ABSTRACT Diabetes mellitus (DM) is a metabolic disorder that is marked by high blood glucose levels. Members of the Rosaceae family are a good source of antioxidants. Therefore, the current work sought to examine the potential for in-vitro alpha-amylase and alpha-glucosidase inhibition and the antidiabetic activity of Rosa brunonii L. fruit chloroform extract (RBFCE) against Alloxan (ALXN) induced diabetes in rats. RBFCE concentrations ranging from 20, 50, 100, 250, 500, and 750 g/mL were used in in-vitro activities, while oral doses of 500 mg/kg, 750 mg/kg, and 1000 mg/kg were given to rats in an in-vivo trial for 21 days. Isolation was carried out through column chromatography and modern spectroscopic techniques were used for characterization and structure elucidation. The isolated compound was identified as catechin. For alpha-amylase and alpha-glucosidase inhibition activity, RBFCE had IC50 values of 322.06±17.40 and 248.93±1.62, respectively. The IC50 values for acarbose against alpha-amylase and alpha-glucosidase inhibition were 64.64±3.70 and 67.60±4.20, respectively. RBFCE treatment regulated blood glucose levels dose-dependently over a 21-day study period. Histopathological studies revealed that RBFCE has recovered the damaged acinar structures to some extent in pancreatic tissue. Only focal tissue destruction observed. RBFCE treatment displayed normal glomeruli with no signs of inflammation, proliferation, necrosis, cipher of thyroidization and fibrosis. All the extract-treated groups had more protected pancreatic and kidney tissue than control group in dose-dependent manner. The current study results revealed that RBFCE had prominent alpha-amylase and alpha-glucosidase inhibition activity, regulates blood glucose level and normalize histopathological markers in diabetic rats compared to the negative control group.

Abstract Pregabalin, a GABA analogue is used to treat epilepsy and neuropathic pain. The drug poses problems in analytical quantification when estimated at a shorter UV wavelength. The expensive and non-repetitive reported analytical methods necessitate the utility and development of an accurate, precise, repetitive, simple and highly sensitive colorimetric method for pregabalin in solution as well as sustained release mini matrices. Pregabalin (having primary amino group) was derivatized at alkaline pH of mixture with optimized ninhydrin solution at ambient temperature (25oC). The ninhydrin-pregabalin derivatized complex (Ruhemann’s Purple) was analyzed for drug concentration at absorption maximum (λmax) of 570nm. The linearity was observed in the concentration range of 5-150 µg/mL with coefficient of correlation, 0.998. The developed analytical method was validated according to ICH guidelines and proved to be highly sensitive (LOD 0.917µg/mL, LOQ 3.055µg/mL), with good inter-day as well as intra-day accuracy and precision as 4.65% and 3.75%, respectively. The proposed method was proved to be a simple, sensitive, precise and accurate for the estimation of the minute concentrations of pregabalin in pure form and the developed formulations. Results verified that the proposed method could determine pregabalin at the ambient temperature without requiring high temperatures used in the existing methods. It was concluded that developed method was easier and more suitable for analysis of pregabalin in quality control of commercial preparations. pain wavelength nonrepetitive non repetitive matrices having group 25oC. 25oC oC . (25oC) ninhydrinpregabalin Ruhemanns Ruhemann s Purple λmax (λmax 570nm nm 5150 5 150 5-15 µgmL µg mL correlation 0998 0 998 0.998 LOD 0917µgmL 917µg 0.917µg/mL 3.055µg/mL, 3055µgmL 3.055µg/mL , 3 055µg 3.055µg/mL) interday inter day intraday intra 465 4 65 4.65 375 75 3.75% respectively formulations preparations (25oC 515 15 5-1 099 99 0.99 46 6 4.6 37 7 3.75 51 1 5- 09 9 0.9 4. 3.7 0. 3.

RESUMO O presente estudo descreve o desenvolvimento de microcápsulas de teofilina pelo método sem adição de solvente e o efeito da adição de plastificante na microencapsulação. A liberação foi estudada em água destilada e os dados foram analisados por vários modelos matemáticos para determinação do mecanismo de liberação. As microcápsulas preparadas mostraram-se esféricas, livres de corrente e com mais de 80% de fármaco encapsulado. O polímero - ftalato de acetato de celulose e o plastificante - polietileno glicol - afetaram as propriedades das microcápsulas, incluindo a liberação do fármaco (tempo para liberação de 50% do fármaco, T50). A formulação com a maior proporção de polímero e sem plastificante (F3) se mostrou como a de liberação mais lenta, com T50 = 4,3 h, enquanto as formulações com menor proporção de polímero e 20% de plastificante (m/m) (F13 &14) apresentaram a liberação mais rápida do fármaco, com T50 de 1,2 h e 1,3 h, respectivamente. A liberação do fármaco para a maioria das formulações seguiu o modelo de Higuchi. Concluiu-se, dos resultados do presente estudo, que o ftalato do acetato de celulose afeta significativamente a liberação controlada do fármaco em água, enquanto que a adição de polietileno glicol aumenta ligeiramente a liberação do fármaco.

ABSTRACT The present study describes the development of theophylline microcapsules by a non-solvent addition method and the effect of plasticizer addition on microencapsulation. The release was studied in distilled water and the data were analysed by various mathematical models for determining the mechanism of release. Prepared microcapsules were found to be spherical, free flowing and having more than 80% entrapped drug. The polymer - cellulose acetate phthalate and plasticizer - polyethylene glycol was considered to be affecting the properties of microcapsules including drug release (time for 50% drug release, T50). The formulation with the highest proportion of polymer and without plasticizer (F3) showed the slowest release with T50 = 4.3 h, while the formulation with lower proportion of polymer and 20% (w/w) plasticizer (F13 &14) showed the fastest release of drug with T50 values of 1.2 h and 1.3 h, respectively. The drug release from most of the formulations was found to be following Higuchi model. It is concluded from the results of the present study that cellulose acetate phthalate significantly affects the sustained release of the drug in water, whereas the addition of polyethylene glycol slightly enhances the drug release.