[In vitro and in vivo biopharmaceutical evaluation of lorazepam commercial tablets].
OBJECTIVE
Lorazepam (LZM) is a broadly used tranquillizer for the treatment of anxiety. Tavor is one of the most diffused registered drug products containing LZM. Lots of generic drug products containing LZM have been registered in Italy by several pharmaceutical groups and are present in the Italian market. Due to the wide medical prescription of products containing LZM, it seemed interesting, from a technological and biopharmaceutical point of view, to perform a comparative bioequivalence evaluation of a trade marked and generic tablet formulations containing LZM available in the Italian market.


METHODS
The trial vas carried out on four preparations, including Tavor (1 mg) as reference product and three generics named A, B and C. In vitro technological parameters (dissolution, uniformity of content, uniformity of weight) and in vivo (pharmacokinetic on rabbit) studies were performed.


RESULTS
All the examined brands passed technological tests according the European Pharmacopeia 5th ed. and USP25. Tavor ensures a faster dissolution behaviour than the tree generics in vitro. All the pharmacokinetic parameters were within the prescriptions of EMEA, even if the reference product showed the highest values of AUC0-infinity and of Cmax.


CONCLUSIONS
Obtained results show that Tavor ensures a faster dissolution behaviour than the tree generics in vitro. Moreover, considering the pharmacokinetic data, it is possible to suppose that the generics B and C are not able to provide the same therapeutic effect as the reference product.
Giannone
I
I
Dipartimento di Scienze Farmaceutiche, Università di Catania, Italia.
Musumeci
T
T
Pecora
T M G
TM
Puglisi
G
G
D000704:Analysis of Variance; D001702:Biopharmaceutics; D002626:Chemistry, Pharmaceutical; D016568:Drugs, Generic; D006801:Humans; D008140:Lorazepam / Q000097:blood / Q000493:pharmacokinetics; D008333:Mandelic Acids; D015233:Models, Statistical; D010599:Pharmacokinetics; D013607:Tablets; D013810:Therapeutic Equivalency
D016568:Drugs, Generic; D008333:Mandelic Acids; D013607:Tablets; C005419:oxybutynin; D008140:Lorazepam