Rectal Absorption of Acetaminophen from Polyethylene Glycol and Witepsol Suppositories

아세트아미노펜의 Polyethylene glycol 및 Witepsol 좌제의 직장흡수 - 병원제제를 목적으로 한 아세트아미노펜좌제의 조제 및 유용성 검토-

  • Lee, Hye Suk (College or Pharmacy, Ewha Womans University, Department or Pharmacy, Seoul National University Hospital) ;
  • Jin, Sun Kyung (College or Pharmacy, Ewha Womans University) ;
  • Choi, Jung Hwa (College or Pharmacy, Ewha Womans University) ;
  • Ku, Young Soon (College or Pharmacy, Ewha Womans University)
  • 이혜숙 (이화여자대학교 약학대학, 서울대학교병원 약제부) ;
  • 진선경 (이화여자대학교 약학대학) ;
  • 최정화 (이화여자대학교 약학대학) ;
  • 구영순 (이화여자대학교 약학대학)
  • Published : 1998.12.01

Abstract

Acetaminophen (APAP) suppositories with active ingredients, i.e., polyethylene glycol (PEG), Witepsol H-15 (WH), were prepared for hospital use and investigated on their drug release characteristics and pharmacokinetics. WH was employed as oil-soluble base with an aim of reducing fragility and mucosa irritancy that are common drawbacks found in PEG suppositories. Also hollow type suppository was tried as compared with conventional type suppository. Drug release tests revealed that in most formulations, more than $80\%$ of loaded APAP were released within 20 minutes, except for APAP-WH hollow type suppositories. Significant differences in the plasma concentration profile were observed among four type suppositories. $T_{max}$ of APAP-PEG and APAP-WH suppositories were 90 and 60 minutes, respectively, in hollow types. APAP-WH hollow type suppositories demonstrated fast absorption rates of APAP as compared with those of APAP-PEG suppositories. No burst effect was observed from APAP-WH suppository in contrast to APAP conventional type suppository, whereas AUCs of all the suppositories were similar. APAP-WH hollow type suppository may be an useful dosage form for hospital use.

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