salicylates and benorilate

This paper reports the establishment of a method for rapid identification 15 effective components of anti common cold medicine (paracetamol, aminophenazone, pseudoephedrine hydrochloride, methylephedrine hydrochloride, caffeine, amantadine hydrochloride, phenazone, guaifenesin, chlorphenamine maleate, dextromethorphen hydrobromide, diphenhydramine hydrochloride, promethazine hydrochloride, propyphenazone, benorilate and diclofenac sodium) with MRM by LC-MS/MS. The samples were extracted by methanol and were separated from a Altantis T3 column within 15 min with a gradient of acetonitrile-ammonium acetate (containing 0.25% glacial acetic acid), a tandem quadrupole mass spectrometer equipped with electrospray ionization source (ESI) was used in positive ion mode, and multiple reaction monitoring (MRM) was performed for qualitative analysis of these compounds. The minimum detectable quantity were 0.33-2.5 microg x kg(-1) of the 15 compounds. The method is simple, accurate and with good reproducibility for rapid identification many components in the same chromatographic condition, and provides a reference for qualitative analysis illegally added chemicals in anti common cold medicine.

Topics: Acetaminophen; Acetanilides; Amantadine; Aminopyrine; Anti-Inflammatory Agents, Non-Steroidal; Antipyretics; Antipyrine; Caffeine; Chlorpheniramine; Chromatography, Liquid; Diclofenac; Diphenhydramine; Drug Contamination; Drug Stability; Ephedrine; Guaifenesin; Promethazine; Pseudoephedrine; Reproducibility of Results; Salicylates; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry

A new formulation tablet B was developed and compared with tablet A with the purpose of improving the bioavailability of benorilate by reducing its particle size. The dissolution rate in vitro was determined by paddle method and using surfactant solution medium. The plasma concentrations of hydrolyzates which are salicylic acid and paracetamol from benorilate in vivo were measured by HPLC. The dissolution rates of ground and unground drug are 0.0337 min-1 and 0.0152 min-1 (P < 0.001) respectively. Compared with tablet A, the cumulative dissolution percentage of B is higher. The mean dissolution time of B and A are 15.77 min and 42.25 min (P < 0.001) respectively. The study in vivo showed that the Cmax, Tp and AUC of salicylic acid for these two formulations have no significant difference (P > 0.1). The relative bioavailability of B to A is 125.59%. Their in vivo process fits one-compartment model and first order elimination.

Topics: Acetanilides; Adult; Biological Availability; Humans; Male; Salicylates; Solubility; Tablets