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Paclitaxel nanocrystals for injection and preparation method thereof

A nanocrystal and paclitaxel technology, applied in the field of medicine, can solve the problems of inability to improve solubility and bioavailability, difficult to obtain nanocrystal suspension, difficult to reconstitute particle size, etc., and to reduce adverse drug reactions and achieve good application prospects. , good stability

Active Publication Date: 2018-06-05
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, due to the easy precipitation of paclitaxel nanocrystals in the nanocrystal mixture, agglomeration will occur, making it difficult to redissolve or increase the particle size, so the purpose of improving solubility and bioavailability cannot be achieved.
Therefore, it is still difficult to obtain a stable nanocrystal suspension

Method used

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  • Paclitaxel nanocrystals for injection and preparation method thereof
  • Paclitaxel nanocrystals for injection and preparation method thereof
  • Paclitaxel nanocrystals for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Preparation of paclitaxel nanocrystal suspension (1)

[0058] Prescription composition:

[0059]

[0060] Preparation:

[0061] According to the above ratio, at room temperature, the two stabilizers, poloxamer and docusate sodium, were dissolved in 10 ml of water, and the resulting aqueous mixture was stirred and mixed at a high speed at 1200 rpm as the water phase. An appropriate amount of paclitaxel was dissolved in ethanol as the organic phase, with a concentration of 50 mg / ml. Then, under the condition of high-speed stirring at 1200 rpm, 1 ml of the organic phase was added to the above-mentioned aqueous phase, and then the high-speed stirring was continued at 1200 rpm for 20 min, and most of the ethanol was removed. Then the paclitaxel nanocrystal suspension obtained was sonicated at 100 W for 20 min to fully stabilize it. The particle size of paclitaxel nano crystal suspension can reach 200.9nm.

Embodiment 2

[0062] Example 2: Preparation of paclitaxel nanocrystal suspension (2)

[0063] Prescription composition:

[0064]

[0065] Preparation:

[0066] According to the above ratio, at room temperature, the two stabilizers, poloxamer and docusate sodium, were dissolved in 10 ml of water, and the resulting aqueous mixture was stirred and mixed at a high speed at 1000 rpm as the water phase. An appropriate amount of paclitaxel was dissolved in ethanol as the organic phase, with a concentration of 100 mg / ml. Then, under the condition of high-speed stirring at 1000 rpm, 0.5 ml of organic phase was added to the above-mentioned aqueous phase, and then the high-speed stirring was continued at 1000 rpm for 30 min, and most of the ethanol was removed. Then the paclitaxel nanocrystal suspension obtained was sonicated at 100 W for 30 min to fully stabilize it. The particle size of paclitaxel nano crystal suspension can reach 217.5nm.

Embodiment 3

[0067] Example 3: Preparation of paclitaxel nanocrystal suspension (3)

[0068] Prescription composition:

[0069]

[0070] Preparation:

[0071] According to the above proportions, at room temperature, two stabilizers, hypromellose and sodium lauryl sulfate, were dissolved in 10 ml of water, and the resulting aqueous mixture was stirred and mixed at a high speed at 800 rpm as the water phase. An appropriate amount of paclitaxel was dissolved in ethanol as the organic phase, with a concentration of 100 mg / ml. Then, under the condition of high-speed stirring at 800 rpm, 1 ml of organic phase was added to the above-mentioned aqueous phase, and then the high-speed stirring was continued at 800 rpm for 60 min, and most of the ethanol was removed. Then the paclitaxel nanocrystal suspension obtained was sonicated at 120 W for 10 min to fully stabilize it. The particle size of paclitaxel nano crystal suspension can reach 264.5nm.

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Abstract

The invention belongs to the technical field of medicines, relates to a paclitaxel medicinal composition and a preparation method thereof, and in particular relates to an injection paclitaxel nanocrystal preparation and a preparation method thereof as well as application of the preparation for preparing anti-tumor medicines. The paclitaxel nanocrystal belongs to a nano preparation, is small in grain diameter and good in stability, and cannot be easily separated, so that the dissolubility of paclitaxel is remarkably improved, and in-vivo studies prove that the paclitaxel nanocrystal has certain targeting performance, and can be used in anti-tumor treatment.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a paclitaxel pharmaceutical composition and a preparation method thereof. Specifically, the present invention relates to a paclitaxel nanocrystal preparation for injection, a preparation method thereof, and an application of the preparation in preparing antitumor drugs. Background technique [0002] Paclitaxel (PTX) is a complex secondary metabolite extracted from the bark of Taxus brevifolia, with a chemical name of 5β, 20-epoxy-1, 2α, 4 , 7β, 10β, 13α-hexahydroxytaxane-11-en-9-one-4,10-diacetate-2-benzoate-13[(2'R,3'S)-N-benzene formyl-3-phenylisoserine]. [0003] Paclitaxel is a specific stabilizer of microtubules, which can promote the assembly of microtubules and maintain the stability of microtubules. After the cells are exposed to paclitaxel, a large number of microtubules will accumulate in the cells. The accumulation of these microtubules interferes with various functi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/337A61K9/10A61K9/19A61P35/00
Inventor 郑爱萍张慧杨茜高静李迎孙建绪魏丽莎张晓燕
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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