Taxol medicinal compositions and preparation method thereof

A paclitaxel and composition technology, applied in the field of paclitaxel pharmaceutical compositions and preparation thereof, can solve the problems of low drug yield, high drug yield, easy blockage of filters, etc., and achieves improved curative effect, good chemical stability, The effect of reducing the incidence of adverse reactions

Active Publication Date: 2010-03-03
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0020] In addition, the inventor filters with the filter membrane described in the patent CN1515246A, but as a result, the filter is prone to clogging, and the yield of the medicine is very low, always lower than 30%, which is different from the 70% stated in the patent. - 100% yield results are different and such high drug yields as stated in the patent have never been achieved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] This example demonstrates the stability of a pharmaceutical composition of docetaxel containing sodium chloride (4.0%) and the lyoprotectant aspartic acid.

[0057] Organic phase preparation: docetaxel (10%) was dissolved in a mixed solvent (3%, v / v) containing chloroform and ethanol;

[0058] Aqueous phase preparation: add human serum albumin (5%, m / v), stabilizer sodium chloride (4.0%) into water for injection and stir until dissolved; batch size is 30ml.

[0059] The water phase is added into the microfluidizer, the organic phase is slowly added into the water phase, and the nanoemulsion is prepared by homogenizing under the condition of 5000Psi. The liquid suspension can be sterilized and filtered directly through a 0.22 μm filter membrane, and preparations with 0.5% aspartic acid and no aspartic acid are prepared respectively. The pH values ​​of the above preparations are 3.7 and 6.7 respectively, frozen The organic solvent in the nanoemulsion is dried and removed...

Embodiment 2

[0062] This example demonstrates the stability of a pharmaceutical composition of docetaxel containing sodium chloride (7.7%).

[0063] Organic phase preparation: docetaxel (8%) was dissolved in a mixed solvent (3%, v / v) containing dichloromethane and ethyl acetate;

[0064] Aqueous phase preparation: add human serum albumin (5%, m / v), stabilizer sodium chloride (7.7%) into water for injection and stir until dissolved; batch size is 30ml.

[0065] The water phase is added into the microfluidizer, the organic phase is slowly added into the water phase, and the nanoemulsion is prepared by homogenizing under the pressure condition of 5000Psi. The liquid suspension can be sterilized and filtered directly through a 0.22 μm filter membrane, and the freeze-drying protective agent 0.6% aspartic acid is added to the outside and then packaged and freeze-dried. The pH value of the preparation is 3.6, and the nanoemulsion is removed during the freeze-drying process in organic solvents. ...

Embodiment 3

[0068] This example serves to demonstrate the physical stability of the docetaxel pharmaceutical composition containing sodium citrate (4.2%) and the chemical instability of the docetaxel drug.

[0069] Organic phase preparation: docetaxel (10%) was dissolved in a mixed solvent (3%, v / v) containing chloroform and ethanol;

[0070] Water phase preparation: human serum albumin (weight to volume ratio 5%) and stabilizer sodium citrate (4.2%) were added to water for injection and stirred until dissolved; batch size was 30ml.

[0071] The water phase is added into the microfluidizer, the organic phase is slowly added into the water phase, and the nanoemulsion is prepared by homogenizing under the pressure condition of 5000Psi. The liquid suspension can be sterilized and filtered through a 0.22 μm filter membrane, and the freeze-drying protective agent 2% mannitol is added to the outside, and then the liquid suspension is packaged and freeze-dried, and the organic solvent in the nan...

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PUM

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Abstract

The invention provides medicinal compositions of taxol medicaments and pharmaceutically acceptable biological carriers and preparation method thereof. The medicinal compositions of the taxol medicaments and carrier proteins are nano mixed suspensions prepared from the carrier proteins, organic phases, stabilizers, freeze drying protective agents and the taxol medicaments. The weight volume percentconcentration of the taxol medicaments is 0.075 to 1.0. The taxol medicament nano particles prepared by using high-pressure homogenization can reduce adverse reaction aroused by the taxol medicamentsand improve the safety of the clinical administration of the taxol medicaments. The preparation process of the nano mixed suspensions is simple and feasible and is suitable for large-scale preparation and industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a paclitaxel pharmaceutical composition and a preparation method thereof. Background technique [0002] Paclitaxel drugs (such as paclitaxel, docetaxel, etc.) are one of the most effective anti-tumor drugs currently used clinically. Paclitaxel is a natural product isolated from the bark or needles of Taxus or its species discovered in the 1970s, and docetaxel is a semi-synthetic product, which was later discovered to be a type of anti-tumor drug with a special anti-tumor mechanism. agent. [0003] The anti-tumor mechanism of paclitaxel drugs is to promote the polymerization of microtubules and reduce the depolymerization speed of microtubules, so that the microtubules are in a stable non-functional state, thereby achieving the purpose of preventing tumor cell mitosis and proliferation. And preclinical studies have shown that compared with paclitaxel, docetaxel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K9/19A61K47/42A61P35/00
Inventor 吴培杨清敏姜文妍王栋海张明会王晶翼
Owner QILU PHARMA HAINAN
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