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Bioadhesive type hollow microsphere and preparation method thereof

A technology of bioadhesion and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems affecting the gas production and floating performance of preparations, and affect the residence time. Achieve the effect of improving bioavailability, improving bioadhesion, and good reproducibility

Active Publication Date: 2015-02-25
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to differences in gastric acidity between individuals and after fasting and full meals, the gas production and floating properties of such preparations are often affected, and the result will also affect their residence time in the stomach.

Method used

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  • Bioadhesive type hollow microsphere and preparation method thereof
  • Bioadhesive type hollow microsphere and preparation method thereof
  • Bioadhesive type hollow microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Dipyridamole bioadhesive hollow microspheres

[0041] 1. Basic experimental conditions:

[0042] The ratio of dipyridamole to ethyl cellulose is 1:5; 1.2% (w / v) of carbomer is used as the adhesive material; the ratio of anhydrous ethanol to anhydrous ether is 4:1 (v / v); liquid paraffin is Dispersion medium; the ratio of the dispersed phase to the continuous phase is 1:10 (v / v); 1.0% (w / v) of Span 80 is an emulsifier; 0.02% (w / v) of magnesium stearate is a dispersant; Stirring rate is 300r·min -1 ; Emulsification temperature is 10℃, curing temperature is 30℃; drying condition is 30℃ oven drying for 24h.

[0043] 2. Experimental operation:

[0044] Disperse carbomer, ethyl cellulose and dipyridamole in a mixed organic solvent, stir in a water bath at 10°C to dissolve the dispersed phase; add the dispersed phase slowly under mechanical stirring in a water bath at 10°C In the liquid paraffin containing emulsifier and dispersant, emulsify and volatilize after emulsifica...

Embodiment 2

[0055] Example 2: Selection of Carbomer Concentration

[0056] The concentration of carbomer was changed to prepare microspheres, the appearance was observed, and the floating rate and adhesion rate were measured. The results are shown in Table 2.

[0057] Table 2 The effect of carbomer 934 concentration on the properties of microspheres

[0058]

Embodiment 3

[0059] Example 3: Selection of organic solvent ratio

[0060] The concentration of organic reagents was changed to prepare microspheres, the appearance was observed, and the floating rate and adhesion rate were measured. The results are shown in Table 3.

[0061] Table 3 Effect of the ratio of ethanol to ether on the properties of microspheres

[0062]

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a bioadhesive type hollow microsphere of two alkalescent medicaments: dipyridamole and famotidine, and a preparation method thereof. The bioadhesive type hollow microsphere comprises medicaments, a skeleton material, a bioadhesive material, an emulsifying agent and a dispersing agent, wherein the preferred ratio of the medicaments to the skeleton material is 1 to (4-6). The bioadhesive type hollow microsphere is prepared by adopting an O / O emulsifying agent dispersion-volatilization method including the following steps: mixing the medicaments, the skeleton material and the bioadhesive type material weighed according to the amount of the prescription into an organic solvent, and stirring under low-temperature water bath condition for dissolving the medicaments, the skeleton material and the bioadhesive type material to obtain a dispersion phase; under the condition of 10DEG C water bath mechanical stirring, slowly dropwise adding the dispersion phase into liquid paraffin containing the emulsifying agent and the dispersing agent, performing low-temperature emulsification, heating and volatilizing to remove the organic solvent, separating, washing with n-hexane, drying and screening to obtain the bioadhesive type hollow microsphere. The prepared microsphere is high in encapsulation efficiency and yield, long in in-vivo retention time, and good in floatability, bioadhesion and slow-release property.

Description

Technical field [0001] The invention belongs to the technical field of medical preparations, and specifically relates to two weakly basic drugs dipyridamole and famotidine bioadhesive hollow microspheres and a preparation method thereof. Background technique [0002] Slow and controlled release preparations have always been the focus of pharmaceutical research. The effective absorption site of many drugs is in the upper middle and upper parts of the stomach or small intestine. Therefore, the greater the amount of medicine released in the upper middle and upper parts of the stomach and small intestine, the more absorbed. Ordinary sustained-release preparations can release the drug slowly, but during the process of transporting the drug from the stomach to the intestine, it will be affected by the changing physiological environment, and many drugs have passed the absorption site before being completely released. With the continuous maturity of technology in the medical field, it h...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/519A61K31/426A61K47/38A61K47/32
Inventor 朱澄云韩国华张雨萌王中彦万书彤姜雨萌陈洪涛包志红赵趱郑佳妮孙超周名扬王白红马欣莹张美微
Owner SHENYANG PHARMA UNIVERSITY
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