Abstract: A method of designing a pharmaceutical composition for providing the liver of a person or animal, as a therapeutic target, with a predetermined concentration of a sulfate or sulfonate of a pharmacologically active agent, during a predetermined period, includes determining the correlation between the solubility of a sulfate and/or sulfonate of a pharmacologically active agent of the formula Dn+(R1SO3)?n or Dn+(R2OSO3)?n for various carbon chain lengths X, Y in an aqueous solvent and the expected concentration of the pharmaceutically active agent D in the therapeutic target upon administration of the pharmacologically active agent D to the person or animal, defining a target solubility of the sulfate or sulfonate based on a desired concentration of said pharmaceutically active substance D in the therapeutic target, and determining the carbon chain length(s) X, Y corresponding to the target solubility.
Abstract: An anti-neoplastic stable pharmaceutical composition comprising Temozolomide, high substituted polysaccharide phosphate in salt form, and high substituted polysaccharide phosphate in acidic form, in particular in a weight ratio of from 5 to 20% Temozolomide to 30 to 80% of polysaccharide in salt form, the reminder up to 100% being polysaccharide in acidic form. The level of 5-aminomidazole-4-carboxamide is below 0.5% by weight of Temozolomide in both the composition and the formulation disclosed. Also disclosed is a hydrogel for intrathecal administration obtainable by contacting the composition with sterile water, a method of manufacture of the composition and uses of the composition and the gel.
Type:
Grant
Filed:
April 28, 2017
Date of Patent:
October 20, 2020
Assignees:
Double Bond Pharmaceutical AB, Research Institute of Physical Chemical Problems of the Belarulsna State University
Abstract: A pharmaceutical composition in form of an aqueous colloid or an aqueous suspension of particles up to a size of 100 ?m comprises or consists of amphiphilic sulfonate or sulfate of a hydrophilic cancer drug having a solubility in water or aqueous body fluid of less than 0.1% by weight. Also disclosed are the particles in powderous form, methods for their production and for the production of the colloid and the courser suspension, a method of treating liver cancer, in particular solid liver cancer tumours, by administration of the pharmaceutical composition, and a method of designing a composition according to the invention.