Albendazole liposome and preparation process thereof

Abstract

The invention relates to the technical field of veterinary albendazole preparation, in particular to an albendazole liposome and a preparation process thereof. A liposome of albendazole comprise thatfollowing component in parts by weight: 8 to 15 parts by weight of albendazole; 1- Palmitoyl group- 2- 25 to 35 part of oleoyl phosphatidyl glycerol, 6 to 15 part of dipalmitoyl phosphatidyl serine, 10 to 20 part of dierucyl phosphatidylethanolamine, 1 to 5 part of antioxidant, 2 to 6 part of additive. A liposome of albendazole and its preparation method, It can improve the solubility of albendazole, slow down drug release, increase the absorption rate of albendazole, increase the bioavailability of albendazole, increase the targeting and pertinence of the drug, and has high encapsulation efficiency and ABZ drug loading capacity. In addition, the preparation method is simple in production, easy in operation and low in cost.

Description

technical field [0001] The invention relates to the technical field of veterinary albendazole preparations, in particular to an albendazole liposome and a preparation process thereof. Background technique [0002] Albendazole (ADZ) is a benzimidazole derivative, also known as albendazole, which is white or off-white powder, odorless, tasteless, insoluble in water, slightly soluble in acetone or chloroform, and rapidly dissolves in the body. Metabolized to sulfoxide, sulfone alcohol and 2-amine sulfone alcohol. For intestinal nematodes, selectively and irreversibly inhibit the polymerization of the cytoplasmic microtubule system of the intestinal wall cells of the parasite, block its uptake and absorption of various nutrients and glucose, lead to the depletion of endogenous glycogen in the worm, and inhibit the reduction of fumaric acid The enzyme system prevents the production of adenosine triphosphate, so that the worms cannot survive and reproduce; the drug was chemically...

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Problems solved by technology

However, it has been on the market for more than 20 years, clinical observations have found that the drug can cause multi-system serious adverse drug reactions (SADR), such as encephalopathy, epilepsy, severe drug eruption and even death. There are many reports in the literature, which has attracted the attention of the medical community

[0003] In the clinical use of veterinarians, albendazole is the most widely used benzimidazole anthelmintic drug. It is not only highly effective against a variety of nematodes, but also has a strong repellent effect against certain trematodes and tapeworms, especially against echinococcosis , echinococcosis is an endemic disease that seriously endangers the health of humans and animals. At present, surgical treatment is still the main treatment. Albendazole has been clinically proven to be one of the anti-echinococcosis drugs with good effects, but there is still intestinal absorption Poor, the liver concentration is relatively low, and only about 30% of echinococcosis can be cured. At present, there is no new and more effective anti-echinococcosis drug, it is more economical and practical to develop a new dosage form or change the route of administration

The albendazole reported in current research is mainly common tablets, emulsions or suspensions, but due to the insoluble characteristics of albendazole in water and many organic solvents, its intestinal absorption rate and bioavailability are low, and it is effective The blood concentration is maintained for a short time, and the targeting of the liver and other organs is relatively small, and it cannot be effectively treated for targeted liver echinococcosis, etc., and the absorption process is slow and the absorption rate is low

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