Search results for: A.V. Chandewar

Authors: Anil P. Dewani, Alok S. Tripathi, Anil V. Chandewar

Abstract:

Present manuscript reports the development and validation of a quantitative high performance liquid chromatography method for the pharmacokinetic evaluation of Glimepiride (GLM) and Ilaprazole (ILA) in rat plasma. The plasma samples were involved with Solid phase extraction process (SPE). The analytes were resolved on a Phenomenex C18 column (4.6 mm× 250 mm; 5 µm particle size) using a isocratic elution mode comprising methanol:water (80:20 % v/v) with pH of water modified to 3 using Formic acid, the total run time was 10 min at 225 nm as common wavelength, the flow rate throughout was 1ml/min. The method was validated over the concentration range from 10 to 600 ng/mL for GLM and ILA, in rat plasma. Metformin (MET) was used as Internal Standard. Validation data demonstrated the method to be selective, sensitive, accurate and precise. The limit of detection was 1.54 and 4.08 and limit of quantification was 5.15 and 13.62 for GLM and ILA respectively, the method demonstrated excellent linearity with correlation coefficients (r2) 0.999. The intra and inter-day precision (RSD%) values were < 2.0% for both ILA and GLM. The method was successfully applied in pharmacokinetic studies followed by oral administration in rats.

Keywords: pharmacokinetics, glimepiride, ilaprazole, HPLC, SPE

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Authors: Jiwan P. Lavande, A. V. Chandewar

Abstract:

In the present study, orodispersible tablets of diphenhydramine hydrochloride were prepared using croscarmellose sodium, crospovidone and camphor, menthol (as subliming agents) in different ratios and ODTs prepared with superdisintegrants were compared with ODTs prepared with camphor and menthol (subliming agents) for the following evaluation of in vitro disintegration time, dispersion time, wetting time, hardness and water absorption ratio. Results revealed that the tablets of all formulations have acceptable physical parameters. The drug and excipients compatibility study was evaluated using FTIR technique and has not detected any incompatibility. The in vitro release of drug from DC6 formulation was quick when compared to other formulations. Stability study was carried out as per ICH guidelines for three months and results revealed that upon storage disintegration time of tablets had not shown any significant difference. Microscopic study of different formulations of sublimed tablets showed formation of pores for the tablets prepared by sublimation method. Thus, conclusion can be made that the stable orodispersible tablets of diphenhydramine hydrochloride can be developed for the rapid release of diphenhydramine hydrochloride.

Keywords: orodispersible tablet, subliming agent, super disintegrants, diphenhydramine hydrochloride

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Authors: J. P. Lavande, A. V.Chandewar

Abstract:

Mouth dissolving tablet is the speedily growing and highly accepted drug delivery system. This study was aimed at development of Ketorolac Tromethamine mouth dissolving tablet (MDTs), which can disintegrate or dissolve rapidly once placed in the mouth. Conventional Ketorolac tromethamine tablet requires water to swallow it and has limitation like low disintegration rate, low solubility etc. Ketorolac Tromethamine mouth dissolving tablets (formulation) consist of super-disintegrate like Heat Modified Karaya Gum, Co-treated Heat Modified Agar & Filler microcrystalline cellulose (MCC). The tablets were evaluated for weight variation, friability, hardness, in vitro disintegration time, wetting time, in vitro drug release profile, content uniformity. The obtained results showed that low weight variation, good hardness, acceptable friability, fast wetting time. Tablets in all batches disintegrated within 15-50 sec. The formulation containing superdisintegrants namely heat modified karaya gum and heat modified agar showed better performance in disintegration and drug release profile.

Keywords: mouth dissolving tablet, Ketorolac tromethamine, disintegration time, heat modified karaya gum, co-treated heat modified agar

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Authors: D. S. Mohale, A.V. Chandewar

Abstract:

Study was undertaken to investigate the effect of imipramine on various biochemical parameters and oxidative stress markers in short and long term depression on rats. Rats were subjected for short (21 days) and long term (84 days) social isolation for and checked for depression on force swim test and tail suspension method. Various markers of oxidative stress like lipid peroxidation (LPO), reduced glutathione (GSH), Supersoxide dismutase (SOD), catalase (CAT) and biochemical parameters like Serum glutamate oxaloacetate transaminase (SGOT), Serum glutamate pyruate transaminase (SGPT), and blood glucose were determined in depressed, control, imipramine and Vitamin E treated group. The rats displayed an increase in depression on force swim test and tail suspension method relative to control. There was significant increase in the level of LPO and decrease in the levels of GSH, SOD and CAT after short and long term depression. Increased oxidative stress in depression which may leads to alteration of biochemical parameters. Treatment with imipramine an tricyclic antidepressant significantly decreases in level of LPO, SGOT, SGPT and increase in the levels of GSH, SOD and CAT in long term depression.

Keywords: depression, oxidative stress, lipid peroxidation, reduced glutathione

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Authors: A. V. Shrirao, N. I. Kochar, A. V. Chandewar

Abstract:

The flower extract of Butea monosperma herb has been used traditionally in India for medicinal purposes. The plant has been reported to treat hyperglycemia and associated hyperlipidemia. Hyperlipidemia and oxidative stress are known to accelerate coronary artery disease and progression of atherosclerotic lesions. The present work was undertaken to investigate the possible antihyperlipidemic and antioxidative effect of Butea monosperma flowers on hyperlipidemic rats. Hyperlipidemia was induced in rats by a single intraperitonial (i.p.) injection of Triton WR 1339 (400 mg/kg) and it showed sustained elevated levels of serum cholesterol and triglyceride. Ethanolic extract of Butea monosperma flowers (Et-BM) (250 and 500 mg/kg/day) was administered to normal and hyperlipidemic rats for 14 days. Serum and liver tissue were analyzed at three different time intervals for lipid profile and antioxidants enzymes and the activity were compared to the cholesterol-lowering drug, Atorvastatin (10 mg/kg). Parameters were altered during hyperlipidemia and reverted back to near normal values after Et-BM treatment or standard drug Atorvastatin. Lipid peroxidation decreased whereas the activities of superoxide dismutase, glutathione peroxidase and catalase increased in Et-BM treated rats. Pronounced changes were observed at 500 mg/kg of Et-BM for 2 weeks and it was comparable to the standard drug Atorvastatin. The current study provides strong evidence that Et-BM has a remarkable beneficial effect in treating hyperlipidemia and ROS without any side effects at the dosage and duration studied.

Keywords: antioxidant, butea monopserma, hyperlipidemia, triton WR 1339

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Authors: D. S. Mohale, A. V. Chandewar

Abstract:

Anxiety is defined as an exaggerated feeling of apprehension, uncertainty and fear. Nerium indicum is a well-known ornamental and medicinal plant belonging to the family Apocynaceae. A wide spectrum of biological activities has been reported with various constituents isolated from different parts of the plant. This study was conducted to investigate antianxiety activity of flower extract. Flowers were collected and dried in shade and coarsely powdered. Powdered mixture was extracted with ethyl acetate by maceration process. Extract of flowers obtained was subsequently dried in oven at 40-50 °C. This extract is then tested for antianxiety activity at low and high dose using Elevated Plus Maze and Light & dark Model. Rats shown increased open arm entries and time spent in open arm in elevated Plus maze with treatment low and high dose of extract of Nerium indicum flower as compared to their respective control groups. In Light & dark Model, light box entries and time spent in light box increased with treatment low and high dose of extract of Nerium indicum flower as compared to their respective control groups. From result it is concluded that Ethyl acetate extract of flower of Nerium indicum possess antianxiety activity at low and high dose.

Keywords: anxiety, anxieolytic, social isolation, nerium indicum, kaner

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Authors: Deepak Suresh Mohale, Anil V. Chandewar

Abstract:

Anxiety is defined as an exaggerated feeling of apprehension, uncertainty and fear. Nerium indicum is a well-known ornamental and medicinal plant belonging to the family Apocynaceae. A wide spectrum of biological activities has been reported with various constituents isolated from different parts of the plant. This study was conducted to investigate antianxiety activity of flower extract. Flowers were collected and dried in shade and coarsely powdered. Powdered mixture was extracted with ethyl acetate by maceration process. Extract of flowers obtained was subsequently dried in oven at 40-50 °C. This extract is then tested for antianxiety activity at low and high dose using elevated plus maze and light & dark model. Rats shown increased open arm entries and time spent in open arm in elevated Plus maze with treatment low and high dose of extract of Nerium indicum flower as compared to their respective control groups. In Light & dark Model, light box entries and time spent in light box increased with treatment low and high dose of extract of Nerium indicum flower as compared to their respective control groups. From result it is concluded that ethyl acetate extract of flower of Nerium indicum possess antianxiety activity at low and high dose.

Keywords: antianxiety, anxiety, kaner, nerium indicum, social isolation

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Authors: D. S. Mohale, A. P. Dewani, A. S.tripathi, A. V. Chandewar

Abstract:

Present work demonstrates the applicability of high-performance liquid chromatography (HPLC) with UV-Vis detection for the quantification of malondialdehyde as malondialdehyde-thiobarbituric acid complex (MDA-TBA) in-vivo in rats. The HPLC method for MDA-TBA was achieved by isocratic mode on a reverse-phase C18 column (250mm×4.6mm) at a flow rate of 1.0mLmin−1 followed by detection at 532 nm. The chromatographic conditions were optimized by varying the concentration and pH of water followed by changes in percentage of organic phase optimal mobile phase consisted of mixture of water (0.2% triethylamine pH adjusted to 2.3 by ortho-phosphoric acid) and acetonitrile in ratio (80:20v/v). The retention time of MDA-TBA complex was 3.7 min. The developed method was sensitive as limit of detection and quantification (LOD and LOQ) for MDA-TBA complex were (standard deviation and slope of calibration curve) 110 ng/ml and 363 ng/ml respectively. Calibration studies were done by spiking MDA into rat plasma at concentrations ranging from 500 to 1000 ng/ml. The precision of developed method measured in terms of relative standard deviations for intra-day and inter-day studies was 1.6–5.0% and 1.9–3.6% respectively. The HPLC method was applied for monitoring MDA levels in rats subjected to chronic treatment of levofloxacin (LEV) (5mg/kg/day) for 21 days. Results were compared by findings in control group rats. Mean peak areas of both study groups was subjected for statistical treatment to unpaired student t-test to find p-values. The p value was <0.001 indicating significant results and suggesting increased MDA levels in rats subjected to chronic treatment of LEV of 21 days.

Keywords: malondialdehyde-thiobarbituric acid complex, levofloxacin, HPLC, oxidative stress

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Authors: Anil P. Dewani, Ravindra L. Bakal, Anil V. Chandewar

Abstract:

Present work demonstrates the applicability of high-performance liquid chromatography (HPLC) with UV detection for the determination of malondialdehyde as malondialdehyde-thiobarbituric acid complex (MDA-TBA) in-vivo in rats. The HPLC-UV method for MDA-TBA was achieved by isocratic mode on a reverse-phase C18 column (250mm×4.6mm) at a flow rate of 1.0mLmin−1 followed by UV detection at 278 nm. The chromatographic conditions were optimized by varying the concentration and pH followed by changes in percentage of organic phase optimal mobile phase consisted of mixture of water (0.2% Triethylamine pH adjusted to 2.3 by ortho-phosphoric acid) and acetonitrile in ratio (80:20 % v/v). The retention time of MDA-TBA complex was 3.7 min. The developed method was sensitive as limit of detection and quantification (LOD and LOQ) for MDA-TBA complex were (standard deviation and slope of calibration curve) 110 ng/ml and 363 ng/ml respectively. The method was linear for MDA spiked in plasma and subjected to derivatization at concentrations ranging from 100 to 1000 ng/ml. The precision of developed method measured in terms of relative standard deviations for intra-day and inter-day studies was 1.6–5.0% and 1.9–3.6% respectively. The HPLC method was applied for monitoring MDA levels in rats subjected to chronic treatment of ciprofloxacin (CFL) (5mg/kg/day) for 21 days. Results were compared by findings in control group rats. Mean peak areas of both study groups was subjected for statistical treatment to unpaired student t-test to find p-values. The p value was < 0.001 indicating significant results and suggesting increased MDA levels in rats subjected to chronic treatment of CFL of 21 days.

Keywords: MDA, TBA, ciprofloxacin, HPLC-UV

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Authors: A. V. Chandewar, Sanjay Bais

Abstract:

Backgound: In India, drugs of herbal origin have been used in traditional systems of medicines such as Unani and Ayurveda since ancient times. WHO limit for Escherichia coli is 101/gm cfu, for Staphylococus aureus 105/gm cfu, and for Pseudomonas aeruginosa 103/gm cfu and for Salmonella species nil cfu. WHO mentions maximum permissible limits in raw materials only for arsenic, cadmium, and lead, which amount to 1.0, 0.3, and 10 ppm, respectively. Aim: The main purpose of the investigation was to document evidence for the users, and practitioners of marketed haematinic herbal formulations. In the present study haematinic herbal formulations marketed in Yavatmal India were determined for the presence of microbial and heavy metal content. Method: The investigations were performed by using specific medias and atomic absorption spectrometry. Result: The present work indicates the presence of heavy metal contents in herbal formulations selected for study. It was found that arsenic content in formulations was below the permissible limit in all formulations. The cadmium and lead content in six formulations were above the permissible limits. Such formulations are injurious to health of patient if consumed regularly. The specific medias were used to determining the presence of Escherichia coli 4 samples, Staphylococcus aureus 3 samples, and P. aeruginosa 4 samples. The data indicated suggest that there is requirement of in process improvement to provide better quality for consumer health in order to be competitive in international markets. Summary/Conclusion: The presence of microbial and heavy metal content above WHO limits indicates that the GMP was not followed during manufacturing of herbal formulations marketed in India.

Keywords: toxicological standardization, heavy metals, microbial contamination, haematinic herbal formulations

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Authors: Alok Shiomurti Tripathi, Ajay Kumar Timiri, Papiya Mitra Mazumder, Anil Chandewar

Abstract:

The present study evaluates the possible drug interaction between glimepiride (GLIM) and sildenafil citrate (SIL) in streptozotocin (STZ) induced in diabetic nephropathic (DN) animals and also postulates the possible mechanism of interaction by molecular modeling studies. Diabetic nephropathy was induced by single dose of STZ (60 mg/kg, ip) and confirms it by assessing the blood and urine biochemical parameters on 28th day of its induction. Selected DN animals were used for the drug interaction between GLIM (0.5mg/kg, p.o.) and SIL (2.5 mg/kg, p.o.) after 29th and 70th day of protocol. Drug interaction were assessed by evaluating the plasma drug concentration using HPLC-UV and also determine the change in the biochemical parameter in blood and urine. Mechanism of the interaction was postulated by molecular modeling study using Maestro module of Schrodinger software. DN was confirmed as there was significant alteration in the blood and urine biochemical parameter in STZ treated groups. The concentration of SIL increased significantly (p<0.001) in rat plasma when co administered with GLIM after 70th day of protocol. Molecular modelling study revealed few important interactions with rat serum albumin and CYP2C9.GLIM has strong hydrophobic interaction with binding site residues of rat serum albumin compared to SIL. Whereas, for CYP2C9, GLIM has strong hydrogen bond with polar contacts and hydrophobic interactions than SIL. Present study concludes that bioavailability of SIL increases when co-administered chronically with GLIM in the management of DN animals and mechanism has been supported by molecular modeling studies.

Keywords: diabetic nephropathy, glimepiride, sildenafil citrate, pharmacokinetics, homology modeling, schrodinger

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