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pharmaceutical composition

A composition and drug technology, applied in the directions of drug combination, drug delivery, boron compound active ingredients, etc., can solve the problems of bortezomib degradation and complex research on prefabrication

Inactive Publication Date: 2011-12-21
SUN PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The literature mentions that the degradation and preformation studies of bortezomib have been found to be very complicated

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment I

[0057] Take 3.5 mg of bortezomib containing 2.75% of total impurities. Weigh 3.31 mg of trometamol and mix in vial. With continuous stirring, water for injection (enough to make 1 ml) was added. The solution was heated at 45°C to 50°C to form a clear solution. The solution was cooled and 30 mg of sodium chloride was added to the cooled solution. The solution was filtered through a 0.45 micron needle filter and the pH was determined. The pH of the clear solution was found to be 8.68, which was adjusted to 8.01 with 5% hydrochloric acid. The clear solution was lyophilized. Reconstitution of the lyophilized cake takes less than 30 seconds and does not require an ultrasonic bath. After reconstitution, the solution was found to be stable with respect to particle formation for 24 hours, ie no particles were observed. The IR spectrum of the lyophilized composition was recorded. figure 1The IR spectrum is given. The IR spectrum of this formulation shows the formation of tromet...

Embodiment II

[0059] Take 3.5 mg of bortezomib containing 2.75% of total impurities. Weigh 3.31 mg of trometamol, wherein the total impurities are less than 0.51%, and the optical rotation is -53.4 °, and the impurity A is accurately weighed and put into a vial. Weigh 3.31 mg of trometamol and mix in the vial. With continuous stirring, water for injection (enough to make 1 ml) was added. The solution was heated at 45°C to 50°C to form a clear solution. The solution was cooled and 30 mg of sodium chloride was added to the cooled solution. The solution was filtered through a 0.45 micron needle filter and the pH was determined. The pH of the clear solution was found to be 8.68, which was adjusted to 8.01 with 5% hydrochloric acid. The clear solution was lyophilized. Reconstitution of the lyophilized cake takes less than 30 seconds and does not require an ultrasonic bath. After reconstitution, the solution was found to be stable with respect to particle formation for 24 hours, ie no parti...

Embodiment III

[0061] Take 3.5 mg of bortezomib containing 2.75% of total impurities. Accurately weigh 3.5 mg of bortezomib into a 5 ml vial. Weigh 3.31 mg of trometamol and mix in vial. With continuous stirring, water for injection (enough to make 1 ml) was added. The solution was heated at 45°C to 50°C to form a clear solution. The solution was filtered through a 0.45 micron needle filter and the pH was determined. The pH of the clear solution was found to be 8.75 and was adjusted to 7.89 with 5% hydrochloric acid. The clear solution was lyophilized. Reconstitution of the lyophilized cake required less than 30 seconds and did not require an ultrasonic bath. After reconstitution, the solution was found to be stable with respect to particle formation for 24 hours, ie no particles were observed. The IR spectrum of the lyophilized composition was recorded. figure 2 The IR spectrum is given. The IR spectrum of this formulation shows the formation of tromethamine salts with strong B-N b...

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PUM

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Abstract

The present invention relates to a parenteral pharmaceutical composition comprising therapeutically effective amounts of N-(2-yrazine) carbonyl-L-phenylalanine-L-leucine boronic acid or its salts or its derivatives and tromethamine wherein the composition is stable.

Description

technical field [0001] The invention relates to a novel pharmaceutical composition for injection, which contains N-(2-pyrazinyl)carbonyl-L-phenylalanyl-L-leucine boronic acid and tromethamine. The composition in lyophilized form is stable at room temperature and when reconstituted, the resulting aqueous solution is stable for at least 12 hours. Background technique [0002] Bortezomib is N-(2-pyrazinyl)carbonyl-L-phenylalanyl-L-leucine boronic acid. [0003] [0004] Solid bortezomib is insoluble in 0.9% w / v sodium chloride at a concentration of 1 mg / ml. It is marketed as an injection under the brand name Velcade. It is given intravenously only and contains the mannitol ester of bortezomib. It is available in lyophilized form and when reconstituted forms an equilibrated solution of mannitol esters and bortezomib. Using 0.9% sodium chloride will Reconstitute to bortezomib at a final concentration of 1 mg / ml. The use of mannitol provides the required solubility. The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4985A61K38/05A61K9/08
CPCA61K9/0019A61K31/133A61K31/69A61K9/19A61K45/06A61P35/00A61K2300/00A61K31/4985A61K38/05A61K9/08
Inventor 奥克B·纳姆多N·萨布拉玛尼安撒布哈斯巴拉姆·博米克
Owner SUN PHARMA INDS
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