MIDAZOLAM MICROENCAPSULATION AS A METHOD OF MODIFYING ITS PHARMACOKINETICS

DOI: https://doi.org/10.29296/25877313-2019-08-05
Issue: 
8
Year: 
2019

M.A. Judin Dr.Sc. (Med.), Associate Professor, Head of Department, Federal State Budgetary Institution State Scientific-Research Testing Institute of Military Medicine of the Ministry of Defense of the Russian Federation (St. Petersburg) S.V. Chepur Dr.Sc. (Med.), Professor, Head of Federal State Budgetary Institution State Scientific-Research Testing Institute of Military Medicine of the Ministry of Defense of the Russian Federation (St. Petersburg) O.I. Aleshina Junior Research Scientist, Federal State Budgetary Institution State Scientific-Research Testing Institute of Military Medicine of the Ministry of Defense of the Russian Federation (St. Petersburg) A.F. Bykova Ph.D. (Biol.), Senior Research Scientist, Federal State Budgetary Institution State Scientific-Research Testing Institute of Military Medicine of the Ministry of Defense of the Russian Federation (St. Petersburg) E-mail: anna-kurpyakova@rambler.ru I.M. Ivanov Ph.D. (Med.), Deputy Head of Department, , Federal State Budgetary Institution State Scientific-Research Testing Institute of Military Medicine of the Ministry of Defense of the Russian Federation (St. Petersburg)

Purpose of the study. The selection of the most optimal method for obtaining the microencapsulated form of midazolam, which improves the kinetics of its release from microparticles. Materials and methods. Methods of emulsification, double emulsification, nanoprecipitation and spray drying were used to create a microencapsulated form of midazolam. The efficiency of incorporation and distribution of midazolam between the matrix and the surface of the particles was evaluated using the HPLC methods. Results. It’s shown that the application of the spray drying method provides the maximum inclusion of midazolam in polymer matrices for samples based on alginate (more than 44 %) and polylactide-co-glicolide (more than 60 %). The in vitro release kinetics of midazolam is characterized by a gentle curve for sodium alginate-based samples compared to polylactide-co-glicolide samples. Findings. The most optimal midazolam incorporation and release parameters are achieved using PLGA- and alginate-based polymeric matrices. This allows us to consider samples based on them as promising means to increase the anticonvulsant effect in the treatment of toxic convulsive syn-drome

Keywords: 
midazolam
microencapsulation
pharmacokinetic
prolonged form

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