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Wieslaw Sawicki and Stanislaw Janicki
Medical University of Gdansk, Poland
Posters & Accepted Abstracts: J Develop Drugs
Pharmacokinetics of verapamil (V) and its metabolite norverapamil (NV), from buccal drug formulation (BDF) administered in a dose 20 mg in relation to conventional tablets of V 40 mg, used in medical practice, was determined. The employed BDF have a form of a thin elastic disc made of two layers. Composition of the dosing layer is: V 0.02 g; Povidone K-30 0.076 g; glycerol 0.0173 g; polyoxyethylene alkyl ethers (Brij 96) 0.0199. Diameter of the form is 10 mm; thickness is 0.38 mm. Composition of the protective layer is: Povidone K-30 0.152 g; glycerol 0.035 g. Diameter is 12.5 mm, thickness 0.5 mm. Conventional tablets Staveran 40 mg (Polpharma S.A., Starogard Gda√?¬?ski, Poland) were used as the reference drug. BDF has previously been designed as an alternative form of dosing V. Bioavailability was determined by a crossover method in 12 healthy volunteers. Drug concentration in plasma was determined by means of HPLC with a fluorescence detector. For BDF the average values of Cmax and AUC0-24h for V were much higher than for the reference Staveran 40 mg tablets and amounted to 51.28 and 320.23 ng/ml h, respectively. However, for NV the corresponding values for BDF were much lower than for a conventional tablet. It has been demonstrated that the proposed buccal V dosing ensures different metabolism of the drug as compared to tablets. Better parameters of bioavailability of V from BDF of twice a smaller dose than that in the tablet, prove that this new drug might be form more effective clinically than the conventional one. The above data indicate that V released from a BDF to buccal mucosa is quickly absorbed into the blood stream and undergoes metabolism in the liver to only a small extent. More favourable bioavailability parameters of V from a BDF compared to standard Staveran tablets containing twice the dose of drug is clear evidence that the buccal delivery from the system designed in our laboratory is promising.
Wies√?¬?aw Sawicki completed his PhD and DSc from Faculty of Pharmacy, Medical University of Gda√?¬?sk (Poland). He is the Head of the Department of Physical Chemistry, Dean (2008-2016) of the Faculty of Pharmacy, Medical University of Gda√?¬?sk and Member of several scientific and professional bodies. He is the Reviewer of ca. 200 manuscripts of publications and research projects- pharmaceutical technology - tablets, pellets, therapetic systems and physical pharmacy.
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