Design of oral intestinal-specific alginate-vitexin nanoparticulate system to modulate blood glucose level of diabetic rats

Most drug substances are poorly soluble in water so that their efficacies must be improved by increasing the dosage, which not only creates economic problems but also increases the toxicity of the future medicine These problems can be solved by developing various dosage forms, which involves additional financial costs, complicates the technology, increases development times to introduce the future medicine, etc Another approach to improving the solubility of such drug substances is the development of methods and technologies for producing solid dispersions of these drug substances with excipients (polymers, dispersants, surfactants, etc) The present review covers the development and application of mechanochemical technology to modify sparingly soluble anthelmintic drugs The technology consists essentially of joint mechanical treatment of a drug substance and polymer in grinder-activators of controlled energy This technology uses one stage and avoids the use of solvents, heating, evaporation, etc The resulting solid dispersions include supramolecular systems with increased solubility and better bioavailability and are also highly active with reduced consumption of the active ingredients

Strategies for Solubility Enhancement of Anthelmintics (Review)

Solid dispersions of medamine and albendazole with water-soluble polymers (PVP, arabinogalactan) were obtained by mechanochemical technology to increase the aqueous solubility of poorly soluble anthelmintic drug substances. An analysis of solid dispersions of drug–polymer systems showed that their solubilities depended on the nature of both the drug and polymer. The aqueous solubilities of medamine and albendazole could be increased by greater than 50 and 27 times, respectively, by varying the joint processing time with the polymers. An analysis of IR spectra and a comparison of them with published data suggested that intermolecular complexes were formed in these systems. Innovative anthelmintic drugs with increased solubility for medicine and veterinary medicine could be created by using the proposed mechanochemical technology for obtaining solid dispersions. The resulting solid dispersions had several advantages over conventional dosage forms, in particular, they were obtained in one stage, their preparation did not require excipients (dispersants, surfactants, wetting agents, etc.), and they were more conveniently used and inexpensively priced.

Solid Dispersions of Medamine and Albendazole with Water-Soluble Polymers: Preparation and Properties

The effect of solid dispersions (SDs) on the solubility of furazolidone is studied. Furazolidone and its SDs with polyvinylpyrrolidone (PVP), PVP-10 000, PVP-12 600, and PVP-24 000 are examined. When using SDs, the solubility and dissolution rate of the nitrofuran derivative is increased. The solubility of furazolidone from SD is increased by a factor of 1.1 to 1.6. The dissolution rate of SDs is increased by a factor of 1.8 to 2.8. The complex of physicochemical methods of investigation suggests that an increase in solubility from SDs is caused by the loss of crystallinity and the formation of a solid solution of furazolidone during the preparation of SDs, as well as the solubilizing effect of the polymer during the subsequent dissolution of the SD in water. The results can be used in the development of hydrophilic soft and fast dissolving solid dosage forms of furazolidone with increased release and bioavailability.

Study of the Solubility of Furazolidone from Solid Dispersions with Polyvinylpyrrolidone

Taking into account the current Product specification file, the aim of the work was to develop the composition and technology for obtaining effervescent tablets based on solid dispersions of furazolidone in the form of an aqueous solution for external use.Materials and methods. The used substances were: furazolidone, anhydrous sodium carbonate (chemically pure), polyvinylpyrrolidone-24000±2000 (chemically pure), malic acid (analytically pure), tartaric acid (chemically pure), citric acid (chemically pure), sodium benzoate (chemically pure), ethyl alcohol 96% (chemically pure), purified water. Preparation of granulates is separate wet granulation in a fluidized bed (Mycrolab, BOSCH, Germany). Obtaining tablets is the process of pressing on a manual hydraulic test press (“PRG”, VNIR, Russia). The dependence of disintegration, abrasion capacity and crushing resistance on compacting pressure was investigated. Technological parameters of granulates, еру obtained effervescent tablets, shelf life and storage conditions were investigated according to the State Pharmacopoeia of the Russian Federation XIVth ed.Results. Two compositions of effervescent tablets containing solid dispersions of furazolidone as an active substance were obtained, which, when dissolved in 100 ml of water at room temperature (20°C), form a solution of furazolidone with a concentration of 0.004% in less than 5 minutes. The method of quantitative determination of the furazolidone content in the effervescent tablets was validated. A complex of physicochemical methods for the analysis of tablets was carried out. Quality standards have been developed. The developed compositions stability of instant tablets during storage during accelerated and long-term tests has been experimentally confirmed. The preliminary shelf life and storage conditions have been determined.Conclusion. The result of technological and chemical-pharmaceutical research is the creation and evaluation of the quality of a new instant furazolidone dosage form as effervescent tablet formulations.

https://www.pharmpharm.ru/jour/article/download/1026/819

Development of nitrofuran derivative: composition and technology of effervescent tablets with solid dispersions

The effect of solid dispersions (SDs) on the solubility of the nonsteroidal anti-inflammatory drug ketoprofen was determined. Ketoprofen and its SDs with poly(ethylene glycol) PEG-400, -1000, -1500, -2000, and -3000 were studied. Dissolution of ketoprofen from the SDs increased by 1.2 – 1.8 times; the dissolution rate, by 1.7 – 2.4 times. The improved release of ketoprofen from the SDs was proposed to be due to several factors such as solubilization and amorphization of the compound and formation of intermolecular H-bonds. The results could be used to develop rapidly dissolving ketoprofen solid dosage forms.

Dissolution of Ketoprofen from Poly(Ethylene Glycol) Solid Dispersions

The solubility of ketoprofen (nonsteroidal anti-inflammatory drug) from solid dispersions based on polyvinylpyrrolidone (PVP-10000, PVP-12600 and PVP-24000) is studied. The use of solid dispersions (SDs) increases the solubility and dissolution rate. The solubility of ketoprofen from SD increases by 1.5–2.6 times. The rate of dissolution from SDs increases by 1.5–3.2 times. The studies conducted by a complex of physical and chemical methods suggest that an improved release of ketoprofen from SDs is due to the generation of solid solution of the active substance in the polymer, the formation of intermolecular hydrogen bonds of the active substance with polyvinylpyrrolidone and the solubilizing effect of the polymer during the dissolution of ketoprofen. The results obtained can be used in the development of fast-dissolving solid dosage forms of ketoprofen with enhanced bioavailability.

T. P. Kudinova

Papers

Dissolution of Ketoprofen from Poly(Ethylene Glycol) Solid Dispersions

Study on the Solubility of Ketoprofen From Solid Dispersions with Polyvinylpyrrolidone