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Insoluble medicine gel composition and preparation method for same

A technology for insoluble drugs and gel compositions, which is applied in the field of insoluble drug gel compositions and their preparation, temperature-sensitive gel compositions containing insoluble drug nanocrystals and their preparations, and can solve the problems of poor physical stability and temperature-sensitive gel loading. Low drug dosage, short drug release time, etc., to achieve the effect of improving stability, increasing drug loading, and avoiding deposition problems

Inactive Publication Date: 2013-04-24
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Based on the above background technology, aiming at the deficiencies in the prior art, the object of the present invention is to provide a stable composition of insoluble drug nanocrystals and temperature-sensitive gels and a preparation method thereof to overcome the poor physical stability of drug nanocrystals, General temperature-sensitive gels have technical problems such as low drug loading and short drug release time, to achieve the purpose of long-acting treatment after local administration

Method used

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  • Insoluble medicine gel composition and preparation method for same
  • Insoluble medicine gel composition and preparation method for same
  • Insoluble medicine gel composition and preparation method for same

Examples

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Effect test

Embodiment 1

[0045] Embodiment 1, the preparation of paclitaxel nanocrystalline gel composition

[0046] 1. Preparation of drug nanocrystals: Weigh 32 mg of paclitaxel and 160 mg of pluronic F127 respectively, add the drug and surface stabilizer to 4 ml of chloroform, dissolve them completely by ultrasonication, and evaporate the organic matter by nitrogen blowing at a constant flow rate. solvent, and placed in a vacuum oven at 25°C for 12h to remove residual organic solvent. Add 8ml of purified water to the above dried paclitaxel and Pluronic F127 film, hydrate for 40 minutes, vortex for 10 minutes, and sonicate for 10-15 minutes to obtain paclitaxel nanocrystal suspension.

[0047] 2. Preparation of the drug nanocrystal gel composition: Weigh 2 g of Pluronic F127, directly add it to the suspension of paclitaxel nanocrystals, and stir magnetically in an ice bath for more than 6 hours to obtain the combination of paclitaxel drug nanocrystal gel things.

Embodiment 2

[0048] Embodiment 2, the preparation of docetaxel nanocrystalline gel composition

[0049] 1. Preparation of drug nanocrystals: Weigh 32 mg of docetaxel and 160 mg of polyethylene glycol vitamin E succinic acid (TPGS) respectively, add the drug and surface stabilizer to 3 ml of dichloromethane, and ultrasonically dissolve them completely , dried by rotary evaporation under reduced pressure to remove the organic solvent, and placed in a vacuum oven at 25° C. for 12 hours to remove the residual organic solvent. Add 7.5ml of purified water to the above dried docetaxel and TPGS film, hydrate for 40 minutes, vortex for 10 minutes, and sonicate for 10-15 minutes to obtain a suspension of docetaxel nanocrystals.

[0050] 2. Preparation of pharmaceutical nanocrystalline gel composition: Weigh 2.5 g of polycaprolactone-polyethylene glycol-polycaprolactone and directly add it to the suspension of docetaxel nanocrystals, and stir magnetically in an ice bath for 6 hours As above, the com...

Embodiment 3

[0051] Embodiment 3, preparation of docetaxel-paclitaxel nanocrystalline gel composition

[0052] 1. Preparation of docetaxel drug nanocrystals: Weigh 16 mg of docetaxel and 160 mg of Tween 80 respectively, add the drug and surface stabilizer to 5 ml of absolute ethanol, and ultrasonically dissolve it completely. The organic solvent was evaporated by nitrogen blowing at a flow rate, and placed in vacuum drying at 25° C. for 12 h to remove residual organic solvent. Add 5ml of purified water to the above dried docetaxel and Tween 80 film, hydrate for 40 minutes, vortex for 10 minutes, and sonicate for 10-15 minutes to obtain a suspension of docetaxel nanocrystals.

[0053] 2. Preparation of paclitaxel drug nanocrystals: Weigh 16 mg of paclitaxel and 160 mg of surface stabilizer Pluronic F127, respectively, add the drug and surface stabilizer to 4 ml of absolute ethanol, dissolve them completely by ultrasonication, and pass through at a constant flow rate Nitrogen was blown to d...

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Abstract

The invention discloses an insoluble medicine gel composition and a preparation method for the same, and particularly relates to a temperature-sensitive gel composition containing insoluble medicine nanocrystallines and a preparation method for the same. The medicine nanocrystallines are uniformly dispersed in a temperature-sensitive gel, and belongs to the field of medicinal preparation. The preparation process comprises the following steps of: preparing a medicine nanocrystalline suspension at first, and then directly adding a temperature-sensitive material into the medicine nanocrystalline suspension and preparing the medicine nanocrystalline gel composition; or preparing medicine nanocrystallines and a blank temperature-sensitive gel respectively, and then uniformly dispersing the medicine nanocrystallines in the prepared temperature-sensitive gel. The insoluble medicine gel composition disclosed by the invention is simple in preparation method, and capable of improving the stability of common medicine nanocrystallines, increasing the medicine-loading capacity of the insoluble medicine gel, and obviously prolonging the release time of the medicine.

Description

technical field [0001] The invention relates to an insoluble drug gel composition and a preparation method thereof, in particular to a temperature-sensitive gel composition containing insoluble drug nanocrystals and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique: [0002] In the field of pharmacy, nanocrystals refer to solid particles of drugs with nanoscale. If dispersed in a suitable liquid medium, nanosuspensions can be formed. Generally, nanoscale drug particles can be dispersed in water to form a relatively stable colloidal dispersion system through the stabilization of surfactants. In recent years, a series of oral nano-drugs have been developed mainly for the problem of low oral bioavailability of insoluble drugs. These insoluble drugs are prepared into nanoparticles through special technology. Studies have proved that the oral absorption of insoluble drugs can be significantly improved. At the same time, th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K45/00A61K47/38A61K47/36A61K47/34
CPCA61K9/06A61K9/0019A61K47/10A61K47/34
Inventor 张强代文兵林志强王学清
Owner PEKING UNIV
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