Solid Dispersions of Medamine and Albendazole with Water-Soluble Polymers: Preparation and Properties
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Pharmaceutical Chemistry Journal, Vol. 54, No. 8, November, 2020 (Russian Original Vol. 54, No. 8, August, 2020)
SOLID DISPERSIONS OF MEDAMINE AND ALBENDAZOLE WITH WATER-SOLUBLE POLYMERS: PREPARATION AND PROPERTIES S. S. Khalikov,1,* B. V. Lokshin,1 and M. M. Il’in1 Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 8, pp. 23 – 28, August, 2020.
Original article submitted January 25, 2019. 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. Keywords: solid dispersions, solubility, medamine, albendazole, polymers.
This method was first used for mechanochemical modification of poorly soluble (1 mg/L) anthelmintic medamine drug substance to increase its solubility [5]. Joint milling of medamine with apple pectin in an AGO-2U planetary ball mill (Gefest, St. Petersburg) produced medapec preparation with improved aqueous solubility (45 mg/L) [6]. Medapec remained highly active against nematodes and was highly effective and well tolerated in experimental larval alveolar echinococcosis in cotton rats [7, 8]. This result was explained by us by the formation of intermolecular complexes based on our own IR spectroscopic data, dissolution and dialysis of medapec, and a comparison with the literature [9]. In particular, intermolecular complexes of several drugs (Sibazon, indomethacin, Mezapam, nifedipine, etc.) with polysaccharides and other polymers were reported [10]. The obtained complexes were more soluble and pharmacologically active than the starting drugs. The formation of analogous complexes was reported earlier [11] during studies of complexes produced by two methods: a) joint solid-state mechanochemical processing of nonsteroidal anti-inflammatory drugs with glycyrrhizic acid; b) chemical synthesis in solutions.
Mechanical technology (milling, mixing, compression, etc.) is known to play an important role in pharmacy because it is used to prepare several dosage forms and its effect on the finished drug must
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