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Sonīpat, India

Aggarwal A.K.,Rayat Institute of Pharmacy | Gupta M.,A And G Pharmaceutical, Inc.
Drug Development and Industrial Pharmacy | Year: 2012

Objective: The aim of the present study was to prepare the amino acid prodrugs of bromhexine hydrochloride to improve its solubility. Methods: All the prodrugs were synthesized by first reacting bromhexine with tert-butoxycarbonyl (Boc) protected amino acid and then deprotection was carried out by using trifluoroacetic acid. These prodrugs were characterized by their melting points, NMR, mass and FTIR spectroscopy. Solubility and partition coefficient of bromhexine and various prodrugs were determined. The solution stability of various prodrugs was also determined in various buffers of pH ranging from 2 to 10. Degradation rate constants and half-life were also determined at various pH. Results and discussion: The structures of all the synthesized prodrugs were confirmed by NMR, mass and FTIR spectra. The prodrug 2-N-l-alanyl-bromhexine hydrochloride showed maximum solubility and minimum partition coefficient value. These prodrugs may hydrolyze by one or more mechanisms. The order of decreasing rates of hydrolysis was 2-N-l-prolyl-bromhexine hydrochloride > 2-N-glycyl-bromhexine hydrochloride > 2-N-l-alanyl-bromhexine hydrochloride. All the prodrugs exhibited maximum stability in the acidic pH range and undergo base catalyzed hydrolysis. Conclusion: Solubility studies and partition coefficient values indicated that the synthesized prodrug, 2-N-l-alanyl- bromhexine hydrochloride, was least lipophilic as compared to other synthesized prodrugs. Solution stability studies showed that this prodrug undergo minimum hydrolysis at 37°C. So, it is concluded that 2-N-l-alanyl-bromhexine hydrochloride exhibits better solubility and stability as compared to other synthesized prodrugs. © 2012 Informa Healthcare USA, Inc. Source

Muthuraman A.,Punjabi University | Muthuraman A.,Rayat Institute of Pharmacy | Ramesh M.,National Institute of Pharmaceutical Education and Research | Sood S.,Rayat Institute of Pharmacy
Life Sciences | Year: 2012

Aims: Ischemia -reperfusion (I/R) event in vascular and nervous system has been documented to rising ischemic and vasculitic neuropathic pain, clinically resembles the complex regional pain syndrome (CRPS). The present study evaluated the effect of montelukast, a cysteinyl leukotriene receptor (Cys-LTC 4 and Cys-LTD 4) antagonist on ischemia -reperfusion (I/R) induced vasculitic neuropathic pain in rats. Main Methods: Behavioral parameters were assessed at different time intervals (i.e. 0, 1, 7, 14 and 21st day) and biochemical analysis in sciatic nerve tissue samples were also performed along with histopathological studies. Key Findings: Behavioral pain assessment has shown increase in paw and tail withdrawal threshold in montelukast treated groups against thermal and mechanical stimuli as compared to I/R control group. We observed a decrease in the total calcium, thiobarbituric acid reactive substance (TBARS) and myeloperoxidase (MPO) activity levels, whereas there is rise in reduced glutathione level in montelukast treated groups as compared to I/R control group. However, significant behavioral and biochemical results were observed only in medium and high dose of treated groups which were comparable to normal control group. Moreover, histopathological study has revealed the reduction of I/R induced neuronal edema and axonal degeneration due to montelukast. Significance: Montelukast has ameliorated I/R induced vasculitic neuropathic pain, these effects may be due to inhibition of lipid peroxidation, reduction of oxidative stress, release of inflammatory mediators and neuroprotective actions. Hence, it could be used as a novel therapeutic agent for the management of vasculitic inflammation related neuropathic pain. © 2012 Elsevier Inc. Source

Sharma N.,Rayat Institute of Pharmacy | Bafna P.,Rayat Institute of Pharmacy
Oriental Pharmacy and Experimental Medicine | Year: 2012

In the present study, the aqueous extract of Cynodon dactylon (AECD) Pers. (Graminae) was evaluated for anti-parkinson's activity in rats. The anti-parkinson's effect of AECD was studied against rotenone (2 mg/kg, s. c.) - induced parkinsons in rats. In this study, chronic administration of rotenone in rats (28 days) produced motor dysfunctions like catalepsy and muscle rigidity along with a reduction in locomotor activity. Rotenone administration was also found to generate oxidative stress in the brain as evident from an increase in the level of TBARS and decrease in the levels of SOD and GSH. Pretreatment with AECD resulted in a significant (p <0.001) decrease in catalepsy and muscle rigidity along with a significant (p <0.001) increase in locomotion as compared to the rotenone-treated control group. AECD treated rats also showed a reduction in the TBARS level and an increase in the GSH, SOD and CAT levels; thus reducing the oxidative stress in the brain of animals. The study thus proved that Cynodon dactylon treatment significantly attenuated the motor defects and also protected the brain from oxidative stress, both induced by rotenone. These results strongly indicate the possible therapeutic potential of Cynodon dactylon as an antioxidant in Parkinson's disease and other movement disorders. © 2012 Institute of Oriental Medicine, Kyung Hee University. Source

Muthuraman A.,Rayat Institute of Pharmacy | Sood S.,Rayat Institute of Pharmacy
Journal of Brachial Plexus and Peripheral Nerve Injury | Year: 2010

Background: Ischemia reperfusion (I/R) is common in various pathological conditions like diabetic complication, rheumatic arthritis, necrotizing vascular occlusive disease and trauma.Methods: We have evaluated the effect of tacrolimus (1, 2 and 3 mg/kg, p.o. for 10 consecutive days) on femoral arterial ischemic reperfusion (I/R) induced neuropathic pain in rats. Behavioral parameters (i.e. hot plate, radiant heat, acetone drop, tail heat hyperalgesia, tail flick and tail cold allodynia tests) were assessed at different time intervals (i.e. 0, 1, 4, 7, 10, 13 and 16thday) and biochemical analysis in serum and tissue samples were also performed along with histopathological studies.Results: Behavioral pain assessment revealed increase in the paw and tail withdrawal threshold in tacrolimus treated groups against hyperalgesic and allodynic stimuli as compared to the sham control group. We observed a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, rise in tissue reduced glutathione levels in tacrolimus treated groups. However, significant results were obtained in medium and high dose treated group as compared to sham control group. Histopathological study had revealed the increase in the neuronal edema and axonal degeneration in the I/R group whereas, tacrolimus ameliorate these effects.Conclusion: Our results indicate the anti-oxidative, anti-inflammatory and calcium modulatory actions of tacrolimus. Therefore, it can be used as a therapeutic agent for the treatment of vascular inflammatory related neuropathic pain. © 2010 Muthuraman and Sood; licensee BioMed Central Ltd. Source

Vij T.,Rayat Institute of Pharmacy | Prashar Y.,Rayat Institute of Pharmacy
Asian Pacific Journal of Tropical Disease | Year: 2015

Papaya (Carica papaya L.) is a popular and important fruit tree in tropical and subtropical parts of the world. The fruit is consumed worldwide as fresh fruit and vegetable or used as processed product. The fruit is healthy and delicious and the whole plant parts including fruit, root, bark, peel, seeds and pulp are also known to have medicinal properties. The many benefits of papaya are owed due to high content of vitamin A, B and C, proteolytic enzymes like papain and chymopapain which have antiviral, antifungal and antibacterial properties. During the last few years, major insight has been achieved regarding the biological activity and medicinal application of papaya and now it is considered a valuable neutraceutical fruit plant. In the present review, nutritional value of the fruit and medicinal properties of its various parts have been discussed to provide collective information on this multipurpose commercial fruit crop. © 2015 Asian Pacific Tropical Medicine Press. Source

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