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Docetaxel solid lipid nanoparticle lyophilized preparation and preparation method

A technology of solid lipid nano and docetaxel, which is applied in the direction of microcapsules, nanocapsules, and capsule delivery, can solve the problems of unfavorable drug absorption, electrostatic repulsion, etc., reduce the first-pass effect, increase adhesion, The effect of extending the contact area

Inactive Publication Date: 2015-05-06
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the disadvantages that ordinary solid lipid nanoparticles are prone to electrostatic repulsion with cell membranes and are not conducive to drug absorption, the object of the present invention is to provide a docetaxel solid lipid nanoparticle modified with quaternized chitosan Freeze-dried preparations, on the basis of ordinary chitosan-modified solid lipid nanoparticles, improve the stability in the intestinal tract and further increase the bioavailability, while there is no quaternary ammonium salt modified chitosan at home and abroad Docetaxel solid lipid nanoparticles related research or marketed products

Method used

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  • Docetaxel solid lipid nanoparticle lyophilized preparation and preparation method
  • Docetaxel solid lipid nanoparticle lyophilized preparation and preparation method
  • Docetaxel solid lipid nanoparticle lyophilized preparation and preparation method

Examples

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Embodiment 1

[0043] Example 1: Preparation of unmodified docetaxel solid lipid nanoparticles.

[0044] First, weigh 3 mg of docetaxel and 20 mg of lecithin and place them in a vial, add 2 ml of dichloromethane to dissolve to obtain a drug solution; secondly, weigh 60 mg of glyceryl monostearate, melt it in a water bath at 70°C, and mix with The above drug solution was mixed to obtain a uniform oil phase; then, the above oil phase was added to 4ml Tween 80 aqueous solution (the mass concentration of Tween 80 was 1.0g / 100ml), and 200w ultrasonic dispersion was performed for 60s to obtain a dispersion liquid. The above dispersion was stirred at room temperature for 3 hours, and the organic solvent was evaporated to obtain 4ml of docetaxel solid lipid nanoparticle suspension, which contained 0.123g of docetaxel solid lipid nanoparticles, and the particle diameter was 160.5nm. The potential is -20.2mv. According to the weight-to-volume ratio of lyoprotectant:suspension=2.5g:100ml, add 0.1g suc...

Embodiment 2

[0045] Example 2: Preparation of chitosan-modified docetaxel solid lipid nanoparticles.

[0046] First, weigh 3 mg of docetaxel and 20 mg of lecithin and place them in a vial, add 2 ml of dichloromethane to dissolve to obtain a drug solution; secondly, weigh 60 mg of glyceryl monostearate, melt it in a water bath at 70°C, and mix with The above drug solution was mixed to obtain a uniform oil phase; then, the above oil phase was added to 4ml Tween 80 aqueous solution (the mass concentration of Tween 80 was 1.0g / 100ml), and 200w ultrasonic dispersion was performed for 60s to obtain a dispersion liquid. The above-mentioned dispersion liquid was stirred at room temperature for 3h, and the organic solvent was evaporated to obtain 4ml docetaxel solid lipid nanoparticle suspension; then, according to the docetaxel solid lipid nanoparticle suspension: chitosan aqueous solution =1:2 volume ratio, slowly drop 8ml chitosan aqueous solution (the mass concentration of chitosan is 0.1g / 100m...

Embodiment 3

[0047] Example 3: Preparation of chitosan-modified docetaxel solid lipid nanoparticles.

[0048] First, weigh 3 mg of docetaxel and 20 mg of lecithin and place them in a vial, add 2 ml of dichloromethane to dissolve to obtain a drug solution; secondly, weigh 60 mg of glyceryl monostearate, melt it in a water bath at 70°C, and mix with The above drug solution was mixed to obtain a uniform oil phase; then, the above oil phase was added to 4ml Tween 80 aqueous solution (the mass concentration of Tween 80 was 1.0g / 100ml), and 200w ultrasonic dispersion was performed for 60s to obtain a dispersion liquid. The above-mentioned dispersion liquid was stirred at room temperature for 3h, and the organic solvent was evaporated to obtain 4ml docetaxel solid lipid nanoparticle suspension; then, according to the docetaxel solid lipid nanoparticle suspension: chitosan aqueous solution =1:4 volume ratio, slowly drop 16ml chitosan aqueous solution (the mass concentration of chitosan is 0.1g / 100...

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Abstract

The invention discloses a docetaxel solid lipid nanoparticle lyophilized preparation and a preparation method. The quaternary ammonium salt chitosan-modified docetaxel solid lipid nanoparticle lyophilized preparation comprises the following components in parts by weight: 1 part of docetaxel, 20-50 parts of lipid materials, 10-25 parts of emulsifier, 3-7 parts of quaternary ammonium salt chitosan and 150-200 parts of lyophilization protecting agent. The preparation method comprises the following steps: 1) preparation of an oil phase; 2) preparation of diffusion liquid; 3) preparation of nanoparticle suspension; 4) modification of nanotparticles; and 5) lyophilized drying. The quaternary ammonium salt chitosan-modified docetaxel solid lipid nanoparticle has pH universality, the dissolution speed of the medicament can be effectively increased, the problem that the traditional chitosan modified docetaxel solid lipid nanoparticles are instable in succus entericus can be improved, the oral bioavailability can be improved, and the clinical application of the docetaxel solid lipid nanoparticle lyophilized preparation becomes possible.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a freeze-dried preparation of docetaxel solid lipid nanoparticles modified by quaternized chitosan and a preparation method thereof. Background technique [0002] Docetaxel (also known as docetaxel, whose structure is shown below) is a second-generation taxane anticancer drug extracted from the needles of yew, which stops cell growth by blocking the microtubule system and disrupt cell proliferation. Docetaxel has high anti-tumor activity and has good curative effect on various tumors, but it has strong fat solubility and low solubility, so its oral bioavailability is low, tissue specificity is poor, and it has toxic and side effects on healthy tissues larger. As the only dosage form in clinical application at present, docetaxel Tween 80 injection has been widely used in the treatment of breast cancer, ovarian cancer, non-small cell lung cancer, p...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/337A61K47/36A61P35/00
Inventor 曹青日施丽丽曹悦崔京浩
Owner SUZHOU UNIV
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