Gabapentin–saccharin co-crystals with enhanced physicochemical properties and in vivo absorption formulated as oro-dispersible tablets

Abstract

The physicochemical properties and in vivo absorption of a drug can be altered through cocrystallization with a suitable coformer. The aim of this study was to prepare and characterize Gabapentin (Gaba)–saccharine (sacch) sweet cocrystals for improvement of Gaba physicochemical properties, stability and in vivo absorption in addition to masking its taste. The prepared cocrystals were incorporated into oro-dispersible tablets as an attractive dosage form for pediatrics and adults. Gaba–sacch sweet cocrystals were prepared and characterized using FTIR, DSC, XRD and SEM analysis. They enhanced Gaba solubility and particle size distribution. Oro-dispersible tablets of the sweet cocrystals were prepared and evaluated in comparison to tablets prepared by Gaba–sacch physical mixture (PM). The tablets prepared by the cocrystals had lower wetting and disintegration time with enhanced drug release than those prepared with the physical mixture. The optimized formulation was evaluated for Gaba pharmacokinetics in rabbits in comparison to Gaba–sacch PM tablet and Gaba commercial oral capsules. This formulation had enhanced in vivo drug absorption through significant higher C_max and AUC_0–24 with shorter T_max. The prepared Gaba–sacch sweet cocrystals oro-dispersible tablets, in addition to its enhanced in vitro and in vivo performance, can also enhance patient compliance through its palatable taste and ease of administration.

Graphical Abstract

Keywords:

• Cocrystal
• gabapentin
• oro-dispersible
• pediatric
• saccharine

Disclosure statement

The authors have no conflicts of interest. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.