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Stable alprostadil injection emulsion and preparation method thereof

A technology for alprostadil and injection milk, which is applied in the field of alprostadil injection emulsion and its preparation, can solve the problems of enhancing the chemical stability of alprostadil and not revealing it, and achieves prolonging the shelf life, enhancing drug efficacy, and improving bioavailability. degree of effect

Inactive Publication Date: 2011-10-19
四川思达康药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is mentioned in the summary of the invention that poloxamer 188 (F-68) can be used as an auxiliary emulsifier, it does not reveal the following unexpected beneficial effects: that is, to improve poloxamer 188 (F-68) in the forefront The dosage of dil in the injection emulsion can significantly enhance the chemical stability of alprostadil in the injection emulsion and reduce its metabolic inactivation in the lung

Method used

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  • Stable alprostadil injection emulsion and preparation method thereof
  • Stable alprostadil injection emulsion and preparation method thereof
  • Stable alprostadil injection emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Add 5 mg of alprostadil to 100 g of preheated soybean oil, stir until the alprostadil dissolves completely to obtain an oil phase. Dissolve 15g of poloxamer 188 (F-68), 3g of lecithin for injection and 22g of glycerin for injection in an appropriate amount of water for injection preheated to 50°C and mix uniformly to obtain an aqueous phase. Slowly add the oil phase to the water phase, and stir in a high-speed tissue grinder for 10 minutes (10000 rpm) to disperse the oil phase evenly in the water phase to obtain milky white colostrum. Add the colostrum to 1000 ml of water for injection, and place in In a high-pressure homogenizer, homogenize for 3 times under the pressure of 5000Psi-15000Psi, then adjust the pH of the emulsion to 4.0-6.0, fill with nitrogen, and sterilize with rotary hot-press to obtain the alprostadil injection emulsion.

Embodiment 2

[0031] Add 5 mg of alprostadil to 100 g of preheated soybean oil, stir until the alprostadil dissolves completely to obtain an oil phase. Dissolve 30 g of poloxamer 188 (F-68), 6 g of lecithin for injection and 22 g of glycerin for injection in an appropriate amount of water for injection preheated to 50° C. and mix uniformly to obtain an aqueous phase. Slowly add the oil phase to the water phase, and stir in a high-speed tissue grinder for 10 minutes (10000 rpm) to disperse the oil phase evenly in the water phase to obtain milky white colostrum. Add the colostrum to 1000 ml of water for injection, and place in In a high-pressure homogenizer, homogenize for 3 times under the pressure of 5000Psi-15000Psi, then adjust the pH of the emulsion to 4.0-6.0, fill with nitrogen, and sterilize with rotary hot-press to obtain the alprostadil injection emulsion.

Embodiment 3

[0033] Add 5 mg of alprostadil to 100 g of preheated soybean oil, stir until the alprostadil dissolves completely to obtain an oil phase. Dissolve 30 g of poloxamer 188 (F-68), 3 g of lecithin for injection and 22 g of glycerin for injection in an appropriate amount of water for injection preheated to 50° C. and mix uniformly to obtain an aqueous phase. Slowly add the oil phase to the water phase, and stir in a high-speed tissue grinder for 10 minutes (10000 rpm) to disperse the oil phase evenly in the water phase to obtain milky white colostrum. Add the colostrum to 1000 ml of water for injection, and place in In a high-pressure homogenizer, homogenize for 3 times under the pressure of 5000Psi-15000Psi, then adjust the pH of the emulsion to 4.0-6.0, fill with nitrogen, and sterilize with rotary hot-press to obtain the alprostadil injection emulsion.

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Abstract

The invention discloses a stable alprostadil injection latex which takes alprostadil as active ingredient, contains oil for injection, emulsifier, glycerin for injection and water for injection which are accepted by pharmacy, and is prepared by emulsification technology. Compared with the existing alprostadil injection latex on the market, the stable alprostadil injection latex prepared by the invention can remarkably enhance the thermal stability of the alprostadil, prolong the period of validity of the alprostadil injection latex while reducing the degradation of the alprostadil at the lungand being beneficial to improving the bioavailability, thus further improving the drug effect.

Description

technical field [0001] The invention relates to an alprostadil injection emulsion and a preparation method thereof, belonging to the field of medicines. Background technique [0002] Alprostadil aka prostaglandin E 1 (prostaglandin E 1 , PGE 1 ) Its chemical name is: 11α, 15(S)-bishydroxyl-9-keto-13-reprostenic acid, and its chemical structural formula is as follows: [0003] [0004] Alprostadil is an endogenous physiologically active substance with various physiological and pharmacological effects. It dilates blood vessels, inhibits platelet aggregation, thromboxane A 2 Generation, atherosclerosis lipid plaque formation and the role of immune complexes, and can expand peripheral and coronary blood vessels, reduce gastric juice secretion, stimulate small intestine, uterine peristalsis. Clinically, it can be used to prevent and treat various cardiovascular and cerebrovascular diseases, male erectile dysfunction, severe peripheral vascular disease, adult respiratory d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/44A61K31/5575A61P9/00A61P11/00A61P15/10
Inventor 毛声俊袁菊勇李慧金辉吴宇储婷沈千万
Owner 四川思达康药业有限公司
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