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Pharmaceutical composition comprising racemic aminopterin

A technology of aminopterin and composition, applied in the field of pharmaceutical compositions comprising racemic aminopterin, can solve the problem of high cost, achieve the effects of low production cost, increase system exposure, and reduce regulatory burden

Active Publication Date: 2015-09-02
安密诺普特凌公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A disadvantage of this method is that it is more expensive to produce the essentially single enantiomer than to produce the same racemate

Method used

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  • Pharmaceutical composition comprising racemic aminopterin
  • Pharmaceutical composition comprising racemic aminopterin
  • Pharmaceutical composition comprising racemic aminopterin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] pharmaceutical composition

[0063] See Table 1 for optically pure, racemic, scored, immediate release (IR) tablet formulations in dosage strengths of 0.25 mg (Lot No. 157I0907) and 1.0 mg (Lot Nos. 387I1100 and 116I0604).

[0064] Table 1

[0065]

[0066] * In any event, the drug in the tablet is the disodium salt and the dosage strength required for the tablet is the free acid (ie diacid) equivalents of the L-isomer or the D-isomer plus the L-isomer.

Embodiment 2

[0068] Analysis of L-isomers and D-isomers in Tablet Preparations

[0069] Determination of enantiomeric purity in levorotatory tablet formulations (lots 387I1100 and 116I0604) and determination of levorotatory in racemic tablet formulations (lot 157I0907) using isocratic reversed-phase high performance liquid chromatography with a chiral mobile phase The relative content of body and dextrorotatory body. The method includes the following steps:

[0070] Step 1: Analytical chiral mobile phase for HPLC. L-proline (1.86 g, 16 mmol, Sigma Aldrich product P-0380) and copper(II) nitrate hydrate (1.86 g, 8 mmol, Sigma Aldrich product 229636) were dissolved in 1 L of filtered and degassed HPLC grade water ( J.T.Baker product 4218-03). Using a pH meter, the pH of the solution was adjusted to 6.00 with 5N NaOH (approximately 2.5 ml).

[0071] Step 2: L-aminopterin standard preparation. A 1.0 mg / ml solution of L-aminopterin (Sigma Aldrich product A1784) was prepared in dimethylaceta...

Embodiment 3

[0083] Quantification of Total Aminopterin Isomers in Tablet Formulations

[0084] The total amount of aminopterin isomers in the pure levorotatory tablet formulations (Lot No. 387I1100 and 116I0604) and in the racemic tablet formulation (Lot No. 157I0907) were analyzed by reversed-phase HPLC gradient method. The method includes the following steps:

[0085] Step 1: Mobile Phase Preparation. Dissolve 100ml of 1.0M triethylammonium acetate buffer solution (1.0M TEAAC, Fluka product 90357) in 900ml of HPLC grade water to make 1L filtered and degassed 0.1M triethylammonium acetate buffer solution as solvent a. 1 L of filtered and degassed acetonitrile was used as solvent B.

[0086] Step 2: L-aminopterin standard. A certain amount (50 mg x 565.2 / 440.4) of L-aminopterin standard (disodium salt) was weighed (that is, the amount equivalent to 50 mg of free acid). Transfer the L-aminopterin standard to a 50 ml volumetric flask and dissolve to 50 ml with solvent A to provide a 1....

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Abstract

Pharmaceutical compositions containing racemic aminopterin or a pharmaceutically acceptable salt thereof are disclosed. Also disclosed is a method of treating a disease in a patient comprising administering a therapeutically effective amount of racemic aminopterin or a pharmaceutically acceptable salt thereof. More specifically, a method of treating diseases modulated by at least dihydrofolate reductase activity, such as cancer and inflammatory diseases, wherein the method comprises administering a therapeutically effective amount of racemic aminopterin or a pharmaceutically acceptable salt to administer to patients in need.

Description

technical field [0001] The present invention provides pharmaceutical compositions comprising racemic aminopterin or a pharmaceutically acceptable salt thereof. The present invention also provides a method of treating a disease in a patient comprising administering a therapeutically effective amount of racemic aminopterin or a pharmaceutically acceptable salt thereof. More specifically, the invention provides methods of treating diseases modulated at least by the activity of dihydrofolate reductase, such as cancer and inflammatory diseases, wherein the methods comprise administering a therapeutically effective amount of racemic aminopterin or a pharmaceutically acceptable Receive salt to administer to patients in need. [0002] This invention was made with government support under grants 1R43AI068282, 3R43AI068282-01S1, 3R43AI068282-S2, 5R43AR056547 from the National Institutes of Health. The government has certain rights in this invention. Background technique [0003] An...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/495A61P19/02
CPCA61K31/519A61P1/00A61P1/04A61P11/00A61P17/00A61P17/06A61P19/02A61P29/00A61P35/00A61P35/02A61P37/08A61P43/00A61K9/0053A61K9/20A61K9/48A61K31/4985
Inventor 约翰·A·泽贝拉迪安·Y·密达约耳·R·摩根斯图亚特·J·卡恩
Owner 安密诺普特凌公司
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