As commercially available pregabalin preparations are limited to oral administration, it is impossible to use it as an adjuvant analgesic for neuropathic cancer-related pain in terminally ill cancer patients with oral feeding difficulties. The objective of this study was to develop a pregabalin suppository to be available at hospitals. Pregabalin suppositories were prepared using bases comprising six different compositions of Witepsol H-15, Witepsol S-55, and Witepsol E-75. The suppository release test and stability test were performed invitro. The pharmacokinetics and pharmacodynamics of the suppositories were assessed in rats. In the invitro releasing test, the pregabalin suppositories with H-15, H-15:S-55=1:1, H-15:S-55=2:1, H-15:S-55=1:2 released approximately 100% of the pregabalin within 180min. Among these pregabalin suppositories, only the suppository with H-15:S-55=2:1 demonstrated an equivalent AUC0-∞ with the oral administration group. Consistent with the results of the pharmacokinetic study, the pregabalin suppository with H-15:S-55=2:1 exhibited antinociceptive effects. In addition, the pregabalin suppository with H-15:S-55=2:1 was stable for 12weeks when refrigerated with light shielding. The pregabalin suppositories prepared in this study may be applicable for pain control for terminally cancer ill patients with oral feeding difficulties.