities. Low content, reduced myalgia side effects, improved solubility

Inactive Publication Date: 2015-11-11
QINGDAO HUAZHICAO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Chinese patent CN102139115B discloses the cyclodextrin inclusion compound of atorvastatin and the preparation method of oral solid preparation thereof, the sulfobutyl-β-cyclodextrin used has high moisture content, which easily leads to the degradation of atorvastatin calcium
[0012] In a word, in the methods for preparing atorvastatin calcium crystalline compounds reported in existing research reports and patent documents, the obtained atorvastatin calcium in various crystal forms or non-crystalline forms still has a relatively high total amount of impurities, Low optical purity, low bioavailability

Method used

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  • Medicinal atorvastatin calcium composition capsules for treating coronary heart disease
  • Medicinal atorvastatin calcium composition capsules for treating coronary heart disease
  • Medicinal atorvastatin calcium composition capsules for treating coronary heart disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of Atorvastatin Calcium Crystals

[0035] Dissolving atorvastatin calcium in a mixed solvent of ethanol and N-methylpyrrolidone whose volume is 10 times the weight of atorvastatin calcium at 35°C, the volume ratio of ethanol and N-methylpyrrolidone is 3:1, After the dissolution is complete, add a chloroform solvent whose volume is 8 times the weight of atorvastatin calcium, lower the temperature to room temperature within 2 hours, keep it at room temperature for 3 hours, and then further lower the temperature to -5°C, and then - After standing at 5°C for 3 hours, crystals were precipitated to obtain atorvastatin calcium crystals.

[0036] The prepared atorvastatin calcium crystals are obtained by measuring the X-ray powder diffraction pattern using Cu-Kα rays as shown in figure 1 shown.

Embodiment 2

[0037] Example 2: Preparation of Atorvastatin Calcium Capsules

[0038] Prescription: 1 part by weight of atorvastatin calcium crystal compound obtained in Example 1, 15 parts by weight of starch, 0.4 part by weight of hypromellose, 0.25 part by weight of dioctyl sodium sulfosuccinate, 95% ethanol 3.1 parts by weight, 0.7 parts by weight of talcum powder;

[0039] Preparation:

[0040] (1) Processing of raw and auxiliary materials: sieve atorvastatin calcium to 100 mesh;

[0041] (2) Weighing: Weighing according to the process prescription;

[0042] (3) Preparation of adhesive: Dissolve the prescribed amount of hypromellose and dioctyl sodium sulfosuccinate in 95% ethanol and set aside;

[0043] (4) Mixing and granulation: Add atorvastatin calcium and starch to the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared binder, wet mix and cut, and use a 16-mesh sieve to soften material;

[0044] (5) Drying: Add the wet granules obta...

Embodiment 3

[0048] Example 3: Preparation of Atorvastatin Calcium Capsules

[0049] Prescription: 1 part by weight of atorvastatin calcium crystal compound obtained in Example 1, 18 parts by weight of starch, 0.5 part by weight of hypromellose, 0.3 part by weight of dioctyl sodium sulfosuccinate, 95% ethanol 3.2 parts by weight, 0.8 parts by weight of talcum powder;

[0050] Preparation:

[0051] (1) Processing of raw and auxiliary materials: sieve atorvastatin calcium to 100 mesh;

[0052] (2) Weighing: Weighing according to the process prescription;

[0053] (3) Preparation of adhesive: Dissolve the prescribed amount of hypromellose and dioctyl sodium sulfosuccinate in 95% ethanol and set aside;

[0054] (4) Mixing and granulation: Add atorvastatin calcium and starch to the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared binder, wet mix and cut, and use a 16-mesh sieve to soften material;

[0055] (5) Drying: Add the wet granules obt...

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Abstract

The invention discloses medicinal atorvastatin calcium composition capsules for treating a coronary heart disease and belongs to the technical field of medicines. The capsules are prepared by atorvastatin calcium, starch, hydroxypropyl methylcellulose, dioctyl sodium sulphosuccinate, 95% of ethyl alcohol and talcum powder. The atorvastatin calcium is a novel crystal form compound, an X-ray powder diffraction diagram obtained through Cu-Ka ray measurement is shown in Figure 1 and is different from the atorvastatin calcium reported in the prior art, a test shows that the novel crystal form compound has obvious improved moisture absorption, solubility of the medicine in an acid medium and water is improved, the moisture and impurity content is low, the stability is good, the atorvastatin calcium is prevented from being destroyed in the acid environment of the stomach, the occurrence rate of the side effect of myalgia is reduced, and the prepared capsules are high in dissolution rate and good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a capsule of atorvastatin calcium composition for treating coronary heart disease. Background technique [0002] Atorvastatin calcium (Atorvastatin Calcium) belongs to the inhibitor of hydroxymethylglutaryl CoA (HMG-CoA) reductase, which can reduce the concentration of cholesterol in plasma and serum lipoprotein by inhibiting the biosynthesis of HMG-COA reductase and cholesterol in the liver. And by increasing the liver low-density lipoprotein receptors on the cell surface to enhance the uptake and metabolism of low-density lipoprotein. Atorvastatin calcium can effectively reduce plasma total cholesterol, low-density lipoprotein cholesterol, apolipoprotein and triglyceride in patients with homozygous and heterozygous familial hypercholesterolemia, nonfamilial cholesterolemia and mixed lipid metabolism disorders At the same time, the levels of high-density lipoprotein cholesterol a...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/40C07D207/34A61P9/10A61P3/06A61K47/38
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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