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Lipid microspherical asarol prepn and its prepn process

A technology of octylolipid and lipid microspheres, which is applied in the field of asaronelolipid microsphere preparation and its preparation, to achieve the effect of reducing the amount of normal tissue distribution, reducing the dosage, and overcoming the instability of chemical properties

Inactive Publication Date: 2005-12-14
四川思达康药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no literature and patent reports on the preparation of asarum cerebrolipid microspheres at home and abroad.

Method used

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  • Lipid microspherical asarol prepn and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Preparation of lipid microsphere preparation of the present invention

[0034]Put 1.5 g of soybean lecithin for injection and 2.5 g of glycerol for injection into a high-speed tissue masher, add an appropriate amount of water for injection, and prepare a uniform dispersed phase at a speed of 12000 rpm; mix the dispersed phase with Asarone 240 10 milligrams of oil for injection is preheated to 60-80°C, mixed to make colostrum, and the colostrum is added to water for injection to 100 milliliters, placed in a high-pressure homogenizer for repeated emulsification, and filtered through a 3-micron microporous membrane , and then filled with nitrogen and filled in an ampoule or an infusion bottle, and sterilized to obtain the lipid microsphere preparation for intravenous injection, which can also be taken orally.

Embodiment 2

[0035] Example 2 Preparation of lipid microsphere preparation of the present invention

[0036] Soybean lecithin for injection 1.2g and pronic (F-68) 0.3g and water for injection are first prepared into a uniform dispersed phase; add preheated 10 milliliters of oil for injection that is dissolved with 480 mg of asarone to make colostrum, Add water for injection to make up to 100 ml; emulsify under high pressure, filter through a 0.8-micron microporous membrane, fill it in an ampoule or an infusion bottle with nitrogen filling, and sterilize to obtain a lipid microsphere preparation for intravenous injection.

Embodiment 3

[0037] Example 3 Preparation of lipid microsphere preparation of the present invention

[0038] 1.5g of soybean lecithin for injection, 2.5g of glycerol for injection and water for injection are first prepared into a uniform dispersed phase; 20 ml of oil for injection that is dissolved with 240 mg of asarone in preheating is added to make colostrum, and water for injection is mixed to 100 ml, high-pressure emulsification, and filling with nitrogen to prepare intravenous lipid microsphere preparation.

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Abstract

The present invention provides one kind of lipid micropherical asarol preparation, which has alpha-asarol as active component and pharmaceutically used oil, emulsifier and water for injection and oral preparation. The lipid micropherical asarol preparation has high heat stability, no obvious change in physical and chemical properties in appertizing, high safety, no hemolysis, no allergy and no irritation.

Description

technical field [0001] The invention relates to an asarum cerebrolipid microsphere preparation and a preparation method thereof, belonging to the field of medicines. Background technique [0002] α-Asarone, also known as α-Asarone and Asarone, has a chemical name of 2,4,5-trimethoxy-1-propenylbenzene, and is one of the main active ingredients of the traditional Chinese medicine Shichangpu. Since the 1960s, extensive research has been carried out at home and abroad on it, and it has been proved that α-asarone monomer has strong pharmacological activity. In 1982, Guangxi Liuzhou Pharmaceutical Factory successfully synthesized it for the first time in China, and then tablets, capsules and injections were approved to be put on the market. It has been clinically proven that the drug has good curative effect in the treatment of chronic bronchitis, bronchial asthma and epileptic seizures [1-2] . [0003] Asarone is a highly fat-soluble compound, which is difficult to dissolve in...

Claims

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Application Information

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IPC IPC(8): A61K31/09
Inventor 金辉毛声俊吴宇梁臻
Owner 四川思达康药业有限公司
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