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Soluble pharmaceutical forms of N,N'-diaminodiphenyl sulphone for optimum use in the treatment of various diseases

A diaminodiphenyl sulfone, disease technology, used in drug combinations, blood diseases, drug delivery and other directions

Active Publication Date: 2012-07-04
UNIV AUTONOMA METROPOLITANA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The surfactant compound Tween-80 has been reported at a rate of 90% [Helton DR, Osborne DW, Pierson SK, Buonarati MH, Bethem RA., Pharmacokinetic profiles in rats after intravenous, oral, or dermal administration of dapsone, Drug Metabolism and Disposition 28: 925-929 (2000)] N,N'-diaminodiphenyl sulfone solution, but there is a serious disadvantage that Tween-80 is a toxic compound at the concentration necessary to dissolve the sulfone, which is excluded for humans

Method used

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  • Soluble pharmaceutical forms of N,N'-diaminodiphenyl sulphone for optimum use in the treatment of various diseases
  • Soluble pharmaceutical forms of N,N'-diaminodiphenyl sulphone for optimum use in the treatment of various diseases
  • Soluble pharmaceutical forms of N,N'-diaminodiphenyl sulphone for optimum use in the treatment of various diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1. Dissolution of N,N'-diaminodiphenylsulfone for administration as a solution for administration by any enteral or parenteral route.

[0032] 50 mg to 500 g of N,N'-diaminodiphenylsulfone are weighed and placed in a test tube. A 5-volume mixture containing 2.9 volumes of propylene glycol, 1.25 volumes of ethanol and 0.85 volumes of water was added. Shake the tube until the N,N'-diaminodiphenylsulfone is completely dissolved.

[0033] The obtained solution was transferred to a glass, sealed and sterilized by autoclaving.

[0034] To determine whether N,N'-diaminodiphenylsulfone was completely dissolved and whether there was appreciable N,N'-diaminodiphenylsulfone degradation caused by the sterilization step, N,N'-diaminodiphenylsulfone was analyzed by high-resolution liquid chromatography by UV light detection. , N'-diaminodiphenylsulfone solution.

[0035] Assessing the effect of a soluble formulation of N,N'-diaminodiphenylsulfone on nervous system pro...

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Abstract

The object of the present invention is to demonstrate that it is possible to prepare a soluble pharmaceutical form of N,N'-diaminodiphenyl sulphone that can be used to produce an optimum drug for use against cerebral infarction, epilepsy, traumatic lesion of the spinal column, cranial-encephalic lesion, leprosy, Pneumocystis carinii infections, and any condition requiring rapid and complete absorption of the compound. As a representative example of this use, a solution of N,N'-diaminodiphenyl sulphone was evaluated as neuroprotector in an acute cerebral infarction model in rats. In this study, N,N'-diaminodiphenyl sulphone demonstrated significant prevention of cerebral damage without exhibiting adverse effects in the animals. It was also demonstrated that the soluble pharmaceutical forms prepared from this form produce maximum blood concentrations 30 minutes after oral administration and immediately after intravenous administration.

Description

technical field [0001] The present invention relates to the pharmaceutical production industry, and more particularly to the industry for the preparation of pharmaceuticals for various diseases. Background technique [0002] Chemotherapy for leprosy and pneumocystis carinii infection is administered with N,N'-diaminodiphenylsulfone pills. The pharmaceutical formulation of N,N'-diaminodiphenylsulfone in solution as a drug causes technical problems due to the low solubility of N,N'-diaminodiphenylsulfone in aqueous media, therefore, in the present invention , using co-solvents compatible with safe use in human pharmaceuticals, the new formulations are presented to allow solubilization of up to 200 mg sulfone / 3 mL. [0003] The use of the surfactant compound Tween-80 at 90% has been reported [Helton DR, Osborne DW, Pierson SK, Buonarati MH, Bethem RA., Pharmacokinetic profiles in rats after intravenous, oral, or dermal administration of dapsone, Drug Metabolism and Dispo...

Claims

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Application Information

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IPC IPC(8): A61K31/10C07C317/32C07C317/34
CPCA61K9/0019A61K31/136A61K9/08A61K31/145A61K47/10A61P25/00A61P25/16A61P25/20A61P25/28A61P31/00A61P31/04A61P31/08A61P7/04A61P9/10A61K31/10C07C317/32C07C317/34
Inventor M·阿尔塔格拉希亚马提内兹L·C·里奥斯卡斯塔纳达J·克拉弗佐夫吉尼克M·D·L·A·A·戴兹鲁尔兹
Owner UNIV AUTONOMA METROPOLITANA
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