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Preparation and application of insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle

An amphiphilic polysaccharide and insoluble drug technology, which is applied in the directions of drug delivery, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the poloxamer micelle encapsulation efficiency and drug loading The problems of low amount, low micellar stability, and high critical micellar concentration can achieve good solubilization, improve stability, and improve oral bioavailability.

Inactive Publication Date: 2012-08-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the encapsulation efficiency and drug loading of poloxamer micelles are low, and the critical micelle concentration (CMC) is high, which reduces the stability of the micelles, thus limiting its application.

Method used

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  • Preparation and application of insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle
  • Preparation and application of insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle
  • Preparation and application of insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Determination of CMC value of poloxamer / amphipathic polysaccharide conjugate

[0025] 1. Critical micelle concentration (CMC): CMC was determined by fluorescent probe method. Using pyrene as a fluorescent probe, pyrene is a hydrophobic aromatic compound that is extremely sensitive to changes in the polarity of the environment. When the concentration of the poloxamer / amphiphilic polysaccharide conjugate is lower than the CMC, micelles will not form in the solution, and pyrene dissolves in polar water; when the concentration is higher than the CMC, micelles form, and pyrene The hydrophobic part of the micelle core is assigned to enter the non-polar environment, and then a series of changes can be observed in its fluorescence spectrum, such as the enhancement of the fluorescence intensity, the change of the vibration fine structure in the emission spectrum, and the (0,0 ) band redshift. Therefore, by taking the I in the emission spectrum of pyrene 1 / I 3 Rat...

Embodiment 2

[0032] Example 2: Preparation and characterization of poloxamer / low molecular weight heparin-all-trans retinoic acid mixed micelles loaded with paclitaxel

[0033] 1. Preparation process:

[0034] (1) Dialysis

[0035] 18mg of low molecular weight heparin-all-trans retinoic acid was dissolved in 3ml of distilled water, 20mg of poloxamer was dissolved in 1ml of distilled water, and stirred for 30min respectively. The low molecular weight heparin-all-trans retinoic acid solution was mixed with poloxamer P188 in different weight ratios. Paclitaxel 10mg was dissolved in ethanol. Add paclitaxel / ethanol solution to the mixed solution, stir at room temperature for 15 minutes, sonicate with an ice bath probe for 30 minutes, dialyze in distilled water for 1 day (MWCO=3500), centrifuge the product after dialysis at 3000 rpm for 10 minutes, filter the supernatant with a 0.8 μm filter membrane, and freeze The paclitaxel-loaded poloxamer / low molecular weight heparin-all-trans retinoic aci...

Embodiment 3

[0045] Example 3: Preparation of poloxamer / chondroitin sulfate-glycyrrhetinic acid mixed micelles loaded with itraconazole

[0046] 20mg of chondroitin sulfate-glycyrrhetinic acid was dissolved in 4ml of distilled water, 20mg of poloxamer was dissolved in 1ml of distilled water, and stirred for 30min respectively. Chondroitin sulfate-glycyrrhetinic acid solution was mixed with 250 μL of poloxamer. Itraconazole 10mg was dissolved in ethanol. Add itraconazole / ethanol solution to the mixed solution, stir at room temperature for 15 minutes, sonicate with an ice bath probe for 30 minutes, dialyze with distilled water for 1 day (MWCO=3500), centrifuge the product after dialysis at 3000 rpm for 10 minutes, and filter the supernatant with a 0.8 μm membrane Filter and freeze-dry to obtain the poloxamer / chondroitin sulfate-glycyrrhetinic acid mixed micelles loaded with itraconazole, measure the content of itraconazole in the mixed micelles by HPLC, and calculate according to formula (1...

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Abstract

The invention discloses preparation and application of an insoluble drug-entrapped poloxamer / amphiphilic polysaccharide mixed micelle. The insoluble drug-entrapped poloxamer / amphiphilic polysaccharide mixed micelle is prepared through a dialysis method or a solvent evaporation method. The mixed micelle is low in critical micelle concentration, is high in drug-loading rate, is capable of obviously prolonging the stabilization time and has the long-circulation function of a nanomicelle and has dual functions of restraining the metabolism of P-glycoprotein and cytochrome P450 enzyme and is capable of increasing the bioavailability of oral administration. The mixed micelle is simple in preparation method, is mature in process and is high in yield and can be prepared into preparations for the oral administration, such as tablets, capsules, pills and syrups.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a preparation method of poloxamer / amphiphilic polysaccharide mixed micelles for insoluble drugs and its application in oral administration. Background technique [0002] Oral administration is the most common way of administration among many routes of administration, because it is easy to take and carry, and is easily accepted by general patients, especially for those patients who need long-term or daily medication, the compliance of oral administration of drugs Sex is much better than other routes of administration. In addition, in order to reduce toxic and side effects, oral administration of cytotoxic agents is more suitable for long-term administration than injection administration, and can achieve better disease treatment effects. [0003] For drugs that can be administered orally, their active ingredients should first be dissolved in the fluid of the human gastroin...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K47/48A61K47/34A61K45/00A61K9/00
Inventor 周建平姚静法蒂玛杨晖刘宏盼
Owner CHINA PHARM UNIV
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