Neurosteroid derivative solid dispersion, preparation method and application thereof, and therapeutic drug for central nervous system disorder related diseases

The solid dispersion of neurosteroid derivatives prepared by the hot melt extrusion process solved the problems of poor water solubility and low solubility of neurosteroid compounds, and significantly improved their oral bioavailability.

CN119632996APending Publication Date: 2025-03-18HUNAN MINGRUI PHARMACEUTICAL CO LTD
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Patent Information

Application Number
CN202411783308.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-06
Publication Date
2025-03-18

AI Technical Summary

Technical Problem

Neurosteroidal compounds generally have poor water solubility and low solubility, which leads to insufficient bioavailability of drugs in the human body, limiting their clinical application.

Method used

A hot melt extrusion process is used to prepare a solid dispersion of neurosteroid derivatives. By melting and extruding the active ingredient, plasticizer and carrier material at a suitable temperature, the active ingredient exists in an amorphous state, and its solubility and bioavailability are improved.

Benefits of technology

The oral bioavailability of neurosteroid derivatives is significantly improved, the active ingredient has a suitable dissolution rate and a high absolute dissolution, which solves the problem of insufficient bioavailability of the original drug.

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Abstract

The invention provides a neurosteroid derivative solid dispersion, a preparation method and application thereof, and a medicine containing a hot-melt extrusion solid dispersion, and belongs to the technical field of pharmacy. The preparation method comprises the following steps: carrying out melt extrusion on a raw material mixture at 125-160 DEG C to obtain the neurosteroid derivative solid dispersion, the mixed material comprises an active component, a plasticizer and a carrier material in a mass ratio of 10: (1-15): (10-90); the active component comprises at least one of a neurosteroid derivative (with a structure as shown in a formula 1), an isomer, a solvate and a pharmaceutically acceptable salt thereof; the plasticizer is selected from one or more of polyethylene glycol, poloxamer and Tween, and the average molecular weight of the polyethylene glycol is 1t; 6000, 6000; active components in the neurosteroid derivative solid dispersion exist in an amorphous state. The neurosteroid derivative in the neurosteroid derivative solid dispersion disclosed by the invention has relatively high oral bioavailability. # imgabs0 #
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