Chronopharmacokinetic study of a prolonged release form of indomethacin

Guissou, Pierre I.; Cuisinaud, G.; Llorca, G.; Lejeune, E; Sassard, J

doi:10.1007/bf00542219

Cited by 44 publications

(18 citation statements)

References 7 publications

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“…This diurnal effect has been suggested for other drugs (Guisson et al, 1983), and could reflect the effect of food (Woodcock et al, 1986), hepatic blood flow (Woodcock et al, 1981a,b) or posture (Daneshmend et al, 1981) on the pharmacokinetic profile.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and pharmacodynamics of two formulations of verapamil.

Hla

Henry

Latham

1987

Brit J Clinical Pharma

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The pharmacokinetics and pharmacodynamics of sustained release verapamil were compared with the conventional formulation in 10 healthy adult volunteers after single and multiple dosing. The mean time of maximum plasma concentrations of verapamil were significantly prolonged and the absorption rate constants significantly reduced after sustained release verapamil on both day 1 and day 10. On day 10 there was no significant difference between formulations in the relative bioavailability of verapamil. However, the area under the plasma concentration‐time curve and maximum concentration (Cmax) for both formulations increased significantly with repeat dosing. On day 10, the difference in Cmax between formulations was significant. The day 10 mean peak/trough plasma verapamil concentration ratio was significantly less following the sustained release dose form. The mean PR interval was significantly prolonged by both formulations on day 1 and day 10. There were no differences between formulations other than a significantly longer PR interval following the conventional formulation 2 h after dosing on day 10.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and pharmacodynamics of two formulations of verapamil.

Hla

Henry

Latham

1987

Brit J Clinical Pharma

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“…These time-dependent variations could be due to the parallel changes in physiological functions and variables involved in the absorption, distribution, metabolism, and excretion of drugs. [1][2][3] The clearance of ampicillin is known to exhibit a circadian rhythm which peaks at 2400 and reaches a nadir at 1200. 8 Liposomal encapsulation is known to significantly alter the disposition of drugs.…”

Section: Discussionmentioning

confidence: 99%

“…The rhythm generally reaches the peak and nadir of its sinusoidal wave once daily during the active and resting phase, respectively. [1][2][3] Some examples of drugs which exhibit circadian rhythms include calcium channel blockers, theophylline, and indomethacin. [1][2][3] These studies found that experimental subjects were more susceptible to the toxic effects of drugs during the rest period as opposed to the active period.…”

Section: Introductionmentioning

confidence: 99%

Chronokinetics of Liposomal Encapsulated Ampicillin in Fasting and Nonfasting Rats

Pardue

White

1996

Journal of Pharmaceutical Sciences

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The chronobiological effect on the pharmacokinetics of liposomal encapsulated ampicillin (LEA) was compared at noon (1200) and midnight (2400) after intravenous injection of 50 mg/kg of LEA in rats. The effects of fasting on the circadian rhythms of LEA were also investigated. Serial blood samples were collected for 2 h. Bile and urine were collected during the entire study. Plasma data was analyzed by noncompartmental methods. Dosing of LEA at 2400, when the animals were active, resulted in a 50% decrease in mean residence time (MRT) and a 20% increase in systemic clearance (Cltotal). The increase in Cltotal was reflected by increases in biliary (Clbile) and renal (Clrenal) clearance at 2400. In addition, the steady-state volume of distribution (Vss) at 2400 was also decreased by about 50% as compared to dosing at 1200. Interestingly, no difference in the pharmacokinetic parameters were observed in fasting animals at 1200 and 2400. Since rats consume very little food during their sleep cycle, restriction of food intake did not have any affect on the pharmacokinetics of LEA at 1200. However, fasting rats had an approximately 36% decrease in Cltotal as compared to nonfasting rats at 2400. This decrease in systemic clearance was paralleled by a 60% and 24% decrease in Clbile and Clrenal, respectively. These variations could be attributed to changes in bile composition and/or lipoprotein concentrations in the plasma as a result of "forced" fasting at 2400 when the animals are generally more active and food intake is high.

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“…Earlier and higher peak concentrations were obtained when indomethacin was given at 07:00 or 11:00 than at other times of the day or night [21]. Better morning absorption has also been observed with controlled release indomethacin and ketoprofen formulations [22,23]. The clinical relevance of such variations is that high plasma concentrations correlate with high incidence of adverse effects.…”

Section: Anti-inflammatory Drugsmentioning

confidence: 99%