Journal of Young Pharmacists

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The present study evaluated the antihyperglycemic, hepatoprotective, and hypolipidemic effects of F. racemosa bark powder and aqueous extract in streptozotocin-induced diabetic rats. Streptozotocin-induced diabetic rats ( n = 6) were treated with F. racemosa Linn (Moraceae) bark powder (FRP) and aqueous extract (FRAE) for six weeks. Blood glucose was determined every 15 days using a portable glucometer. At the end of the study period, the rats were sacrificed and levels of serum glucose, protein, total cholesterol, triglycerides, AST, ALT, TBARS, and glutathione were determined as indicators of antihyperglycemic, hypolipidemic, and hepatoprotective activities, as well as of antioxidant potential. TBARS and glutathione levels were determined in the liver and the kidneys also. Both the bark powder and aqueous extract of F. racemosa bark caused a significant reduction ( P ≤ 0.05) in blood glucose (54 and 66% respectively). A significant reduction ( P ≤ 0.05) was also observed in serum cholesterol and triglyceride levels to the control levels. The aqueous extract was more effective and caused a significant reduction ( P ≤ 0.05) in TBARS, AST, ALT levels compared to untreated diabetic rats. However, it did not reach control levels. A significant increase in glutathione concentrations over the control levels was also observed in rats treated with F. racemosa bark. It is concluded that F. racemosa bark has a significant hypolipidemic and hepatoprotective effect besides being a potent antihyperglycemic agent.

The aim of the present investigation was to develop sustained release ethylcellulose-coated egg albumin microspheres of diltiazem hydrochloride (DH) to improve patient compliance. The microspheres were prepared by the w/o emulsion thermal cross-linking method using different proportion of the polymer to drug ratio (1.0:1.0, 1.0:1.5 and 1.0:2.0). A 3² full factorial design was employed to optimize two independent variables, polymer to drug ratio (X1 ) and surfactant concentration (X2 ) on dependent variables, namely % drug loading, % drug release in 60 min (Y60 ) and the time required for 80 % drug release (t80 ) were selected as dependable variable. Optimized formulation was compared to its sustained release tablet available in market. The polymer to drug ratio was optimized to 1:1 at which a high drug entrapment efficiency 79.20% ± 0.7% and the geometric mean diameter 47.30 ± 1.5 mm were found. All batches showed a biphasic release pattern; initial burst release effect (55% DH in 1 h) and then were released completely within 6 h. In situ coating of optimized egg albumin DH microspheres using 7.5% ethylcellulose significantly reduced the burst effect and provided a slow release of DH for 8-10 h. Finally, it was concluded that ethylcellulose-coated egg albumin DH microspheres is suitable for oral SR devices in the treatment of angina pectoris, cardiac arrhythmias, and hypertension due to their size and release profile.

The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating sustained release microspheres of Glipizide. An anti-diabetic drug, Glipizide, is delivered through the microparticulate system using ethyl cellulose as the controlled release polymer. Microspheres were developed by the emulsion solvent diffusion-evaporation technique by using the modified ethanol,-dichloromethane co-solvent system. The polymer mixture of ethyl cellulose and Eudragit^® S100 was used in different ratios (1:0, 1:1, 2:3, 1:4 and 0:1) to formulate batches F1 to F5. The resulting microspheres were evaluated for particle size, densities, flow properties, morphology, recovery yield, drug content, and in vitro drug release behavior. The formulated microspheres were discrete, spherical with relatively smooth surface, and with good flow properties. Among different formulations, the fabricated microspheres of batch F3 had shown the optimum percent drug encapsulation of microspheres and the sustained release of the Glipizide for about 12 h. Release pattern of Glipizide from microspheres of batch F3 followed Korsmeyers-peppas model and zero-order release kinetic model. The value of 'n' was found to be 0.960, which indicates that the drug release was followed by anomalous (non-fickian) diffusion. The data obtained thus suggest that a microparticulate system can be successfully designed for sustained delivery of Glipizide and to improve dosage form characteristics for easy formulation.

The use of medicinal plants with therapeutics properties represents a secular tradition in different cultures, mainly in underdeveloped countries. Lantana camara Linn and Lantana montevidensis Briq (Verbenaceae) found in tropical and subtropical areas around the world are popularly known as "camará" or "chumbinho." In popular medicines, both plants are used as antipyretic and carminative and in the treatment of respiratory system infections. In this study, the antibacterial activity of the ethanolic extracts of L. camara and L. montevidensis leaves and roots against gram-positive and gram-negative strains standard and multi-resistant bacteria isolated from clinical material are presented. In order to determine the minimal inhibitory concentration (MIC), the microdilution method was used. The extracts demonstrated antibacterial activity against all tested bacteria, but the L. montevidensis fresh leaves extract present the best result against P. aeruginosa (MIC 8 µg/mL) and against multi-resistant E. coli (Ec 27) (MIC 16 µg/mL). These results drive new researches with both species in order to isolate the constituents responsible for the activity.

Stephania hernandifolia (Menispermaceae) is a medicinal plant, used by herbalists for treating various diseases, one of which is diabetes mellitus, in Darjeeling. However, its antidiabetic activity has not been scientifically investigated so far. The aim of this study, therefore, is to investigate the antidiabetic and antioxidant potential of the powdered corm of Stephania hernandifolia. This was tested in normal and Streptozotocin (STZ)-induced diabetic rats, using oral administration of ethanol and an aqueous extract (400 mg/kg body weight) of Stephania hernandifolia corm. After the oral administration of water and ethanol extracts at doses of 400 mg/kg body weight, blood glucose levels were monitored at specific intervals and it was found that they were significant lowered. Glibenclamide was used as a standard drug at a dose of 0.25 mg/kg. The experimental data revealed that both extracts has significant antihyperglycemic and antioxidant activity in Streptozotocin-induced rats compared to the standard drug. The antioxidant activity in vitro was measured by means of the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and Superoxide-free radical scavenging assay. Ascorbic acid, a natural antioxidant, was used as a control. The extracts of ethanol and aqueous were strongly scavenged DPPH radicals, with IC ₅₀ being 265.33 and 217.90 μg/ml, respectively. Although the extracts of ethanol and aqueous were moderately scavenged, the superoxide radical were with IC ₅₀ values of 526.87 and 440.89 μg/ml. The study revealed that the ethanolic extract exhibited more significant antidiabetic and antioxidant activity then the aqueous extract.

The aim of this study was to design, synthesize, and investigate the in vivo anti-inflammatory activity of some novel 2, 5-disubstituted - 1, 3, 4-oxadiazole derivatives. Ethyl-4-acetamido phenoxy acetate (I) was prepared by the condensation of ethyl chloroacetate with starting material p-acetamidophenol in the presence of dry acetone and anhydrous potassium carbonate. Hydrazinolysis of (I) with hydrazine hydrate results in the formation of 4-acetamidophenoxy acetyl hydrazide (II), which on cyclisation with various substituted aromatic carboxylic acids in the presence of phosphorous oxychloride affords various 2, 5-disubstituted - 1, 3, 4-oxadiazole derivatives (IIIa-IIIi). The newly synthesized compounds were characterized by IR, ¹ HNMR, and MS spectral data. The titled compounds were screened for in vivo anti- inflammatory activity using the carrageenan-induced paw edema method. A few of them manifested promising activity when compared with the standard drug Diclofenac sodium.