Solid pharmaceutical composition containing atorvastatin calcium

A technology of atorvastatin calcium and its composition, which is applied in the field of medicine, can solve the problems of no lipid-lowering activity and side effects of myalgia, achieve stable quality, reduce the incidence of side effects of myalgia, and achieve the effects of simple prescription and preparation process

Active Publication Date: 2014-11-05
SHANGHAI BOCIMED PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] In summary, atorvastatin calcium will be degraded to its lactone form under acidic conditions, specifically gastric acid conditions. The lactone form of molecules has no lipid-lowering activity, but it can cause the well-known statins side effects of drugs for myalgia

Method used

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  • Solid pharmaceutical composition containing atorvastatin calcium
  • Solid pharmaceutical composition containing atorvastatin calcium
  • Solid pharmaceutical composition containing atorvastatin calcium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 Compatibility experiment of auxiliary materials

[0036]Mix atorvastatin calcium raw material, filler microcrystalline cellulose, lactose monohydrate, mannitol, calcium carbonate, and disintegrating agent croscarmellose sodium in a weight ratio of 1:5, and mix the Torvastatin calcium raw material and lubricant magnesium stearate, isolation layer coating powder (hydroxypropyl methylcellulose: polyethylene glycol 2000: sodium lauryl sulfate = 10:1:1 (mass ratio) ) according to the total ratio of 20:1, mix evenly, place them in culture dishes and spread them into thin layers <5mm thick. The sample numbers are A, B, C, D, E, F, G, respectively, and another copy of atorvastatin calcium raw material is placed under the same experimental conditions, numbered H, as a standard reference.

[0037] In addition, since the enteric coating powder is not in direct contact with the tablet core containing atorvastatin calcium raw material, there is no interaction, so it is...

Embodiment 2- Embodiment 6

[0047] Embodiment 2-embodiment 6 (unit: g) prescription design:

[0048] In order to make the tablet core disintegrate quickly after it reaches the small intestine, microcrystalline cellulose is selected as a filler with high porosity and good compressibility. At the same time, to increase the hardness of the tablet core and facilitate coating, lactose monohydrate is selected as the second Two fillers. Also in order to disintegrate quickly after the tablet core reaches the small intestine, croscarmellose sodium with the largest water absorption multiple is selected as the disintegrating agent; in terms of lubricant, a conventional lubricant, magnesium stearate, is selected with a small amount of addition and stable properties. Easy to form into tablets.

[0049] Obtain different doses of atorvastatin calcium enteric-coated tablet prescription and form as follows:

[0050]

[0051] Preparation Process:

[0052] 1) Preparation of tablet core:

[0053] Weigh atorvastatin c...

Embodiment 7

[0058] Example 7 Sample release detection

[0059] Get each 6 of the finished enteric-coated tablets of embodiment 2-embodiment 6, according to Chinese Pharmacopoeia 2010 edition two release assay methods (Appendix X D second method), adopt dissolution assay (Appendix X C first method, Rotating basket method) device, using 750mL of hydrochloric acid solution (9→1000mL) as the release medium, the temperature of the eluate is 37±0.5°C, and the rotation speed is 100 rpm. Operate according to the law. After 120 minutes, immediately lift the rotating basket out of the liquid surface , Discard the hydrochloric acid solution, immediately add 1000ml of phosphate buffer (pH 6.8) preheated to 37°C, continue to operate according to the law, after 45 minutes, take a sample for testing, the results are shown in the following table:

[0060] Table 4 Example 2~Example 6 sample release test results

[0061]

[0062] The above results are in full compliance with the requirements for the re...

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Abstract

The invention relates to a solid pharmaceutical composition containing atorvastatin calcium as well as a preparation and an application thereof. Specifically, the solid pharmaceutical composition containing atorvastatin calcium can be further prepared into an enteric-coated tablet through a certain preparation process. According to the solid pharmaceutical composition containing atorvastatin calcium, the condition that the atorvastatin calcium in common tablets is degraded into lactone form in gastric acid environment to lose lipid lowering activity; due to the decrease of lactone type impurities, the occurrence rate of the untoward effect myalgia can be reduced. Accelerated stability studies find that the prepared enteric-coated tablet containing atorvastatin calcium is stable in quality and controllable and is capable of providing an effective atorvastatin calcium oral solid preparation for clinic tests.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a solid pharmaceutical composition containing atorvastatin calcium, a preparation method and application thereof. Background technique [0002] With the continuous development of medical science, people realize that the high content of cholesterol and fat is the basic cause of cardiovascular disease, and hyperlipidemia is the main risk factor of coronary heart disease and hypertension. Therefore, people began to focus on the development of blood lipid regulating drugs as the prevention and treatment of cardiovascular diseases. Since the late 1980s, a large number of blood lipid-lowering drugs have been launched, among which statins have been well received by people, and their clinical efficacy is unmatched by other types of blood lipid regulating drugs. [0003] Over the past ten years, the completion of several international large-scale coronary heart disease preve...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/40A61K47/38A61K47/34A61P3/06
Inventor 不公告发明人
Owner SHANGHAI BOCIMED PHARMA CO LTD
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