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Paclitaxel alhumin submicron for injection and preparation method thereof

A technology of paclitaxel and albumin, which is applied in the directions of pharmaceutical formulations, non-active ingredients of polymer compounds, powder delivery, etc., can solve the problems of organic solvent residue, complicated preparation process, high preparation cost, etc., and achieve reduction of preparation cost, simple preparation process, The effect of convenient clinical use

Active Publication Date: 2012-12-05
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Therefore, the technical problem to be solved in the present invention is to use highly toxic organic solvents in the preparation process of the existing paclitaxel albumin nanoparticles for injection, resulting in residues of highly toxic organic solvents, and the preparation process is relatively complicated, and the preparation cost However, it provides a paclitaxel albumin subparticle for injection and a preparation method thereof, the paclitaxel albumin subparticle does not use highly toxic organic solvents, the preparation method is relatively simple, and the preparation cost is relatively low

Method used

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  • Paclitaxel alhumin submicron for injection and preparation method thereof
  • Paclitaxel alhumin submicron for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0039] Weigh 50 mg of paclitaxel, dissolve in 16 ml of tert-butanol as the organic phase; weigh 400 mg of human serum albumin, 200 mg of mannitol, and 200 mg of glycine, dissolve in 24 ml of water for injection as the water phase. The organic phase and the aqueous phase were mixed evenly under the condition of stirring (500 rpm), dissolved and clarified, filtered and sterilized through a 0.22 μm microporous membrane, and distributed into clean vials. The vial is frozen at a temperature of -30°C to -50°C, lyophilized in a freeze dryer to remove tert-butanol and moisture, filled with nitrogen, stoppered, and capped to obtain the product.

Embodiment 2

[0041]Weigh 20 mg of paclitaxel, dissolve in 20 ml of tert-butanol as the organic phase; weigh 400 mg of human serum albumin, 100 mg of glucose, dissolve in 80 ml of water for injection as the water phase. The organic phase and the aqueous phase were mixed evenly under stirring (manual stirring), dissolved and clarified, filtered and sterilized through a 0.22 μm microporous membrane, and then packed into clean vials. The vial is frozen at a temperature of -30°C to -50°C, lyophilized in a freeze dryer to remove tert-butanol and moisture, filled with nitrogen, stoppered, and capped to obtain the product.

Embodiment 3

[0043] Weigh 20 mg of paclitaxel, dissolve in 20 ml of tert-butanol as the organic phase; weigh 600 mg of human serum albumin, 500 mg of glycine, dissolve in 60 ml of water for injection as the water phase. The organic phase and the aqueous phase were mixed evenly under the condition of stirring (1500 rpm), dissolved and clarified, filtered and sterilized through a 0.22 μm microporous membrane, and distributed into clean vials. The vial is frozen at a temperature of -30°C to -50°C, lyophilized in a freeze dryer to remove tert-butanol and moisture, filled with nitrogen, stoppered, and capped to obtain the product.

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Abstract

The invention discloses a paclitaxel alhumin submicron for injection. The paclitaxel alhumin submicron comprises 1-10% (W / W) of paclitaxel, 10-80%(W / W) of alhumin and 10-85% (W / W) of freeze-drying protective agent. The invention also discloses a preparation method of the paclitaxel alhumin submicron. The method comprises the following steps of 1) adding paclitaxel into tert-butyl alcohol, stirring and dissolving to be used as an organic phase; 2) adding the alhumin and the freeze-drying protective agent to water or a buffer with a pH within 6.0-8.5, stirring and dissolving to be used as a water phase; 3) adding the organic phase into water with stirring, stirring and dissolving, filtering and degerming through a millipore filtration method, and placing in a clean container; 4) freezing at-30- -50 DEG C, removing tert-butyl alcohol and water through freeze-drying by a lyophilizer to obtain freeze-drying powder with good profile and loosening quality. During usage, the freeze-drying powder is added to a solvent for injection and redissolved, so that paclitaxel alhumin submicrons with an average particle size of 100-600nm are formed. The paclitaxel alhumin submicron for injection ofthe invention has advantages of a simple preparation technology, no high toxic organic solvent and long-term storage, etc.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a paclitaxel albumin subparticle for injection and a preparation method thereof. Background technique [0002] Paclitaxel (Taxol) is a natural active ingredient extracted and developed from the trunk and bark of Taxus yew. Treatment of breast cancer, ovarian cancer, non-small cell lung cancer and prostate cancer, etc. Although the antitumor effect of paclitaxel was recognized by people in the 1960s, it was not until 1992 that Bristol-Myers Squibb successfully developed paclitaxel injection (Taxol) and applied it clinically. One of the reasons is that its Water solubility is very low. The solvent system used in commercially available paclitaxel injections is polyoxyethylene castor oil (Cremophor EL, CrEL): ethanol (≈1:1, V / V). In the case of clinically given therapeutic doses, CrEL can cause severe respiratory symptoms. Distress, hypotension, angioedema and generalize...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/19A61K31/337A61K47/42A61K47/26A61K47/16A61K9/08A61P35/00
Inventor 何军陈辰陆伟根
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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