Cyclosporine emulsion and the preparing method

A cyclosporine and self-emulsification technology, applied in the field of medicine, can solve the problems of low bioavailability, and achieve the effects of accurate quantification, easy storage, and good consistency

Inactive Publication Date: 2007-09-12
SHANGHAI KAIZHAO PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most cyclosporine drugs on the market have low bioavailability (such as Samdimmune), and polyoxyethylene castor oils (such as Cremophor EL and ethanol, etc.) are excipients that have obvious side effects on the human body

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The components and contents of the present embodiment cyclosporine self-emulsifying preparation are: 350mg (43.8%) Vitamin E-TPGS, 280mg (35.0%) Tween 80 (Tween 80), 70mg (8.7%) Pharmasolve, 100mg (12.5%) ) cyclosporine.

[0027] At the same time, 350mg vitamin E-TPGS (solid state), 280mg Tween 80 (Tween80, liquid state) and 70mg Pharmasolve (liquid state) were added while heating and stirring to 40°C. After these excipients are completely melted and mixed evenly, add 100 mg of cyclosporine powder. Continue heating and stirring at 50°C for 3 hours until the cyclosporine powder is completely dissolved in the liquid, and then it can be filled into capsules while hot. It is semi-solid after natural cooling to room temperature.

[0028] After inspection, the melting point of the formula is 30°C. This semi-solid formulation is waxy below 30°C for long-term storage. And when the temperature rises above 32°C, it will be in a liquid state, which is beneficial to the capsule...

Embodiment 2

[0032] The components and contents of the present embodiment cyclosporine self-emulsifying preparation are: 350mg (31.8%) Vitamin E-TPGS, 130mg (11.8%) Tween 80 (Tween 80), 520mg (47.3%) Pharmasolve, 100mg (9.1%) ) cyclosporine.

[0033] Add 350mg Vitamin E-TPGS (solid), 130mg Tween 80 (Tween 80, liquid) and 520mg Pharmasolve (liquid) successively or simultaneously and heat and stir to 40°C at the same time. After these excipients are completely melted and mixed evenly, add 100 mg of cyclosporine powder. Continue heating and stirring at 40° C. for 2 hours until the cyclosporine powder is completely dissolved in the liquid. It is liquid after natural cooling to room temperature.

[0034] The formula can always remain liquid at room temperature or generally low temperature, and does not start to solidify until 3-5°C. In water at 37°C under standard conditions, the formula itself is completely dissolved immediately, and the drug is dispersed into the whole system as a milky wh...

Embodiment 3

[0036] The components and content of cyclosporine self-emulsifying preparation in this example are: 315mg vitamin E-TPGS, 280mg Tween 80 (Tween 80), 105mg Pharmasolve, 100mg cyclosporine. It is semi-solid.

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Abstract

The present invention provides one kind of self-emulsified ciclosporin preparation and its preparation process. The self-emulsified ciclosporin preparation contains ciclosporin 5-25 wt%, vitamin E-TPGS 25-70 wt% and Pharmasolve 5-50 wt%. It has high stability, high medicine concentration, great capacity of self emulsifying, high bioactivity and easy taking, and may be used as orally taken liposoluble medicine.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a cyclosporine self-emulsifying preparation and a preparation method thereof. Background technique [0002] Self-emulsifying fat-soluble emulsification-based pharmaceutical formulations have attracted extensive attention and research due to their unique physical and chemical characteristics (Pannyiotis P. Conslantinides, 1995 "Pharmaceutical Research" 12 11). Generally speaking, microemulsifiers have good thermodynamic stability, and can make two types of immiscible media such as oil and water reach equilibrium through the interfacial film produced by the dispersant, thereby forming a transparent homogeneous emulsion. This feature can be used to improve the dissolution rate and bioabsorption rate of fat-soluble drugs in aqueous solution. [0003] Self-emulsifying drug delivery system (SEDDS for short) is a homogeneous, clear, isotropic solution that forms spontaneously in the aqueous pha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/13A61K9/08A61K9/107A61K9/48A61K47/34A61P37/06A61K47/26
Inventor 张凯曾昭氚
Owner SHANGHAI KAIZHAO PHARMA TECH
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