Solid self-microemulsion based on spherical crystallization technique and preparation method thereof

A self-microemulsion, solid technology, applied in the field of medicine, achieves the effects of low production cost, high yield, and reduced liver and kidney toxicity

Inactive Publication Date: 2013-09-25
胡容峰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no reports related to the preparation of solid self-microemulsion or solidification of self-microemulsion by spherulite technology in the literature.

Method used

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  • Solid self-microemulsion based on spherical crystallization technique and preparation method thereof
  • Solid self-microemulsion based on spherical crystallization technique and preparation method thereof
  • Solid self-microemulsion based on spherical crystallization technique and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 【Prescription】

[0035]

[0036] 【Preparation Process】

[0037] Preparation of fenofibrate self-microemulsion: Weigh 1.0g of the insoluble drug according to the prescription, dissolve it in 1.0ml ethanol, and then add the prescription amount of caprylic capric triglyceride, polyoxyethylene hydrogenated sesame oil and propylene glycol in sequence, and stir. The fenofibrate self-microemulsion is obtained evenly.

[0038] Preparation of fenofibrate solid self-microemulsion: weigh 0.5 ethyl cellulose, 0.05g PEG4000 in a small beaker, add 2ml of acetone and 4ml of dichloromethane to completely dissolve or suspend it, add fenofibrate to Microemulsion is placed in a small beaker, add an appropriate amount of micronized silica gel, slowly inject it into a poor solvent containing 0.08% SDS aqueous solution, the temperature is controlled at 25 ℃, the speed is 400 rpm, continuous stirring for 1 hour, add appropriate amount of distilled water, continue to stir for 10 minutes, until Ful...

Embodiment 2

[0041] 【Prescription】

[0042]

[0043] 【Preparation Process】

[0044] Preparation of fenofibrate self-microemulsion: Weigh 2.50g of fenofibrate according to the prescription, dissolve it in 1.0ml ethanol, and add the prescription amount of caprylic capric triglyceride, polyoxyethylene hydrogenated sesame oil and propylene glycol in sequence , Stir evenly to obtain fenofibrate self-microemulsion.

[0045] Preparation of fenofibrate solid self-microemulsion: Weigh 0.5g ethyl cellulose and 0.05g PEG4000 in a small beaker, add 2ml acetone and 4ml chloroform to completely dissolve or suspend it, add the above-mentioned fenofibrate self-microemulsion Milk in a small beaker, add an appropriate amount of micronized silica gel, slowly inject it into a poor solvent containing 0.08% SDS aqueous solution, control the temperature at 25°C, rotate at 400rpm, continue stirring for 1h, add appropriate amount of distilled water, continue stirring for 10min, until aggregate The body particles are n...

Embodiment 3

[0048] 【Prescription】

[0049]

[0050]

[0051] 【Preparation Process】

[0052] Preparation of glimepiride self-microemulsion: Weigh 1.0g glimepiride according to the prescription, dissolve it in 1.0ml ethanol, and add the prescription amount of caprylic acid capric triglyceride, polyoxyethylene hydrogenated sesame oil and propylene glycol in sequence. Stir evenly to obtain glimepiride self-microemulsion.

[0053] Preparation of glimepiride solid self-microemulsion: weigh 0.5mg ethyl cellulose and 0.05g PEG4000 into a small beaker, add 2ml acetone and 4ml dichloromethane to completely dissolve or suspend it, add the above glimepiride Add 1.0g of self-microemulsion in a small beaker, add appropriate amount of micronized silica gel, slowly inject it into a poor solvent containing 1% PVA aqueous solution, control the temperature at 25°C, rotate at 400rpm, continue stirring for 1h, add appropriate amount of distilled water, and continue stirring 10min, until the aggregate particles do...

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Abstract

The invention relates to the medical technology field, and particularly relates to a solid self-microemulsion based on a spherical crystallization technique and a preparation method thereof. The solid self-microemulsion is characterized in that: with the use of the spherical crystallization technique, the solid self-microemulsifying micoparticles are prepared from poorly water soluble drugs in a liquid phase by one step. The solid self-microemulsion with the poorly water soluble drugs comprises the components, by weight: 0.1 to 1.5 g of the poorly water soluble drugs, 4.0 g of a polyoxyethylene hydrogenated castor oil, 2.0 g of capric caprylic triglyceride, 2.0 g of tpropylene glycol, 1.0 ml of ethanol, 4.0 ml of dichloromethane, 0.5 to 1.1 g of ethylcellulose (or Eudragit RS100, RL100), 0.05 g of PEG4000, and 0.5 g of colloidal silicon dioxide. The poorly water soluble drugs include cyclosporine A, fenofibrate, glimepiride, cilnidipine, isradipine, simvastatin, baicalein, neogambogic acid, puerarin, cyclovirobuxine D, silymarin and the like.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of a pharmaceutical preparation, specifically, a kind of insoluble drug solid self-microemulsion particle and a preparation method thereof. Specifically, it is a kind of insoluble drug solid self-microemulsion particles prepared in one step in the liquid phase. 2. Background technology [0002] Self-microemulsifying drug delivery system (SMEDDS) is composed of emulsifier, co-emulsifier and oil phase, and its basic feature is that it can be formed spontaneously under gastrointestinal peristalsis or ambient temperature (usually body temperature) and gentle stirring Isotropic transparent or translucent o / w dispersion system with a particle size of 10-100nm. In 1994, Novartis's Sandimmun Neoral (cyclosporine soft capsule / Sandimmun Neoral) was successfully listed, which greatly promoted the research of self-microemulsion. SMEDDS has the following advantages: ①...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/107A61K47/32A61K47/38A61K47/44
Inventor 胡容峰白中稳高松
Owner 胡容峰
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