Lopinavir and ritonavir compound high-uniformity nano co-dispersion body and preparation method thereof

Abstract

The invention provides a lopinavir and ritonavir compound high-uniformity nano co-dispersion body. The lopinavir and ritonavir compound high-uniformity nano co-dispersion body consists of lopinavir and ritonavir which are taken as active ingredients, a dispersing aid, an anti-agglormeration material, a dispersing stabilizer, a dispersion supporter and a lubricant. The lopinavir and ritonavir which are taken as active ingredients account for 25%-60%. The lopinavir and ritonavir compound high-uniformity nano co-dispersion body prepared by the preparation method disclosed by the invention can be prepared into a single-dose preparation according to a normal method. According to a dissolution rate experiment, the preparation disclosed by the invention has release amount of 40%-80% within 30 minutes. The preparation prepared by the dispersion body disclosed by the invention is high in dissolution rate, and can be used for improving the bioavailability. The lopinavir and ritonavir compound high-uniformity nano co-dispersion body prepared by the preparation method disclosed by the invention satisfies and is superior to mixing uniformity standards. The preparation method disclosed by the invention is simple and easy to implement, can be used for popularizing application of a nano mechanical grinding technology on the pharmaceutical industry and promoting the development of the technology, and is suitable for industrial production and greater in application value.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a high-uniformity nanometer co-dispersion, in particular to a compound high-uniformity nanometer co-dispersion of lopinavir and ritonavir and a preparation method thereof. Background technique [0002] According to reports, about 40% of the active substances that play the main pharmacological activity in drugs are insoluble in water. Poorly water-soluble drugs (poorly water-soluble drugs) are difficult to be absorbed by the body due to their low solubility in water, and the elimination speed in the body is relatively fast, with poor bioavailability. At present, it is more and more difficult to find drugs with new chemical structures, and even if new candidate drugs are found, about 40% of the candidate drugs cannot be marketed due to the defect of poor water solubility. According to reports, it is estimated that about 65 billion US dollars of drugs are produced globally every year ...

AI Technical Summary

Problems solved by technology

Hot-melt extrusion technology is a kind of solid dispersion technology, which can well form solid dispersion of drugs and solid excipients in the molten state, but the hot-melt extrusion process has its limitations, such as: 1. When extruding The temperature generally needs to be above 100 degrees. When the production is in operation, the uniformity of the temperature control of each part of the extrusion is not very good; second, the extruded material is generally in the shape of strips or columns and needs to be crushed. It is necessary to add a certain amount of plasticizer, so it is difficult to crush these materials; third, the hygroscopicity of hot-melt extruded materials is relatively high, and the humidity needs to be controlled during storage, and the operating conditions need to be adjusted during subsequent operations. Strict control; four, because lopinavir and ritonavir need to be hot-melt dispersed in the matrix, so the mass of the matrix is ​​required to be more than 3 times the amount of the raw material, resulting in the made tablets being too heavy and unsuitable for taking. convenient

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