Solid bicyclic alcohol dispersion

A technology of solid dispersion and bicyclic alcohol, which is applied in the direction of organic active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as high rebound rate, lack of multi-center clinical verification, and slow dissolution rate. Effects of improved bioavailability and improved dissolution rate in vitro

Active Publication Date: 2008-11-26
BEIJING UNION PHARMA FACTORY
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem is that the rebound rate is high after stopping the drug. Although it has been found to have a certain inhibitory effect on the replication of hepatitis B virus, it lacks multi-center clinical verification. In addition, bifendate has no patent protection, so it is not competitive internationally
[0007] Due to the poor water solubility of bicyclic alcohol in the prior art, the in vitro dissolution rate of its ordinary tablet is relatively slow. When distilled water is used as the dissolution medium, it can only dissolve 60%-70% within two hours. The degree is low, showing more significant individual differences, which is not conducive to the exertion of its curative effect

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Solid bicyclic alcohol dispersion
  • Solid bicyclic alcohol dispersion
  • Solid bicyclic alcohol dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1: preparation of bicyclic alcohol / PVP solid dispersion

[0059] Ratio of drug to carrier: Execute according to the table.

[0060] Table 1 drug / PVP solid dispersion feed ratio

[0061] Test No.

[0062] Preparation: Prepared by solvent method. According to the dosage in Table 1, weigh PVP and dissolve it in a certain volume of absolute ethanol, add bicyclic alcohol, and heat at 50°C to dissolve completely. Then, the solvent was removed by rotary evaporation under reduced pressure at 50°C, placed in a vacuum drying oven, and dried overnight at 40°C. The next day, it was taken out and crushed through a 60-mesh sieve to obtain four groups of bicyclic alcohol / PVP solid dispersions.

Embodiment 2

[0063] Embodiment 2: preparation of bicyclic alcohol / PVP physical mixture

[0064] Ratio of drug to carrier: Execute according to the table.

[0065] Table 2 Drug / PVP physical mixture feed ratio

[0066] Test No.

[0067] PVP volume

[0068] Preparation: Prepare directly by mixing. Pass PVP and bicyclic alcohol through 80-mesh sieve respectively, feed according to the ratio in Table 2, sieve and mix, and obtain four groups of bicyclic alcohol / PVP physical mixtures.

Embodiment 3

[0069] Embodiment 3: preparation of bicyclic alcohol / PEG solid dispersion

[0070] Ratio of drug to carrier: Execute according to the table.

[0071] Table 3 drug / PEG solid dispersion feed ratio

[0072] Test No.

[0073] Preparation: Prepared by melting method. According to the dosage in Table 3, weigh PEG8000, heat it at 70~80°C until it is completely melted, add bicyclic alcohol, stir well, continue heating until it is completely melted, quickly put it into an ice-water bath to cool and solidify, and crush it through a 60-mesh sieve to obtain Four sets of bicyclic alcohol / PEG solid dispersions.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The present invention discloses solid dispersion prepared with bicyclic alcohol and polymer material PEG6000 and Poloxemer 188 treated via melting process and PVP treated via solvent process, and medicine and carrier are mixed directly to prepare physical mixture. The prepared sample is measured via X-powder diffraction, differential thermal analysis, dissolvability and leaching rate determination to examine the dispersion state and the improvement of solid dispersion on medicine water solubility and leaching rate. The extracorporal research shows the promotion of solid dispersion technology on the intracorporal absorption of bicyclic alcohol and the intracorporal and extracorporal relationship.

Description

technical field [0001] The present invention relates to a solid dispersion comprising a bicyclic alcohol and a hydrophilic material. In particular, it relates to a solid dispersion of bicyclic alcohol and polymer materials such as PEG6000, PVP and Poloxemer188, and a pharmaceutical composition containing the solid dispersion and a pharmaceutically acceptable carrier. Background technique [0002] Viral hepatitis has a high incidence in my country and is one of the common diseases that seriously endanger people's health. According to the serum epidemiological survey, the prevalence rate of hepatitis A virus infection is 80.9%, the prevalence rate of hepatitis B virus infection is 57.6%, the positive rate of hepatitis B surface antigen (HBsAg) is 9.75%, and the infection rate of hepatitis C virus is 3.2%. , D and E hepatitis are also popular. In the acute stage of viral hepatitis, except for hepatitis C, most of them are self-limiting diseases, especially hepatitis A and E, ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61K9/20A61K9/16A61K9/48A61P1/16A61P31/12
Inventor 刘玉玲李燕陈丙跃
Owner BEIJING UNION PHARMA FACTORY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap