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Stable amorphous amifostine compositions and methods for the preparation and use of same

A technology for forming amifostine and amifostine, which is applied in the field of heat-stable dosage forms and preparation of the same substance, and can solve the problems of undisclosed amorphous heat-stable amifostine, etc.

Inactive Publication Date: 2002-01-30
MEDIMMUNE ONCOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To the applicant's knowledge, no amorphous thermally stable amifostine has been disclosed so far

Method used

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  • Stable amorphous amifostine compositions and methods for the preparation and use of same
  • Stable amorphous amifostine compositions and methods for the preparation and use of same
  • Stable amorphous amifostine compositions and methods for the preparation and use of same

Examples

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Embodiment 1

[0089] The following examples are intended to illustrate the invention and do not constitute a limitation on them in any way. 5.1. Example 1 Stable amorphous amifostine dosage form containing nicotinamide

[0090] At 25°C, an aqueous solution of 100 mg / mL amifostine and 12.5 mg / mL nicotinamide (Aldrich) was sterilized and filtered through a 0.2 μm filter membrane, and then divided into 5 mL aliquots, and each of them was transferred to 10mL vial. Place the freeze-drying stopper in the vial and place the sample on the shelf of the freeze dryer to maintain at 5°C. Reduce the shelf temperature to -45°C within 60 minutes and keep it at this temperature for about 3 hours. Then the condenser of the freeze dryer was opened and the chamber was evacuated to approximately 100 μmHg. After the chamber vacuum has reached equilibrium, the shelf temperature is increased to -25°C within 60 minutes, and the vacuum degree is kept constant during this period. Keep the shelf temperature at -25°C for ...

Embodiment 2

[0091] The stability test of the dosage form prepared according to this method was carried out, and the results provided in Table 1 below were obtained. 5.2. Example 2 Stable amorphous amifostine dosage form containing nicotinamide and PVP

[0092] At 25° C., 100 mg / mL amifostine, 12.5 mg / mL nicotinamide (Aldrich) and 10 mg / mL polyvinylpyrrolidone 30 (PVP30: BASFAktiengesellschaft, Feinchemie, 0-6700 Ludwigshafen, Germany) The aqueous solution was sterilized and filtered, and then divided into 5 mL aliquots, each of which was transferred to a 10 mL vial. Place the freeze-drying stopper in the vial and place the sample on the shelf of the freeze dryer to maintain at 5°C. Reduce the shelf temperature to -45°C within 60 minutes and keep it at this temperature for about 3 hours. Then the condenser of the freeze dryer was opened and the chamber was evacuated to approximately 100 μmHg. After the chamber vacuum has reached equilibrium, the shelf temperature is increased to -25°C within 6...

Embodiment 3

[0093] The stability test of the dosage form prepared according to this method was carried out, and the results provided in Table 4 below were obtained. 5.3. Example 3 Determination of crystallinity

[0094] The crystallinity of the dosage form of the present invention can be determined by powder x-ray diffraction, as described, for example, in Remington's Pharmacy, 18th edition, page 173; United States Pharmacopeia, 23rd edition (1995), 1843-1844.

[0095] figure 2 The general powder x-ray diffraction spectrum of the amorphous amifostine dosage form prepared according to the method of Example 1 is shown, measured with a Geiger-Muller detector using nickel-filtered CuKα radiation. The diffraction pattern contains the broad baseline nature of the amorphous material. The peaks at 2θ≈14.8, 25.6, and 26.3 are due to nicotinamide and / or noise. From image 3 From a point of view, the arrangement is clear. It shows the x-ray powder diffraction pattern of crystalline nicotinamide.

[00...

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PUM

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Abstract

The present invention relates to sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous amifostine.

Description

1. Field of Invention [0001] The present invention relates to a heat stabilized dosage form of S-2-(3-aminopropylamino)ethyl dihydrogen thiophosphate (amifostine) and a method for preparing the same substance. The reformulated form of the invention is suitable for administration to humans, for example, as a radioprotectant or chemoprotectant. 2. Background of the invention [0002] U.S. Patent No. 3,892,824 discloses the compound S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate (which is also known as amifostine, ethiofos, Ethyol  , NSC296961 and WR-2721 and it is hereinafter referred to as "Amifostine") and other aminothiol compounds. These compounds were originally developed as anti-radiation drugs (radioprotectants), especially before exposure to x-rays or nuclear radiation, to avoid the harmful effects of such exposure that may be encountered during military conflicts. [0003] In addition to its use as a military anti-radiation drug, it has been proven that amifost...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/19A61K31/66A61K47/18A61K47/22A61P35/00A61P39/00
CPCA61K9/0019A61K47/183A61K9/19A61K31/66A61K31/661A61P35/00A61P39/00
Inventor M·斯托格纽J·M·扎戴
Owner MEDIMMUNE ONCOLOGY
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