Influence of route of administration and dosage form in the pharmacokinetics and bioavailability of salbutamol

Abstract

The present study was carried out to define the pharmacokinetics of salbutamol sulfate administered to mongrel dogs in five pharmaceutical forms via two routes of administration. One pharmaceutical form was administered intravenously (Ventolin i.v.) while the other four were administered orally (Ventolin: immediate-release formulation, Volmax: commercial osmotic pump, SG7 and SG14: sustained-release hydrophilic matrices developed in our laboratory). We obtained a first-order release kinetic of the salbutamol from Ventolin and SG7, whereas a zero-order release kinetic was observed for SG14 and Volmax formulations. Oral bioavailability was 80% and there were neither significant differences (P > 0.05) in terms of the calculation method used (relation of the areas under the plasma level curve Loo-Riegelman, deconvolution) nor in terms of the dosage form (Ventolin Volmax, SG7 and SG14). The elimination half-life value of salbutamol was 1.2 h when administered intravenously; this parameter had a value of 3.0 h for the immediate-release formulation and ranged between 5.4 and 7.2 h in the sustained-release formulations when administered orally. These changes in the half-life value of the sustained-release formulations will allow us to modify the frequency of administration in relation to immediate-release formulations.

Flip-flop Pharmacokinetics – Delivering a Reversal of Disposition: Challenges and Opportunities During Drug Development

“…Furthermore, deconvolution application for flip-flop pharmacokinetics involves its capacity to estimate the rate and extent of systemic availability following extravascular routes of administration such as oral, intranasal, rectal and transdermal, among others [42,43]. In addition to being used to characterize the absorption of different dosage forms, deconvolution is used to assess drug–drug interactions [44] by taking the iv. data as the weighing function and the test formulation data, following extravascular administration, as the response function.…”

Inhibition of TNBC Cell Growth by Paroxetine: Induction of Apoptosis and Blockage of Autophagy Flux

“…Previous clinical trials have shown that, contingent on the specific condition being treated, the total daily dosage of PX for adult psychiatric patients ranges from 20 to 50 mg [ 74 , 75 , 76 ]. It is worth noting that the dosage form of PX used in our current study differed from that used in clinical practice, potentially resulting in variations in pharmacokinetic parameters [ 77 ]. Therefore, the dose in our animal experiments may differ from the dose used in humans.…”