Pharmacokinetic and Pharmacodynamic Evaluations of Novel Oral Morphine Sustained Release Granules(Pharmacology)
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概要
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Pharmacokinetics and pharmacodynamics of novel oral sustained-release granules based on swelling polymer incorporation layer system (SPILA granules) containing morphine hydrochloride was evaluated. SPILA granules were designed to release morphine faster in neutral environment than in acidic one to keep higher plasma levels over a protracted period, especially after 12 h post dose. SPILA granules were orally administered to beagle dogs to compare the pharmacokinetics with commercially available twice-a-day dosage form, MS Contin^[○!R]. Tmn and AUC_<0-24h> values of SPILA granules were 6h and 191 μg・h/ml, respectively. T_<max> and AUC_<0-24h> values of MS Contin^[○!R] were 2h and 146 μg・h/ml, respectively. Relative bioavailability following SPILA granules administration to twice-a-day MS Contin^[○!R] (30 mg) administration was 131%. In rats, analgesic effect was evaluated over 24 h. SPILA granules and aqueous solutions were administered to rats to compare the analgesic effect. AUC_<0-24h> value for SPILA granules was 8.88μg・h/ml, which was a little lower than that for the aqueous solution (10.1 μg・h/ml), whereas the analgesic effect after SPILA granules once-a-day administration expressed as AURC (1701% Analgesia・h) was similar to that after the aqueous solution 4 times-a-day administration (1603% Analgesia・h). These results indicate that SPILA granules based on the pH-dependent release regulating polymer system can be a good candidate for an oral once-a-day sustained-release dosage form.
- 2007-08-01
著者
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NAKAMURA Kenji
Pharmaceutical Technology Research & Development Laboratories, Pharmaceutical Production Division, T
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NARA Eiji
Intellectual Property Department, Takeda Pharmaceutical Company Limited
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FUSE Takako
Pharmacology Research Laboratories I, Pharmacology Research Division, Takeda Pharmaceutical Company
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AKIYAMA Yohko
Pharmaceutical Technology Research & Development Laboratories, Pharmaceutical Production Division, T
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Nara Eiji
Intellectual Property Department Takeda Pharmaceutical Company Limited
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Fuse Takako
Pharmacology Research Laboratories I Pharmacology Research Division Takeda Pharmaceutical Company Li
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Akiyama Yohko
Pharmaceutical Technology Research & Development Laboratories Pharmaceutical Production Division
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Nakamura Kenji
Pharmaceutical Technology Research & Development Laboratories Pharmaceutical Production Division
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Nakamura Kenji
Pharma Foods International Co. Ltd.
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