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Bullatacin ethosome gel and preparation method thereof

A technology of ethosomes and gels, which is applied in the field of bratasine preparations and its preparation, can solve the problems of large drug administration irritation and poor drug penetration effect, and achieve good biocompatibility and good fluidity , Promote the effect of percutaneous penetration

Inactive Publication Date: 2012-07-11
STAIDSON (BEIJING) BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the shortcomings of the prior art that the percutaneous administration of buratasine is highly irritating and the penetration effect of the drug is poor, and to provide a buratasine alcohol plastid gel and its preparation method

Method used

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  • Bullatacin ethosome gel and preparation method thereof
  • Bullatacin ethosome gel and preparation method thereof
  • Bullatacin ethosome gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0088] This example is used to illustrate the burata octanol plastid gel of the present invention and its preparation method.

[0089] 1. Preparation of Brataoctanol Plastids

[0090] Weigh 15.0 mg (mg) of blataxine, 0.30 g (gram) of hydrogenated soybean lecithin, 15.0 mg of stabilizer and 10 mg of antioxidant, dissolve them in 3.00 g of ethanol, place the above-mentioned ethanol solution in the conical flask for 40 ~60°C, 600rpm (rev / min) magnetic stirring conditions, inject 6.66g of distilled water at a constant speed and slowly (0.8ml / min) (this process is guaranteed to be carried out under airtight conditions to prevent ethanol volatilization), and continue the magnetic force after the distilled water is added. Stir for 10.0 min (minutes) to obtain the burataoctanol plastid suspension.

[0091] The obtained brataoctanol plastid suspension is sized, and the specific method is: under the condition of an ice-water bath, a digital display high-speed dispersing homogenizer (Sh...

preparation Embodiment 2

[0100] This example is used to illustrate the burata octanol plastid gel of the present invention and its preparation method.

[0101] 1. Preparation of Brataoctanol Plastids

[0102] Weigh 20.0 mg of bratasine, 0.40 g of soybean lecithin, 80.0 mg of cholesterol, 20.0 mg of stabilizer and 30 mg of antioxidant, dissolve them in 4.00 g of ethanol, and place the ethanol solution containing lipids and bratasine in the cone Into the shaped bottle, inject 5.45g of distilled water at a constant speed and slowly (0.6ml / min) under 45~55°C and 500rpm magnetic stirring (this process is guaranteed to be carried out under airtight conditions to prevent ethanol from volatilizing), and continue to stir for 8.00 min after the distilled water is added. min, that is, the suspension of brataoctanol plastids.

[0103] The obtained ethosome suspension was subjected to granulation, and the specific method was: under the condition of an ice-water bath, the probe ultrasonic instrument (Ningbo Xinzhi...

Embodiment 3-14

[0111] Examples 3-6 were prepared according to the method of Example 1, and Examples 7-14 were prepared according to the method of Example 2, and the differences are shown in Table 1.

[0112] Table 1

[0113]

[0114] Continued Table 1

[0115]

[0116] g stands for gram and mg stands for milligram, which is a unit of mass.

[0117] The burataoctanol plastid gel prepared in each embodiment of the above table is 20g.

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Abstract

The invention discloses a bullatacin ethosome gel and a preparation method thereof. The bullatacin ethosome gel comprises ethosomes and a gel, wherein the ethosomes and the gel exit in a uniformly mixed state; the ethosomes are particles containing bullatacin, phospholipids, low-molecular weight alcohols, cholesterol, stabilizers, antioxidants and water; the particle size of the ethosomes ranges from 30 nm to 400 nm; the gel contains a gel matrix, penetration enhancers, humectant, antiseptics, pH regulators and water; and the ethosomes and the gel are combined at a certain weight ratio, and the ethosomes and the gel have specific compositions respectively. The bullatacin ethosome gel provided by the invention can reduce irritation to the skin and has good percutaneous penetration effects.

Description

technical field [0001] The invention relates to a bratasine preparation and a preparation method thereof, in particular to a bratasine plastid gel and a preparation method thereof. Background technique [0002] Annonaceae (Annonaceae) plants belong to the dicotyledonous plant class Magnolia subclass, annonaceous acetogenins (Annonaceous acetogenins) is a class of drugs with a variety of biological activities, as early as the 1980s by American scholars from Annonaceae and other Annonaceae Extracted, separated, and purified from plants of the Litchiaceae family. In 1982, Jolad et al. first discovered that anemone lactone has anti-leukemia activity. Most of the annona lactones have different degrees of anti-tumor, cytotoxic, anti-bacterial, immunosuppressive and other significant activities, and they are also one of the compounds with the strongest anti-tumor activities reported in vivo and in vitro. [0003] Bullatacin is a lactone with the strongest anti-tumor activity among...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/00A61K31/365A61K47/24A61K47/32A61P35/00
Inventor 谭剑平蒋立新常坦然周志文
Owner STAIDSON (BEIJING) BIOPHARMACEUTICALS CO LTD
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