Pharmacokinetic properties Subject

Fourtillan JB, Brisson AM, Girault J, Ingrand I, Decourt JP, Drieu K, Jouenne P, Biber A. (1995). [Pharmacokinetic properties of bilobalide and ginkgolides A and B in healthy subjects after intravenous and oral administration of Ginkgo biloba extract (EGb 761)]. Therapie. 50(2) 137-44. Frewer U. (1990). The effect of betel nut on human performance. PNG MedJ. 33(2) 143-5. 

Pharmacokinetics The pharmacokinetic properties of Infergen have not been evaluated in patients with chronic hepatitis C. Pharmacokinetic profiles were evaluated in normal, healthy volunteer subjects after subcutaneous injection of interferon alfacon-1 at doses up to 9 j,g. Plasma levels of interferon alfacon-1 at any dose were too low to be detected. However, analysis of Infergen-induced cellular products— induction of 2 5 oligoadenylate synthetase and (beta)-2 microglobulin—after treatment in these subjects revealed a statistically significant, dose-related increase in the area under the curve (AUC). 

Fourtillan JB, Brisson AM, Girault J, et al. Pharmacokinetic properties of bilobalide and ginkgolides A and B in healthy subjects after intravenous and oral administration of Ginkgo biloba extract (EGb 761). Therapie 1995 50 137-144. 

Pharmacokinetic properties The compound is subject to an intensive first-pass metabolism via glucuronidation of the free phenolic hydroxyl group (Wilson et al., 1995 Strain et al., 1996). This strongly reduces oral bioavailability and induces a short duration of action. 

Pharmacokinetic properties Naltrexone (Misra, 1981) is absorbed from the gastrointestinal tract, but is subject to considerable first-pass metabolism in the liver, yielding the active metabolite 6-beta-naltrexole. Naltrexone has low plasma binding of about 20%. The half-life of naltrexone is -3 h and of 6-beta-naltrexole is -13 h. 

Pharmacokinetic properties Following parenteral administration sufentanil has a rapid onset and a short duration of action. The compound is very lipophilic and is subject to high plasma protein binding of 90%. The short... 

In conclusion, the rapid acting insulin, HMR1964 (insulin glulisine) maintains its pharmacokinetic properties in subjects with decreased renal function covering a wide range of renal impairment. 

The pharmacokinetic properties of fluoroquinolone antibacterial agents have been well described [23]. Gemifloxacin is rapidly absorbed with a time to maximum plasma concentration (T ax) of 0.5-2 h in healthy subjects and displays linear pharmacokinetics over the dose range studied (20-800 mg), with an apparent plasma terminal half-life (fi/2) after single or repeated administration of about 8 h. A minimum of 20-30% of the oral dose is excreted imchanged in the urine. Following repeat oral... 

Nabumetone is absorbed primarily from the duodenum. Milk and food increase the rate of absorption and the bioavailability of the active metabolite. Plasma concentrations of unchanged drug are too low to be detected in most subjects after oral administration, so most pharmacokinetic studies have involved the disposition of the active metabolite. Pharmacokinetic properties are altered in elderly patients, with higher plasma levels of the active metabolite being noted. Nabumetone undergoes rapid and extensive metabolism in the liver, with a mean absolute bioavailability of the active metabolite of 38%. The metabolism of nabumetone is illustrated in Figure 36.15. The major. 

In ceftizoxime, the whole C-3 side chain has been omitted to prevent deactivation by hydrolysis. It rather resembles cefotaxime in its properties however, not being subject to metabolism, its pharmacokinetic properties are much less complex. 

Song, M., Gao, X., Hang, T-J., Wen, A-D. (2009) Pharmacokinetic properties of lansoprazole (30-mg enteric-coated capsules) and its metabolite a single-dose, open-label study in healthy Chinese male subjects. Current Therapeutic Research, 70,228-238. 

According to the EMA two products are considered to be bioequivalent when they contain the same active substance and when their respective bioavailabilities (rate and extent) after administration in the same molar dose and via the same route, lie within acceptable predefined limits. These limits are set to ensure comparable in vivo performance, i.e. similarity in terms of safety and efficacy. The design and number of studies that is to be carried out to establish bioequivalence depends on the physico-chemical and pharmacokinetic properties of the active substance. In this respect reference is made to the BCS classification of the active substance. For BCS class I active substances it may even be possible to obtain a waiver for the in vivo studies (a so-called biowaiver), whereas for the active substances showing more complex pharmacokinetic behaviour extensive studies are to be carried out. In general bioequivalence will be determined from the parameters Cmax and AUC. Two products are considered to be bioequivalent when the 90 % confidence interval of the ratio of test and reference product falls within the 85-125 % acceptance interval. However, for the required design of the bioequivalence study and statistical evaluation details for a specific active substance reference is made to the appropriate (most recent) guideline on this subject [2, 3]. 

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