Characterization of venlafaxine hydrochloride and compatibility studies with pharmaceutical excipients

Bernardi, Luana; Oliveira, Paulo Renato de; Murakami, Fábio S.; Silva, M. A. S.; Borgmann, S. H. M.; Cardoso, Simone Gonçalves

doi:10.1007/s10973-009-0282-2

Cited by 41 publications

(11 citation statements)

References 20 publications

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“…Microcrystalline cellulose showed interaction with desloratadine [40], enalapril maleate [28], risperidone [41], but it was compatible with venlafaxine hydrochloride [19], sibutramine hydrochloride monohydrate [31], norfloxacin [32], and ketoprofen [42].…”

Section: Dsc Compatibility Studiesmentioning

confidence: 99%

“…The indepth characterization and understanding of the physicochemical interactions of an API in the dosage forms is an integral part of pre-formulation studies, during the development of a new pharmaceutical formulation. Although excipients are usually considered to be pharmacologically inert, they can interact with APIs and affect various aspects of the product, such as the organoleptic properties, dissolution, or drug degradation [16][17][18][19], impairing its stability and/or bioavailability. The assessment of API-excipient interactions could be considered to be even more critical for medicines which are candidates for the BE biowaiver, since they will not be submitted to in vivo studies.…”

Section: Introductionmentioning

confidence: 99%

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Fluconazole–excipient compatibility studies as the first step in the development of a formulation candidate for biowaiver

Teleginski

Maciel

Mendes

et al. 2014

J Therm Anal Calorim

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The biowaiver of bioequivalence studies on class I drugs of the biopharmaceutics classification system (BCS) is aimed mainly at reducing the costs and the exposure of health volunteers to a new pharmaceutical formulation. Fluconazole is an important antifungal agent but in the literature it is not clear whether it belongs to BCS class I or III. Compatibility studies are considered to be the first step in product development and on considering a biowaiver candidate these gain even greater importance since the final product will not be submitted to in vivo tests. The aim of this study was to qualitatively determine the composition of a commercially available fluconazole formulation in the form of capsules with regard to the presence of critical excipients and to carry out compatibility studies by differential scanning calorimetry (DSC). One formulation did not contain sodium lauryl sulfate and contained mannitol, in contrast to the reference formulation, which could hinder the acceptance of the biowaiver. The interaction of fluconazole with microcrystalline cellulose and calcium hydrogen phosphate dihydrate was observed; however, no indication of incompatibility was found in the DSC analysis of the commercial pharmaceutical formulations. These interactions were also studied by Fourier transform infrared spectroscopy, where small changes in the bands were observed, and by X-ray Powder diffraction and scanning electron microscopy that did not evidence any modification in the solid state characteristics.

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Section: Dsc Compatibility Studiesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Fluconazole–excipient compatibility studies as the first step in the development of a formulation candidate for biowaiver

Teleginski

Maciel

Mendes

et al. 2014

J Therm Anal Calorim

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“…DSC has been proposed to be a rapid method for evaluating physicochemical interactions between components of the formulation through the comparison of thermal curves of pure substances with the curve obtained from a 1:1 physical mixture and, therefore, select adequate excipients with suitable compatibility (18). The DSC thermogram of the drug gave a sharp melting endotherm at 212.87°C.…”

Section: Drug-excipients Compatibility Studiesmentioning

confidence: 99%

Optimization and In vivo Pharmacokinetic Study of a Novel Controlled Release Venlafaxine Hydrochloride Three-Layer Tablet

Aboelwafa

Basalious

2010

AAPS PharmSciTech

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Abstract. Several matrix tablet formulations (hydrophilic-based, wax-based, and three-layer tablets) were designed for controlling the release of the highly water soluble drug, venlafaxine hydrochloride (VenHCl) for once-daily administration. The three-layer tablets consist of non-swellable, compritol-based middle layers containing the drug to which hydrophilic top and bottom barrier layers were applied. A 2 3 full-factorial design was employed for optimization and to explore the effect of different variables on the release rate of the drug from the three-layer tablets. The optimized levels of each independent variable were based on the criterion of desirability. The calculated values of f 1 and f 2 were 4.131 and 79.356, respectively; indicating that the release profile of the optimized PEO layered tablet formulation is comparable to that of the target release model. The pharmacokinetic parameters of VenHCl from the optimized three-layer tablet was compared to the marketed extended release capsule as a reference in healthy human subjects using a randomized crossover design. In this study, the 90% confidence interval for AUC 0-24 and AUC 0−∞ are within (0.8-1.25), which satisfied the bioequivalence criteria. It could be concluded that a promising once-daily extended-release three-layer tablet of the highly water soluble drug, VenHCl, was successfully designed.

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“…DSC and related techniques widely contribute to the study of, e.g., the stability of drugs [31][32][33], their polymorphism [34], and drug-excipient compatibility or chemical interactions [35][36][37].…”

Section: Introductionmentioning

confidence: 99%

Phase diagram and dissolution studies of the fenofibrate–acetylsalicylic acid system

Gòrniak

Wojakowska

Karolewicz

et al. 2010

J Therm Anal Calorim

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Enhancement of the dissolution rate of poorly soluble compounds through the formation of drug-drug eutectics was investigated using fenofibrate and acetylsalicylic acid. Solid-liquid equilibria in the system under study were investigated by differential scanning calorimetry (DSC). The phase diagram for the whole range of compositions was constructed. In addition, existence of a metastable polymorph of fenofibrate has been confirmed. The investigation has revealed that acetylsalicylic acid and fenofibrate form a simple eutectic mixture containing 0.958 mol fraction of fenofibrate at the eutectic point. Dissolution rate improvement of fenofibrate correlated with the phase diagram. The amount of fenofibrate released from the solid dispersions that contained fenofibrate as the eutectic mixture with acetylsalicylic acid was at least threefold higher compared to untreated fenofibrate.

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Characterization of venlafaxine hydrochloride and compatibility studies with pharmaceutical excipients

Cited by 41 publications

References 20 publications

Fluconazole–excipient compatibility studies as the first step in the development of a formulation candidate for biowaiver

Fluconazole–excipient compatibility studies as the first step in the development of a formulation candidate for biowaiver

Optimization and In vivo Pharmacokinetic Study of a Novel Controlled Release Venlafaxine Hydrochloride Three-Layer Tablet

Phase diagram and dissolution studies of the fenofibrate–acetylsalicylic acid system

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