Characterization of Pharmacokinetic Parameters for Hospital Preparation of a Suppository Containing Gabapentin Tablet

Narutoshi Arai, Isamu Murata, Arina Ashiguchi, Taisei Nishiyama, Yutaka Inoue, Masayuki Kimura, Ikuo Kanamoto
2015 Iryo Yakugaku (Japanese Journal of Pharmaceutical Health Care and Sciences)  
Cancer pain often causes a decreased quality of life in patients. Gabapentin (GBP) is recommended as a supplementary analgesic for cancer-related pain, and can be taken at all steps of the World Health Organization pain relief ladder. However, GBP treatment is limited to oral administration. Therefore, a new route of administration is required for cancer patients who are unable to take oral medications. In this study, we demonstrate the preparation method and characterize the pharmacokinetics
more » ... a suppository containing GBP in tablet form. The suppository bases polyethylene glycol (P), Witepsol H-15 (H), and Witepsol S-55 (S) were compared to find the optimal base for the suppositories. We compared intravenous (iv), per os (po), and intrarectal (ir) administration of GBP powder and tablet formulations: (GBPp and GBPt) prepared in a base of P, H, or S (GBPp/P, GBPp/H, GBPp/S, GBPt/P, GBPt/H, and GBPt/S). The hardness of the GBPt group was significantly lower than that of the GBPp group. The drug-release profiles of the GBPt suppository groups were highest, in the order H, P, and S. The drug-release profile of the GBPt/S group was significantly higher than that of the GBPp/S group. The time to maximum drug concentration of the GBPt/S group was significantly increased compared with the po, GBPt/P, and GBPt/H groups. The GBPt/H group had similar pharmacokinetic parameters to the po group. These results suggest that a suppository containing GBP tablet is better than the conventional preparation method for hospital preparation.
doi:10.5649/jjphcs.41.861 fatcat:jyhkaqlqmjcsddj3xmit4pxvha