Taxol nanosuspension and preparation method thereof

A technology of nano-suspension and paclitaxel, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients. The process is simple, the effect of enhancing safety and reducing energy consumption

Active Publication Date: 2010-09-29
南京百思福医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the shortcomings of the existing dosage forms of paclitaxel, such as low drug loading, strong toxic and side effects, poor stability, complicated preparation process, and high price, to achieve a technological breakthrough in this field, and to provide a drug that can increase drug content and reduce drug administration. Paclitaxel nanosuspensions that reduce toxicity, reduce production costs, and improve patient adaptability and compliance for clinical use

Method used

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  • Taxol nanosuspension and preparation method thereof
  • Taxol nanosuspension and preparation method thereof
  • Taxol nanosuspension and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Weigh 18825 mg of poloxamer and 25 mg of PEG400, add it into 50 ml of triple distilled water, stir it magnetically to dissolve it completely, weigh 50 mg of paclitaxel raw material and dissolve it in a mixed solution of 2.5 ml of ethyl acetate and 2.5 ml of ethanol, 10000 rpm high shear milk In the case of homogenization, inject the oil phase into the water phase slowly and at a constant speed to precipitate drug crystals, and rotate the initial suspension to remove the organic solvent, and homogenize under high pressure. The conditions are 6 cycles at 300 bar, 6 cycles at 500 bar, and 20 cycles at 800 bar. The milky white nanosuspension was obtained, the measured particle size was 256.1nm, and the zeta potential was -25.61mv.

Embodiment 2

[0036] Weigh 18820 mg of poloxamer and 40 mg of PEG400, add 50 ml of three-distilled water, and magnetically stir to dissolve it completely, weigh 30 mg of paclitaxel raw material and dissolve it in a mixed solution of 2 ml of ethyl acetate and 2 ml of ethanol. In some cases, the oil phase is slowly injected into the water phase at a constant speed to precipitate drug crystals, and the initial suspension is rotary evaporated to remove the organic solvent and homogenized under high pressure. 20 times, a milky white nanosuspension was obtained, the measured particle size was 186.3nm, and the zeta potential was -20.87mv.

Embodiment 3

[0038] Weigh 18820mg of poloxamer, PEG40060mg, add 50ml of three-distilled water, magnetically stir to make it completely dissolved, weigh 40mg of paclitaxel raw material drug and dissolve in 2ml of ethyl acetate and 2ml of ethanol mixed solution, 10000rpm high shear emulsion In some cases, the oil phase is slowly injected into the water phase at a constant speed to precipitate drug crystals, and the initial suspension is rotary evaporated to remove the organic solvent and homogenized under high pressure. 20 times, the milky white nanosuspension was obtained, the measured particle size was 234.1nm, and the zeta potential was -25.21mv.

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Abstract

The invention relates to the field of medicinal preparations, in particular to a taxol nanosuspension and a preparation method thereof. The taxol nanosuspension is characterized in that: a surfactant consists of poloxamer 188 and polyethylene glycol in a weight ratio of 1:1-1:3. According to the invention, the defects of low medicament loading rate, strong toxic or side effect, low stability, complex preparation process, high cost and the like in the conventional taxol preparation are overcome, and the technical breakthrough in the field is achieved; and the taxol nanosuspension has the advantages of increasing medicament content, reducing administration toxicity and production cost and improving the adaptability and compliance of a patient so as to realize clinical use.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a paclitaxel intravenously administered nanosuspension injection, its preparation method and application. Background technique [0002] Paclitaxel (PTX) is a diterpenoid extracted from the bark of Taxus genus Taxus. It is a new type of microtubule stabilizer with unique anti-tumor activity. It is considered by the National Cancer Institute of the United States to be the most important progress in tumor chemotherapy in the past 15 to 20 years. At present, the United States has listed the drug as a first-line drug for various tumors. [0003] Although paclitaxel has good antitumor activity, its solubility in water is very small. According to literature reports, paclitaxel is soluble in organic solvents such as methanol, ethanol, and dimethyl sulfoxide, while its solubility in water is less than 30 μg / mL. The extremely low water solubility of paclitaxel brings great dif...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/337A61K47/34A61K47/36A61P35/00A61K47/10
Inventor 李学明程晓丹王永禄
Owner 南京百思福医药科技有限公司
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