The Experts below are selected from a list of 21 Experts worldwide ranked by ideXlab platform
Jun Watanabe - One of the best experts on this subject based on the ideXlab platform.
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pharmacokinetic pharmacodynamic relationship of eptazocine a Narcotic Antagonist analgesic in rats
Biological & Pharmaceutical Bulletin, 2000Co-Authors: Toyofumi Suzuki, Ryo Shimizu, Taiyo Suganuma, Junichi Nishino, Kazuo Tomono, Manabu Hanano, Jun WatanabeAbstract:The relstionship between the pharmacokinetics and the pharmacodynamics of eptazocine, a Narcotic-Antagonist analgesic, was investigated in rats. The analgesic effect of eptazocine (2.5, 5 and 10 mg/kg) following intravenous (i.v) administration was evaluated by both the Randall-Selitto method and the D'Amour-Smith method. The analgesic effects were determined before and at designed intervals for a period of 120 min after eptazocine administration, and are expressed as area under the effect-time curve (AUCE). The plasma concentration of eptazocine was determined by fluorescence HPLC and was analyzed with a two compartment open model using the nonlinear least-squares method. Eptazocine produced a dose-dependent analgesic effect. It was demonstrated that eptazocine has a linear relationship between AUCE and the area under the plasma concentration-time curve (AUC) following i.v. administration for three different doses ranging from 2.5 to 10 mg/kg.
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Pharmacokinetic/Pharmacodynamic Relationship of Eptazocine, a Narcotic-Antagonist Analgesic, in Rats
Biological & Pharmaceutical Bulletin, 2000Co-Authors: Toyofumi Suzuki, Ryo Shimizu, Taiyo Suganuma, Junichi Nishino, Kazuo Tomono, Manabu Hanano, Jun WatanabeAbstract:The relstionship between the pharmacokinetics and the pharmacodynamics of eptazocine, a Narcotic-Antagonist analgesic, was investigated in rats. The analgesic effect of eptazocine (2.5, 5 and 10 mg/kg) following intravenous (i.v) administration was evaluated by both the Randall-Selitto method and the D'Amour-Smith method. The analgesic effects were determined before and at designed intervals for a period of 120 min after eptazocine administration, and are expressed as area under the effect-time curve (AUCE). The plasma concentration of eptazocine was determined by fluorescence HPLC and was analyzed with a two compartment open model using the nonlinear least-squares method. Eptazocine produced a dose-dependent analgesic effect. It was demonstrated that eptazocine has a linear relationship between AUCE and the area under the plasma concentration-time curve (AUC) following i.v. administration for three different doses ranging from 2.5 to 10 mg/kg.
Toyofumi Suzuki - One of the best experts on this subject based on the ideXlab platform.
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pharmacokinetic pharmacodynamic relationship of eptazocine a Narcotic Antagonist analgesic in rats
Biological & Pharmaceutical Bulletin, 2000Co-Authors: Toyofumi Suzuki, Ryo Shimizu, Taiyo Suganuma, Junichi Nishino, Kazuo Tomono, Manabu Hanano, Jun WatanabeAbstract:The relstionship between the pharmacokinetics and the pharmacodynamics of eptazocine, a Narcotic-Antagonist analgesic, was investigated in rats. The analgesic effect of eptazocine (2.5, 5 and 10 mg/kg) following intravenous (i.v) administration was evaluated by both the Randall-Selitto method and the D'Amour-Smith method. The analgesic effects were determined before and at designed intervals for a period of 120 min after eptazocine administration, and are expressed as area under the effect-time curve (AUCE). The plasma concentration of eptazocine was determined by fluorescence HPLC and was analyzed with a two compartment open model using the nonlinear least-squares method. Eptazocine produced a dose-dependent analgesic effect. It was demonstrated that eptazocine has a linear relationship between AUCE and the area under the plasma concentration-time curve (AUC) following i.v. administration for three different doses ranging from 2.5 to 10 mg/kg.
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Pharmacokinetic/Pharmacodynamic Relationship of Eptazocine, a Narcotic-Antagonist Analgesic, in Rats
Biological & Pharmaceutical Bulletin, 2000Co-Authors: Toyofumi Suzuki, Ryo Shimizu, Taiyo Suganuma, Junichi Nishino, Kazuo Tomono, Manabu Hanano, Jun WatanabeAbstract:The relstionship between the pharmacokinetics and the pharmacodynamics of eptazocine, a Narcotic-Antagonist analgesic, was investigated in rats. The analgesic effect of eptazocine (2.5, 5 and 10 mg/kg) following intravenous (i.v) administration was evaluated by both the Randall-Selitto method and the D'Amour-Smith method. The analgesic effects were determined before and at designed intervals for a period of 120 min after eptazocine administration, and are expressed as area under the effect-time curve (AUCE). The plasma concentration of eptazocine was determined by fluorescence HPLC and was analyzed with a two compartment open model using the nonlinear least-squares method. Eptazocine produced a dose-dependent analgesic effect. It was demonstrated that eptazocine has a linear relationship between AUCE and the area under the plasma concentration-time curve (AUC) following i.v. administration for three different doses ranging from 2.5 to 10 mg/kg.
Mikio Takeda - One of the best experts on this subject based on the ideXlab platform.
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HOMOBENZOMORPHAN COMPOUNDS WITH A POTENT Narcotic Antagonist PROPERTY
Japanese Journal of Pharmacology, 2019Co-Authors: Seiichi Nurimoto, Shogo Suzuki, Goro Hayashi, Mikio TakedaAbstract:In consequence of testing Antagonistic activity on morphine-induced analgesia and respiratory depression of the, 2'-hydroxy-6, 10-dimethy-7, 8-homobenzomorphans, it was found that the order of Antagonistic activity is N-cyclopropylmethyl (trans isomer TA-414 and cis isomer TA-576)>N-allyl (trans isomer TA-412)>N-dimethylallyl (trans isomer TA-413 and cis isomer TA-415) with respect to the influence of replacing Antagonistic substitution on the tertiary nitrogen. The properties of TA-414 and TA-576 in this regard were higher than those of nalorphine but slightly less than levallorphan. Moreover, the Narcotic Antagonist action of TA-414 was of long duration, comparable to that of nalorphine. On the other hand, TA-414 was entirely lacking an agonistic (analgesic) activity even at large doses, while TA-576 equalled nalorphine and pentazocine in the potency of agonistic activity in mice. Conclusively, TA-414 appears to fall under the category of a pure Antagonist such as naloxone.
Jooae Park - One of the best experts on this subject based on the ideXlab platform.
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controlled release dosage form of Narcotic Antagonist i synthesis of biodegradable polyphosphazenes and preparation and release characteristics of naloxone implant
Journal of Pharmaceutical Investigation, 1995Co-Authors: Jooae ParkAbstract:For the administration of Narcotic Antagonist with short half-life and low patient compliance, the sustained release system using biodegradable matrix is effective. Polyphosphazenes are of considerable interest as biodegradable matrix systems for controlled release of drugs. In this study, biodegradable polyphosphazenes available for the sustained release implantable device were synthesized, and their application was examined. Poly[dichlorophosphazene] was synthesized by solution polymerization method and confirmed with IR spectrum. Poly[bis(ethyl glycinate) phosphazene] and poly[ (diethyl glutamate)-co-(ethyl glycinate)phosphazene] were then produced by substitution of amino acid alkyl esters for chloride side groups. Using these polymers, the implantable devices of 1 mm thickness and size containing naloxone hydrochloride were prepared and their release and degradation profiles were measured. In the case of poly[bis(ethyl glycinate)phosphazene] with swelling characteristics, degradation rate was slower than the release rate, showing that the release rate is partly dependent on the swelling rate. In contrast, the degradation rate of polyl[(diethyl glutamate)-co-(ethyl glycinate)phosphazene] matrix was identical with release rate of naloxone hydrochloride. On the basis of these results, it is expected that these polymers can be applied to sustained release implantable systems delivering Narcotic Antagonist.
Ryo Shimizu - One of the best experts on this subject based on the ideXlab platform.
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pharmacokinetic pharmacodynamic relationship of eptazocine a Narcotic Antagonist analgesic in rats
Biological & Pharmaceutical Bulletin, 2000Co-Authors: Toyofumi Suzuki, Ryo Shimizu, Taiyo Suganuma, Junichi Nishino, Kazuo Tomono, Manabu Hanano, Jun WatanabeAbstract:The relstionship between the pharmacokinetics and the pharmacodynamics of eptazocine, a Narcotic-Antagonist analgesic, was investigated in rats. The analgesic effect of eptazocine (2.5, 5 and 10 mg/kg) following intravenous (i.v) administration was evaluated by both the Randall-Selitto method and the D'Amour-Smith method. The analgesic effects were determined before and at designed intervals for a period of 120 min after eptazocine administration, and are expressed as area under the effect-time curve (AUCE). The plasma concentration of eptazocine was determined by fluorescence HPLC and was analyzed with a two compartment open model using the nonlinear least-squares method. Eptazocine produced a dose-dependent analgesic effect. It was demonstrated that eptazocine has a linear relationship between AUCE and the area under the plasma concentration-time curve (AUC) following i.v. administration for three different doses ranging from 2.5 to 10 mg/kg.
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Pharmacokinetic/Pharmacodynamic Relationship of Eptazocine, a Narcotic-Antagonist Analgesic, in Rats
Biological & Pharmaceutical Bulletin, 2000Co-Authors: Toyofumi Suzuki, Ryo Shimizu, Taiyo Suganuma, Junichi Nishino, Kazuo Tomono, Manabu Hanano, Jun WatanabeAbstract:The relstionship between the pharmacokinetics and the pharmacodynamics of eptazocine, a Narcotic-Antagonist analgesic, was investigated in rats. The analgesic effect of eptazocine (2.5, 5 and 10 mg/kg) following intravenous (i.v) administration was evaluated by both the Randall-Selitto method and the D'Amour-Smith method. The analgesic effects were determined before and at designed intervals for a period of 120 min after eptazocine administration, and are expressed as area under the effect-time curve (AUCE). The plasma concentration of eptazocine was determined by fluorescence HPLC and was analyzed with a two compartment open model using the nonlinear least-squares method. Eptazocine produced a dose-dependent analgesic effect. It was demonstrated that eptazocine has a linear relationship between AUCE and the area under the plasma concentration-time curve (AUC) following i.v. administration for three different doses ranging from 2.5 to 10 mg/kg.
