Alprostadil liposome and preparation method thereof

Abstract

The invention provides alprostadil liposome, which contains alprostadil, egg yolk lecithin, maltose and butylated hydroxytoluene, wherein the average double-layer number L is 1.1-1.5, preferably 1.3,each preparation unit of the alprostadil liposome contains 10 to 40 [mu]g of alprostadil, 3 to 40 mg of egg yolk lecithin, 50 to 600 mg of maltose and 20 to 160 [mu]g of butylated hydroxytoluene, andthe particle size of the liposome is 80 to 200 nm. According to the invention, more few-layer liposome is formed in the preparation process, the active ingredients are wrapped in different layers, andduring release, the medicine wrapped in the inner layer needs to cross the multi-layer film, so that the release of the medicine from the liposome is delayed so as to achieve slow release effect andgood curative effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an alprostadil liposome and a preparation method thereof. Background technique [0002] Alprostadil (PGE1) has a wide range of biological effects, clinically in cardiovascular disease, respiratory system disease, cerebrovascular disease, diabetic complications, pulmonary hypertension, kidney disease, male infertility disease, hepatorenal syndrome (HRS) and other aspects Both have applications. However, the adverse reactions of alprostadil are manifested in local pain, swelling, irritation, heating, redness, itching and other phenomena during injection. The mechanism is that after alprostadil enters the human body, it will stimulate the blood vessels of the body and produce serotonin and bradykinin. , causing inflammation and pain to the blood vessels, with the increase of drug concentration, the adverse reactions will be more serious. And in the process of blood circu...

AI Technical Summary

Problems solved by technology

And in the process of blood circulation, alprostadil will be rapidly inactivated by 15-hydroxydehydrogenase in the lung, liver and kidney, resulting in the loss of curative effect

[0003] The first generation of alprostadil is an ordinary powder injection, which does not have targeting properties. It is easily inactivated in the lungs, and the side effects are also very large. After injection, the patient has severe vascular pain and severe digestive tract reactions. Good, but not clinically applicable

The second-generation alprostadil is a cyclodextrin inclusion compound. Although some local side effects are reduced by cyclodextrin encapsulation, it does not have targeting, and the dosage is relatively large, generally 100-200 μg. The active ingredients are less, which affects the clinical effect

But liposphere preparation still has certain irritation, and stability is poor, must be stored at 0-5 ℃, and the validity period of product is only 12 months, and its degradation product prostaglandin A1 limit is high, about 60% of main drug, not Easy for clinical use

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