Vaagdevi Institute of Pharmaceutical science

Warangal, India

Vaagdevi Institute of Pharmaceutical science

Warangal, India
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Palle S.,Vaagdevi Institute of Pharmaceutical science | Kanakalatha A.,St Peters Institute of Pharmaceutical science | Kavitha C.N.,Nirmala Institute of Pharmaceutical science
Journal of Dietary Supplements | Year: 2017

Peptic ulcer is a recurrent chronic illness and has become almost a hallmark of the so-called civilized life. In folk medicine, the Celastrus paniculatus plant has been used for the prevention and treatment of various diseases and gastrointestinal disturbances, including dyspepsia and stomach ulcers. The aim of this study is to evaluate the gastroprotective and antiulcer effects of Celastrus paniculatus seed oil (CPO) against several gastric ulcer models in rats. The gastroprotective and antiulcer effects of CPO were evaluated using pylorus-ligated ulcer ethanol- and indomethacin-induced ulcers using rantidine (40 mg/kg per os [PO]) as standard. Gastrointestinal motility was determined by gastric emptying time and gastrointestinal transit ratio. The results of the pharmacological studies of CPO (200 mg/kg, 400 mg/kg) demonstrated effective gastroprotection against ethanol- and indomethacin-induced ulcer models. In pylorus-ligated rats, the seed oil showed gastroprotective activity by decreasing total gastric juice volume and gastric acidity while increasing the gastric pH. The gastroprotection against ethanol and indomethacin is partially attributed to effective inhibition of proinflammatory cytokines, TNF-α and IL-6, and increase in the levels of IL-10. Treatment with CPO in ethanol-induced ulcer rats significantly (p < .05) decreased MDA (malondialdehyde) levels, which were accompanied by an increase in the activities of SOD (superoxide dismutase) and catalase. CPO reduced the rate of gastric emptying but had no effect on gastrointestinal transit. The present findings indicate that CPO has potent gastroprotective effects and support the folkloric usage of the seed oil to treat various gastrointestinal disturbances. © 2017 Taylor & Francis Group, LLC


Chaitanya G.,Jawaharlal Nehru Technological University | Prakash P.,Vaagdevi Institute of Pharmaceutical science | Eswar Kumar K.,Andhra University
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2013

Objective: The study was undertaken to find out the influence of amiodarone on the pharmacodynamic activity of gliclazide following single and multiple dose treatment in normal and diabetic rats, normal rabbits. Methods: Studies were conducted in normal rats, diabetic rats and normal rabbits following oral doses of gliclazide, amiodarone and their combination with adequate washout between each period. Serial blood samples were collected through retro-orbital plexus in rats and marginal ear vein in rabbits at regular intervals and analyzed for glucose by glucose oxidase/peroxidise method. Results: Gliclazide produced biphasic reduction of blood glucose levels in normal and diabetic rats with maximum activity attained at 2 h and 8 h. In rabbits, maximum hypoglycemic activity is observed at 4 h post dose. Amiodarone per se has negligible hypoglycemic activity, but in combination with gliclazide produced a marked reduction of blood glucose levels in rats/rabbits with more significant effect observed at multiple dose than at single dose treatment. A significant hypoglycemic effect is observed at the terminal elimination phase in combination treated rabbits following single and multiple dose amiodarone whereas negligible hypoglycemic activity at 24 h is observed following gliclazide alone. Literature indicates that amiodarone is known to be weak inhibitor of CYP2C9, CYP3A4 and CYP2D6 isozymes. Thus amiodarone appears to affect the isozymes responsible for gliclazide hydroxylation (CYP2C9 and CYP3A4) resulting in prolongation of its half-life and hypoglycemic activity. Conclusions: There observed to be an interaction between the two drugs, but the interaction seems to be not of pharmacodynamic type. However the combination warrants close monitoring of blood glucose levels when such drugs are co administered.


Butreddy A.,Jangaon Institute of Pharmaceutical science | Dudhipala N.,Vaagdevi Institute of Pharmaceutical science
Asian Journal of Pharmaceutics | Year: 2015

Trandolapril (TLP), is an antihypertensive agent, administered orally. It is having low oral bioavailability (4-9%) due to poor aqueous solubility, it undergoes CYP3A4 mediated hepatic first-pass metabolism. Liquisolid compact (LSC), the technique has the potential to improve the oral bioavailability by increasing solubility and dissolution rate of poorly water-soluble drugs. In the present work, TLP LSCs were prepared with polyethylene glycol-400 as a vehicle, Avicel, Neusilin as carriers and Aerosil as coating material. LSC and sustained release tablets of LSC containing hydroxypropyl methylcellulose K15M polymer, were prepared by direct compression method and characterized for hardness, friability, drug content and in vitro release studies in pH 6.8 phosphate buffer for LSC and 0N HCl for 2 h followed by pH 6.8 phosphate buffer for subsequent hours for SR LSC, using USP type-1 apparatus. Solid state characterization of TLP and TLP-LSC was examined using differential scanning calorimeter (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) studies. Physical parameters of the prepared LSC tablets were found to be within the acceptable limits. In vitro dissolution studies of optimized SR LSC (F3) formulation had shown sustained drug release of 97.3 ± 2.59% in 14 h with Peppas model (r2 = 0.981) followed by non-Fickian diffusion (n = 0.659) mechanism, whereas LSC tablets showed 94.1 ± 3.11% drug release in 120 min. DSC and XRD analysis indicated that TLP was amorphous form in LSC mixture. SEM studies revealed that TLP was adsorbed onto the surface of carrier material compared with the pure drug having needle-shaped crystal lattice. Therefore, LSC technique can improve the solubility and dissolution rate of poorly water-soluble drug such as TLP.


Gurunath S.,Vaagdevi Institute of Pharmaceutical science | Pradeep Kumar S.,Vaagdevi Institute of Pharmaceutical science | Patil P.A.,Vaagdevi Institute of Pharmaceutical science
Journal of Pharmacy Research | Year: 2013

Amorphous solid dispersions are one of the most promising strategies to improve the oral bioavailability of sparingly water-soluble drugs. Drug particle size reduction improved the drug wettability and bioavailability significantly. Poorly soluble drugs may benefit from formulation approaches that overcome poor solubility and dissolution rate limited bioavailability. The solubility of a compound in the amorphous form is higher than the more stable crystalline form because the Gibbs free energy is higher. In addition, glasses or amorphous forms are kinetically trapped high energy disordered materials that lack the periodicity of crystals but behave mechanically as solids. Lipophilic molecules, especially those belonging to the biopharmaceutics classification system (BCS) class II and IV, dissolve slowly, like incomplete release from the dosage form, poor bioavailability, increased food effect, and high inter-patient variability. Hence, several formulation approaches can be taken to improve the solubility and dissolution of poorly water-soluble compounds, such as formulating the API in an amorphous form. Amorphous solid dispersions of poorly water-soluble drugs with water-soluble carriers have been reduced the incidence of these problems and enhanced dissolution. This review is mainly focus on advantages, methods of preparation, and characterization of the amorphous solid dispersion. © 2013, JPR Solutions; Published by Reed Elsevier India Pvt. Ltd.


Gurunath S.,Vaagdevi Institute of Pharmaceutical science | Patil P.A.,KLE University
Drug Development and Industrial Pharmacy | Year: 2015

Objective: The aim of the study is to explore the pharmacokinetic behavior of candesartan solid dispersions prepared by different pharmaceutical interventions using P-gp inhibitor in rabbits to validate the effectiveness of naringin as a pharmaceutical excipient in enhancing the oral delivery of lipophilic candesartan cilexetil. Methods: Male albino rabbits (1-1.5kg) were orally administered pure CAN suspensions and various candesartan solid dispersions (10mg/kg) with and without naringin (15mg/kg) and blood samples were collected at specified time points. CAN plasma samples were measured using HPLC. Key findings: After oral dosing of pure CAN suspension, the mean AUC0-8h was found to be 0.14±0.09μgh/ml which was increased significantly, i.e. 0.52±0.13μgh/ml with freeze-dried solid dispersions in the presence of naringin (p<0.01). Similarly, the mean Cmax of pure CAN suspension increased from 35.81±0.13μg/ml (without naringin) to 112.23±0.13μg/ml (freeze-dried solid dispersions with naringin) (p<0.01). A 3.7-folds increase in apparent bioavailability was noticed with freeze-dried solid dispersions with naringin as compared to free CAN suspension administered alone. Conclusion: These results are quite stimulating for further development of a clinically useful oral formulation of candesartan cilexetil based on P-gp inhibition using naringin, a natural flavonoid as a pharmaceutical excipient. © 2015 Informa Healthcare USA, Inc. All rights reserved.


Reddy N.D.,Vaagdevi Institute of Pharmaceutical SciencesTelangana | Reddy N.D.,Vaagdevi Institute of Pharmaceutical science | Reddy A.B.,Vaagdevi Institute of Pharmaceutical SciencesTelangana
Drug Research | Year: 2017

Clarithromycin (CM), a broad spectrum macrolide antibiotic used to eradicate H. pylori in peptic ulcer. Clarithromycin (CM) is well absorbed from the gastrointestinal tract, but has a bioavailability of 50% due to rapid biodegradation. The aim of this investigation was to increase the gastric residence time, and to control the drug release of clarithromycin by formulating into multiple unit floating mini-tablets. Floating tablets were prepared by using direct compression method with HPMC K 4 M and Polyox WSR 1105 as release retarded polymers and sodium bicarbonate as gas generating agent. The prepared mini-tablets were evaluated for thickness, weight variation, friability, hardness, drug content, in vitro buoyancy, swelling studies, in vitro dissolution studies by using modified Rossett-Rice test and in vivo radiographic studies in healthy human volunteers in fasting conditions. DSC analysis revealed that no interaction between drug and excipients. All the physical parameters of the tablets were within the acceptable limits. The optimized formulation (F6) had showed controlled drug release of 99.16±3.22% in 12 h, by zero-order release kinetics, along with floating lag time of 9.5±1.28 s and total floating time of 12±0.14 h. X-ray imaging studies revealed that in vivo gastric residence time of clarithromycin floating mini-tablet in the stomach was about 3.5 h. The results demonstrated that the developed floating mini-tablets of clarithromycin caused significant enhancement in gastric retention time along with sustained effect and increased oral bioavailability. © Georg Thieme Verlag KG Stuttgart, New York.


PubMed | KLE University, Vaagdevi Institute of Pharmaceutical science and Omer Al Mukhtar University
Type: Comparative Study | Journal: Drug delivery | Year: 2016

To assess the effect of naringenin on the intestinal biochemical composition, function and histology for gastrointestinal toxicity since it has not yet been adequately exploited for safety through standard assays.Here, we describe naringenin (1mM, 10mM and 100mM, respectively) or sodium deoxycholate (10mM) effects on isolated brush border membrane from intestinal segments with single pass intestinal perfusion using lactate dehydrogenase, alkaline phosphatase and protein assays. MTT assay was used for cytotoxicity studies. Everted gut sac studies were used for evaluating the transport of nutrients across the intestinal segments. Lucifer yellow was used for paracellular permeability, followed by histological changes and surface characteristic studies of intestinal sacs.The results indicated no significant alterations with naringenin, although significant (p<0.01) changes were noticed with sodium deoxycholate in the activity of the rat intestinal brush border associated enzymes such as LDH, followed by intact cell viability with marked decrease in the villi height of the intestinal segments.These observations indicate that naringenin was harmless upon exposure to rat gastrointestinal epithelium, clearly demonstrating the potential use of naturally occurring bioflavonoid as safe and novel pharmaceutical adjuvant in oral dosage forms as P-gp inhibitor.


PubMed | KLE University, Vaagdevi Institute of Pharmaceutical science and Omer Al Mukhtar University
Type: Journal Article | Journal: The Journal of pharmacy and pharmacology | Year: 2015

In this study, a comprehensive and comparative cytotoxic evaluation of morin against verapamil on rat intestinal epithelium as P-gp inhibitors through in-vitro gastrointestinal short-term toxicity assays involving permeability studies for safety evaluation was investigated.In this study, the effect of morin (1mM or 10mM) or verapamil (1mM or 10mM) or sodium deoxycholate (10mM) was investigated on intestinal epithelium and isolated brush border membrane using biomarker assays. Cytotoxicity was determined using 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay. The nutrients transport was assessed using everted sacs studies. Paracellular permeability was measured using Lucifer yellow, followed by morphometric analysis of intestinal sacs.Our results indicated that morin was effective in maintaining cell viability with no significant changes (P>0.05) in the activity of intestinal brush border markers, membrane integrity and morphometric analysis as compared with control. On the contrary, dramatic (P<0.01) changes were noticed in the release of membrane markers, cell viability and surface characteristics of intestinal segments when treated with verapamil or sodium deoxycholate as compared with control or morin.Our findings confirm that morin is non-toxic to rat intestinal epithelium against verapamil demonstrating the potential use of bioflavonoid as safe and novel pharmaceutical adjuvant as P-gp inhibitor.


PubMed | Vaagdevi institute of pharmaceutical science and Kakatiya University
Type: | Journal: Drug research | Year: 2016

Isradipine (ID), is an antihypertensive drug, having low oral bioavailability (15-24%) due to poor aqueous solubility (0.01mg/mL) and also hepatic first-pass metabolism. Among various approaches, Solid lipid nanoparticles (SLNs) were developed using stearic acid, glyceryl monostearate as lipid matrices for improving the oral bioavailability of ID. ID-SLNs were prepared by using hot homogenization followed by ultrasonication. The prepared SLNs were characterized for size, PDI, zeta potential (ZP), entrapment efficiency (EE) and drug content.


Prasad D.K.,Vaagdevi Institute of Pharmaceutical science | Spoorthy S.,Vaagdevi Institute of Pharmaceutical science
International Journal of Pharmacy and Technology | Year: 2015

Inflammation is a pathophysiological response of living tissue to injury that leads to local accumulation of plasmatic fluid and blood cells. In recent years, research is focused on existing molecules and their modifications in order to reduce their side effects and to explore their pharmacological and biological effects. Most of anti-inflammatory drugs exert their beneficial effect by inhibiting either release of lysosomal enzymes orstabilizing membrane. Isatin Spiropyrazoline is an endogenous compound and it has a wide variety of pharmacological activities like anticancer, anti-inflammatory, antifungal and antibacterial. Anti-inflammatory was evaluated in animal models with a doses of 75 and 150 mg/kg as a test doses and using diclofenac (0. 45mg/kg) as a standard. Anti-inflammatory activity by carrageenan induced rat paw edema and cotton pellet granuloma, respectively the % inhibition of paw volume and granuloma tissue. Synthetic test compound (ISP) shows high significant with (***p<0. 001) level of inhibition against proteinases which is implicated in the development of inflammation which is further supported by the biochemical parameters SGPT, SGOT and ALP showed extremely significant(***P<0. 001),which helps to conclude the result that test compound able to reduce the enzyme activity which is the main cause of the inflammation. Inhibition of albumin denaturation and proteinase inhibitory activity, the test compound (ISP) showed anti-inflammatory activity with dose dependent effect when compared with the control group. In inflammatory condition 150mg/kg dose of the test drug possessed greater significance (***p<0. 001), the results of experimental findings suggest that ISP act as anti-inflammatory activity in the treatment of inflammation. © 2015, International Journal of Pharmacy and Technology. All rights reserved.

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