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Beraprost acid nanolipid microsphere preparation

A technology of beraprost acid and lipid microspheres, which is applied in the direction of medical preparations with non-active ingredients, oil/fat/wax non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of poor stability, oral preparations, biological Problems such as low availability and high storage conditions

Active Publication Date: 2013-05-08
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the common problems of poor stability, short validity period, high storage conditions and low bioavailability of oral preparations in the current prostacyclin preparations, the purpose of the present invention is to prepare a prostacyclin that can be stored at room temperature, has a long validity period, and has high bioavailability. Injectable Beraprost Acid Nanolipid Microsphere Injection

Method used

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  • Beraprost acid nanolipid microsphere preparation
  • Beraprost acid nanolipid microsphere preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]Preheat 60g of refined soybean oil to 60-70°C, add 10g of refined soybean lecithin, stir with hand to form a uniform oil phase, then add 5mg of beraprost acid raw material drug into 1ml of ethanol to dissolve, slowly add to the above oil phase, Stir at 60-70°C at high speed (8000 rpm) for 3 minutes; add 35g of glycerin for injection, 3g of edetate disodium, 10mg of vitamin E, and 10mg of sorbitol with an appropriate amount of water for injection preheated to 60-70°C Form a uniform water phase after dilution; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10000 rpm, stir for 10 minutes, and form milky white colostrum after uniform dispersion ;Add colostrum to water for injection preheated to 60~70℃ to reach the full amount of 1000ml, transfer it to a high-pressure milk homogenizer, homogenize it under 5000~15000 Psi pressure for 10~12 times, take a sample to measure the particle size to the average ...

Embodiment 2

[0042] Preheat 70g of refined soybean oil to 60-70°C, add 12g of polyoxyethylene castor oil, stir with hand to form a uniform oil phase, then add 10mg of beraprost acid raw material drug to 1ml of ethanol to dissolve, slowly add to the above oil phase In the medium, stir at 60-70°C at high speed (8000 rpm) for 3 minutes; add 10g of glycerin for injection, 2g of edetate disodium, 15mg of vitamin E, and 10mg of sorbitol with an appropriate amount of preheated to 60-70°C Dilute with water for injection to form a uniform water phase; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10,000 rpm, stir for 10 minutes, and form a milky white after uniform dispersion Colostrum: add colostrum to the water for injection preheated to 60~70℃ to reach the full amount of 1000ml, transfer it to the high-pressure milk homogenizer, homogenize it under the pressure of 5000~15000 Psi for 10~12 times, take samples to measure th...

Embodiment 3

[0044] Mix 45g of refined soybean oil and 20g of coconut oil C8 / C10 triglyceride, preheat to 60-70°C, add 16g of poloxamer 188, stir with hand to form a uniform oil phase, then add 25mg of shellfish into 1ml of ethanol Dissolve the prostaglandin acid raw material, slowly add it to the above oil phase, stir at 60-70°C at high speed (8000 rpm) for 3 minutes; add 30g glycerin for injection, 1g sodium carbonate, 20mg vitamin E, and 15mg sorbitol Dilute an appropriate amount of water for injection preheated to 60~70°C to form a uniform water phase; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10000 rpm, Stir for 10 minutes to form milky white colostrum after uniform dispersion; add the colostrum to the water for injection preheated to 60~70℃ to reach the full amount of 1000ml, transfer it to a high-pressure homogenizer, and homogenize under the pressure of 5000~15000 Psi 10-12 times, take samples to measur...

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PUM

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Abstract

The present invention provides a beraprost acid nanolipid microsphere preparation, specifically relates to a beraprost acid nanolipid microsphere preparation which is stored at a normal temperature. The preparation comprises, by weight, 0.005-0.05 parts of an active ingredient of beraprost acid, 50-80 parts of oil for injection, 8-20 parts of an emulsifying agent, 1-5 parts of an emulsion stabilizer, 10-40 parts of glycerol for injection, an antioxidant, an osmotic pressure regulator and water for injection. According to the present invention, the nanopreparation has targeting property, and can be rapidly distributed on the lesion location to act on the lesion location after intravenous injection of the nanopreparation; the preparation provides the significant therapeutic effect for patients with severe arterial occlusion; the disadvantage of low bioavailability of the oral preparation due to the first pass effect is overcome; the preparation can be stored at the normal temperature, the storage period is two years, such that the convenience is provided for drug producing, drug storing, drug transporting and drug using, and the production cost of the drug is reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a beraprost acid nano-lipid microsphere preparation, in particular to a stable beraprost acid nano-lipid microsphere preparation with high bioavailability. Background technique [0002] Beraprost acid, also known as beraprost acid, chemical name is 2,3,3a-8b-tetrahydro-2-hydroxy-1-(3-hydroxy-4-methyl-1-octen-6 -ynyl)-1H-cyclopenta[b]benzofuran-5-butanoate, the chemical structure is as follows: [0003] [0004] Beraprost acid is a prostacyclin (PGI 2 )Derivatives. Among the various humoral factors synthesized by the vessel wall, prostacyclin (PGI 2 ) is the first substance on the market that can regulate blood vessel tension and maintain blood flow in various tissues. It is mainly produced by the metabolism of arachidonic acid in the blood vessel wall. Platelet aggregation and vasodilation, not only vascular endothelial cells but also vascular smooth muscle cells...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/5585A61K47/44A61K47/34A61K47/24A61P9/14
Inventor 刘红星张扬程栎王伟肖萱周丽莹
Owner BEIJING TIDE PHARMA