PHARMACEUTICAL COMPOSITION CONTAINING DOCETAXEL

• US 20170157050A1
• Filed: 07/14/2015
• Published: 06/08/2017
• Est. Priority Date: 07/15/2014
• Status: Active Grant

• Current Assignee: Gainia (Shanghai) Patent Technologies Ltd, Shanghai Simple Biotech Ltd.
• Original Assignee: Xin Teng
• Inventors: TENG, Xin
• Granted Patent: US 10,080,720 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/337 having four-membered rings, e.g. taxol
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/19 lyophilised , i.e. freeze-dried, solutions or dispersions lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention is a technical filed of pharmaceutical preparation agent, and more particular to a pharmaceutical composition containing docetaxe. The pharmaceutical composition containing docetaxe includes docetaxel and a polyethylene glycol methyl ether-polylactide block copolymer with amino acid end groups. The advantage of the present invention is subjected to a tri-block copolymer with low toxicity as the drug carrier. In addition to the pharmaceutical active ingredients and carrier, there is no other additive in pharmaceutical composition containing docetaxe. Thus, the prescription is simpler and the security is higher. In pharmaceutical component containing docetaxel, docetaxel content is more than 20%, such that the preparation process of pharmaceutical component containing docetaxel is simple, and easy for the industrial applications.

Claims

1. A pharmaceutical composition containing docetaxel, the characteristic is in that:

the pharmaceutical composition includes docetaxel and polyethylene glycol methyl ether-polylactide block copolymer with amino acid end groups, wherein the component of docetaxel is 3.21-27.75 by weight and the component of polyethylene glycol methyl ether-polylactide block copolymer with amino acid end groups is 100 by weight, and the chemical formula of polyethylene glycol methyl ether-polylactide block copolymer with amino acid end groups is

2. The pharmaceutical composition containing docetaxel according to claim 1, wherein the chemical formula of the amino acid R is

3. The pharmaceutical composition containing docetaxel according to claim 1, wherein the pharmaceutical composition is a freeze-dried powder preparation agent.

4. The pharmaceutical composition containing docetaxel according to claim 3, wherein the average particle size in a redissolved solution of the freeze-dried powder preparation agent is ranging from 18.6-29.5 nm.

5. The pharmaceutical composition containing docetaxel according to claim 3, wherein the freeze-dried powder preparation agent is preparation by a lyophilization, and the steps of lyopilization include:

Step a;

disposing a shelf is performed pre-cooling process to 0°

C. and the docetaxel micelles on the shelf to cool to below −

45°

C., so as to a solution temperature with docetaxel micelles is dropped to −

45°

C., and the solution is maintained at a temperature −

45°

C. for 2-4 hours;

Step b;

turning on a vacuum pump and vacuuming for 1-1.5 hours after the step a.

Step c;

setting a temperature of a spacer plate from −

45°

C. to −

25°

C., maintaining the temperature of the spacer plate is more than 12 hours, and setting an ultimate vacuum at 0.013 Bar.

Step d;

setting the temperature of the spacer plate from −

25°

C. to 0°

C., maintaining the temperature of the spacer plate is more than 8 hours and setting the ultimate vacuum at 0.013 Bar;

Step e;

setting a temperature of the spacer plate from 0°

C. to 5°

C., maintaining the temperature of the spacer plate more than 3 hours and setting the ultimate vacuum at 0.013 Bar;

Step f;

setting a temperature of the spacer plate from 5°

C. to 20°

C. after the temperature of the reached at 20°

C., the temperature of the product is maintained more than 4 hours whereby, the lyophilization process is finished and a freeze-dried powder with loose block is obtained.

6. The pharmaceutical composition containing docetaxel according to claim 1, wherein the pharmaceutical composition is micelles which is prepared by a film hydration method, and the method includes:

(1) weighting docetaxel and polyethylene glycol methyl ether-polylactide block copolymer with an amino acid end group respectively according to different feed ratios;

(2) disposing docetaxel and polyethylene glycol methyl ether-polylactide block copolymer with an amino acid end group into a container, and an organic solvent is added into container until the docetaxel and polyethylene glycol methyl ether-polylactide block copolymer with an amino acid end group dissolved completely;

(3) rotating and evaporating the container under 30-50°

C. for 2 hours until the organic solvent was evaporated to dryness and drying the remaining organic solvent is dried in vacuo at 10-60°

C. for more than 12 hours, so as to a polymeric mixed film of docetaxel-containing is obtained;

(4) disposing the polymer mixed film in a water bath with a temperature at 40-60°

C. until the polymer mixed film becomes the transparent, a preheated ultrapure water, physiological saline, or phosphate buffer with same temperature as the polymer mixed film is added into the polymer mixed film and is shaken and hydrated well to obtain a transparent drug loading micellar solution.

7. The pharmaceutical composition containing docetaxel according to claim 1, wherein the average particle size of the micelles is ranging from 18.0-29.5 nm.