Scientific journal
Balanced diet, nutritional supplements and biostimulants
ISSN 2414-1054
ISSN 2414-1054
MECHANOCHEMICAL TECHNOLOGY FOR IMPROVING SOLUBILITY OF DRUGS
Dushkin A.V. 1
Suntsova L.P. 1
Khalikov S.S. 2
1 Institute of Solid State chemistry and Mechanochemistry SB RAS
2 A.N. Nesmeyanov Institute of Organoelement Compounds of RAS
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The possibilities of mechanochemical technology for solid dispersions of poorly soluble drugs (PSD) with various adjuvants are discussed. The choice of the composition of solid dispersions, depending on the physical and chemical mechanisms of increasing the solubility of PSD is considered. On the example of the benzodiazepine substances – diazepam, oxazepam and medazepam – demonstrated the possibility of obtaining their solid dispersions in which the PSD in amorphous states and have a high release properties (solubility and dissolution rate) in aqueous solutions. This is accompanied by the increasing in the bioavailability determined in experiments with laboratory animals. Consider obtaining and properties of solid dispersions of PSD with acidic affi nity and excipients of alkaline nature, which forming water-soluble salts by hydration. Solid dispersions of acetylsalicylic acid with metal carbonate – sodium, calcium and magnesium are described in detail. The especial innovative drug of effervescent aspirin was developed on the base of our approach and registered in the Russian Federation. The solid dispersions of plant fl avonoids – rutinum and taxifolinum with carbonates metals having high (> 10 times) water solubility was obtained and studied.