Pharmacokinetic and pharmacodynamic studies of pregabalin suppositories based on pharmacological research

Ryo Yajima, Kazuaki Matsumoto, Kanako Yokono, Yuki Watabe, Yuki Enoki, Kazuaki Taguchi, Yuya Ise, Shiro Katayama, Junko Kizu

Research output: Contribution to journalArticle

Abstract

Objectives: 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. Methods: 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 in vitro. The pharmacokinetics and pharmacodynamics of the suppositories were assessed in rats. Key findings: In the in vitro 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 180 min. Among these pregabalin suppositories, only the suppository with H-15 : S-55 = 2 : 1 demonstrated an equivalent AUC 0−∞ 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 12 weeks when refrigerated with light shielding. Conclusions: The pregabalin suppositories prepared in this study may be applicable for pain control for terminally cancer ill patients with oral feeding difficulties.

Original languageEnglish
Pages (from-to)746-752
Number of pages7
JournalJournal of Pharmacy and Pharmacology
Volume71
Issue number5
DOIs
Publication statusPublished - 2019 May

Keywords

  • pharmacokinetics
  • pregabalin
  • release test
  • suppository
  • tail-flick test

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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