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Anisetti R.,Osmania University | Reddy M.S.,St Peters Institute Of Pharmaceutical Science
Journal of Sulfur Chemistry | Year: 2012

An efficient synthesis of novel spiro(imidazo[4′,5′:4,5′] benzo[1,2-e][1,4]thiazepine)-9,3′-indolines has been accomplished from 5-amino-2-mercapto benzimidazole, istains and mercapto acetic acid. Compounds 6 were characterized by IR, 1HNMR, 13C NMR and mass spectral data. The title compounds 6a-6e were evaluated for their antimicrobial, anti-inflammatory and antioxidant activity. Compounds 6a-6e exhibited significant antimicrobial activity, and as potent anti-inflammatory and antioxidant activities as that shown by standard drugs. © 2012 Taylor & Francis.


Ravindernath A.,Osmania University | Reddy M.S.,St Peters Institute Of Pharmaceutical Science
Arabian Journal of Chemistry | Year: 2013

A series of novel benzo[d]imidazolyl tetrahydropyridine carboxylates 7a-n have been synthesized by one-pot multi-component reaction of (E)-5-(benzylidene amino)-1H-benzo[d]imidazole-2-thiol 3, 5-amino-2-mercapto-benzimidazole 4, aromatic aldehyde 5, and ethyl acetoacetate 6 in acetonitrile using ceric ammonium nitrate (CAN) as Lewis acid catalyst, and evaluated for their anti-inflammatory, antioxidant, antibacterial and antifungal activities. All tested compounds showed appreciable activity against the standard drugs. © 2013.


Veerareddy P.R.,Chaitanya Institute of Pharmaceutical Education and Research | Bobbala S.K.R.,St Peters Institute Of Pharmaceutical Science
Drug Development and Industrial Pharmacy | Year: 2013

The objective of the present research was to develop a proniosomal formulation of isradipine and to evaluate the influence of proniosomal systems on the oral bioavailability of the drug in albino Wistar rats. Proniosomes were prepared by film deposition on carrier's method using various molar ratios of nonionic surfactants such as span20, span40, span60, and span80 with cholesterol as membrane stabilizing agent and dicetylphosphate as a charge inducer. The formation of niosomes and surface morphology of proniosome formulations were studied by optical and scanning electron microscopy (SEM), respectively. The prepared proniosomes have shown higher dissolution of isradipine compared with pure drug powder. Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffractometry studies were performed to understand the solid state properties of the drug. Ex vivo permeation enhancement assessed from flux, permeability coefficient, and enhancement ratio were significantly higher for proniosomes compared with control. The pharmacokinetic parameters were evaluated in male albino Wistar rats and a significant enhancement in the bioavailability (2.3-fold) was observed from optimized proniosome formulation compared with control (oral suspension). The stability study reveals that the proniosome formulations are stable when stored at 4°C. © 2013 Informa Healthcare USA, Inc.


Suresh P.,St Peters Institute Of Pharmaceutical Science | Kavitha C.N.,St Peters Institute Of Pharmaceutical Science | Babu S.M.,St Peters Institute Of Pharmaceutical Science | Reddy V.P.,St Peters Institute Of Pharmaceutical Science | Latha A.K.,St Peters Institute Of Pharmaceutical Science
Inflammation | Year: 2012

Trigonella foenum graecum is an Iranian medicinal plant used for the treatment of rheumatoid arthritis and inflammation. The present study was designed to investigate the beneficial outcome of the plant T. foenum graecum on adjuvant-induced arthritis in albino rats. Ethanol extract of T. foenum graecum was tested against Freund's complete adjuvant-induced arthritis in rats. In the present study, paw volume was measured on the 4th, 8th, 14th and 21st day. On day 22, animals were anaesthetized, and blood samples were collected for the estimation of haemoglobin, white blood cells (WBC), differential white blood cells, erythrocyte sedimentation rate (ESR), red blood cells (RBC), interleukins (IL-1a, IL-1β, IL-2, IL-6) and tumour necrosis factor-a (TNF-a). The animals were sacrificed, and the cartilage tissue was isolated for estimation of lipid peroxidation (LPO), superoxide dismutase (SOD) and glutathione (GSH). Administration with both doses of T. foenum graecum (200 and 400 mg/kg) significantly (P<0.05) decreased the paw oedema and restored body weight. T. foenum graecum significantly (P<0.05) reduced the differential WBC count, ESR and WBC (5.833±0.703, 6.989±58.5) content and also showed significant (P<0.05) increase in RBC and Hb (4.783±0.46, 15.46±0.158) content. T. foenum graecum significantly (P<0.05) decreased the IL-1a, IL-1β, IL-2, IL-6 and TNF-a levels. It also significantly decreased the levels of LPO and increased the SOD and GSH levels in cartilage tissue. In this study, T. foenum graecum 400-mg/kg dose showed more prominent results compared to the 200-mg/kg dose of T. foenum graecum. The results obtained in this study suggest that anti-inflammatory and antioxidant activities of T. foenum graecum may be the possible reason behind the observed anti-arthritic activity. © 2012 Springer Science+Business Media, LLC.


Alikatte K.L.,St Peters Institute Of Pharmaceutical Science | Akondi B.R.,St Peters Institute Of Pharmaceutical Science | Yerragunta V.G.,St Peters Institute Of Pharmaceutical Science | Veerareddy P.R.,St Peters Institute Of Pharmaceutical Science | Palle S.,St Peters Institute Of Pharmaceutical Science
Brain and Development | Year: 2012

We evaluated the Antiamnesic effects of methanolic extract of Syzygium cumini (MESC) on spatial memory impairments induced by scopolamine (1. mg/kg, i.p.), a muscarinic antagonist, using the Radial arm maze, Morris water maze, learned helpless ness tests. Effect of MESC was evaluated and compared to standard drug, piracetam (200. mg/kg, i.p.). The MESC significantly (p< 0.05) improved the impairment of short term or working memory induced by scopolamine in the Radial arm maze test, and significantly (p< 0.05) reversed cognitive impairments in rats as measured by the learned helplessness test. In addition, MESC decreased escape latencies in the Morris water maze test. The activity of acetylcholinesterase in the brain was inhibited significantly (p< 0.05) by treatment with MESC to a level similar to that observed in rats treated with piracetam. Moreover treatment with MESC (200 and 400. mg/kg, p.o.) to scopolamine induced rats significantly (p< 0.05) decreased TBARS levels which was accompanied by an increase in the activities of SOD and Catalase. MESC has dose dependent effect and 400. mg/kg dose shown more prominent results when compared to 200. mg/kg dose of MESC. These results indicate that MESC may exert anti-amnesic activity via inhibition of acetylcholinesterase and antioxidant mechanisms in the brain. © 2012 The Japanese Society of Child Neurology.


Anil M.,St Peters Institute Of Pharmaceutical Science
International Journal of Pharma and Bio Sciences | Year: 2014

Stroke is the second leading cause of death. Ischemia leads to cellular dysfunction and necrosis. Wistar albino rats were treated with alcoholic extract of Bauhinia variegata (200 and 400 mg/kg; p.o) for 15 days prior to Ischemia/Reperfusion. Ascorbic acid (50 mg/kg) was used as a reference standard. Ischemia/Reperfusion was induced by occluding common carotid arteries for 25 min, followed by 40 min reperfusion. Ischemia/Reperfusion caused significant depletion in superoxide dismutase, catalase, glutathione and significant increase in LPO in brain homogenate. All the alterations induced by cerebral ischemia were significantly attenuated by pretreatment with bark extract at the doses of 200 and 400 mg/kg, and the effect was comparable to that of ascorbic acid (p value < 0.05). In conclusion alcoholic bark extract containing the flavonoids and phenolic antioxidants was found to protect rat brain against Ischemia/Reperfusion induced oxidative stress, and the observed effect may be attributed to its antioxidant properties.


Suresh P.,St Peters Institute Of Pharmaceutical Science | Raju A.B.,St Peters Institute Of Pharmaceutical Science
Neurosciences | Year: 2013

Objectives: To evaluate the effect of leucine and genistein on the dopaminergic system in a rat model of schizophrenia. Methods: Behavioral effects of leucine and genistein on apomorphine induced stereotyped behavior, haloperidol induced catalepsy, foot shock induced aggression, and apomorphine induced locomotor activity were conducted. In each of these tests, the leucine (0.7g/kg p.o.) and genistein (30mg/kg i.p.) were administered 30 minutes before performing the test in rats. Each experiment has 6 groups of rats with 6 rats in each group. The current study was conducted between April 2011 and September 2011 at the Department of Pharmacology, St.Peters Institute of Pharmaceutical Sciences, Warangal, Andhra Pradesh, India. The results were expressed as mean ± S.E.M. and the statistical analysis of data was carried out using one-way analysis of variance (ANOVA), followed by Bonferroni multiple comparison test. Probability level (P) less than 0.05 was considered statistically significant. Results: Leucine and genistein significantly (p<0.05) reduced the number of fights and increased latency to fights in foot shock-induced aggression; it also decreased apomorphine (5mg/kg, i.p.) induced stereotyped behavior and apomorphine induced (10mg/kg, s.c.) locomotor activity when compared with the positive control group. Pretreatment with leucine and genistein significantly (p<0.01, 55.5±5.898 minutes) potentiated the haloperidol induced catalepsy compared with the haloperidol treated group. Conclusion: The individual administration of leucine and genistein had less anti dopaminergic activity when compared with their combined administration. These results suggest that leucine and genistein may have a potential clinical application in the management of psychiatric disorders.


Kallakunta V.R.,St Peters Institute Of Pharmaceutical Science | Bandari S.,St Peters Institute Of Pharmaceutical Science | Jukanti R.,St Peters Institute Of Pharmaceutical Science | Veerareddy P.R.,St Peters Institute Of Pharmaceutical Science
Powder Technology | Year: 2012

The current investigation was aimed to improve the solubility of poorly soluble lercanidipine hydrochloride as self emulsifying powder (SEP). Liquid SEDDS of LCH was formulated with Capmul MCM L8 as oil, Tween (R) 80 as surfactant and PEG 400 as co surfactant after screening various vehicles. The prepared formulations were evaluated for self emulsifying ability and phase diagram was constructed to optimize the system. These systems were further characterized for globule size, effect of pH and robustness to dilution, cloud point, thermodynamic stability, surface morphology and drug release. The system was robust to different pH media and dilution volumes. The optimized system possessed a mean globule size of 169. ±. 06. nm and cloud point of 76. °C. The self emulsifying powder was prepared by adsorbing the liquid SEDDS on to neusilin as carrier. The SEP formulated was free flowing with similar emulsification characteristics as that of liquid SEDDS. The X-ray diffraction, Differential Scanning Calorimetric studies of SEP revealed transformation of crystalline structure of LCH because of its molecularly dissolved state in the liquid SEDDS. This was further confirmed by scanning electron microscopy. High dissolution efficiency value of SEP compared with pure drug indicated the increase in dissolution characteristics of LCH in SEP. © 2012 Elsevier B.V.


Potluri R.H.K.,St Peters Institute Of Pharmaceutical Science | Bandari S.,St Peters Institute Of Pharmaceutical Science | Jukanti R.,St Peters Institute Of Pharmaceutical Science | Veerareddy P.R.,St Peters Institute Of Pharmaceutical Science
Archives of Pharmacal Research | Year: 2011

The objective of the study was enhancement of dissolution of poorly soluble carvedilol by solid dispersions (SDs) with Gelucire 50/13 using solvent evaporation method. The solubility of carvedilol showed linear increase with increasing concentrations of Gelucire indicating AL type solubility diagrams. SDs characterized for physicochemical characteristics using differential scanning calorimetry and X-ray diffractometry revealed transformation of crystalline form of drug to amorphous form which was confirmed by scanning electron micrographs. Further fourier transform infrared spectroscopy results suggested there is no drug carrier interaction. From the dissolution parameters such as mean dissolution time, dissolution efficiency and drug release rate, improved dissolution characteristics for SDs were observed compared with physical mixture and pure drug. Thus SDs of carvedilol in Gelucire 50/13 showed enhanced solubility and dissolution rate compared to pure drug. © 2011 The Pharmaceutical Society of Korea and Springer Netherlands.


Eedara B.B.,St Peters Institute Of Pharmaceutical Science | Veerareddy P.R.,St Peters Institute Of Pharmaceutical Science | Jukanti R.,St Peters Institute Of Pharmaceutical Science | Bandari S.,St Peters Institute Of Pharmaceutical Science
Drug Development and Industrial Pharmacy | Year: 2014

The aim of the present study was to improve the dissolution, permeability and therefore oral bioavailability of the fexofenadine hydrochloride (FEX), by preparing lipid surfactant based dispersions using self-emulsifying carriers, i.e. Gelucire 44/14 (GLC) and d-α-tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS or TPGS). The reprecipitation studies were conducted using these carriers to evaluate inhibition of reprecipitation by maintaining super saturation state. The aqueous solubility of the FEX was increased linearly with increasing GLC, TPGS concentrations as verified by the phase solubility studies. The dispersions of FEX were prepared in different drug/GLC (GD) and drug/TPGS (TD) ratios by melt method and evaluated. The prepared dispersions showed improved dissolution rate in distilled water as dissolution media and highest dissolution rate was achieved with dispersions prepared using TPGS. The solid state characterization was carried by differential scanning calorimetry and scanning electron microscopy indicated reduced crystallinity of the drug. Fourier transform infrared spectroscopy revealed the compatibility of drug with carriers. The ex vivo permeation studies conducted using intestinal gut sac technique, resulted in reduced efflux of the drug by inhibiting intestinal P-glycoprotein from the dispersions. The in situ perfusion studies and in vivo pharmacokinetic studies in male wistar rats showed improved absorption and oral bioavailability from the prepared dispersions as compared to pure drug. © 2014 Informa Healthcare USA, Inc.

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