Albendazole large tablets and preparation technology thereof

Abstract

The invention discloses albendazole large tablets and a preparation technology thereof. The large albendazole tablets comprise 25wt% of glucosyl beta-cyclodextrin and 41.6wt% of albendazole as well as various auxiliary materials such as starch, apple green, brilliant blue, talcum powder, magnesium stearate and aluminium hydroxide. The preparation technology comprises the following steps of: preparation of starch slurry and a glucosyl beta-cyclodextrin inclusion compound of the albendazole, mixing, pelleting and tabletting. The albendazole large tablets have the advantages that the glucosyl beta-cyclodextrin inclusion compound is used for inclusion of the albendazole so as to improve the slow-release effect and the bioavailability of the albendazole, so that the effective haemoconcentration plasma concentration time of medicines is prolonged, the problem of difficulty in absorption by gastrointestinal tracts is solved, and the pharmaceutical effect is improved; the forming effect of the large tablets is good by the reasonable distribution of the contents of the components in the albendazole large tablets in combination with an inclusion process. The preparation technology is simple and convenient to operate. The albendazole large tablets are used for treating nematodosis in cattle gastrointestinal tracts in clinic, the expelling rate reaches 100%, after the albendazole large tablets are taken for 7 days, the negative conversion ratio and decrement rate of eggs are respectively 86.7% and 98.9%, after 14 days, the negative conversion ratio and the decrement rate reach 100% respectively, and the parasite expelling effect of the albendazole large tablets is obviously superior to those of medicine control groups.

Description

technical field [0001] The invention relates to the technical field of veterinary albendazole preparations, in particular to a large albendazole tablet and a preparation process thereof. Background technique [0002] Albendazole is a benzimidazole derivative, white or off-white powder, odorless, tasteless, insoluble in water, slightly soluble in acetone or chloroform, and rapidly metabolized into sulfoxide, sulfone alcohol and 2-amine sulfone in the body 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 worm cannot survive and reproduce. [0003] In the clinical use of veterinarians, albendazole is the most ...

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Problems solved by technology

[0004] In view of this, the present invention provides a kind of large albendazole tablet and preparation technology thereof, can improve the bioavailability of albendazole, solve the problem that large-scale albendazole molding effect is not good, some quality indicators such as disintegration time Unqualified, difficult to absorb in the gastrointestinal tract, etc.

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