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Fabrication and evaluation of pH dependent polymeric microspheres of ivabradine and their in vitro and in vivo studies

Abdul Majeed1, Nazar Muhammad Ranjha1, Mussadique Hussain1, 2, Muhammad Fawad Rasool1

Aim of this work was the development and evaluation of controlled release formulations consisting of methacrylate derivatives and ethyl cellulose (EC) were synthesized using oil-in-oil (O/O) solvent evaporation method. Drug release studies were performed in different dissolution media. Maximum drug released was observed at pH 7.4. Fourier transform infrared spectroscopy (FTIR) spectra, SEM, and thermal analysis showed compatibility between drug and polymers. Pharmacokinetic parameters were calculated by Phoenix WinNonLin® Version 6.3 software. The average AUC0-t was found to be 2483.71 ± 13.173 ng/ml.h, 5954.37 ± 12.110 ng/ml.h, 6400.82 ± 19.131 ng/ml.h and 7427.4 ± 49.322 ng/ml.h for group 1-4 respectively. The maximum concentration (Cmax) of IBH for all groups predicted from pharmacokinetics data were 880.38 ng/ml, 718.43 ng/ml, 721.87 ng/ml and 805.11 ng/ml respectively. Thus, in-vitro and in-vivo drug release studies of polymeric microspheres proved their controlled release behavior with preferential delivery for an extended period of time.

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