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Reddy G.S.,Manipal University India | Nayak U.Y.,Manipal University India | Deshpande P.B.,Manipal University India | Deshpande P.B.,Unichem Laboratories Ltd | Mutalik S.,Manipal University India
Scientific World Journal | Year: 2014

The present study was aimed at the development of gastroretentive floating pulsatile release tablets (FPRTs) of lercanidipine HCl to enhance the bioavailability and treat early morning surge in blood pressure. Immediate release core tablets containing lercanidipine HCl were prepared and optimized core tablets were compression-coated using buoyant layer containing polyethylene oxide (PEO) WSR coagulant, sodium bicarbonate, and directly compressible lactose. FPRTs were evaluated for various in vitro physicochemical parameters, drug-excipient compatibility, buoyancy, swelling, and release studies. The optimized FPRTs were tested in vivo in New Zealand white rabbits for buoyancy and pharmacokinetics. DoE optimization of data revealed FPRTs containing PEO (20% w/w) with coat weight 480 mg were promising systems exhibiting good floating behavior and lag time in drug release. Abdominal X-ray imaging of rabbits after oral administration of the tablets, confirmed the floating behavior and lag time. A quadratic model was suggested for release at 7th and 12th h and a linear model was suggested for release lag time. The FPRT formulation improved pharmacokinetic parameters compared to immediate release tablet formulation in terms of extent of absorption in rabbits. As the formulation showed delay in drug release both in vitro and in vivo, nighttime administration could be beneficial to reduce the cardiovascular complications due to early morning surge in blood pressure. © 2014 Gagganapalli Santhoshi Reddy et al. Source


Lalan B.K.,Unichem Laboratories Ltd | Hiray R.S.,B J Government Medical College And Sassoon General Hospitals | Ghongane B.B.,B J Government Medical College And Sassoon General Hospitals
Journal of Clinical and Diagnostic Research | Year: 2015

Background: Long term use of NSAIDs, opioids and corticosteroids was associated with serious adverse effects. Hence, the search for a safer analgesic and anti-inflammatory agent was always going on. It was considered worthwhile to evaluate analgesic and anti-inflammatory activities of Holoptelea integrifolia and Argyreia speciosa. Aim: To evaluate analgesic and anti-inflammatory activities of aqueous extract of leaves of Holoptelea Integrifolia and methanolic extract of Argyreia Speciosa root powder in mice and rats. Materials and Methods: After obtaining permission from animal ethics committee, the animals were divided into 7 groups of 6 animals each {control, standard – ibuprofen 100mg/kg, Holoptelea integrifolia (250 and 500 mg/kg), Argyreia speciosa (100 and 300 mg/kg) and combination of Holoptelea integrifolia (250 mg/kg) and Argyreia speciosa (100 mg/kg)}. The analgesic activity of the extracts was evaluated using tail-flick with radiant heat and acetic acid induced writhing method and the anti-inflammatory activity was evaluated using carrageenan induced paw oedema method. Statistical Analysis: One-way ANOVA followed by post-hoc test. p < 0.05 was considered to be significant. Results: In tail-flick method, both Holoptelea integrifolia and Argyreia speciosa produced significant (p<0.05) increase in latency as compared to control, their combination showed a significant increase in latency as compared to control as well as to the standard – ibuprofen. In writhing method, Holoptelea integrifolia and Argyreia speciosa, alone and in combination, significantly decreased the number of writhes as compared to control. In paw oedema method, both Holoptelea integrifolia and Argyreia speciosa showed significant inhibition of paw oedema as compared to control and the activity was comparable to ibuprofen. Conclusion: Extracts of Holoptelea integrifolia and Argyreia speciosa exhibits significant central and peripheral analgesic and anti-inflammatory activity. © 2015, Journal of Clinical and Diagnostic Research. All rights reserved. Source


The present invention is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: wherein R, R and X are as described in the specification.


Mehta K.C.,Dr. Suchak Hospital | Rdargad R.,Lilavati Hospital and Research Center | Borade D.M.,Unichem Laboratories Ltd | Swami O.C.,Unichem Laboratories Ltd
Journal of Clinical and Diagnostic Research | Year: 2014

Globally, antimicrobial resistance is alarming concern especially in commonly reported disease entities like respiratory tract infection, enteric fever and infections associated with gram-negative bacilli (GNB). Rational use of antimicrobial drugs reported significant decrease in bacterial burden and may also reduce the risk of disease progression. However, at times in particular indication, certain patient and pathogen factor limits the selection and use of specific antibiotic therapy while in some case, due to presence of additional risk factor, aggressive therapy is required to achieve clinical reemission and prevent complications. Delay in start of suitable antibiotic therapy is another imperative factor for treatment failure and rise of drug resistance. With rapidly increasing antibiotic resistance and decline in new antibiotic drug development, the toughest challenge remains to maintain and preserve the efficacy of currently available antibiotics. Therefore, the best rational approach to fight these infections is to 'hit early and hit hard' and kills drug-susceptible bacteria before they become resistant. The preferred approach is to deploy two antibiotics that produce a stronger effect in combination than if either drug were used alone. Various society guidelines in particular indications also justify and recommend the use of combination of antimicrobial therapy. Combination therapies have distinct advantage over monotherapy in terms of broad coverage, synergistic effect and prevention of emergence of drug resistance. Source


Kaushik D.,St Joseph Hospital | Mohan M.,Yashoda Hospital | Borade D.M.,Unichem Laboratories Ltd | Swami O.C.,Unichem Laboratories Ltd
Journal of Clinical and Diagnostic Research | Year: 2014

Antimicrobial resistance (AMR) is a global problem. AMR has posed new challenges in treatment of infectious diseases. Antimicrobials are losing efficacy due to development of resistant pathogens. It has lead to re-emergence of certain infectious diseases. Treatment of such diseases has undergone changes with use of alternative antimicrobials and drug combinations. Pathogens are likely to develop resistance to alternative antimicrobials also and risk of infections with nonexistent treatment is real. Salmonella showed widespread resistant to ampicillin which resulted in use of alternative antimicrobials like fluroquinolones and cephalosporins in the treatment of enteric fever in last two decades. Unfortunately there are growing reports of resistance to these antimicrobials. Interestingly there are numerous reports of ampicillin regaining activity against salmonella. Speculatively lack of exposure of salmonella to ampicillin for long time resulted in the loss of plasmid mediated resistance in the pathogen. There may have been emergence of de novo ampicillin susceptible strains. This is assuring in the era where problem of AMR is compounded by the scarcity of new antimicrobial development. Source

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