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Improved paclitaxel-based antitumor formulation

A paclitaxel and anti-tumor technology, which is applied in the directions of anti-tumor drugs, medical preparations containing active ingredients, and pill delivery, etc., can solve problems such as filter blockage and low yield of paclitaxel.

Inactive Publication Date: 2007-03-28
ABRAXIS BIOSCI LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The Applicant has made the most patient efforts to filter with the membrane described in US 5916596, but these results always fail, causing the filter to clog and the paclitaxel yield is always less than 30%, as opposed to the claimed 70-100%

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Prepare formulations with HCl and paclitaxel dissolved in chloroform

[0027] Dilute the injectable 25% (w / v) HSA aqueous solution (pH = 6.9 ± 0.5) in accordance with FDA regulations to 3% (w / v) with sterile demineralized water, adjust its pH to 5.6 with 1M HCl, HCl Salt formation with certain basic groups in albumin. 40 ml of the previously sterilized solution was mixed with 1.2 ml of a sterile solution of paclitaxel in chloroform (59.0 mg / ml), and the mixture was treated under high pressure (9000-40000 psi) in a homogenizer (suitably sterilized) until A nanoemulsion (MPS < 0.2 micron) was obtained which was frozen to -25°C under aseptic conditions and lyophilized for 60 hours while warming to +20°C.

[0028] The obtained powder containing 4.25% (w / w) paclitaxel and 3.6% (w / w) water was reconstituted with 0.9% NaCl aqueous solution to form a paclitaxel solution with a concentration of 2 mg / ml. The resulting formulation had an MPS of 0.16 microns, pH = 5.6, and a stab...

Embodiment 2

[0031] Preparation of formulations with citric acid and paclitaxel dissolved in chloroform

[0032] Dilute an injectable 25% (w / v) HSA aqueous solution (pH = 6.9 ± 0.5) that meets FDA specifications to 2.5% (w / v) with sterile demineralized water, and adjust its pH to 5.5 with sterile citric acid , citric acid forms a salt with certain basic groups in albumin. 60 ml of said solution was mixed with 1.7 ml of a sterile solution of Paclitaxel at a concentration of 60.0 mg / ml in chloroform, and the mixture was treated under high pressure (9000-40000 psi) in a homogenizer (suitably sterilized) until a nanoemulsion was obtained (MPS<0.2 microns), which were rapidly frozen to -40°C under aseptic conditions and lyophilized for 55 hours while warming to +35°C.

[0033] The obtained powder containing 5.2% (w / w) paclitaxel and 4.9% (w / w) water was reconstituted with 0.9% NaCl aqueous solution to form a solution with a paclitaxel concentration of 2 mg / ml. The resulting formulation had an...

Embodiment 3

[0035] Formulation prepared with hydrochloric acid and paclitaxel dissolved in chloroform

[0036] Dilute the FDA-compliant injectable 25% (w / v) HSA aqueous solution to 3% (w / v) with sterile demineralized water, adjust its pH to 5.6 with 1M HCl, hydrochloric acid and some albumin Basic groups form salts. 60 ml of said solution was mixed with 1.5 ml of a sterile solution of paclitaxel in chloroform at a concentration of 75 mg / ml, and the mixture was treated under high pressure (9000-40000 psi) in a homogenizer (suitably sterilized) until a nanoemulsion ( MPS<0.2 microns), which were rapidly frozen to -50°C under aseptic conditions and lyophilized for 50 hours while warming to +30°C.

[0037] The obtained powder containing 4.41% (w / w) paclitaxel and 3.8% water was reconstituted with 0.9% NaCl aqueous solution to form a paclitaxel solution with a concentration of 2.5 mg / ml. The resulting formulation had an MPS of 0.175 microns, pH = 5.6, and a stability of >24 hours.

[0038] ...

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Abstract

Antitumor formulation based on nanoparticles of paclitaxel and human serum albumin as obtained by the addition of a biocompatible acid to an aqueous albumin solution before this is mixed with paclitaxel during the nanoparticle production process, the injectable solutions of this formulation having a pH between 5.4 and 5.8 and having stability and inalterability with time.

Description

[0001] The present invention is a divisional application of the Chinese patent application submitted on March 28, 2003 with the application number 03108362.5 and the title of the invention entitled "Improved Paclitaxel-Based Antitumor Preparation". technical field [0002] The present invention relates to an antineoplastic formulation based on paclitaxel and albumin nanoparticles, which yields an injectable reconstituted aqueous mixture that is highly time-stable. Background technique [0003] Paclitaxel is a natural substance known in the literature that has important antitumor activity. Its poor water solubility makes it difficult to administer to humans, and for this reason various systems have been developed which allow it to be injected. [0004] Bristol Myers Squibb (BMS) has designed and patented a composition called TAXOL(R), in which paclitaxel is emulsified with cremophor, which produces multiple Side effects (Lorenz et al., Agents Action 7, 63-67 (1987); Weiss et...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/42A61P35/00A61K9/08A61K9/16A61K9/20A61K9/50A61K9/51A61K31/335
CPCA61K9/0019A61K47/42A61K9/1658A61K9/5169A61K9/5052A61K31/335A61P35/00A61K9/10B82Y5/00A61K9/51A61K31/337
Inventor M·泽诺尼S·玛施奥
Owner ABRAXIS BIOSCI LLC
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