Utility of a Rectal Suppository Containing the Antiepileptic Drug Zonisamide
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概要
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A suppository of zonisamide (ZNS) was investigated from the viewpoint of pharmaceutical evaluation, pharmacokinetics and pharmacological effect. Two types of ZNS suppositories were prepared. One used Witepsol (H-15 : S-55=3 : 1) as a lipophilic base and the other polyethylene glycol (PEG, 4000 : 1500=4 : 1) as a hydrophilic base. The in vitro release rate of ZNS from the PEG suppository was significantly rapid compared with that of ZNS from Witepsol. Male Wistar rats were administered ZNS (20 mg/kg) using an intravenous, oral or rectal (PEG or Witepsol) route. The absorption of ZNS from the PEG suppository was more rapid than that of ZNS from the Witepsol suppository or from the oral preparation. The peak plasma concentration (C_<max>) after a rectal administration of ZNS with Witepsol or PEG suppository was significantly higher than that after the oral administration of ZNS. However, the bioavailability of the three preparations was approximately 100%. Male ICR mice were administered ZNS (80 mg/kg) using the oral or rectal (PEG or Witepsol) route. A positive correlation was observed between the electroshock seizure (ES) threshold and ZNS concentration in plasma or brain. Further, there was no significant difference in the ES threshold or the ZNS concentration in plasma or brain among the three preparations. These results indicate that a ZNS suppository is a very useful preparation from the viewpoint of both pharmacokinetics and pharmacological action.
- 公益社団法人日本薬学会の論文
- 1997-08-15
著者
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HIGUCHI Shun
Department of Clinical Pharmacokinetics, Graduate School, Kyushu University
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TSUZUKI Osami
Department of Pharmaceutics, Daiichi College of Pharmaceutical Sciences
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OHDO Shigehiro
Department of Pharmaceutics, Division of Pharmaceutical Science, Graduate School, Kyushu University
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Mishima Motohiro
Department Of Pharmaceutical Services Kumamoto University Hospital:faculty Of Pharmaceutical Science
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Mishima Motohiro
Department Of Pharmaceutical Sciences Daiichi College Of Pharmaceutical Sciences
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Tsuzuki O
Department Of Pharmaceutics Daiichi College Of Pharmaceutical Sciences
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Ohdo S
Kyushu Univ. Fukuoka Jpn
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Higuchi Shun
Department Of Clinical Pharmacokinetics Division Of Pharmaceutical Sciences Kyushu University
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NAGATOMI Aki
Department of Pharmaceutical Sciences, Daiichi College of Pharmaceutical Sciences
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Ohdo Shigehiro
Department Of Clinical Pharmacokinetics Division Of Pharmaceutical Sciences Kyushu University
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Nagatomi A
Department Of Pharmaceutical Sciences Daiichi College Of Pharmaceutical Sciences
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Tsuzuki Osami
Department of Pharmaceutics, Daiichi College of Pharmaceutical Science
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