Development, physicochemical evaluation, and in vivo permeation studies of topical formulations containing 0.1% tacrolimus

Abstract The objective of this paper was to develop and evaluate two semi-solid pharmaceutical forms containing 0.1% tacrolimus: cream (CRT01) and gel (GLT01). For the evaluation of physicochemical stability, at times 0, 30, 60 and 90 days, at 23°C and at 40°C, High Performance Liquid Chromatography coupled with a Diode Array Detector (HPLC-DAD) was employed. This method was developed and validated for tacrolimus quantification. The occlusivity test and skin permeation assay were also performed, using an animal model (Wistar rats), and the CRT01 and GLT01 were compared to the 0.1% tacrolimus ointment (PFU01) obtained from the University Pharmacy, Federal University of Rio de Janeiro, Brazil. CRT01 and GLT01 presented a homogeneous aspect and consistency adequate for topical products, along with sensory characteristics above PFU01. They also presented adequate physicochemical stability for 90 days and a lower occlusive effect than PFU01 (p<0.05). CRT01 showed greater affinity for the skin when compared to PFU01 and GLT01, with low systemic absorption. The CRT01 semi-solid formulation was considered the most adequate one to treat patients with atopic dermatitis or other dermatologic inflammatory diseases, promoting rational use of tacrolimus

Mupirocin ointments: In vitro x In vivo bioequivalence evaluation

Abstract Bioequivalence (BE) assessment of topical drug products is a long-standing challenge. Agencies such as the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have published several drafts in recent years suggesting different approaches as alternative to evaluate the BE. A proposed Topical Classification System (TCS) has even been discussed. Given the above, the objective of this research was to use in vitro and in vivo BE approaches to evaluate Brazilian marketed mupirocin (MPC) ointments, previously classified as TCS class The in vitro permeation test (IVPT) was performed by applying formulations to pig skin by Franz cells. The in vivo methodology was dermatopharmacokinetic (DPK). These approaches (in vivo tape stripping and IVPT) demonstrated capability of distinguishing among different formulations, thus making them useful methodologies for BE evaluation.

Study of Fluconazole Release from O/W Cream and Water Soluble Ointment Bases.

Aims: Study the release of fluconazole from different O/W creams and PEG ointments. Study Design: In this study, different formulations were prepared with changing one of the added excipients and study the effect of this change on the drug release and then the selected formulations were subjected to antifungal activity study. Place and Duration of Study: Faculty of Pharmacy, Department of Pharmaceutics, Assiut University, Assiut, Egypt, between December 2011 and March 2012. Methodology: O/W creams were prepared with changing either fatty alcohol type or the concentration of the added emulsifying agent. Also, the PEG ointments were prepared with changing the type of the liquid PEG (low molecular weight). Then, the viscosity and the fluconazole release from the prepared formulations were studied. Results: Changing the fatty alcohol type from stearyl to cetostearyl and cetyl alcohol in the O/W creams caused an increase in the viscosity and a decrease in the drug release. Also, changing the liquid PEG from PEG 400 to PEG 600 resulted in an increase in the formulation viscosity and subsequent decrease in the drug release. Both F1 and F6 showed a good inhibition to the fungal growth against Candida albicans and Trichophyton mentagrophyte using cup plate method, also PEG base showed a slight fungal growth inhibition. Conclusion: Results obtained showed that the PEG ointment formulations exhibited higher fluconazole release after three hours over the O/W cream formulations. Also, the nature of the PEG base may be adjunctive to the efficacy of the antifungal agent.

Wound-healing evaluation of ointment from Stryphnodendron adstringens (barbatimão) in rat skin / Avaliação da cicatrização da pomada de Stryphnodendron adstringens (barbatimão) na pele de rato

This study evaluated the cicatrizant effect of an ointment containing 1 percent of the ethyl-acetate fraction extracted from the stem bark of "barbatimão" (Stryphnodendron adstringens), in wounds made in the skin of rats, after 4, 7 and 10 days of treatment. Control wounds were treated with a base ointment without extract. The proliferation of keratinocytes in the area of reepithelialization was evaluated by counting the number of epithelial cells that were blocked in metaphase by vincristine sulfate. The length of the reepithelialized margin and the contraction of the wound were measured. Topical application of the "barbatimão" ointment stimulated proliferation of the keratinocytes, but had no effect on the length of the epithelium or on the contraction of the wounds.

Neste estudo, avaliou-se a atividade cicatrizante de uma pomada contendo uma fração acetato de etila 1 por cento obtida de cascas de "barbatimão" (Stryphnodendron adstringens) em feridas excisionais na pele de ratos após 4, 7 e 10 dias de tratamento. Feridas controle foram tratadas com pomada base, sem extrato. A proliferação dos queratinócitos na área reepitelizada foi avaliada através da contagem do número de queratinócitos bloqueados em metáfase, pelo sulfato de vincristina. O comprimento da margem reepitelizada e a contração das feridas foram mensurados. As feridas tratadas com barbatimão apresentaram um maior número de mitoses do que aquelas tratadas com a pomada base, em todos os tempos avaliados. A aplicação tópica da pomada de "barbatimão" estimulou a proliferação epitelial contudo não teve efeito sobre a migração dos queratinócitos ou sobre a contração das feridas.

Análise química de pastas de hidróxido de cálcio, frente à liberaçäo de íons cálcio, de íons hidroxila e formaçäo de carbonato de cálcio, na presença de tecido conjuntivo de cäo / Chemical analysis of calcium hydroxide paste, through the comparation of calcium and hydroxyl ions, and the formation of calcium carbonate, in the presence of connective tissue of the dog

A presente pesquisa teve como objetivo analisar quimicamente, pastas de hidróxido de cálcio acrescidas a três veículos hidrossolúveis e com características ácido-base diferentes (soro fisiológico, soluçäo anestésica e Polietileno Glicol 400) mediante o implante de tubos de polietileno no tecido conjuntivo subcutâneo de cäo, avaliando a liberaçäo de íons cálcio, de íons hidroxila e a formaçäo de carbonato de cálcio, em períodos de 7, 30, 45 e 60 dias. Para tanto, a análise química dos íons cálcio liberados foi feita por meio da titulaçäo condutimétrica, tendo como complexante o EDTA. A determinaçäo da liberaçäo de íons hidroxila foi obtido por analogia aos íons cálcio liberados, levando em conta o peso molecular do hidróxido de cálcio e a partir de uma regra de três. A determinaçäo da formaçäo de carbonato de cálcio foi avaliada por volumetria de neutralizaçäo com emprego do ácido clorídrico como titulante

Bases dermatológicas utilizadas en preparados magistrales para ácne y rosácea / Dermatological vehicles utilized in masterly preparations for acne and rosacea

Las bases dermatológicas son preparaciones semisólidas que están destinadas a la aplicación de medicamentos en forma externa. La prescripcón de recetas magistrales permite a los dermatológos individulaizar en forma adecuada las terapias de sus pacientes. Las bases pueden ser clasificadas según su composición en: bases oleaginosas, bases de absorción, emulsiones (aceite/agua, agua/aceite), bases hidrosolubles y geles. Por su bajo o nulo contenido en materia grasa, las bases más indicadas en acné o rosácea son las emulsiones de aceite en agua, las bases hidrosolubles, elaboradas con polietilenglicoles, y los geles. Es importante tener presente la posibilidad de interacciones o incompatibilidades entre diversos principios activos y las bases

Identificaçäo de óleos essenciais ou seus componentes isolados em produtos farmacêuticos. Parte I - Pomadas e supositórios / Identification of essential oils or isolated compounds in pharmaceutical preparations. Part I - Ointment and suppository

Oleos essenciais ou seus componentes isolados foram identificados em preparaçöes farmacêuticas semi-sólidas por cromatografia em camada delgada

Determinación cualitativa y cuantitativa de lidocaína clorhidrato en una crema para uso en estomatología / Qualitative and quantitative determination of lidocaine hydrochloride in a cream for use in stomatology

Se describe un método para el control de calidad de la anestesia tópica, crema hidrosoluble, para uso en Estomatología. Se detallan las identificaciones de distintos grupos funcionales en la molécula de clorhidrato de lidocaína, y se caracteriza la melécula por espectrofotometría ultravioleta (UV) en medio de ácido clorhídrico 0,1 N, comparando el espectro de absorción de la lidocaína presente en la muestra con una sustancia de referencia previamente estandarizada. En el máximo de absorción a 263 nm se comprobó la conformidad con la ley de Beer, determinando el valor de la extinción específica. Se valoró el clorhidrato de lidocaína en el máximo de absorción a 263 nm en la concentración de 400 *g/mL. Se valoró también por anhidrovolumetría con indicación visual, comparando las recuperadas obtenidas por los distintos métodos