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Puerarin self-microemulsion composition based on mixed oil and preparation method thereof

A puerarin self-micro-composition technology, applied in the field of pharmaceutical preparations, to achieve the effects of increasing absorption in the body, reducing the risk of adverse reactions, and reducing the proportion

Inactive Publication Date: 2012-03-21
GUANGDONG HUANAN PHARMACEUTICAL GROUP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 02135329.8 reports a puerarin oral preparation and its preparation method. Although phospholipids and polysorbate 80 are also included in its prescription composition, the oral preparation utilizes charge migration, hydrogen bond interaction and The puerarin phospholipid solid dispersion formed by van der Waals force, polysorbate 80 is a solubilizer, and phospholipids and polysorbate 80 are used as emulsifiers in microemulsions and self-microemulsions, so this oral preparation does not belong to microemulsions and self-microemulsions. Microemulsion category, patent application: 200510025418.9 reports a self-microemulsified puerarin oral preparation, example 2 of the patent, the oil phase mass percentage is 55%, the prescription particle size is 341.2nm, also does not belong to the microemulsion category , and the patent right limits the mass percentage of the oil phase to 5-35%
Therefore, microemulsion and self-microemulsion preparations must reduce the amount of emulsifier as much as possible under a certain drug loading. How to reduce the amount of emulsifier and co-emulsifier in microemulsion and self-microemulsion preparations has become the focus of pharmaceutical research. There is no report on the use of mixed oil as the oil phase of the self-microemulsion system in the patents and literature related to puerarin self-microemulsion

Method used

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  • Puerarin self-microemulsion composition based on mixed oil and preparation method thereof
  • Puerarin self-microemulsion composition based on mixed oil and preparation method thereof
  • Puerarin self-microemulsion composition based on mixed oil and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Prescription components and their weight percentages:

[0027] Puerarin 3.5%, Polysorbate 80 29.0%, Polyoxyethylene Castor Oil 14.5%, Propylene Glycol 14.5%, MCT oil 28.9%, Oleic Acid 9.6%

[0028] The preparation process of the puerarin self-microemulsion composition in the present embodiment is: mix the MCT oil and oleic acid of the prescription amount, stir well, and set aside; mix polysorbate 80, polyoxyethylene castor oil and propylene glycol in proportion, Stir evenly; ultrasonically dissolve the prescribed amount of puerarin in a mixture of polysorbate 80, polyoxyethylene castor oil and propylene glycol at 40°C-50°C, after cooling, add the spare MCT oil and oleic acid mixed oil, Stir well and serve.

[0029] After diluting 100 times with water, the particle size distribution was determined to be 18.99 nm by using a Malvern particle size potential analyzer (Nano-ZS90).

[0030] The beneficial effects of the present embodiment are: (1) when respectively adopting ...

Embodiment 2

[0032] Prescription components and their weight percentages:

[0033] Puerarin 1.5%, Polyoxyethylene Castor Oil 32.8%, Isopropanol 16.5%, GTCC 24.6%, Glyceryl Linoleate 24.6%.

[0034] The preparation method is the same as in Example 1. After diluting 100 times with water, the particle size distribution was determined to be 34.07 nm by using a Malvern particle size potentiometer.

[0035] The beneficial effects of the present embodiment are: (1) when respectively adopting GTCC or glyceryl linoleate as the oil phase, polyoxyethylene castor oil as the emulsifier, and isopropyl alcohol as the co-emulsifier, if you want to obtain the self-dilution-resistant During microemulsion, oil: the ratio of mixed emulsifier will be less than or equal to 1: 9, present embodiment adopts GTCC: the mixed oil of linoleic acid glyceride=1: 1 is made oil phase, oil phase: the ratio of mixed emulsifier is 5:5, significantly reducing the quality of the mixed emulsifier. (2) In this embodiment, the...

Embodiment 3

[0037] Prescription composition and its weight percentage:

[0038] Puerarin 2.0%, polyoxyethylene hydrogenated castor oil 26.1%, diethylene glycol monoethyl ether 13.1%, glyceryl linoleate 29.4%, Miglyol 812N 29.4%.

[0039] The preparation method is the same as in Example 1. After diluting 100 times with water, the particle size distribution was determined to be 46.98 nm by using a Malvern particle size potentiometer.

[0040] The beneficial effects of this embodiment are: (1) when using Miglyol 812N or glycerol linoleate as the oil phase, polyoxyethylene hydrogenated castor oil as the emulsifier, and diethylene glycol monoethyl ether as the co-emulsifier, If you want to obtain a self-microemulsion that is resistant to dilution, the oil: the ratio of the mixed emulsifier should be less than or equal to 1:9. This embodiment uses Miglyol 812N: a mixed oil of linoleic acid glyceride=1:1 as the oil phase, and the oil The phase:mixed emulsifier ratio was 6:4, significantly redu...

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Abstract

The invention discloses a puerarin self-microemulsion composition, which consists of puerarin, mixed oil, an emulsifier and an auxiliary emulsifier by weight percent, wherein the puerarin accounts for 0.5-5 percent; the mixed oil accounts for 36-61 percent; the emulsifier accounts for 10-50 percent; and the auxiliary emulsifier accounts for 5-30 percent. The puerarin self-microemulsion composition prepared in the invention not only solves the problems of the traditional emulsion such as large particle size, and poor stability, large storage volume and the like due to existence of the aqueous phase, but also improves the solubility and dispersion of puerarin, increases the in vivo absorption of drugs, and enhances the bioavailability. The invention has the advantages of low viscosity, stable quality and the like, and can improve the drug absorption, enhance the bioavailability and reduce the toxic and side effects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a puerarin self-microemulsion composition and a preparation method thereof, in particular to a self-microemulsion preparation method capable of reducing the amount of emulsifier used in a self-microemulsion system. technical background [0002] Puerarin is the active ingredient isoflavone glycoside extracted and separated from the leguminous plant Pueraria lobata, and its chemical name is 4,7-dihydroxy-8-β-D-glucosyl isoflavone. Clinical studies have shown that puerarin can dilate coronary arteries, protect global ischemic myocardium and myocardial ischemia-reperfusion injury, reduce the size of acute myocardial infarction, reduce myocardial oxygen consumption, and prevent platelet adhesion, aggregation and formation. As a vasodilator, puerarin can be used to treat diseases related to coronary heart disease, angina pectoris and cardio-cerebral circulation disorders, as we...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K31/352A61K9/107A61K9/48A61K9/20A61K9/16A61K9/00A61K47/44A61K47/34A61P9/10A61P7/02A61K47/10A61K47/26
Inventor 陈小新龙超峰谢称石李碧红
Owner GUANGDONG HUANAN PHARMACEUTICAL GROUP CO LTD
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