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Medicine atorvastatin calcium composition dry suspension for treating coronary heart disease

A technology of atorvastatin calcium and dry suspension, which is applied in the field of medicine and can solve problems such as surfactant gastrointestinal irritation, degradation of atorvastatin calcium, complex process, etc., to achieve low moisture and impurity content, reduce Myalgia side effect, high bioavailability effect

Inactive Publication Date: 2015-12-09
杨献美
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the problem caused by a large amount of disintegrants is that it is easy to absorb moisture, which leads to the degradation of atorvastatin calcium
Furthermore, a certain amount of sodium lauryl sulfate is added to the formula to improve the dissolution rate in vitro, but the addition of surfactants will cause gastrointestinal irritation
[0012] Chinese patent CN102309462A provides a kind of atorvastatin calcium tablet, which adopts dry secondary granulation technology, the process is relatively complicated, the stability is poor, and it cannot be completely dissolved in acid
The invention uses slightly acidic lactose and highly hygroscopic crospovidone, which will lead to the degradation of atorvastatin calcium
[0015] Chinese patent CN101791297B discloses a kind of

Method used

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  • Medicine atorvastatin calcium composition dry suspension for treating coronary heart disease
  • Medicine atorvastatin calcium composition dry suspension for treating coronary heart disease
  • Medicine atorvastatin calcium composition dry suspension for treating coronary heart disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1: Preparation of Atorvastatin Calcium Crystals

[0043] (1) Mix acetone and dimethyl sulfoxide into a mixed solvent, and the volume ratio of acetone and dimethyl sulfoxide is 2:1;

[0044] (2) Take the atorvastatin calcium raw material, dissolve it in the mixed solvent of acetone and dimethyl sulfoxide whose volume is 6 times the weight of atorvastatin calcium in step (1), raise the temperature to 40°C, and stir until All dissolved to obtain atorvastatin calcium solution;

[0045] (3) Add the atorvastatin calcium solution in step (2) into ethanol whose volume is 5 times the weight of atorvastatin calcium under the condition of a stirring speed of 560 rpm, mix to form a suspension, Cool down to -15°C at a rate of 15°C / min;

[0046] (4) Perform suction filtration, wash the filter cake, and then vacuum-dry the filter cake to obtain a crystalline powder, which is the atorvastatin calcium compound.

[0047] The prepared atorvastatin calcium crystals use Cu-Kα r...

Embodiment 2

[0048] Example 2: Preparation of Atorvastatin Calcium Dry Suspension

[0049] Prescription: in parts by weight

[0050]

[0051] Preparation:

[0052] (1) Weighing: Weighing according to the process prescription;

[0053] (2) Processing of raw and auxiliary materials: sieve the prescribed amount of atorvastatin calcium through 100 meshes;

[0054] (3) Mixing: Put atorvastatin calcium, xylitol, carbomer, calcium alginate, and aspartame into the three-dimensional motion mixer, set the pre-mixing speed to 13 rpm, and the mixing time to 35 minutes;

[0055] (4) Packaging: Calculate the theoretical loading range according to the content of the materials obtained from the total blending, and then carry out sub-packaging.

Embodiment 3

[0056] Example 3: Preparation of Atorvastatin Calcium Dry Suspension

[0057] Prescription: in parts by weight

[0058]

[0059] Preparation:

[0060] (1) Weighing: Weighing according to the process prescription;

[0061] (2) Processing of raw and auxiliary materials: sieve the prescribed amount of atorvastatin calcium through 100 meshes;

[0062] (3) Mixing: Put atorvastatin calcium, xylitol, carbomer, calcium alginate, and aspartame into the three-dimensional motion mixer, set the pre-mixing speed to 13 rpm, and the mixing time to 35 minutes;

[0063] (4) Packaging: Calculate the theoretical loading range according to the content of the materials obtained from the total blending, and then carry out sub-packaging.

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Abstract

The invention belongs to the technical field of medicine and relates to medicine atorvastatin calcium composition dry suspension for treating the coronary heart disease. The composition is prepared from atorvastatin calcium, xylitol, carbomer, calcium alginate and aspartame. The atorvastatin calcium is a novel crystal form compound, an X-ray powder diffraction pattern measured through a Cu-K alpha ray is shown in the graph 1, the atorvastatin calcium is different from atorvastatin calcium reported in the prior art, and it is found through tests that the compound of the novel crystal structure has the advantages that hygroscopicity is obviously improved, the solubility of the medicine in an acid medium and water is improved, the moisture and impurity content is low, stability is good, the atorvastatin calcium is prevented from being damaged in the gastric acid environment, the occurrence rate of the myalgia side effect of the atorvastatin calcium is reduced, and the dry suspension prepared from the atorvastatin calcium is good in stability and high in bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a dry suspension 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 choles...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/40A61K47/36A61P9/10A61P3/06C07D207/34
Inventor 杨献美
Owner 杨献美