High-bioavailability rapamycin composition and preparation method thereof

A technology of rapamycin and composition, which is applied in the field of high bioavailability rapamycin composition and preparation, can solve the safety problems of polymer materials and surfactants to be evaluated, and the long-term stability of nanoparticles to be evaluated Solve the problems of industrialization and complex preparation methods, and achieve the effects of increasing bioadhesion, low cost, and prolonging residence time

Active Publication Date: 2009-10-14
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Including the limited selection of pharmaceutical carrier materials (for drug-loaded nanoparticles), the industrialization of the preparation method is relatively complicated, the long-term stability of nanoparticles needs to be solved, and the safety issues of polymer materials and surfactants need to be solved. Evaluation, higher cost of preparation, etc.

Method used

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  • High-bioavailability rapamycin composition and preparation method thereof
  • High-bioavailability rapamycin composition and preparation method thereof
  • High-bioavailability rapamycin composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: Preparation of rapamycin composition

[0048] Weigh 1g of Eudragit S100, fully disperse and dissolve in an appropriate amount of absolute ethanol to form a uniform solution, weigh 0.2g of rapamycin, and dissolve in the above solution; take 1.0g of Aerosil 200 and mix with the above solution to make the liquid Fully adsorbed; the container containing the above mixture was placed in a vacuum desiccator, and the solvent was removed under reduced pressure to form a white blocky solid. Take it out, smash it, sieve it, and get it.

Embodiment 2

[0049] Embodiment 2: Preparation of rapamycin composition

[0050] Weigh 0.9g Eudragit S100, fully disperse and dissolve in absolute ethanol to form a homogeneous solution, weigh 0.3g rapamycin, and dissolve it in the solution; take 0.9g Aerosil 300 powder without mixing with the above solution, make The liquid was fully absorbed; the container containing the mixture was placed in a vacuum desiccator, and the solvent was removed under reduced pressure to form a white blocky solid. Take it out, smash it, sieve it, and get it.

Embodiment 3

[0051] Embodiment 3: Preparation of rapamycin composition

[0052] Weigh 140mg Eudragit S100, fully disperse and dissolve it in absolute ethanol to form a homogeneous solution, weigh 20mg rapamycin and dissolve it in the solution; take 120mg Cab-O-Sil H5 and mix with the above solution to make the liquid Fully adsorbed; the container containing the mixture was placed in a vacuum desiccator, and the solvent was removed under reduced pressure to form a white blocky solid. Take it out, smash it, sieve it, and get it.

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Abstract

The invention relates to a high-bioavailability rapamycin composition and a preparation method thereof. The drug release of the solid drug composition in a gastrointestinal tract has pH sensitivity. The high dispersivity of the drug in a carrier can obviously increase the absorption of rapamycin in the gastrointestinal tract or improve other properties of the drug, thereby obviously improving bioavailability, being capable of lowering administration dosage, namely reducing the usage of the raw materials in the preparation, and further saving the production cost greatly. The rapamycin composition can be processed into various oral solid dosage forms and has simple preparation process.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a high bioavailability rapamycin composition and a preparation method. The drug release of the solid pharmaceutical composition in the gastrointestinal tract has pH sensitivity, and the solid pharmaceutical composition can significantly increase the absorption of rapamycin in the gastrointestinal tract or improve other properties of the drug. Background technique [0002] Rapamycin (RAPA), also known as sirolimus, is a new type of high-efficiency macrolide immunosuppressant. It is a triene macrolide antibiotic with antifungal effect produced by the fermentation of Streptomyces filamentous bacteria. Vezina and Sehgal were isolated from soil on RapaNul Island in Canada in 1975. In 1977, Martel et al. reported that it had immunosuppressive effects. In October 1999, the US FDA approved the listing. Rapamycin is a white solid crystal with molecular formula C 51 h 79 NO ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/436A61K47/30A61K47/04A61K47/02A61P31/10
Inventor 王坚成张强郑华张婕
Owner PEKING UNIV
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