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Oral proliposome containing atorvastatin calcium and preparation method of oral proliposome

A technology of atorvastatin calcium and proliposome, which is applied in the direction of liposome delivery, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve the problem that the pharmacological activity of atorvastatin cannot be effectively exerted and the limitations Problems such as clinical application of drugs and poor bioavailability, to meet the needs of clinical drug administration, improve bioavailability, and high production efficiency

Inactive Publication Date: 2014-04-02
RUNZE PHARMACEUTICAL (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent Publication No. CN101804029A discloses an atorvastatin liposome, which is composed of atorvastatin or a pharmaceutically acceptable salt plus an alkalizing agent with a pH greater than 5, and phospholipids, but the preparation has poor bioavailability and cannot effectively Exercising the pharmacological activity of atorvastatin
[0007] At present, liposomes are mostly used for injection administration, but a large amount of organic solvents must be added as solvents for intravenous administration, which limits the clinical application of drugs and causes pain and inconvenience to patients.

Method used

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  • Oral proliposome containing atorvastatin calcium and preparation method of oral proliposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The distribution ratio of the components is: atorvastatin calcium 10mg, soybean lecithin 180mg, poloxamer 50mg, sodium cholate 8mg, absolute ethanol 1ml.

[0026] Preparation process: according to the formula, add the required amount of atorvastatin calcium, soybean lecithin, poloxamer and sodium cholate into the required amount of absolute ethanol solvent, ultrasonically dissolve the mixture to dissolve into a clear anhydrous solution, Obtained atorvastatin calcium proliposome preparation.

[0027] Adding the prepared atorvastatin calcium proliposomes to 50 times the amount of distilled water can quickly form an atorvastatin calcium liposome solution with an average particle size of 470.1 nm and an encapsulation efficiency of >90%.

[0028] The physical and chemical characteristics of the finished product:

[0029] Finished product traits: It is light yellow clear and transparent solution.

[0030] Hydration dispersibility: After adding distilled water and shaking to...

Embodiment 2

[0035] The distribution ratio of the components is: atorvastatin calcium 17mg, soybean lecithin 240mg, poloxamer 58mg, sodium deoxycholate 10mg, absolute ethanol 1.5ml.

[0036] The preparation process is the same as in Example 1.

[0037] Adding the prepared atorvastatin calcium proliposomes to 50 times the amount of distilled water can quickly form an atorvastatin calcium liposome solution with an average particle size of 80%.

Embodiment 3

[0039]The distribution ratio of the components is: atorvastatin calcium 20mg, soybean lecithin 270mg, poloxamer 60mg, Tween 80 16mg, absolute ethanol 1.8ml.

[0040] The preparation process is the same as in Example 1.

[0041] Adding the prepared atorvastatin calcium proliposomes to 50 times the amount of distilled water can quickly form an atorvastatin calcium liposome solution with an average particle size of 85%.

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Abstract

The invention relates to an oral proliposome containing atorvastatin calcium and a preparation method of the oral proliposome. The oral proliposome comprises the following components: 0.5%-10% of the atorvastatin calcium, 10%-30% of phospholipid, 2%-10% of poloxamer, 50%-87.3% of absolute ethanol and 0.2%-3% of a stabilizer. The preparation method comprises the following steps: adding the atorvastatin calcium, the phospholipid, the poloxamer and the stabilizer into the absolute ethanol solvent, mixing in the absence of water, and dissolving the mixture into a clear anhydrous solution so as to obtain an atorvastatin calcium proliposome preparation. The proliposome can be quickly self-assembled into the medicated proliposome preparation with a proper particle size and high encapsulation efficiency after being diluted by a proper hydration medium before use and is used for oral administration, the operation is easy and convenient, and the oral administration mode can be easily accepted by patients.

Description

technical field [0001] The invention relates to an oral proliposome containing atorvastatin calcium and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Cardiovascular and cerebrovascular diseases are the number one killer of human death, and 10 million people worldwide die of cardiovascular diseases every year, and dyslipidemia is the main cause of cardiovascular and cerebrovascular diseases. Therefore, one of the basic methods to effectively prevent and treat cardiovascular and cerebrovascular diseases is to adjust the abnormal blood lipid level of the human body. At present, the most widely used lipid-lowering drugs in clinical practice are statins. A blood lipid revolution triggered by "statins" is emerging around the world. Lipid-lowering therapy will become the main method for preventing cardiovascular diseases in the 21st century. [0003] Among them, atorvastatin calcium is the most effectiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/40A61K47/34A61P3/06
Inventor 孙川棣周志亮陈叶明胡玮沈梦妮
Owner RUNZE PHARMACEUTICAL (SUZHOU) CO LTD
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