Utility of a Rectal Suppository Containing the Antiepileptic Drug Zonisamide
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- Material Type
- 記事
- Author/Editor
- Aki NagatomiMotohiro MishimaOsami Tsuzuki 他
- Author Heading
- Periodical title
- Biological and pharmaceutical bulletin
- No. or year of volume/issue
- 20(8) 1997.08
- Volume
- 20
- Issue
- 8
- Pages
- 892～896
- Publication date of volume/issue (W3CDTF)
- 1997-08
- ISSN (Periodical Title)
- 0918-6158
- ISSN-L (Periodical Title)
- 0918-6158
- Publication (Periodical Title)
- Tokyo : Pharmaceutical Society of Japan
- Place of Publication (Country Code)
- JP
- Text Language Code
- eng
- NDLC
- Target Audience
- 一般
- Holding library
- 国立国会図書館
- Call No.
- Z53-V41
- Data Provider (Database)
- 国立国会図書館 : 国立国会図書館雑誌記事索引
- Bibliographic ID (NDL)
- 4287949
- Bibliographic Record Category (NDL)
- 632
- Summary, etc.
- 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<SUB>max</SUB>) 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.
- DOI
- 10.1248/bpb.20.892
- Access Restrictions
- インターネット公開
- Data Provider (Database)
- 科学技術振興機構 : J-STAGE
- Summary, etc.
- 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<SUB>max</SUB>) 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.
- DOI
- 10.1248/bpb.20.892
- Access Restrictions
- インターネット公開
- Related Material (URI)
- Data Provider (Database)
- 国立情報学研究所 : CiNii Research
- Original Data Provider (Database)
- Japan Link Center雑誌記事索引データベースCrossrefPubMedCiNii Articles
- Bibliographic ID (NDL)
- 4287949
- NAID
- 110003639169