Application of hydroxypropyl-beta-cyclodextrin in preparation of Vilciguat solid preparation, solid preparation and preparation method

By using hydroxypropyl-β-cyclodextrin with an average substitution degree of 3.5-5.5 in Vilixigua to form an inclusion compound, combined with specific conditions and acetone solvent, the problem of low solubility of Vilixigua is solved, and the Efficient drug absorption and stability simplifies the preparation process and reduces costs.

CN119185590AActive Publication Date: 2024-12-27JINAN LIMIN PHARMA
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Patent Information

Application Number
CN202411718855.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-11-28
Publication Date
2024-12-27
Estimated Expiration
2044-11-28

AI Technical Summary

Technical Problem

The prior art is difficult to effectively improve the solubility and bioavailability of Vilixigua, and common methods have high requirements for equipment or lead to problems such as uneven granulation and degradation of active ingredients.

Method used

Hydroxypropyl-β-cyclodextrin with an average substitution degree of 3.5-5.5 was used to form an inclusion compound with Vilicigua. Combined with specific temperature and pH conditions, acetone was used as a solvent to prepare a solid preparation by wet granulation process.

Benefits of technology

The high solubility and stability of Vilixigua are achieved, the in-batch differences are reduced, the drug absorption rate and stability are improved, the production cost is reduced, the active ingredient degradation is avoided, and the preparation process is simple.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention belongs to the technical field of medicine preparation, and particularly relates to application of hydroxypropyl-beta-cyclodextrin in preparation of a Velciguat solid preparation, the solid preparation and a preparation method. The key protection of the invention is as follows: hydroxypropyl-beta-cyclodextrin is applied to the formation of a Vilciguat-cyclodextrin inclusion compound with Vilciguat, and then the inclusion compound is combined with other raw materials to prepare the Vilciguat solid preparation with excellent solubilizing effect, the average substitution degree of the hydroxypropyl-beta-cyclodextrin is 3.5-5.5, the viscosity of the hydroxypropyl-beta-cyclodextrin is 3.5-5.5, the viscosity of the hydroxypropyl-beta-cyclodextrin is 3.5-5.5, the viscosity of the hydroxypropyl-beta-cyclodextrin is 3.5-5.5, and the viscosity of the hydroxypropyl-beta-cyclodextrin is 3.5-5.5. This is one of the keys of the invention. According to the present invention, a large number of experiments are performed, different types of beta-cyclodextrin and beta-cyclodextrin with different substitution degrees are compared, and finally hydroxypropyl-beta-cyclodextrin with an average substitution degree of 3.5-5.5 is selected to clathrate viriciguat, such that compared with hydroxypropyl-beta-cyclodextrin with other substitution degrees or other solubilizers, the solubilizing effect is excellent, and the solubilizing effect is good. Meanwhile, the stability is good, and the total impurity is almost unchanged after acceleration for 3 months.
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Citation Information

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