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Method for preparing biodegradable spherical porous starch foam and application

A porous starch and biological technology, applied in the field of pharmacy, can solve the problems of unseen and improve the water solubility of insoluble drugs, and achieve the effects of low production cost, improved specific surface area and dispersibility, and uniform particle size

Inactive Publication Date: 2010-11-10
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The technology of preparing biodegradable spherical porous starch foam is mainly spray method (G.M.Glenn, S.H.Imam, A.P.Klamczynski, B-S.Chiou, D.F.Wood, W.J.Orts.Structure of Porous StarchMicrocellular Foam Particles.Microsc Microanal 14 (Suppl 2) at present, 2008:150-151.), and so far there is no report on improving the water solubility of insoluble drugs

Method used

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  • Method for preparing biodegradable spherical porous starch foam and application
  • Method for preparing biodegradable spherical porous starch foam and application
  • Method for preparing biodegradable spherical porous starch foam and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 1.25g, 1.6g, and 2g of soluble starch in a 25ml beaker, add 20ml of water to make the concentration of the aqueous starch solution 6%, 8%, and 10%, stir, put in a boiling water bath for 20min, and place it at 80°C as the water phase. Toluene: chloroform (3:1) is the oil phase, Span80 is the emulsifier, mix the water phase and the oil phase (1:20), stir or homogenize at high speed to form a uniform W / O emulsion, and put it in a -20°C refrigerator Freeze and stratify, add 40% ethanol to separate and remove the organic layer, and the obtained aqueous phase is equilibrated for 6 hours and then equilibrated with 60% ethanol for suction filtration, and then followed the previous steps to equilibrate with 80% and 100% ethanol to remove the gel beads. Water, form the alcohol gel pellet of porous structure, after suction filtration, the product is put in the vacuum desiccator and dried 24h.

Embodiment 2

[0044] Weigh 1.25g, 1.6g, and 2g of pressed rice starch into a 25ml beaker, add 20ml of water to make the concentration of the aqueous starch solution 6%, 8%, and 10%, stir, stir, put in a boiling water bath for 20 minutes, and place at 80°C as water phase, using toluene: chloroform (3:1) as the oil phase, Span80 as the emulsifier, mixing the water phase with the oil phase (1:20), stirring or homogenizing at a high speed to form a uniform W / O emulsion, and adding- Refrigerate and stratify at 20°C, add 40% ethanol to separate and remove the organic layer, and balance the obtained aqueous phase with 60% ethanol for 6 hours, then balance with 80% and 100% ethanol according to the previous steps to remove gel particles. The water in the ball forms the alcohol gel pellet of porous structure, after suction filtration, the product is put in vacuum desiccator and dried 24h.

Embodiment 3

[0046] Drug loading by dipping and volatilization method

[0047] The biodegradable spherical porous starch foam is prepared and passed through an 80-mesh sieve. About 400 mg of the model drug (lovastatin) was accurately weighed and dissolved in 20 ml of chloroform to obtain a chloroform solution of the drug. Weigh 0.06, 0.18, 0.3g of biodegradable spherical porous starch foam respectively, add 3ml of drug chloroform solution respectively, so that the ratio of drug: carrier is 1:1, 1:3, 1:5 respectively, stir and mix, equilibrate for 12h, reduce Volatilize the organic solvent under pressure and dry in vacuum to obtain the drug-loaded biodegradable spherical porous starch foam drug delivery system.

[0048] Carry out in vitro dissolution test according to the second method of appendix two of version 2000: pH7.0 buffer salt 900ml is dissolution medium, temperature 37.5 ± 0.5 ℃, stirring paddle rotating speed is 50rpm, measure absorbance value at wavelength 238nm place, calculat...

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Abstract

The invention relates to a process for preparing biodegradable spherical porous starch foam and a biodegradable spherical porous starch foam administration system for an insoluble medicament. The process adopts an emulsifying-freeze thawing combined solvent displacement method, and comprises the following steps of: performing high-speed stirring or homogenizing treatment (emulsion homogenizing machine) on starch-melted aqueous solution with certain concentration serving as a water phase, methylbenzene / chloroform mixed solution (or other emulsion oil phase) serving as an oil phase and Span80 (or other W / O emulsifying agent) serving as an emulsifying agent to form uniform W / O emulsion, standing the emulsion for certain time at the temperature of 20 DEG C below zero, demixing the emulsion by gelling, dehydrating the layers in turn by adopting balance of aqueous solution of methanol with different concentrations, separating and removing the methylbenzene / chloroform layer by adopting a separating funnel, balancing the solution by using anhydrous ethanol, filtering the solution, and drying the filtrate with vacuum to obtain the biodegradable spherical porous starch foam. The foam material suitable to be used as an insoluble medicament carrier increases the specific surface area and water solubility of the insoluble medicament, and finally improves the bioavailability of the insoluble medicament.

Description

Technical field: [0001] The invention relates to a preparation method of biodegradable global porous starch foam (biodegradable global porous starch foam, BGPSF) and a biodegradable spherical porous starch foam drug delivery system using it as a carrier of insoluble drugs, which are used to improve the water solubility of insoluble drugs. properties, thereby improving its bioavailability, and solving the problems of poor water solubility and low oral bioavailability of insoluble drugs, which belong to the field of pharmacy. Background technique [0002] Oral administration of drugs is currently the preferred route of administration for most drugs due to its strong compliance, economical safety. However, about 40% or more of the new active substances are difficult to dissolve in the gastrointestinal tract due to poor water solubility, and there are problems in oral gastrointestinal absorption. Therefore, in order to maximize the efficacy of insoluble drugs, how to use new te...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08J9/28C08J3/00C08J3/075C08L3/02C08L3/12A61K47/36
Inventor 王思玲姜同英吴超
Owner SHENYANG PHARMA UNIVERSITY
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