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Paclitaxel lipid nanoparticle preparation method

A lipid nanoparticle and solid lipid nanotechnology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations, can solve the problems of limited absorption, mucosal damage, and bioavailability of paclitaxel oral preparations Low concentration and other problems, to achieve the effect of increasing amphiphilicity, easy absorption, and enhanced cell uptake of penetrating peptides

Inactive Publication Date: 2016-02-10
孙仁
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AI Technical Summary

Problems solved by technology

The bioavailability of oral preparations of paclitaxel is very low, how to improve the absorption of paclitaxel in the gastrointestinal tract and improve its bioavailability is the key to the development of oral preparations of paclitaxel
Solid lipid nanoparticles can improve the oral absorption of insoluble drugs to a certain extent, but after oral administration, nanoparticles are mainly transported by M cells or pinocytosis on Peyer's junction, and the absorption is relatively limited
The continuous use of common absorption enhancers will cause direct damage to the mucosa, which limits its clinical application.

Method used

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Embodiment Construction

[0013] The preparation method of paclitaxel lipid nanoparticles comprises the following steps.

[0014] (1) Prepare paclitaxel solid lipid nanoparticles according to the film dispersion method. Precisely weigh 10mg of paclitaxel, 225mg of soybean lecithin and 225mg of glyceryl monostearate into a 500mL eggplant-shaped bottle, add 3mL of chloroform to shake and dissolve, vacuum rotary evaporation to remove the organic solvent to form a drug-containing film, and vacuum overnight to remove traces of organic solvent. Accurately weigh 100 mg of Poloxamer 188 and 100 mg of Tween 80 into 10 mL of distilled water to form an aqueous phase. The water phase was added to an eggplant-shaped bottle for hydration to form a uniform emulsion, and the probe was sonicated to obtain the crude PTX-SLN, which was centrifuged at a low speed and filtered through a 0.8 μm filter membrane for three times to granulate to obtain the final PTX-SLN dispersion.

[0015] (2) Prepare SA-R8-PTX-SLN by i...

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Abstract

The invention belongs to the technical field of medicines, particularly relates to a paclitaxel lipid nanoparticle preparation method and provides a method for preparing paclitaxel lipid nanoparticles easy for intestinal mucosae to absorb. The method includes the steps: (1) preparing paclitaxel solid lipid nanoparticle according to a film dispersion method; (2) preparing SA-R8-PTX-SLN according to an incubation method, to be more specific, precisely weighing 10mg of SA-R8, adding into 5ml of PTX-SLN dispersion liquid, magnetically stirring, staying overnight at a temperature of 4 DEG C to obtain the SA-R8-PTX-SLN; (3) precisely weighing 10mg of paclitaxel, putting into a 100ml volumetric flask, dissolving in methyl alcohol to a certain volume, and well shaking to obtain a PTX methanol stock solution with the density being 100 microgram / ml; (4) putting 1ml of SLN containing paclitaxel in a dialysis bag (14000 in molecular weight), tightening two ends of the dialysis bag, respectively adding 100ml of dissolution media, observing paclitaxel release conditions under the conditions of 37 DEG C and 100r / min, taking 1ml of dialysis media, lyophilizing, adding 0.25ml of methanol, whirling, centrifuging at a high speed, and taking supernatant for sampling by 20 microlitres.

Description

Technical field [0001] The present invention is a drug technology field, especially the preparation method of paclitaxel lipid nanoparticles. Background technique [0002] The development of enabled soluble drugs such as paclitox oral preparations is a research hotspot of pharmacy.The biological utilization of paclitaxel oral preparations is very low. How to improve the absorption of paclitaxel in the gastrointestinal tract and increase their biological utilization is the key to the development of paclitaxel oral preparations.Solid lipid nanoparticles can improve the oral absorption of enabled soluble drugs to a certain extent. However, after nanoprocinone is taken, it is mainly transferred by M cells or cells on PEYER. The absorption is relatively limited.Common absorption Promotional continuous use will cause direct damage to the mucous membrane, which limits its clinical application.Membrane peptide is a type of polypeptide with strong cell membrane penetration. It is almost n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/51A61K31/337A61K47/12A61P35/00
Inventor 孙仁
Owner 孙仁
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