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Triple combination of Planick-cholate phosphate in use for carrier of hard-soluble medication

A technology of ternary composition and insoluble drugs, which is applied in the direction of pharmaceutical formulations and medical preparations of non-active ingredients, etc., can solve the problems of insufficient absorption and utilization, good biocompatibility and safety, etc., and achieve large drug loading capacity , The effect of treatment, the effect of increasing the area

Inactive Publication Date: 2006-08-30
句容市策宇生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the carrier materials used for PM reported so far, the most common is the ethylene oxide polymer material Pluronic (see: 1. Kabanov AV, Batrakova EV, Alakhov VY. Pluronic block copolymers as novel polymertherapeutics for drug and gene delivery. J Controlled Release, 2002, 82: 189; 2. CroySR, Kwon GS. The effects of Pluronic block copolymers on the aggregation state of nystatin. J Controlled Release, 2004, 95(2): 161; 3. Oh KT , Bronich TK, Kabanov AV.Micellarformulations for drug delivery based on mixtures of hydrophobic and hydrophilic Pluronic blockcopolymers.J Controlled Release, 2004,94(2-3):411], which is characterized by good biocompatibility and safety; although In this way, PM is still insufficient in promoting the absorption and utilization of drugs by the body

Method used

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  • Triple combination of Planick-cholate phosphate in use for carrier of hard-soluble medication
  • Triple combination of Planick-cholate phosphate in use for carrier of hard-soluble medication

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1. The pluronic polymer sample was F68, and the insoluble drug was erythromycin. Weigh 0.350g of erythromycin, 0.325g of sodium cholate, 0.515g of phosphoester, and 0.400g of F68, put them in the same round-bottom flask, add 75ml of absolute ethanol, sonicate until the solution is clear, and remove the absolute ethanol by rotary evaporation. Add 10 ml of pH 7.4 buffer, shake and clarify to obtain a liquid preparation.

Embodiment 2

[0023] Example 2. The pluronic polymer sample was F68, and the poorly soluble drug was roxithromycin. Weigh 0.151g of roxithromycin, 0.325g of sodium cholate, 0.622g of phosphoester, and 0.401g of F68, put them in the same round-bottom flask, add 75ml of absolute ethanol, sonicate until the solution is clear, and remove the absolute ethanol by rotary evaporation. 20ml of pH7.4 buffer solution was added, and the solution was clarified after shaking to obtain a liquid preparation.

Embodiment 3

[0024] Example 3. The pluronic polymer sample was F68, and the poorly soluble drug was rifaximin. Weigh 0.050g of rifaximin, 0.320g of sodium cholate, 0.508g of phosphoester, and 0.399g of F68, put them in the same round-bottom flask, add 75ml of absolute ethanol, sonicate until the solution is clear, and remove the absolute ethanol by rotary evaporation. 20ml of pH7.4 buffer solution was added, and the solution was clarified after shaking to obtain a liquid preparation.

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Abstract

A pulangnike-phosphatide-cholate composition used as the carrier of the medicines difficult to dissolve is proportionally prepared from Pulangnike, phosphatide and cholate. Its advantage is high effect to increase the solubility of said medicines.

Description

1. Technical field: [0001] The present invention relates to a nanoscale drug carrier, in particular, a ternary composition used as a poorly soluble drug. 2. Background technology: [0002] Using micelles as carriers, the bioavailability of poorly soluble drugs can be improved by the solubilization effect of micelles. According to the different molecular weight of the carrier material, micelles can be divided into low molecular weight micelles and polymer micelles. Low-molecular-weight micelles use small-molecule surface-active groups as carrier materials, and their solubilization capacity, drug-loading capacity, and promotion of drug utilization by the body are limited; in the 1970s, researchers learned from "lipids in food" After the ingredients are emulsified into micelles by bile, they can promote the absorption of intestinal cells." Mixed micelles, LBMM), using LBMM as a poorly soluble drug carrier, not only solves the problem of solubilization, but also achieves the p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/10A61K47/24A61K47/28
Inventor 徐希明余江南朱源
Owner 句容市策宇生物科技有限公司
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