The purpose of this investigation was to design and develop trilayer matrix tablets of Nelfinavir prepared by
direct compression method and consisted of middle active layer with different grades of hydroxypropyl
methylcellulose (HPMC), PVK K 30 and MCC. Barrier layers are prepared with Polyox WSR 303, Xanthan gum,
microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile
and release drug kinetics DF8 was found to be optimized formulation. The developed drug delivery system
provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation
(DF8) was described by the Zero-order and best fitted to Higuchi model. From in vivo bioavailability studies the
extended release of Nelfinavir from trilayer matrix tablets also provides for higher plasma drug content and
improved bioavailability. The results indicate that the approach used could lead to a successful development of
low biological half life Nelfinavir with controlled drug release in the effective management of AIDS.
The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.
The present study was aimed to develop and optimize extended release (ER) matrix tablets of Lamivudine trilayer tablets to achieve zero-order drug release for prolonged period of time.Lamivudine tablets were prepared by direct compression and consist of middle active layer with different grades of HPMC, MCC and PVP K30, upper and lower layers were prepared with Carnauba wax, Xanthan gum, EC and MCC. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF23) was described by the Zero-order and Higuchi model. The results indicate that the approach used could lead to a successful development of extended release formulation of short biological half-life drug. These results also demonstrated the suitability of three-layered tablet formulation of Lamivudine to provide controlled release for prolonged period of time and improved linearity for Lamivudine in comparison to marketed product in the effective management of AIDS with patient compliance.
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