In vitro evaluation of domperidone mouth dissolving tablets.

In the present research work mouth dissolving tablets of domperidone were developed with superdisintegrants like crospovidone, croscarmellose sodium and sodium starch glycollate in various concentrations like 3%, 4% and 6% w/w by direct compression method. All formulations were evaluated for physical characteristics of compressed tablets such as weight variation, hardness, friability, content uniformity, in vitro disintegration time, wetting time and in vitro dissolution study. Among all, the formulation F3 (containing 6% w/w concentration of crospovidone) was considered to be the best formulation, having disintegration time of 9 s, wetting time of 15 s and in vitro drug release of 99.22% in 15 min.

Copper and ceruloplasmin levels in relation to total thiols and GST in type 2 diabetes mellitus patients.

Presence of oxidative stress in type 2 diabetes mellitus (DM) is well proved. Current study was undertaken to know the relation between fasting plasma glucose (FPG) and copper along with antioxidants like total thiols and ceruloplasmin, and antioxidant enzyme glutathione S transferase (GST). The study group consisted of a total of 201 subjects which included nondiabetic healthy control subjects (n = 78) and diabetic patients (n = 123). Plasma total thiols, GST, copper and ceruloplasmin levels were measured all the subjects using spectrophotometric methods and FPG levels were determined in clinical chemistry analyzer Hitachi 912. There was significant increase in FPG (P<0.001) and copper (P<0.001) and decrease in ceruloplasmin (P<0.001) and protein thiols (P<0.001) in type 2 DM cases compared to healthy controls. There was no significant change in GST between type 2 DM cases and controls. There was significant negative correlation of FPG with antioxidants like ceruloplasmin (r = -0.420, P<0.001) and total thiols (r = -0.565, P<0.001). Protein thiols correlated positively with ceruloplasmin (r = 0.364, P<0.001). Our study indicates possible increase in copper mediated generation of ROS leading to increased consumption of available antioxidants in the body.

Taste masking of Etoricoxib by using ion-exchange resin.

The present study was carried out in order to mask the bitter taste of the Etoricoxib by complexation with cation-exchange resin, Indion 204. The drug resin complexes (DRC) were prepared by batch process and efficient drug loading was obtained by using inactivated form of resin in the drug-resin ratio 1:3.3 with 30 min swelling time of resin in 25 mL of water with 5 min stirring time. Drug-resin complexes were characterized for dissolution studies and spectral studies. Drug release from drug-resin complex in salivary pH was insufficient to impart bitter taste. Volunteers rated the drug resin complex as tasteless and agreeable.

Therapeutic effect of ferulic acid, an ethereal fraction of ethanolic extract of seed of Syzygium cumini against streptozotocin-induced diabetes in male rat.

Diabetic therapeutic and antioxidative effects of an ethereal fraction of the ethanolic extract of the seed of Syzygium cumini was studied in streptozotocin (STZ)-induced diabetic rats. Diabetes resulted in a significant elevation in the fasting blood glucose level and in the activity of hepatic glucose-6-phosphatase. There was diminution in the levels of glycogen in the liver and skeletal muscle along with diminution in the activities of hepatic glucose-6-phosphate dehydrogenase, catalase and peroxidase in diabetic rats when compared with controls. Hepatic levels of thiobarbituric acid reactive substance (TBARS) and conjugated dienes (CD) were elevated in respect to control. Oral coadministration of the above fraction to diabetic rats resulted in significant protection in all these parameters. Histological studies of the pancreas showed a qualitative diminution in the area and volume of the islet's of Langerhans, but coadministration of the specific fraction resulted in a significant recovery of the islet's of Langerhans. Chromatography study revealed that the used fraction was ferulic acid (FA). Treatment with FA in normoglycemic rats did not show any significant change in the levels of the selected biosensors. The possible hypothesis for the therapeutic effect of FA against diabetes may be due to its pancreatic beta-cell regenerative effect and/or due to its antioxidant properties.

Formulation and evaluation of gelatin micropellets of aceclofenac: effect of process variables on encapsulation efficiency, particle size and drug release.

In the present study aceclofenac-gelatin micropellets were prepared by the cross linking technique using gluteraldehyde as cross linking agent and characterized by X-ray diffractometry, differential scanning calorimetry and scanning electron microscopy. The effect of drug: polymer ratio, temperature of oil phase, amount of gluteraldehyde and stirring time was studied with respect to entrapment efficiency, micropellet size and drug release characteristics. Spherical micropellets having an entrapment efficiency of 57% to 97% were obtained. Differential scanning calorimetric analysis confirmed the absence of any drug-polymer interaction. The micromeritic studies of micropellets show improved flow property. The entrapment efficiency, micropellet size and drug release profile was altered significantly by changing various processing parameters.

Determination of urinary peptides in patients with proteinuria.

Although considered useful in the diagnosis and prognosis of renal diseases, proteinuria can only be detected after significant renal paranchymal changes. There is considerable interest in the estimation of urinary peptides as an early marker of renal disease. In the current study, we have estimated urinary peptides in patients with different grades of proteinuria. Twenty-four hour urine samples were collected from 138 subjects and classified into three groups based on the urine protein excreted: group I (normoproteinuria, 0-150 mg/day, n = 37), group II (microproteinuria, 150-300 mg/day, n = 31), and group III (macroproteinuria, > 300 mg/day, n = 70). Urine proteins were determined using Bradford's method and urinary peptide levels were determined by subtracting Bradford's value from the Lowry value of the same sample. There was a significant decrease in the levels of urinary peptides in group III compared to group I (P < 0.01), however, there was no difference in peptides between groups I and II. The percentage of urinary peptides was decreased in both groups II and III compared to group I (P < 0.01), and there was a significant difference in % urinary peptide content in group II compared to group III (P < 0.01). On correlation, % urinary peptides correlated negatively with urinary proteins/g creatinine (r = - 0.782, P < 0.01) and positively with urinary peptides/g creatinine (r = 0.238, P < 0.01). Our data suggest that there is a marked decrease in urinary peptide levels with an increase in proteinuria. This may suggest impaired tubular protein reabsorption and degradation capacity of renal tubules.

Effect of processing temperature on Eudragit RS PO microsphere characteristics in the solvent evaporation process.

Eudragit RS PO microspheres containing stavudine as a model drug were prepared by the solvent evaporation method using acetone liquid paraffin system. The influence of processing temperature: 10, 30 and 40 degrees C on various parameters like particle shape, size distribution, drug loading, drug polymer interaction and release kinetic were studied. It was found that at lower temperature (10 degrees C) small particles of irregular size, rough and wrinkled surface were formed, whereas higher temperature gradually increases the particle size as well as improves the shape and smoothness of microspheres. It was found that temperature had no effect on encapsulation efficiency and drug polymer compatibility. Drug release rate from microspheres were found to be a function of mean particle size distribution.

Preparation and in vitro evaluation of ethyl cellulose microspheres containing stavudine by the double emulsion method.

The aim of this study was to formulate and evaluate microspheres of stavudine by water-in-oil-in-oil (w/o/o) double emulsion solvent diffusion method using ethyl cellulose and ethyl cellulose in combination with polyvinyl pyrrolidone. A mixed solvent system consisting of acetonitrile and dichloromethane in an 1: 1 ratio and light liquid paraffin was chosen as primary and secondary oil phase, respectively. Span 80 was used as surfactant for stabilizing the secondary oil phase. The influence of formulation factors like stirring speed, surfactant concentration on particle size and polymer:drug ratio and combination of polymers on drug release characteristics of the microspheres was investigated. The prepared microspheres characterized by micrometric properties, drug loading, Fourier transform infrared spectroscopy, X-ray powder difractometry and scanning electron microscopy. The prepared microspheres were white, free flowing and spherical in shape, stable in nature, with 41-65% of drug entrapment efficiency. The best-fit release kinetics was achieved with Higuchi plot followed by first order and zero order. The release of stavudine was influenced by the drug to polymer ratio, particle size and polymer combination.

Preparation and in vitro dissolution of isoniazid from ethylcellulose microcapsules.

Microcapsules of isoniazid were prepared by phase separation coacervation process induced by non-solvent addition and using ethylcellulose (EC) as coating polymer. When polyisobutylene (PIB)--a protective colloid was present at sufficient concentration, film coated drug particles were formed. At 0-6% PIB concentration, the microcapsules were aggregated. Increase of colloid concentration produced microcapsules of less aggregation and higher drug content because coating became progressively thinner. PIB concentration also controlled the particle size and the release rate of drug from microcapsules. Wall thickness and EC loss were calculated from drug content. Microcapsules coated with EC were prepared with 7-9% PIB. Scanning Electron Microscopy was used to study the nature of aggregation and coating behaviour. The in vitro dissolution study confirmed the first order release pattern and also the Higuchi Matrix model.