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Process for obtaining steroidal phosphate compounds

A technology of compounds and phosphate esters, used in pharmaceutical formulations, drug combinations, medical preparations containing active ingredients, etc.

Active Publication Date: 2010-06-16
HOVION ASSOC LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These sodium phosphate salts are known to undergo rapid degradation

Method used

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  • Process for obtaining steroidal phosphate compounds
  • Process for obtaining steroidal phosphate compounds
  • Process for obtaining steroidal phosphate compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Embodiment 1: the spray drying of betamethasone 21-phosphate disodium

[0068] Wet betamethasone 21-phosphate disodium having a purity of 99.8% (HPLC area %) obtained by applying literature techniques was dissolved in water to obtain a 5% by weight solution on dry matter basis. The pH of the solution was adjusted to 7.6 / 7.9 by adding 1N hydrochloric acid. The outlet temperature was maintained between 80°C and 100°C, the atomization flow rate was 357-670 standard liters per hour, and the solution flow rate was between 5ml / min and 9ml / min. The product was collected in a high performance cyclone. The product [betamethasone 21-phosphate] was obtained with a purity of 99.6% and residual solvents meeting the requirements of the USP and EP pharmacopoeias (methanol: 428 ppm; isopropanol: 2088 ppm; water, by Karl-Fischer method: 8.0% by weight).

Embodiment 2

[0069] Embodiment 2: the spray drying of dexamethasone 21-phosphate disodium

[0070] Dexamethasone disodium 21-phosphate having a purity of 99.2% (HPLC area %) was dissolved in water to obtain a 5% by weight solution. The pH of the solution was adjusted to 7.6 / 7.9 by adding 1N hydrochloric acid. The outlet temperature was maintained between 80°C and 100°C, the atomization flow rate was 357-670 standard liters per hour, and the solution flow rate was between 5ml / min and 9ml / min. The product was collected in a high performance cyclone. The product [dexamethasone 21-phosphate] was obtained with a purity of 99.2% (HPLC area %).

Embodiment 3

[0071] Embodiment 3: the spray drying of prednisolone 21-phosphate disodium

[0072] Disodium prednisolone 21-phosphate with a purity of 98.4% (HPLC area %) was dissolved in water to obtain a 5% by weight solution. The pH of the solution was adjusted to 7.6 / 7.9 by adding 1N hydrochloric acid. The outlet temperature was maintained between 80°C and 100°C, the atomization flow rate was 357-670 standard liters per hour, and the solution flow rate was between 5ml / min and 9ml / min. The product was collected in a high performance cyclone. The product [prednisolone 21-phosphate] was obtained with a purity of 99.2% (HPLC area %).

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Abstract

A process for obtaining 21-disodium phosphate pregnane derivative compounds of formula (I), wherein X=R=H or X=F and R=alpha-CH3 or X=F and R=beta-CH3: comprises spray drying a solution comprising compound of formula (I).

Description

technical field [0001] The present invention relates to a method for preparing 21-phosphate disodium pregnane derivatives, as well as the compounds thus prepared and their use in medicine. [0002] The present invention relates to a new process for obtaining 21-phosphate disodium pregnane derivative compounds of formula [I], wherein X=R=H or X=F and R=α-CH 3 or X=F and R=β-CH 3 , [0003] Contents of the invention [0004] The present invention relates to a novel process for obtaining disodium 21-phosphate pregnane compounds of formula [I], preferably as a solid, which comprises spray drying a solution comprising a compound of formula [I]. Preferably, the solvent is water, wherein the concentration of the solution is preferably 2% to 30% by weight, more preferably 3% to 5% by weight. [0005] A feature of the present invention is that the process disclosed herein minimizes the degradation of the disodium 21-phosphate pregnane compound during drying, thus yielding compo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61P29/00A61K31/573
CPCA61K31/573A61K9/1688A61P29/00
Inventor L·索布拉尔F·加斯帕尔W·赫吉E·莱唐J·R·安图内斯
Owner HOVION ASSOC LTD
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