Hydrochlorothiazide is a common diuretic antihypertensive drug of the thiazide family. Its poor aqueous solubility is one of the reasons for its limited bioavailability after oral administration. This work aimed at the development of a hydrochlorothiazide:β-cyclodextrin (HTZ:β-CD) pharmaceutical composition in order to improve water solubility and bioavailability of the drug. The HTZ:β-CD complexes were prepared by three different methods: spray-drying, freeze-drying and fluid bed. Complexes were characterized by thermal analysis, Fourier transform-infrared (FTIR) spectroscopy, powder X-ray diffractometry, NMR (2D-ROESY), scanning electron microscopy (SEM), particle analysis and intrinsic dissolution. The findings reveal that three binary systems prepared presented better solubility results in comparison with free HTZ. Increased diuretic effect was observed to HTZ:β-CD obtained by fluid bed in comparison to free drug in rats. Results taken together suggest that pharmacological effect of HTZ in complex was increased by solubility improvement promoted by cyclodextrin.
In attempts to design delayed-release tablets of diclofenac sodium, seven experimental batches were produced. The influence of super-disintegrant croscarmellose sodium (CCS), the granulation process, and the thickness of Eudragit L 100 coating film were evaluated. The values of dissolution efficiency and the similarity factor were used to compare the dissolution profiles of each experimental batch and the reference Voltaren. Both methods appear to be applicable and useful in comparing dissolution profiles. Based on such values four batches were considered similar when contrasted with the reference. The results suggest an optimal relationship between the amount of CCS and the thickness of the coating film, which provides appropriate dissolution rate of diclofenac sodium from the dosage forms.
A glibenclamida (GLIB)
INTRODUÇÃOO diabetes mellitus (DM) é uma doença crônica, herdada ou adquirida, que atinge todas as faixas etárias. É causada pela deficiência ou ineficiência na produção de insulina pelo pâncreas e pode ser classificada, clinicamente, como tipo I ou tipo II, sendo que o último prevalece em 90% dos casos (WHO, 2002).O DM é um sério problema de saúde pública em praticamente todos os países e implica em elevado impacto sócioeconômico. Além dos elevados custos envolvidos no controle da doença e tratamento das complicações agudas e crônicas associadas, leva à incapacidade física permanente por cegueira e/ou amputação de membros e modifica a qualidade e a expectativa de vida do indivíduo. Até 2025, estima-se que 300 milhões de pessoas possuam a doença em todo o mundo (AHFS, 2000; WHO, 2002).Em 1998, o DM foi a sétima causa de morte no Brasil. Em 2001, a Campanha Nacional de Detecção de Diabetes rastreou, pela primeira vez no país, os suspeitos do diabetes. De 20,23 milhões de pessoas examinadas, 14,67% apresentaram suspeita da doença.
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