Compound ivermectin solid dispersion and preparation method thereof

Abstract

The invention discloses a compound ivermectin solid dispersion. The compound ivermectin solid dispersion is prepared from the following raw materials in parts by weight: 0.1-5 parts of ivermectin, 1-20 parts of albendazole, 10-80 parts of an organic solvent, 5-90 parts of a macromolecular carrier and 2-15 parts of a surfactant. The invention also discloses a preparation method of the compound ivermectin solid dispersion. The preparation method comprises the following steps: solving the albendazole and the surfactant in the organic solvent to obtain a mixed solution; adding the ivermectin in the macromolecular carrier and heating for melting to obtain a melted liquid; mixing the mixed solution and the melted liquid, then heating and stirring to fully volatilize the organic solvent; and solidifying at low temperature, grinding and sieving to obtain a finished product. By virtue of a solid dispersion technology, the solubility of the ivermectin and the albendazole in water is enhanced, the oral bioavailability of the ivermectin and the albendazole is improved, the medicine dosage is reduced and the toxic and side effects are lowered; in addition, the compound ivermectin solid dispersion has good stability and excellent application prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a compound ivermectin solid dispersion and a preparation method thereof. Background technique [0002] Ivermectin is an antibiotic antiparasitic drug, which has a good killing effect on internal and external parasites, especially nematodes and arthropods. The effect of macrolide antiparasitic drugs on nematodes and arthropods is due to Increase the release of the inhibitory transmitter γ-aminobutyric acid (GABA) of the worm body, and open the Cl ion channel controlled by glutamate, enhance the permeability of the nerve membrane to Cl, thereby blocking the transmission of nerve signals, and eventually nerve Paralysis causes muscle cells to lose their ability to contract, resulting in the death of the parasite. [0003] Albendazole is a broad-spectrum anthelmintic with high efficiency and low toxicity. Clinically, it can be used to drive away round...

AI Technical Summary

Problems solved by technology

After being metabolized into sulfoxides or sulfones in the body, it can inhibit the absorption of glucose by parasites, resulting in the depletion of glycogen in the parasites, or inhibit the fumarate reductase system, hinder the production of ATP, and make the parasites unable to survive and reproduce

[0004] Ivermectin and albendazole, as commonly used clinical anti-nematode drugs, have a broad anti-worm spectrum and significant curative effect. However, due to the large-scale use of anti-worm drugs in recent years, drug-resistant parasites continue to appear. It is difficult to achieve the ideal therapeutic effect with insecticides. Since these two medicines are insoluble in water, they can only be administered through mixing materials, which requires a lot of labor and is prone to uneven mixing.

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