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1.
Anim Biotechnol ; 30(2): 151-158, 2019 Apr.
Article in English | MEDLINE | ID: mdl-29592658

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/pharmacology , Mastitis, Bovine/drug therapy , Plant Extracts/pharmacology , Terminalia/chemistry , Animals , Bacillus megaterium/drug effects , Cattle , Escherichia coli/drug effects , Female , Mastitis, Bovine/microbiology , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects
2.
Int J Pharm Investig ; 5(4): 247-58, 2015.
Article in English | MEDLINE | ID: mdl-26682195

ABSTRACT

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.

3.
Rev. bras. farmacogn ; 25(5): 485-490, Sept.-Oct. 2015. tab, graf
Article in English | LILACS | ID: lil-765078

ABSTRACT

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.

4.
J Ayurveda Integr Med ; 6(2): 75-81, 2015.
Article in English | MEDLINE | ID: mdl-26166996

ABSTRACT

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.

5.
Ayu ; 36(2): 208-13, 2015.
Article in English | MEDLINE | ID: mdl-27011725

ABSTRACT

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.

6.
Sci Pharm ; 83(2): 297-309, 2015.
Article in English | MEDLINE | ID: mdl-26839816

ABSTRACT

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.

7.
Article in English | MEDLINE | ID: mdl-25240204

ABSTRACT

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.


Subject(s)
Chromatography, Liquid/methods , Hydrochlorothiazide/blood , Ramipril/blood , Tandem Mass Spectrometry/methods , Drug Stability , Humans , Hydrochlorothiazide/chemistry , Linear Models , Ramipril/chemistry , Reproducibility of Results , Sensitivity and Specificity
8.
Int J Pharm Investig ; 3(4): 203-11, 2013 Oct.
Article in English | MEDLINE | ID: mdl-24350040

ABSTRACT

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.

9.
PDA J Pharm Sci Technol ; 67(3): 201-13, 2013.
Article in English | MEDLINE | ID: mdl-23752748

ABSTRACT

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.


Subject(s)
Drug Delivery Systems , Emulsions , Chemistry, Pharmaceutical , Humans , Particle Size , Solubility , Surface-Active Agents
10.
Drug Dev Ind Pharm ; 39(3): 437-46, 2013 Mar.
Article in English | MEDLINE | ID: mdl-22380546

ABSTRACT

BACKGROUND: Direct tabletting is a need of Pharmaceutical industries. Poor mechanical properties of drug particles require wet granulation which is uneconomical, laborious, and tedious. OBJECTIVE: Objective of this work was to study influence of various polymers/excipients on formation of directly compressible Crystallo-co-agglomerates (CCA) of water soluble drug Secnidazole (hydroxy-2-propyl)-1-methyl-2-nitro-5-imidazole), an antimicrobial agent. METHOD: Acetone-petroleum ether system was used to develop CCA of drug in the presence of polymers/excipients. Clarity of the supernatant was considered an endpoint for completion of agglomeration. The prepared CCA were subjected for topographic, micromeritic, mechanical, compressional, and drug release properties. RESULTS: The process yielded ~92 to 98% wt/wt CCA containing secnidazole with the diameter between 0.2 and 0.7 mm. CCA showed excellent flow, packability, compatibility, and crushing strength. Heckel plot showed lower σ(0) and higher tensile strength with lower elastic recovery (0.55-1.28%) of CCA. Dissolution profile of CCA was improved. Differential scanning calorimetry , fourier transform infra-red, and x-ray diffractometry results showed absence of drug-excipient interaction. DISCUSSION: Matrix beads were generated with uniform dispersion of crystallized drug. Excellent flow, packability, and compactability were due to sphericity of agglomerates. Higher crushing strength of CCA was an indication of good handling qualities. Lower σ(0), higher tensile strength, and lower elastic recovery indicated excellent compressibility of agglomerates. Improvement in dissolution profile was due to porous nature of CCA. CONCLUSION: Excipients and polymers can play a key role to prepare CCA, an excellent alternative to wet granulation process to prepare particles for direct compression.


Subject(s)
Antiprotozoal Agents/chemistry , Chemistry, Pharmaceutical , Drug Compounding/methods , Excipients/chemistry , Metronidazole/analogs & derivatives , Polymers/chemistry , Crystallization/methods , Metronidazole/chemistry , Particle Size
11.
Drug Dev Ind Pharm ; 39(3): 425-36, 2013 Mar.
Article in English | MEDLINE | ID: mdl-22393879

ABSTRACT

The objective of the present investigation was to develop and evaluate physiological environment responsive periodontal drug delivery system (PERPDDS) for local delivery of metronidazole benzoate. Poly-ϵ-caprolactone an in situ precipitating polymer was used in combination with, carbopol 934P, a pH simulative polymer to develop PERPDDS. The prepared PERPDDS was evaluated for various parameters such as in vitro gelling capacity, viscosity, rheology, compatibility study, and in vitro diffusion study. A 3(2) full factorial design was used to investigate the influence of formulation variables. Drug release data from all formulations were fitted to different kinetic models and the korsemeyer-peppas model was found the best fit model. The value of diffusional exponent (n) was in between 0.3283 and 0.3979 indicating purely fickian diffusion release mechanism. Increasing the concentration of each polymeric component increases viscosity, and time for 50% and 90% drug release was observed and graphically represented by the surface response and contour plots.


Subject(s)
Anti-Infective Agents/administration & dosage , Drug Delivery Systems , Metronidazole/administration & dosage , Periodontitis/drug therapy , Chemistry, Pharmaceutical , Diffusion , Drug Design , Gels/chemistry , Humans , Models, Theoretical , Mouth Mucosa/chemistry , Polyesters/chemistry
12.
J Young Pharm ; 5(4): 180-7, 2013 Dec.
Article in English | MEDLINE | ID: mdl-24563599

ABSTRACT

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.

13.
J Assoc Physicians India ; 61(3): 179-84, 2013 Mar.
Article in English | MEDLINE | ID: mdl-24475680

ABSTRACT

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.


Subject(s)
Blood Glucose/metabolism , Glucose Intolerance/epidemiology , Prediabetic State/epidemiology , Adult , Age Factors , Blood Pressure , Body Mass Index , Cross-Sectional Studies , Fasting , Female , Glucose Intolerance/metabolism , Glucose Tolerance Test , Humans , India/epidemiology , Male , Middle Aged , Prevalence , Rural Population/statistics & numerical data , Urban Population/statistics & numerical data , Waist-Hip Ratio
14.
Gut Microbes ; 2(6): 319-25, 2011.
Article in English | MEDLINE | ID: mdl-22157237

ABSTRACT

The protective effect of Lactobacillus rhamnosus 231 (Lr 231) against potent carcinogen N-Methyl-N'-Nitro-N-Nitrosoguanidine (MNNG) in the rat model is studied. Daily feeding with Lr 231 improved the body weight of male Wistar rats compared with control groups. Fecal azoreductase (p < 0.001) and nitroreductase (p < 0.01) enzyme activity decreased significantly in Lr 231 group in comparison with control groups that received only phosphate buffer or MNNG. Oral administration of MNNG led to a significant increase in Glutathione transferase (GST) while Glutathione reductase (GSH) showed decreased activity. Conversely, feeding Lr 231 showed significantly increased GSH and decreased GST activity in comparison to the MNNG group, emphasizing the protection provided by Lr 231 against MNNG. Histopathological analysis of liver, spleen and colon showed decreased signs of inflammation in the Lr 231 group. The present study highlights that inclusion of active Lr 231 in regular diets could be used to prevent MNNG induced colon carcinoma.


Subject(s)
Inflammation/therapy , Lacticaseibacillus rhamnosus/metabolism , Methylnitronitrosoguanidine/adverse effects , Probiotics/therapeutic use , Animals , Body Weight , Colon/enzymology , Colon/pathology , Enzyme Activation , Enzyme Assays , Feces/enzymology , Glutathione Transferase/metabolism , Inflammation/chemically induced , Inflammation/pathology , Liver/enzymology , Liver/pathology , Male , NADH, NADPH Oxidoreductases/metabolism , Nitroreductases , Probiotics/administration & dosage , Probiotics/metabolism , Rats , Rats, Wistar , Spleen/enzymology , Spleen/pathology
15.
Int J Anal Chem ; 2011: 124917, 2011.
Article in English | MEDLINE | ID: mdl-22007220

ABSTRACT

The objective of the current study was to develop a validated stability-indicating assay method (SIAM) for risperidone after subjecting it to forced decomposition under hydrolysis, oxidation, photolysis, and thermal stress conditions. The liquid chromatographic separation was achieved isocratically on a symmetry C18 column (5 µm size, 250 mm × 4.6 mm i.d.) using a mobile phase containing methanol: acetonitrile (80 : 20, v/v) at a flow rate of 1 mL/min and UV detection at 280 nm. Retention time of risperidone was found to be 3.35 ± 0.01. The method was linear over the concentration range of 10-60 µg/mL(r(2) = 0.998) with a limit of detection and quantitation of 1.79 and 5.44 µg/mL, respectively. The method has the requisite accuracy, specificity, sensitivity, and precision to assay risperidone in bulk form and pharmaceutical dosage forms. Degradation products resulting from the stress studies did not interfere with the detection of Risperidone, and the assay is thus stability indicating.

16.
Pharmazie ; 66(2): 119-23, 2011 Feb.
Article in English | MEDLINE | ID: mdl-21434574

ABSTRACT

The aim of the present work was to improve the dissolution characteristics of the poorly water soluble antiepileptic drug lamotrigine (LMN) by inclusion complexation using hydroxy propyl beta-cyclodextrin (HP beta-CD) by co-evaporation technique and by, solid dispersion, prepared by the melt method using poloxamer 407 (L 127). Phase solubility studies showed AL type curves with both the carriers. Dissolution of LMN was significantly improved (p < 0.05) by inclusion complexation and solid dispersion preparation. Results of solid state characterization performed by Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry and Powder X-ray Diffractrometry techniques revealed a decrease in the crystallinity of LMN that might be accounting for improvement in the dissolution properties as seen from dissolution studies.


Subject(s)
Anticonvulsants/chemistry , Triazines/chemistry , Anticonvulsants/administration & dosage , Calorimetry, Differential Scanning , Delayed-Action Preparations , Lamotrigine , Solubility , Solutions , Spectroscopy, Fourier Transform Infrared , Triazines/administration & dosage , X-Ray Diffraction
17.
J Nephrol ; 24(5): 631-5, 2011.
Article in English | MEDLINE | ID: mdl-21240877

ABSTRACT

BACKGROUND: Elevation of serum homocysteine is considered to contribute to endothelial dysfunction, which is considered to be the initial event in vascular disease following renal transplantation. We sought to investigate whether an association existed between serum homocysteine levels and endothelial dysfunction after renal ischemia/reperfusion (I/R) injury. MATERIALS AND METHODS: Acetylcholine (Ach)-induced endothelium-dependent and sodium nitroprusside (SNP)-induced endothelial-independent relaxation responses were determined in thoracic aortas from different I/R groups. A correlation analysis was performed between Ach responses and homocysteine levels. RESULTS: Long-term I/R injury decreased the responses to acetylcholine and the pD2 values of the concentration response curves compared with controls. While vascular responses to SNP were unchanged among all groups. Homocysteine levels correlated with the pD2 values of acetylcholine among control and I/R groups, indicating that the increase in homocysteine was associated with decreased sensitivity to acetylcholine. In short-term I/R rats, no association was observed between these parameters. CONCLUSION: These data suggest a possible link between serum homocysteine and decreased vascular reactivity to endothelium-dependent relaxation in I/R aorta.


Subject(s)
Endothelium, Vascular/metabolism , Homocysteine/blood , Kidney/blood supply , Reperfusion Injury/blood , Vasodilation , Acetylcholine/pharmacology , Animals , Disease Models, Animal , Dose-Response Relationship, Drug , Endothelium, Vascular/drug effects , Endothelium, Vascular/physiopathology , Male , Nitroprusside/pharmacology , Rats , Rats, Wistar , Reperfusion Injury/physiopathology , Up-Regulation , Vasodilation/drug effects , Vasodilator Agents/pharmacology
18.
Ayu ; 32(4): 576-84, 2011 Oct.
Article in English | MEDLINE | ID: mdl-22661858

ABSTRACT

The whole plant of Stellaria media (family: Caryophyllaceae) has been tested for its antiobesity activity by using progesterone-induced obesity model in female albino mice. The effect of S. media on food consumption pattern, change in body weight, thermogenesis, lipid metabolism, and histology of fat pad. were examined. Methanolic and alcoholic extracts of the S. media were used in the study. Methanolic extract of S. media (MESM) have prevented the increase in body weight, adipose tissue weight and size, and upturned obesity and associated complications. MESM has also shown promising effects compared with alcoholic extract of S. media may be because of its multiple mechanisms. These findings suggest that antiobesity activity produced by MESM is because of its anorexic property mediated by saponin and flavonoid and partly of by its ß-sitosterol content. ß-Sitosterol in the plant extract was confirmed by thin-layer chromatography study. ß-sitosterol is plant sterol having structural similarity with dietary fat which do the physical competition in the gastrointestinal tract and reduces fat absorption. Before carrying in vivo activity detail pharmacognostic and phytochemical analysis of the extracts was carried out. The plant has shown the presence of saponin, flavonoids, steroids and triterpenoids, glycosides, and anthocynidine. By this study, it can be concluded that, MESM is beneficial in suppression of obesity induced by progesterone.

19.
Saudi J Gastroenterol ; 16(3): 174-80, 2010.
Article in English | MEDLINE | ID: mdl-20616412

ABSTRACT

BACKGROUND/AIM: This study was designed to investigate the possible effect of exenatide (Glucagon like Peptide-1 receptor agonist) on liver injury (distant organ) induced by renal ischemia reperfusion (IR) in diabetic rats. MATERIALS AND METHODS: In vivo renal IR was performed in both type 2 diabetic and normal rats. Each protocol comprised ischemia for 30 minutes followed by reperfusion for 24 hours and a treatment period of 14 days before induction of ischemia. RESULTS: Lipid peroxidation, xanthine oxidase activity, myeloperoxidase activity and nitric oxide level in liver tissue were significantly increased (P < 0.01, P < 0.001, P < 0.001, P < 0.05, respectively), after IR in diabetic rats compared to normal rats. Antioxidant enzymes like glutathione, superoxide dismutase, catalase and glutathione peroxidase were significantly reduced (P < 0.05, P < 0.05, P < 0.01, P < 0.05, respectively), after IR in diabetic rats compared to normal rats. Exenatide treatment significantly normalized (P < 0.01), these biochemical parameters in treated rats compared to diabetic IR rats. Serum creatinine phosphokinase activity and liver function enzymes were also significantly normalized (P < 0.001, P < 0.001, respectively), after administration of exenatide. CONCLUSION: Exenatide exerted protective effect on exaggerated remote organ (liver) injury induced by renal IR in diabetes.


Subject(s)
Diabetes Mellitus, Experimental/drug therapy , Kidney Diseases/drug therapy , Kidney/blood supply , Liver Diseases/drug therapy , Liver/blood supply , Peptides/pharmacology , Reperfusion Injury/drug therapy , Venoms/pharmacology , Animals , Catalase/metabolism , Creatine Kinase/metabolism , Diabetes Mellitus, Experimental/enzymology , Exenatide , Glutathione/metabolism , Glutathione Peroxidase/metabolism , Kidney/drug effects , Kidney/enzymology , Kidney Diseases/enzymology , Kidney Diseases/etiology , Lipid Peroxidation , Liver/drug effects , Liver/enzymology , Liver Diseases/enzymology , Liver Diseases/etiology , Liver Function Tests , Nitric Oxide/metabolism , Rats , Rats, Wistar , Reperfusion Injury/etiology , Superoxide Dismutase/metabolism , Treatment Outcome , Xanthine Oxidase/metabolism
20.
Drug Deliv ; 17(7): 520-31, 2010.
Article in English | MEDLINE | ID: mdl-20553104

ABSTRACT

Smart gel periodontal drug delivery systems (SGPDDS) containing gellan gum (0.1-0.8% w/v), lutrol F127 (14, 16, and 18% w/v), and ornidazole (1% w/v) were designed for the treatment of periodontal diseases. Each formulation was characterized in terms of in vitro gelling capacity, viscosity, rheology, content uniformity, in vitro drug release, and syringeability. In vitro gelation time and the nature of the gel formed in simulated saliva for prepared formulations showed polymeric concentration dependency. Drug release data from all formulations was fitted to different kinetic models and the Korsemeyer-Peppas model was the best fit model. Drug release was significantly decreased as the concentration of each polymer component was increased. Increasing the concentration of each polymeric component significantly increased viscosity, syringeability, and time for 50%, 70%, and 90% drug release. In conclusion, the formulations described offer a wide range of physical and drug release characteristics. The formulation containing 0.8% w/v of gellan gum and 16% w/v of lutrol F127 exhibited superior physical characteristics.


Subject(s)
Anti-Infective Agents, Local/chemistry , Gels/chemistry , Ornidazole/chemistry , Polyethylenes/chemistry , Polypropylenes/chemistry , Polysaccharides, Bacterial/chemistry , Anti-Infective Agents, Local/therapeutic use , Chemistry, Pharmaceutical , Delayed-Action Preparations , Drug Combinations , Drug Delivery Systems , Drug Stability , Kinetics , Ornidazole/therapeutic use , Periodontal Diseases/drug therapy , Rheology , Temperature , Viscosity
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