Formulation and optimization of gastro-retentive in situ gel of antiepileptic agent by using a Box–Behnken factorial design

Autor: Jakasaniya, Pratik, Patel, Jaydeep, Dudhat, Kiran, Mori, Dhaval
Zdroj: Proceedings of the Indian National Science Academy; 20240101, Issue: Preprints p1-14, 14p
Abstrakt: Objective: Pregabalin is the drug use for the treatment of partial epilepsy; however, absorption of the pregabalin mainly occurs in stomach and some extent of the upper part of GIT. Hence, pregabalin is a suitable drug candidate for the floating delivery system. Additionally, pregabalin having a short biological half-life of about 3–6 h; it is given in frequent dosing. Hence, pregabalin is suitable candidate for a sustained drug delivery. Methods: Various polymers were screened out and among them, sodium alginate and gellan gum were used for the preparation of various formulations. The drug-loaded in situ gel was optimized using a Box–Behnken experimental design, with sodium alginate concentration (X1), gellan gum concentration (X2), and calcium carbonate concentration (X3) as the independent variables. While floating lag time (Y1), viscosity (Y2), CPR 15 (Y3), CPR 50 (Y4), and CPR 480 (Y5) as dependent variables. All the formulated batches were characterized for pH, drug content, viscosity, in vitro buoyancy, in vitro gelation, and in vitro drug release. Results: An optimized batch was evaluated, revealing minimal differences among the tested samples. Stability studies indicated that the formulation maintained consistent drug content, floating lag time, viscosity, pH, in vitro gelation, and in vitro drug release, without significant changes. A gastro-retentive dosage form of pregabalin was developed to enhance its retention time in the stomach and to control its release. Conclusions: Floating in situ gel is the better approach for pregabalin with higher total floating time. Graphical Abstract:
Databáze: Supplemental Index