Allometric scaling is an empirical examination of the relationships between the pharmacokinetic parameters and size (usually body weight, ratio of organ- and body weight, breathing number, etc.). Interspecies pharmacokinetics tend to approximate, the organism, as the sum of organs and tissues according to material balance. The allometric equations for the pharmacokinetic parameters were applied to scale the data with respect to pharmacokinetic time and remove the chronological time dependency. When the data of at least three species are available, the pharmacokinetic parameters can be fit according to body weight in log-log regression. Allometric scaling is not applicable in all cases, only when the selected species has similar physiological behaviour, such as protein-binding, metabolism, etc. Valuable information for the evaluation of the effect and the biopharmaceutical characteristics may emerge from more creative data analysis based on all result collected during the preclinical evaluation of a new drug. Author examined the applicability of the interspecies scaling method in the case of a new drug depogen, using drotaverin as reference. The pharmacokinetic data were collected from mouse, rat and dog and during the evaluation human data were applied too. The usual pharmacokinetic parameters were determined (MRT, MAT, beta, etc.), the results of allometric analysis were collected and the standard deviation of measured and calculated values were given.

01 Jun 1992·Thrombosis ResearchQ3 · MEDICINE

Comparative studies of drotaverine-acephyllinate (Depogen) and pentoxifylline (Trental)

Q3 · MEDICINE

Article

Author: Z. Kapui ; L. Tardos ; Gy. Blaskó ; P. Szentmiklósi ; I. Hermecz ; B. Sarkadi

Pentoxifylline is an orally active agent for the treatment of peripherial and cerebral vascular diseases. Pentoxifylline increases the deformability of red blood cells in vitro, reduces blood viscosity and decreases platelet aggregation and thrombus formation. Depogen has shown antiaggregatory effect both in vitro and in ex vivo. The inhibitory effect of Pentoxifylline was about 3-5 times weaker than that of Depogen. IC50 = 900/micrograms/ml for Depogén and 3600/micrograms/ml for Pentoxifylline on human platelet rich plasma. Depogen has shown ex vivo antiaggregatory effect on anesthetised rabbits, ID50 = 7 mg/kg in case of iv. administration, and ID50 = 300 mg/kg in case of orally administration. Both compound inhibit the release of platelet precoagulation factor, but the effect of Pentoxifylline was slighter.

01 Jan 1984·European Journal of Drug Metabolism and PharmacokineticsQ4 · MEDICINE

The fate of Drotaverine-Acephyllinate in rat and man II. Human pharmacokinetics of Drotaverine-14C-Acephyllinate

Q4 · MEDICINE

Article

Author: Varkonyi, T. ; Vargay, Z. ; Szatmari, I. ; Kerpel-Fronius, S. ; Deutsch, T. ; Eckhardt, S. ; Szuts, T.

Pharmacokinetics of Drotaverine-Acephyllinate, Chinoin was investigated in seven male volunteers using 14C labelled drug. Drotaverine-Acephyllinate was administered at a 100 mg single oral dose. Measurements of total radioactivity showed that the drug was absorbed completely and was eliminated by renal and biliary routes. Within 72 hours 39.9 +/- 9.9% and 47.1 +/- 4.9% of the dose were recovered in the urine and faeces respectively. Experimental results were interpreted on the basis of a complex linear compartment model. The structural identifiability of the model was proved by computer analysis, and the pharmacokinetic parameters were determined.

100 Deals associated with Drotaverine acephyllinate

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Indication	Highest Phase	Country/Location	Organization	Date
Peripheral Vascular Diseases	Phase 3	HU	Chinoin Zrt.	-
Peripheral Vascular Diseases	Phase 3	-	Sanofi	-

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