In Vitro Antibacterial Evaluation of Terminalia chebula as an Alternative of Antibiotics against Bovine Subclinical Mastitis.

The extent of subclinical mastitis in three breeds of cattle, Kankrej, Gir, and Crossbred, was performed at cattle farms in Anand town of Gujarat State, India. The prevalence of subclinical mastitis in crossbred cattle was higher compared to local breed of cattle. Causative agents identified using 16S rDNA polymerase chain reaction (PCR)-based molecular method were Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Bacillus megaterium. In vitro antibacterial activity of ethyl acetate extract of plant Terminalia chebula (Combretaceae) was checked by agar well diffusion method against four isolated and molecularly identified microorganisms. Ethyl acetate extract shows antimicrobial activity with varying magnitudes against all identified isolates. Among the three different concentrations, 500 µg/mL conc. of extract is as effective as that of standard amoxicillin. In vitro results support the use of plant extract from T. chebula as an alternative to antibiotics therapy against bovine subclinical mastitis.

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route.

The problem of inadequate oral bioavailability of Quetiapine Fumarate, a lipophilic drug used for schizophrenia, due to hepatic metabolism and repulsion by brain barrier was attempted in this study. Combination of two approaches, viz. Quetiapine inclusion into the liposomal carrier for better diffusion and administration through nasal route to avoid hepatic metabolism and barrier elimination was applied. Thin film hydration followed by sonication method was employed in liposome preparation and the formulation was optimized using 32 full factorial design. The number of sonication cycles (X1) of 2 min and 80% amplitude and molar ratio of constructional components such as cholesterol to egg phosphatidylcholine (X2) as independent variables and a % of entrapment efficiency (Y1) and cumulative in vitro drug release (Y2) at 6 h as dependent variables was selected. Batch F7 prepared by 2 cycles of sonication and 1:3 M ratio of cholesterol:egg phosphatidylcholine was optimized as a consequence of substantial entrapment efficiency of 75.63 ± 3.77%, and 99.92 ± 1.88% drug release and 32.33 ± 1.53% drug diffusion, which was optimum among all other batches at 6 h. Diffusion study was done for all the batches of liposomal formulation by using sheep nasal mucosa and good amount with better diffusion rate was measured which proved liposomal dispersion a virtuous delivery system for brain drug delivery through nasal route. Results of in vivo, ciliotoxicity and gamma scintigraphy studies on mice supported the above inference.

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability.

A novel cationic nanoemulsified in-situ ophthalmic gel of loteprednol etabonate (LE) was developed to improve the permeability and retention time of formulations for overall improvement of drug's ocular bioavability. Capryol 90 (oil phase), tween 80 (surfactant) and transcutol P (cosurfactant) was selected as formulation excipients to construct pseudoternary phase diagrams and nanoemulsion region was recognized from diagrams. Spontaneous emulsification method was used to manufacture LE nanoemulsion and it was optimized using 32 factorial design by considering the amount of oil and the ratio of surfactant to cosurfactant (Smix) as independent variables and evaluated for various physicochemical properties. Optimized NE was dispersed in Poloxamer 407 and 188 solution to form nanoemulsified sols that were predictable to transform into in-situ gels at corneal temperature. Drug pharmacokinetics of sterilized optimized in situ NE gel, NE-ISG2 [0.69% w/w Capryol 90, 0.99%w/w Smix (3:1), 13% Poloxamer 407, 4% w/w Poloxamer 188] and marketed formulation were assessed in rabbit aqueous humor. The in-situ gels were clear, shear thinning in nature and displayed zero-order drug release kinetics. NE-ISG2 showed the minimum ocular irritation potential and significantly (p < 0.01) higher Cmax and AUC(0-10 h), delayed Tmax, extended mean residence time and improved (2.54-fold times) bioavailability compared to marketed formulation.

Mitigation of acrylamide by l-asparaginase from Bacillus subtilis KDPS1 and analysis of degradation products by HPLC and HPTLC.

The use of bacterial l-asparaginase (LA) is one of the alternative approaches for acrylamide reduction in food stuffs as it catalyzes the conversion of l-asparagine to l-aspartic acid and ammonia. In present investigation, purification of extracellular LA from isolate of Bacillus subtilis sp. strain KDPS-1 was carried out by solid state fermentation process. The effects of solid substrates, initial moisture content, moistening agents, temperature, and incubation time on LA production was studied, and the highest asparaginase activity (47 IU/ml) was achieved in the medium having orange peel as substrate. The enzyme was purified to homogeneity by diethylaminoethyl (DEAE) cellulose ion exchange chromatography; with 84.89 % yield and 12.11 fold purity. LA showed stimulant activity against ß-mercaptoethanol and was greatly inhibited by Zn(2+) and Hg(2+) metal ions. Reduction of acrylamide in fried potatoes was detected by high performance liquid chromatography, which showed clear degradation of acrylamide by height and area (%) in the chromatograms of standard sample to that of the test sample. Hydrolysates analysis by high performance thin layer chromatography confirmed the test sample to be LA.

A novel alkaline keratinase from Bacillus subtilis DP1 with potential utility in cosmetic formulation.

The Bacillus subtilis DP1 was isolated from poultry farm soil at Anand district, India. The highest enzyme production (379.65U/ml) was obtained at pH 10.0, a temperature of 37°C and a growth period of 72h. The extracellular keratinase was purified by gel filtration chromatography with 27.98 purification fold. Purity was also confirmed by High-Performance Liquid Chromatography (HPLC) analysis, where a major peak having retention time of 2.5min was obtained on C18 column using photo diode array detector. Purified keratinase was stable in a broad range of pH (8-12) and temperature (20-50°C) with optimum at pH 10.0 and 37°C. The metallic ions, Ca(2+) and Mg(2+) enhance keratinase activity. Secondary structure from Circular Dichroism (CD) spectra implies that purified keratinase is largely ß-pleated sheet rich protein. For preparation of dehairing cream formulation, compatibility studies of excipients were carried out. Fourier transform infrared spectroscopy (FTIR) spectra of sodium stearate, calcium carbonate and sodium lauryl sulphate shows no reactivity of functional groups and hence mixture was compatible for formulation of keratinase dehairing cream. Prepared biological depilatory was able to remove hair more efficiently compared to marketed formulations.

Ficus recemosa bark extract attenuates diabetic complications and oxidative stress in STZ-induced diabetic rats.

Context Ficus recemosa Linn. (Moraceae) has been reported as a natural folk medicine with diverse pathological activities such as antioxidant, antidiabetic, renoprotective and cardioprotective. Objective The present study evaluates the preventive effect of standardised ethanol extract of F. racemosa stem bark (EEFSB) on diabetic cardiomyopathy (DC) and diabetic nephropathy (DN). Materials and methods Animals were rendered diabetic by one time administration of STZ (45 mg kg(-1), i.v.) and, after 7 d, diabetic rats were randomised into four groups of eight rats each. EEFSB (200 and 400 mg kg(-1)) was administered to diabetic rats once daily for 8 weeks. Furthermore, the presence of phytochemicals was evaluated by HPTLC. Results Treatment with EEFSB markedly restores the blood glucose and lipid level (p < 0.001), also reduced creatinine kinase (p < 0.001), lactate dehydrogenase (p < 0.001), C-reactive protein (p < 0.001), creatinine (p < 0.001), blood urea nitrogen (p < 0.001), collagen (p < 0.05) and albumin (p < 0.001) levels. Reduced level of sodium (p < 0.001), creatinine (p < 0.001), albumin (p < 0.001) and malondialdehyde (p < 0.01) in heart and kidney tissue along with enhanced activities of superoxide dismutase (p < 0.001) and reduced glutathione (p < 0.001). Moreover, left ventricular hypertrophic index and cardiac hypertrophic index were markedly reduced by EEFSB treatment. Conclusion The findings of this study provided strong scientific evidence for the traditional use of F. racemosa and postulate protective effects against diabetes and its complications such as DC and DN.

Comparative study between simple and optimized liposomal dispersion of quetiapine fumarate for diffusion through nasal route.

CONTEXT: Nasal route of drug administration is preferred more and more for the targeted delivery to the brain in current drug development scenario due to its ease of use, reliability, quick action, and lesser side effects. Those CNS drugs which have limited oral bioavailability due to pharmacokinetic consequences and brain barrier repulsion are getting onto this direction. OBJECTIVE: Quetiapine fumarate, an analogous to above and an antischizophrenic agent, is tested for its diffusion property with and without lipophilic carrier through sheep nasal membrane. Being a BCS class II' and high permeable candidate, it tends to crossover easily, so made up in a simple dispersion. MATERIALS AND METHODS: To improve its diffusion rate, it was embedded into liposomal dispersion, which has proven that it has advanced efficiency for diffusion. For this, both the formulations were checked and compared for their diffusion profile, as it is an essential property for bioavailability through nasal route. Comparison was made on the basis of % drug diffusion within 6 h, rate, mechanism, profile, and coefficient. RESULTS: Liposomal dispersion has been proved superior with greater percentage diffusion of 32.61 ± 1.70 and very high permeability with a coefficient value of 4.1334 ± 0.7321 (× 10 (-) (5 )cm/s). Diffusion profile comparison bearing dissimilarity of 18 and similarity of 74 indicated that the diffusion profiles of liposomal dispersions and simple dispersion were similar but not identical. CONCLUSION: Liposomal diffusion supremacy was further sustained by in vivo, ciliotoxicity, and gamma scintigraphy studies.

Dissolution enhancement of chlorzoxazone using cogrinding technique.

PURPOSE: The aim of the present work was to improve rate of dissolution and processing parameters of BCS class II drug, chlorzoxazone using cogrinding technique in the presence of different excipients as a carrier. MATERIALS AND METHODS: The drug was coground with various carriers like polyethylene glycol (PEG 4000), hydroxypropyl methylcellulose (HPMC) E50LV, polyvinylpyrrolidone (PVP)K30, Kaolin and Neusilin US2 using ball mill, where only PEG 4000 improved dissolution rate of drug by bringing amorphization in 1:3 ratio. The coground mixture after 3 and 6 h was evaluated for various analytical, physicochemical and mechanical parameters. RESULTS: The analysis showed conversion of Chlorzoxazone from its crystalline to amorphization form upon grinding with PEG 4000. Coground mixture as well as its directly compressed tablet showed 2.5-fold increment in the dissolution rate compared with pure drug. Directly compressible tablets prepared from pure drug required a large quantity of microcrystalline cellulose (MCC) during compression. The coground mixture and formulation was found stable in nature even after storage (40°C/75% relative humidity). CONCLUSIONS: Cogrinding can be successfully utilized to improve the rate of dissolution of poorly water soluble drugs and hence bioavailability.

Screening of flavonoids rich fractions of three Indian medicinal plants used for the management of liver diseases

ABSTRACTThe decoctions of the Butea monosperma (Lam.) Taub., Fabaceae, Bauhinia variegata L., Fabaceae, and Ocimum gratissimum L., Lamiaceae, are traditionally used for the treatment of various types of hepatic disorder. Phytochemical studies have shown that total flavonoids from these plants were the major constituents of the picked out part of each plant. The present study was planned to investigate the hepatoprotective effect of flavonoid rich fractions of the B. monosperma, B. variegata and O. gratissimum against paracetamol induced liver damage. Flavonoid rich fractions were isolated by solvent fractionation from each plant. Each fraction was subjected to various qualitative chemical tests to findout the metabolites. Flavonoid fractions of each plant were subjected for pharmacological screening. The rats were monitored for change in liver morphology, biochemical parameters like serum glutamate pyruvate transaminase, serum glutamate oxaloacetate transaminase, alkaline phosphatase and total bilirubin for the groups receiving the flavonoid-rich fractions. All flavonoid rich fractions showed significant hepatoprotective activity. The histological studies supported the biochemical parameters. From the results of biochemical analysis and histopathological studies, it can be accomplished that in the ethyl acetate fraction of O. gratissimum showed highest hepatoprotective activity as compared to other fractions. The present study was the first evidence of flavonoid-rich fractions of each plant have a remarkable hepatoprotective effect. All fractions contain a potent hepatoprotective agent suggested to be a flavone, which may find clinical application in amelioration of paracetamol-induced liver damage.

Analgesic and Anti-inflammatory action of Opuntia elatior Mill fruits.

BACKGROUND: Opuntia elatio Mill is a xerophytic plant with potentially active nutrients. It is traditionally appreciated for its pharmacological properties; however, the scientific information on this plant is insufficient. OBJECTIVE: The present study evaluates the antinociceptive and anti-inflammatory action of prickly pear. MATERIALS AND METHODS: Writhing and tail-immersion tests were carried out to evaluate analgesic action, while the carrageenan-induced paw edema and neutrophil adhesion tests were conducted in Albino wistar rats to assess anti-inflammatory action. RESULTS: ED50 values of the fruit juice in writhing, tail immersion, and paw edema test were 0.919, 2.77, and 9.282 ml/kg, respectively. The fruits of Opuntia produced analgesic and anti-inflammatory action in a dose-dependent manner. CONCLUSION: The results establish the folklore use of prickly pear may be due to the presence of betacyanin and/or other phenolic compounds.

Effect of hydroalcoholic extract of leaves of Colocasia esculenta on marble-burying behavior in mice: Implications for obsessive-compulsive disorder.

CONTEXT: Over the past decades, the inhibition of spontaneous burying of glass marbles by mice has been used as an index of anxiolytic drug action in the so-called marble-burying test. Although Colocasia esculenta Linn. (Araceae), commonly known as elephant ear (English), possesses several medicinal properties, little is known for its use in neurological activity. OBJECTIVE: The current research evaluated the anti-obsessive-compulsive disorder (anti-compulsive) activity of the hydroalcoholic extract of leaves of Colocasia esculenta (HECE) for the first time using the marble-burying behavior test in mice. MATERIALS AND METHODS: In the present study, the effect of HECE (25 and 50 mg/kg) intraperitoneally (i.p.) was examined using the marble-burying behavior test, which is an animal model of obsessive compulsive disorder (OCD), using Swiss albino mice. RESULTS AND DISCUSSION: The acute toxicity studies showed that the LD50 value of the HECE in mice was 1000 mg/kg by i.p. route. The effect of HECE (25 and 50 mg/kg, i.p.) was characterized by significant reduction in the number of buried marbles as compared with the control group (p < 0.001). The effect of HECE was comparable with that of fluoxetine (5 mg/kg, i.p.) - a reference standard drug used in the treatment of obsessive-compulsive disorder (p < 0.001). Fluoxetine and HECE do not produce any overt motor dysfunction. CONCLUSIONS: The results of the study for the first time show that the plant possesses anti-compulsive activity, confirming the traditional claims. Future research should focus on the identification and the anti-compulsive activity of the constituents from this plant.

Forced Degradation Behaviour of Fluphenazine Hydrochloride by LC and Characterization of its Oxidative Degradation Product by LC-MS/MS.

A novel, stability-indicating high-performance liquid chromatographic (HPLC) method is delivered for the determination of fluphenazine hydrochloride (FPZ) and its degradation products. The forced degradation testing of FPZ was carried out for hydrolytic, oxidative, photolytic, and thermal degradation. The degradation appeared using a reversed-phase C18 column at ambient temperature with a mobile phase comprised of methanol : acetonitrile : (10 mM) ammonium acetate (70:15:15, v/v/v) pH 6.0, adjusted with acetic acid, having a flow rate of 1 ml min(-1) and a detection wavelength at 259 nm. Primarily, the maximum degradation products were formed under oxidative stress conditions. The product was distinguished through LC-MS/MS fragmentation studies. Based on the results, a more complete degradation pathway for the drug could be proposed. The modernized method was found to be precise, accurate, specific, and selective. The method was found to be suitable for the quality control of fluphenazine hydrochloride in the tablet as well as in stability-indicating studies.

Hematinic effect of fruits of Opuntia elatior Mill. on phenylhydrazine-induced anemia in rats.

INTRODUCTION: The fruits of Opuntia elatior Mill. are known as prickly pear and folkloric use as hematinic, anti-inflammatory and antiasthmatic action. Previously, the fruit juice of prickly pear was evaluated in reversed anemia induced by HgCl2 in a dose dependant manner and present study revealed about its effect in acute hemolytic anemia. AIM: To evaluate the hematinic activity of fruits of Opuntia elatior Mill. MATERIALS AND METHODS: The hematinic activity of an orally administered fruit juice was studied on phenylhydrazine (PHZ)-induced anemic rats. The hematological parameters such as hemoglobin (Hb) content, red blood cell (RBC), packed cell volume (PCV), and reticulocyte count were analyzed as indices of anemia. RESULTS: PHZ altered the hematological parameters by hemolysis characterized by a decrease in Hb content, total RBC counts and PCV (P < 0.001) on day 3. The Hb content (g%) was significantly increased (P < 0.05) at day 7 in 10 and 15 ml/kg fruit juice treated rats, which was a good improvement compared to the standard. CONCLUSION: The speedy and progressive recovery of anemic rats responding to treatment of the O. elatior Mill. fruits may be due to increased erythropoiesis and/or antioxidant property of betacyanin.

Development and validation of bioanalytical method for simultaneous estimation of ramipril and hydrochlorothiazide in human plasma using liquid chromatography-tandem mass spectrometry.

The present study describes a novel liquid chromatographic-tandem mass spectrometric (LC-MS/MS) method for the simultaneous estimation of ramipril (RAM) and hydrochlorothiazide (HCTZ) in human plasma using liquid-liquid extraction technique. This method made use of electrospray ionization in positive mode for RAM and in negative mode for HCTZ using triple quadrupole mass spectrometry where carbamazepine was used as an internal standard (IS). Analytes were recovered by methyl tertiary butyl ether:dichloromethane (85:15) subsequently separated on an Enable C18 G column (150 mm × 4.6 mm, 5 µm) using methanol:0.1% formic acid in water (85:15) as a mobile phase, at a flow rate of 0.5 mL/min. Quantification of RAM, HCTZ and IS was performed using multi-reaction monitoring mode (MRM) where transition of m/z 417.2→234.1 (RAM) and 237.0→194.0 (IS) in positive mode and 296.1→205.0 for HCTZ in negative mode. The calibration curve was linear (r(2)>0.99) over the concentration range of 2-170 ng/mL for RAM and 8-680 ng/mL for HCTZ. The intra-day and inter-day precisions were <15% and the accuracy was all within ±15% (at LLOQ level ±20%). Additionally, the LC-MS/MS method was fully validated for all the other parameters such as selectivity, matrix effect, recovery and stability as well. In conclusion, the findings of the present study revealed the selectivity and sensitivity of this method for the simultaneous estimation of RAM and HCTZ in human plasma.

Solasodine protects rat brain against ischemia/reperfusion injury through its antioxidant activity.

Ischemic stroke is the second leading cause of death worldwide. The major limitation of stroke management is the lack of clinically effective therapy. Antioxidants have been demonstrated as potent neuroprotective agents by enhancing the defense mechanism(s), whereas reducing the oxidative stress in the ischemic stroke models. In the present study, we evaluated neuroprotective potential of solasodine, an antioxidant glycoalkaloid of Solanum species, against global model of ischemia in rats. Ischemia/reperfusion (I/R)-injury produced marked elevation in lipid peroxidation (LPO) and nitric oxide (NO), whereas superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) levels were decreased in experimental animals. Prior administration of solasodine (100 and 200mg/kg, p.o.) significantly heightened SOD, CAT, GSH and total thiols, whereas reduced LPO and NO levels in the brain. Interestingly, brain coronal sectioning and histopathology studies revealed a marked reversal of I/R-provoked neuronal damage in the solasodine treatment groups. Taken together, our study, for the first time, demonstrates neuroprotective potential of solasodine against global ischemia-induced cerebral injury in experimental rats. We propose that the neuroprotection offered by solasodine could be attributed, at least in part, to its anti-oxidant property.

Quality by design approach for oral bioavailability enhancement of irbesartan by self-nanoemulsifying tablets.

The present investigation was aimed to develop self-nanoemulsifying tablets (SNETs) as novel nanosized solid oral dosage forms for Irbesartan (IRB). In the first part of the investigation, IRB-loaded self-nanoemulsifying drug delivery systems (SNEDDS) were developed using Capryol 90 - Cremophor RH40 - Transcutol P as three component (oil - surfactant - cosurfactant) SNEDDS system. On the basis of ternary phase diagram IRB-loaded SNEDDS were optimized by using Design of Experiments (DoE) and Principal component analysis (PCA) with amount of oil and surfactant: cosurfactant ratio (Km) as factors. The optimized batch of IRB-loaded SNEDDS comprised of 31.62% w/w of Capryol 90 as oil phase, 49.90% w/w Cremophor RH40 as surfactant and 18.48% w/w of Transcutol P as cosurfactant exemplified a mean globule size as 23.94 nm. Further, with an aim to provide enhanced patient compliance the optimized batch of liquid SNEDDS was transformed into SNETs by liquisolid compaction technique. Solid state characterization of IRB-loaded liquisolid mixtures revealed a decrease in the magnitude of crystallinity of IRB. The results of in vitro drug release study of optimized batch of IRB-loaded SNET illustrated a remarkable improvement in the dissolution rate as compared to marketed tablets (Avapro® 75). The results of in vivo pharmacokinetic study on Wister rats revealed 1.78-fold enhancement in oral bioavailability for IRB-loaded SNETs against marketed tablets. The present study proposed SNEDDS as one of the suitable approach for developing nanosized solid oral dosage forms of poorly water soluble drugs like Irbesartan.

Formulation and evaluation of sustained release enteric-coated pellets of budesonide for intestinal delivery.

INTRODUCTION: The aim of present work was to develop intestinal-targeted pellets of Budesonide, a potent glucocorticoid, used for the treatment of ulcerative colitis and Crohn's disease by extrusion and spheronization method. Current available oral formulations of Budesonide have low efficacy because of the premature drug release in the upper part of the gastrointestinal tract. In this study, a pH-controlled intestinal-targeted pellet of budesonide was established using 3(2) full factorial design by giving an enteric coating with Eudragit S100. MATERIALS AND METHODS: Budesonide-sustained release pellets were prepared by extruder and spheronization technique using a combination of water-soluble and permeable polymers by applying 3(2) full factorial design. The pellets were coated by spray coating technique using Eudragit S100 as an enteric polymer. The pellets were characterized for its flowability, sphericity, friability, and in vitro drug release. Release behaviour was studied in different pH media. The release profile was studied for the mechanism of drug release. RESULT: The optimized formulation showed negligible drug release in the stomach followed by release for 12 h in the intestinal pH. Differential scanning calorimetry and Fourier Transform Infrared Spectroscopy studies indicated no interaction between drug and polymer. Scanning Electron Microscopy image of coated pellets suggested a uniform and smooth coat over the surface of pellets. Accelerated stability studies showed a stable nature of drug in the formulation. All evaluation parameter showed that pellets were good in spherocity and flowability. CONCLUSION: Sustained release pellets of Budesonide could be prepared by extrusion and spheronization which released the drug in intestinal pH for an intestine to treat inflammatory bowel disease. A ratio of polymer combination could be decided using a full factorial design.

Self-nanoemulsifying drug delivery system of glimepiride: design, development, and optimization.

The objective of the present investigation was to develop and characterize the self-nanoemulsifying drug delivery system (SNEDDS) of glimepiride, a poorly soluble drug. Solubility of glimepiride in various vehicles was determined, and ternary phase diagrams were constructed using a suitable oil, surfactant, and cosurfactant system to find out the efficient self-emulsification system. A three factor, three level Box-Behnken statistical design was employed to explore the main and interaction effect of independent variables, namely X1 (amount of Capmul MCM), X2 (amount of Acrysol K 140), and X3 (amount of Transcutol P). Percent transmittance value (Y1), droplet diameter (Y2), and percent drug released at 5 min (Y3) were the dependent variables. Formulation optimization was carried out to optimize the droplet diameter and percent drug dissolved at 5 min. The batch prepared according to the optimized formulation showed a close agreement between observed and predicted values. Box-Behnken statistical design allowed us to understand the effect of formulation variables on the rapid dissolution of drug from SNEDDS and to optimize the formulation to obtain a rapid drug dissolution at 5 min. LAY ABSTRACT: A self-nanoemulsifying drug delivery system of glimepiride has been design, developed, and optimized. A three factor, three level Box-Behnken statistical design was employed to explore the main and interaction effect of independent variables, namely X1 (amount of Capmul MCM), X2 (amount of Acrysol K 140), and X3 (amount of Transcutol P). Percent transmittance value (Y1), droplet diameter (Y2), and percent drug released at 5 min (Y3) were the dependent variables. The Capmul MCM-Akcrysol K 140-Transcutol system was found to be the suitable ternary system that was able to release almost 80% of drug within the first 5 min. The improved dissolution of glimepiride might improve patient compliance.

Design and evaluation of herbal hepatoprotective formulation against paracetamol induced liver toxicity.

AIM: To isolate and identify the quercetin from polyherbal hepatoprotective formulation. Polyherbal formulations were developed by using five bioactive fractionated extracts of Butea monosperma, Bauhinia variegata and Ocimum gratissimum for treatment of liver disorders by exploiting the knowledge of traditional system of medicine and evaluated for hepatoprotective activity using acute liver toxicity model of paracetamol induced liver damage in rats. METHODS: Major active fractions were isolated by solvent fractionation and quantified by HPTLC method. Two polyherbal tablet formulations were developed by the wet granulation method using microcrystalline cellulose, aerosil and other excipients and subjected for physicochemical evaluation to assess physical stability followed by pharmacological screening. The prepared tablets were finally subjected to stability testing to assess its shelf-life. The rats were monitored for change in liver morphology, biochemical parameters like serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP) and total bilirubin for polyherbal tablet formulation at 50 mg/kg and polyherbal tablet formulation at 100 mg/kg. RESULTS: Active principle was isolated, quantified by HPTLC and characterized with IR. Both formulations showed significant hepatoprotective activity. The histological studies were also support the biochemical parameters. From the results of biochemical analysis and histopathological studies, it can be accomplished that polyherbal tablet formulation at 100 mg/kg can be effectively formulated into a suitable dosage form with added benefit of no side effects for control and cure of chronic ailments like liver disorders. A comparative histopathological study of liver exhibited almost normal architecture as compared to toxicant group. CONCLUSION: Biochemical marker showed improved results for polyherbal tablet formulation at 100 mg/kg. Polyherbal tablet formulation contains a potent hepatoprotective agent suggested to be a flavone concentrated in polyherbal formulation which may find clinical application in amelioration of paracetamol induced liver damage.

To assess the prevalence of impaired glucose tolerance and impaired fasting glucose in Western Indian population.

OBJECTIVES: The objective of the study to determine the prevalence of Impaired Glucose Tolerance and Impaired Fasting Glucose (both combined termed as Pre Diabetes) in the population of Gujarat. METHODS: In year 2007 and 2008, a cross sectional survey was conducted via mode of camps at various urban and rural part of Gujarat. After obtaining an informed consent, comprehensive questionnaire was used to collect the various anthropological details, physical examination and blood collection was performed from around 1700 subjects > or = 20 years of age from the different areas of Gujarat. Chi square test was used for all categorical comparisons. Also multiple logistic regression was used for detailed exploratory analysis. RESULTS: The crude prevalence of IFG in Gujarati population is around 2.76% and IGT is around 6.12%. But the age adjusted prevalence of IFG is around 2.72% and IGT is around 4.67%. If we extrapolate these to population of Gujarat, it indicates that around 1.3 million people are having impaired fasting glucose and around 2.3 million people have impaired glucose tolerance. The prevalence of IGT found more after age of 40 years. For IFG, there is increase after age of 40 years, but not significant statistically. CONCLUSIONS: High prevalence of IGT validates that there are chances of the pandemic trend in Gujarat, as eventually IGT may get converted into Diabetes in near future. These results need urgent attention to develop a public awareness programme.