Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate

Purpose: To develop and characterize solid dispersions of praziquantel (PZQ) with sodium starch glycolate (SSG) for enhanced drug solubility.Methods: PZQ solid dispersion (SD) was prepared using co-precipitation method by solvent evaporation. The ratios of PZQ to SSG were 2:1, 1:1, 1:2, 1:3 (w/w). PZQ solubility was evaluated in purified water, and PZQ dissolution test was carried out in 0.1N HCl. Structural characterization of the dispersions was accomplished by x-ray diffraction (XRD) and infrared spe ctroscopy (FTIR) while the external morphology of the SDs, SSG and PZQ were studied by scanning electron microscopy (SEM). Mucoadhesion properties of the SD (1:3) and SSG, on mucin disks were examined using texture profile analysis.Results: The highest solubility was obtained with 1:3 solid dispersion, with PZQ solubility of 97.31 %, which is 3.65-fold greater than the solubility of pure PZQ and physical misture (PM, 1:3). XRD results indicate a reduction in PZQ crystallinity while infrared spectra showed that the functional groups of PZQ and SSG were preserved. SEM showed that the physical structure of PZQ was modified from crystalline to amorphous. The amount of PZQ in PM and SD (1:3) that dissolved in 60 min was 70 and 88 %, respectively, and these values increased to 76 and 96 %, respectively. The solid dispersion reduced the mucoadhesive property of the glycolate.Conclusion: Solid dispersion formulation using SSG is a good alternative approach for increasing the dissolution rate of PZQ.Keywords: Praziquantel, Drug bioavailability, Schistosomiasis, Solid dispersion, Co-precipitation, Sodium starch glycolat

Preparation and Evaluation of Modified Release Zidovudine Tablets

Zidovudine is a drug used for the treatment of AIDS. The objective of this work was to prepare tablets for modified release of zidovudine. Hydroxypropyl methylcellulose HPMC K100LV and HPMC K4M at 1250 %, 18.75 % and 25.00 % were used. The tablets produced with 12.50 % of HPMC reached 100 % of the zidovudine release in 6 hours, while those produced with 18.75 and 25.00 %, released 24 h, following the Higuchi and First Order kinetic models, respectively. The calculated release exponent pointed out that formulations follow the anomalous type of release mechanism, with a combined phenomena of diffusion and erosion.3081512151

Intestinal absorption and physical chemical stability in fluconazole extemporaneous preparations

Fluconazole (FCZ) is synthetic antimycotic agent from azois group, with excellent bioavailability in body fluids and used for many treatments such as histoplasmoses, blastomycosis, and candidiasis. FCZ is considered the first chosen drug in the majority types of fungal meningitis. The objective of this work was to evaluate the physical-chemical characteristics of the FCZ in liquid pharmaceutical form and FCZ intestinal absorption in aqueous dispersion, in extemporaneous preparation. The FCZ intestinal absorption was evaluated through inverted intestinal sac and of the physical chemical stability through FCZ concentration in extemporaneous preparations. There is no quality guarantee in the extemporaneous preparation process, in the physical, chemical or biopharmaceutical view. The extemporaneous preparation were evaluated for 15 days and proved to be physically unstable. This may have influenced the FCZ intestinal absorption profile.26574474

Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Purpose: To develop and characterize solid dispersions of praziquantel (PZQ) with sodium starch glycolate (SSG) for enhanced drug solubility. Methods: PZQ solid dispersion (SD) was prepared using co-precipitation method by solvent evaporation. The ratios of PZQ to SSG were 2:1, 1:1, 1:2, 1:3 (w/w). PZQ solubility was evaluated in purified water, and PZQ dissolution test was carried out in 0.1N HCl. Structural characterization of the dispersions was accomplished by x-ray diffraction (XRD) and infrared spectroscopy (FTIR) while the external morphology of the SDs, SSG and PZQ were studied by scanning electron microscopy (SEM). Mucoadhesion properties of the SD (1:3) and SSG, on mucin disks were examined using texture profile analysis. Results: The highest solubility was obtained with 1:3 solid dispersion, with PZQ solubility of 97.31 %, which is 3.65-fold greater than the solubility of pure PZQ and physical misture (PM, 1:3). XRD results indicate a reduction in PZQ crystallinity while infrared spectra showed that the functional groups of PZQ and SSG were preserved. SEM showed that the physical structure of PZQ was modified from crystalline to amorphous. The amount of PZQ in PM and SD (1:3) that dissolved in 60 min was 70 and 88 %, respectively, and these values increased to 76 and 96 %, respectively. The solid dispersion reduced the mucoadhesive property of the glycolate. Conclusion: Solid dispersion formulation using SSG is a good alternative approach for increasing the dissolution rate of PZQ.122163168Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Sorocaba UniversityFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP

Nanoemulsions and nanoparticles for non-melanoma skin cancer: effects of lipid materials

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Basal cell carcinomas and squamous cell carcinomas are non-melanoma skin cancers reported to be among the most common malignancies, being responsible for high human morbidity. Conventional chemotherapy applied to these conditions shows non-specific targeting, thus severe adverse side effects are also commonly reported. New therapeutic strategies based on nanoparticulates technology have emerged as alternatives for site specific chemotherapy. Among the different types of nanoparticulates, lipid nanoemulsions and nanoparticles have several advantages for topical delivery of poorly soluble chemotherapeutics. These particles show sustained drug release and protection of loaded drugs from chemical degradation. This technology is promising to enhance the intracellular concentration of drugs and consequently reduce the cytotoxicity of skin chemotherapy.156417424Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP

Hemodynamic effects of a combination of bupropion and nicotine in anesthetized dogs

Bupropion has been used to treat psychic depression and as a therapy for smoking cessation, the latter mainly in association with nicotine. However, there have been no detailed studies of the hemodynamic effects of the association of bupropion with nicotine during replacement therapy. In this study, we evaluated the effects of such an association on the cardiovascular parameters in anesthetized dogs. Bupropion, either alone or together with nicotine, had no significant effect on the cardiac index (CI; 4.7 +/- 0.2 vs 4.3 +/- 0.1 and 3.5 +/- 0.3 vs 3.4 +/- 0.3 L.min(-1).m(2), respectively; mean +/- SEM) and mean arterial pressure (MAP; 134 +/- 5.0 vs 145 +/- 11.0 and 118 +/- 5.0 vs 133 +/- 10.5 mmHg, respectively). There was a slight but significant increase in the systemic vascular resistance index (SVRI; 2165 +/- 93 vs 2645 +/- 126 and 2335 +/- 100 vs 2737 +/- 200 dyn.cm(-5)m(-2), respectively). However, there was a significant increase in the mean pulmonary artery pressure (MPAP; 20 +/- 0.8 vs 25 +/- 1.6 and 18 +/- 1.3 vs 25 +/- 1.6 mmHg, respectively; p < 0.05) and pulmonary vascular resistance index (IRVP; 194 +/- 11 vs 272 +/- 21 and 206 +/- 32 vs 307 +/- 42 dyn.cm(-5)m(-2), respectively; p < 0.05). These results show that bupropion alone or in association with nicotine does not markedly affect most hemodynamic parameters of the systemic circulation, although the significant increase in MPAP and IRVP can elevate the pulmonary pressure.61636

In vitro evaluation of permeation, toxicity and effect of praziquantel-loaded solid lipid nanoparticles against Schistosoma mansoni as a strategy to improve efficacy of the schistosomiasis treatment

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Solid lipid nanoparticles (SLN) are a promising drug delivery system for oral administration of poorlywater soluble drugs because of their capacity to increase the solubility of drug molecules when loaded in their lipid matrices, with the resulting improvement of the drug bioavailability. In the present work, we have developed praziquantel (PZQ)-loaded SLN and explored the biological applications of this system for intestinal permeation of PZQQ. The effect in vitro on Schistosoma mansoni culture and the cytotoxicity in HepG2 line cell were also evaluated. The results showed a significant decrease in the intestinal absorption of PZQloaded in SLN compared to free PZQ, suggesting that the SLN matrix could act as reservoir system. In culture of S. mansoni, we observed that PZQ-loaded SLN were more effective than free PZQ, leading the death of the parasites in less time. The result was proportional to doses of PZQ (25 and 50 tig mL-1) and lipid concentration. Regarding cytotoxicity, the encapsulation of PZQinto SLN decreased the toxicity in HepG2 cells in comparison to the free PZQ. From the obtained results, PZQ-loaded SLN could be a new drug delivery system for the schistosomiasis treatment especially in marginalized communities, improving the therapeutic efficacy and reducing the toxic effects of PZQ. (C) 2014 Published by Elsevier B.V.46313137Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)European Union Funds [PTDC/SAUFAR/113100/2009, FCOMP-01-0124-FEDER-022696, PEstC/AGR/UI4033/2011]Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)FAPESP [SFRH/BD/60640/2009]European Union Funds [PTDC/SAUFAR/113100/2009, FCOMP-01-0124-FEDER-022696, PEstC/AGR/UI4033/2011

Perfil da assistência farmacêutica na atenção primária do Sistema Único de Saúde Pharmacist care in the Brazilian Primary Health Care System

Este artigo apresenta uma revisão e análise da assistência farmacêutica como parte integrante do sistema de atenção primária à saúde, no qual a qualidade do uso de medicamentos está diretamente relacionada à qualidade do serviço de saúde e aos elementos para a avaliação desta. As Unidades Básicas de Saúde constituem a principal porta de entrada do sistema de assistência à saúde estatal em nosso país. Entretanto, o vínculo do serviço farmacêutico está relacionado com o modelo curativo, centrado na consulta médica e pronto atendimento, com a farmácia apenas atendendo a essas demandas. A atividade de orientação aos usuários na farmácia das Unidades Básicas de Saúde torna-se praticamente impossível, pois na farmácia deságuam quase todas as mazelas do sistema de saúde, por estar no elo final do processo de atendimento. A solução do problema, no âmbito geral, não será simples, se mantida a forma como o serviço está estruturado, pois grande parte das pressões de demanda não depende do serviço de saúde em si, mas de políticas sociais inclusivas, as quais têm impacto direto nas condições de saúde da população. No âmbito específico, é fundamental que os gestores racionalizem a utilização dos medicamentos desde a prescrição até a utilização por parte do usuário.<br>This paper presents a review and analysis of Pharmacist Care as an integrated part of the Primary Health Care System, in which quality use of medicines is directly related to quality health service and to elements for its evaluation. In our country the Basic Health Units represent the main entrance to the public health care system. The pharmaceutical services however are still linked to the care model centered in medical consultation and emergency care, with the pharmacy just satisfying their needs. Provide orientation to the users of a Basic Unit pharmacy is almost impossible because nearly all sore spots of the health system end up at the pharmacy as the final step in the care process. The solution of the problem will not be easy if the present structure of the service is maintained. Great part of the pressure resulting from the demand does not depend on the health service itself but on inclusive social policies with direct impact on the health conditions of the population. Rational use of medicines from the prescriber to the user is fundamental in this specific environment