Promethazine Hydrochloride (promethazine + hydrochloride)

Distribution by Scientific Domains


Selected Abstracts


Electroanalytical Determination of Promethazine Hydrochloride in Pharmaceutical Formulations on Highly Boron-Doped Diamond Electrodes Using Square-Wave Adsorptive Voltammetry

ELECTROANALYSIS, Issue 18 2008
Francisco, Wirley
Abstract The electrochemical oxidation of promethazine hydrochloride was made on highly boron-doped diamond electrodes. Cyclic voltammetry experiments showed that the oxidation mechanisms involved the formation of an adsorbed product that is more readily oxidized, producing a new peak with lower potential values whose intensity can be increased by applying the accumulation potential for given times. The parameters were optimized and the highest current intensities were obtained by applying +0.78,V for 30 seconds. The square-wave adsorptive voltammetry results obtained in BR buffer showed two well-defined peaks, dependent on the pH and on the voltammetric parameters. The best responses were obtained at pH,4.0, frequency of 50,s,1, step of 2,mV, and amplitude of 50,mV. Under these conditions, linear responses were obtained for concentrations from 5.96×10,7 to 4.76×10,6,mol L,1, and calculated detection limits of 2.66×10,8,mol L,1 (8.51,,g L,1) for peak 1 and of 4.61×10,8,mol L,1 (14.77,,g L,1) for peak 2. The precision and accuracy were evaluated by repeatability and reproducibility experiments, which yielded values of less than 5.00% for both voltammetric peaks. The applicability of this procedure was tested on commercial formulations of promethazine hydrochloride by observing the stability, specificity, recovery and precision of the procedure in complex samples. All results obtained were compared to recommended procedure by British Pharmacopeia. The voltammetric results indicate that the proposed procedure is stable and sensitive, with good reproducibility even when the accumulation steps involve short times. It is therefore very suitable for the development of the electroanalytical procedure, providing adequate sensitivity and a reliable method. [source]


Complexation and chiral drug recognition of an amphiphilic phenothiazine derivative with , -cyclodextrin

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2008
Andrés Guerrero-Martínez
Abstract Promethazine hydrochloride (PTZ) is an amphiphilic drug derived from the phenothiazine structure that possesses a charged aliphatic chain with a chiral carbon. In the presence of , -cyclodextrin (, -CD), this drug undergoes significant changes of its photophysical properties in aqueous solution. Fluorescence spectroscopy measurements show the formation of a 1:1 stoichiometry complex with quantum yield lower than that of the pure PTZ, and two fluorescence lifetimes, which can be assigned to the free and complexed forms of the drug. In addition, 1H NMR spectra, and 2D rotating-frame Overhauser enhancement spectroscopy (ROESY) were used to characterize the drug and the complex, and to determine the effects of the complexation on the aggregation. For the drug binary system, a noncooperative association process is observed, and in the presence of macrocycle, the chemical shifts reveal a chiral resolution of the drug enantiomers, with different stability constants of the complexes. , -CD modifies the aggregation of PTZ in an extension that confirms the formation of a 1:1 complex. ROE enhancements and molecular modeling strategies show the most likely structure of the complex in solution, in which one of the phenyl rings is buried into the CD cavity, with a slight inclusion of the aliphatic part. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:1484,1498, 2008 [source]


Electroanalytical Determination of Promethazine Hydrochloride in Pharmaceutical Formulations on Highly Boron-Doped Diamond Electrodes Using Square-Wave Adsorptive Voltammetry

ELECTROANALYSIS, Issue 18 2008
Francisco, Wirley
Abstract The electrochemical oxidation of promethazine hydrochloride was made on highly boron-doped diamond electrodes. Cyclic voltammetry experiments showed that the oxidation mechanisms involved the formation of an adsorbed product that is more readily oxidized, producing a new peak with lower potential values whose intensity can be increased by applying the accumulation potential for given times. The parameters were optimized and the highest current intensities were obtained by applying +0.78,V for 30 seconds. The square-wave adsorptive voltammetry results obtained in BR buffer showed two well-defined peaks, dependent on the pH and on the voltammetric parameters. The best responses were obtained at pH,4.0, frequency of 50,s,1, step of 2,mV, and amplitude of 50,mV. Under these conditions, linear responses were obtained for concentrations from 5.96×10,7 to 4.76×10,6,mol L,1, and calculated detection limits of 2.66×10,8,mol L,1 (8.51,,g L,1) for peak 1 and of 4.61×10,8,mol L,1 (14.77,,g L,1) for peak 2. The precision and accuracy were evaluated by repeatability and reproducibility experiments, which yielded values of less than 5.00% for both voltammetric peaks. The applicability of this procedure was tested on commercial formulations of promethazine hydrochloride by observing the stability, specificity, recovery and precision of the procedure in complex samples. All results obtained were compared to recommended procedure by British Pharmacopeia. The voltammetric results indicate that the proposed procedure is stable and sensitive, with good reproducibility even when the accumulation steps involve short times. It is therefore very suitable for the development of the electroanalytical procedure, providing adequate sensitivity and a reliable method. [source]


Electrochemical, Chemical and Enzymatic Oxidations of Phenothiazines

ELECTROANALYSIS, Issue 17 2005
B. Blankert
Abstract The oxidation of several phenothiazine drugs (phenothiazine, promethazine hydrochloride, promazine hydrochloride, trimeprazine hydrochloride and ethopropazine hydrochloride) has been carried out in aqueous acidic media by electrochemical, chemical and enzymatic methods. The chemical oxidation was performed in acetic acid with hydrogen peroxide or in formate buffers using persulfate. The enzymatic oxidation was performed in acetate or ammonium formate buffer by the enzyme horseradish peroxidase in the presence of H2O2. Molecules with, in the lateral chain, two carbon atoms (2C) separating the ring nitrogen and the terminal nitrogen, showed two parallel oxidation pathways, that is (i) formation of the corresponding sulfoxide and (ii) cleavage of the lateral chain with liberation of phenothiazine (PHZ) oxidized products (PHZ sulfoxide and PHZ quinone imine). Molecules with three carbon atoms (3C) separating the two nitrogens were oxidized to the corresponding sulfoxide. The chemical oxidation of all the studied molecules by hydrogen peroxide resulted in the corresponding sulfoxide with no break of the lateral chain. Oxidation by persulfate yielded, for the 3C derivatives, only the corresponding sulfoxide, but it produced cleavage of the lateral chain for the 2C derivatives. The origin of the distinct oxidation pattern between 2C and 3C molecules might be related to steric effects due to the lateral chain. The data are of interest in drug metabolism studies, especially for the early search. In the case of 2C phenothiazines, the results predict the possibility of an in vivo cleavage of the lateral chain with liberation of phenothiazine oxidized products which are known to produce several adverse side effects. [source]


Synthesis of pH dependent chitosan-EPI hydrogel films and their application for in vitro release of promethazine hydrochloride

JOURNAL OF APPLIED POLYMER SCIENCE, Issue 1 2008
Yolda
Abstract Chitosan-epichlorohydrin hydrogel films (ChitEPI) were synthesized by using chitosan in the presence of epichlorohydrin (EPI) as a crosslinking agent at various amounts. SEM, FTIR, TGA, and DSC analysis were conducted for the characterization of the hydrogels. The DSC measurements indicate that ChitEPI hydrogels did not exhibit better thermal stability when compared to chitosan. Swelling behavior of Chitosan-EPI hydrogel film is pH dependent and showed a reversible swelling behavior with a fast response. The hydrogels were used for in vitro release of promethazine hydrochloride (PHCl) in pH = 1.2 and pH = 7.4 phosphate buffer solutions (PBS). The release of PHCl synthesized from hydrogels at pH = 7.4 is quite low while at pH = 1.2, the highest value was observed as 49% for ChitEPI600. It has been also found that PHCl release from ChitEPI thin films is mainly controlled by diffusion control mechanism. ChitEPI hydrogels may be used for the delivery of drug in stomach and gastrointestinal tract. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008 [source]