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Apogossypolone self-emulsifying drug delivery system and preparation method thereof

A technology of apogossypolone and gossypolone, which is applied in the self-emulsifying drug delivery system of apogossypolone and its preparation field, can solve the problems of low bioavailability and large individual differences, and achieve industrialization High degree, convenient clinical administration, and the effect of increasing drug loading

Inactive Publication Date: 2011-11-23
SHANGHAI YASHENG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] An object of the present invention is to overcome the defects of low in vivo bioavailability and large individual differences of the existing common oral preparations of apogossypolone, and provide a self-emulsifying drug delivery system for apogossypolone

Method used

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  • Apogossypolone self-emulsifying drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The composition of the prescription is as follows: (the dosage unit of each component is g)

[0036] Apogossypolone 6g

[0037] Gelucire 44 / 14 9.6g

[0038] Pluronic F68 7.2g

[0039] Transcotol P 7.2g

[0040] A total of 30g, made into 100 preparations.

[0041] Preparation process: Weigh the prescribed amount of Gelucire 44 / 14 and Pluronic F68, stir and heat in a water bath at 50-60°C, then add the prescribed amount of apogossypolone, stir until the drug is dissolved, then add the prescribed amount of Transcotol P , and stir evenly to obtain a uniform transparent solution, which is filled into capsules.

Embodiment 2

[0043] The composition of the prescription is as follows: (the dosage unit of each component is g)

[0044] Apogossypolone 0.1g

[0045] soybean oil 12g

[0046] Cremophor EL 24g

[0047] Propylene glycol 13.9g

[0048] A total of 50g, made into 150 preparations.

[0049] Preparation process: with embodiment 1.

Embodiment 3

[0051] The composition of the prescription is as follows: (the dosage unit of each component is g)

[0052] Apogossypolone 5g

[0053] Sesame oil 13g

[0054] Lecithin 4g

[0055] Cremophor RH40 15g

[0056] Ethanol 13g

[0057] A total of 50g, made into 150 preparations.

[0058] Preparation process: with embodiment 1.

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Abstract

The invention provides an apogossypolone self-emulsifying drug delivery system, which comprises the following components in percentage by mass: 0.2 to 20 percent of apogossypolone, 10 to 89.8 percent of oil phase, 5 to 50 percent of emulsifier, 5 to 50 percent of auxiliary emulsifier and 0 to 20 percent of organic acid, wherein the components form a uniform semisolid or liquid or solid formulation. The invention also provides a method for preparing the apogossypolone self-emulsifying drug delivery system. Compared with the ordinary apogossypolone oral preparation, the apogossypolone self-emulsifying drug delivery system can increase the biomembrane permeability of apogossypolone, improve bioavailability obviously, increase the solubility of the apogossypolone and improve a drug-loading rate. The preparation method is simple and high in operability and industrial degree; and the apogossypolone self-emulsifying drug delivery system is conveniently and stably taken in clinic.

Description

technical field [0001] The present invention relates to a novel delivery system of third-generation gossypol drugs and a preparation method thereof, in particular to a self-emulsifying drug delivery system of apogossypolone and a preparation method thereof. Background technique [0002] Cancer is a large class of diseases characterized by abnormal cell proliferation and metastasis, and has become one of the diseases that seriously endanger human health. At present, the commonly used antineoplastic drugs in clinical practice are mainly cytotoxic drugs, which have unavoidable disadvantages such as poor selectivity and strong side effects. With the rapid development of biogenetic engineering technology, molecular oncology, and molecular pharmacology research in recent years, people have gradually realized that the essence of cell carcinogenesis is the disorder of cell signal transduction. The overactive signal transduction pathways in most tumors lead to unlimited cell prolife...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/14A61K9/16A61K9/20A61K9/48A61K31/122A61P35/00
Inventor 温剑锋郭明杨大俊林艳琼
Owner SHANGHAI YASHENG MEDICAL TECH
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