Parenteral formulations of the poorly soluble antituberculosis antibiotic rifapentine were developed. Proteins (human serum albumin, succinylated gelatin, and sodium caseinate) were used to produce water-soluble forms of rifapentine by precipitation or homogenization. Ultrasonic homogenization gave the best results, i.e., stable colloidal suspensions with 9 – 10 mg of rifapentine per mL (practically 100 times greater than its water solubility). Dilution of the suspensions led to dissociation of the aggregates formed during the solubilization and formation of a clear solution. The particle size decreased to 10 – 20 nm, which corresponded to the particle size in a solution of the proteins at the same concentration. This would not cause embolization upon infusion of such water-soluble forms of rifapentine. The results indicated that the selected approach was promising for designing parenteral formulations of rifapentine.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 50, No. 6, pp. 39 – 44, June, 2016.
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Ostrovskii, K.P., Osipova, N.S., Vanchugova, L.V. et al. Use of Proteins to Increase the Aqueous Solubility of Rifapentine. Pharm Chem J 50, 407–412 (2016). https://doi.org/10.1007/s11094-016-1460-8
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DOI: https://doi.org/10.1007/s11094-016-1460-8