Impact Factor for Five Years is 1.55 (2012 - 2016). IJPRT Re-launched from 2017, for more details visit www.ijprtonline.com

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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

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IJPR included in UGC-Approved List of Journals - Ref. No. is SL. No. 4812 & J. No. 63703

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0975-2366
5 - Years Impact Factor

Year 2012 - 2016

Impact Factor: 1.55

Total Publications: 317

Total Citation: 491

Year 2011 - 2015

Impact Factor: 1.46

Total Publications: 326

Total Citation: 477

Year 2010 - 2014

Impact Factor: 1.3

Total Publications: 313

Total Citation: 407

Year 2009 - 2013

Impact Factor: 0.973

Total Publications: 293

Total Citation: 285

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ROLE OF AMIODARONE IN ACUTE MYOCARDIAL INFARACTION INDUCED VENTRICULAR TACHYCARDIA IN PATIENTS WITH LEFT ANTERIOR DESCENDING ARTERY INVOLVEMENT
Extraction optimisation, fractionation, standardisation, in vitro antioxidant and anticholinesterase activity of fractions of Indian Propolis
Lung Cancer in Lifelong Never Smokers-Short Review
3D-Quantitative Structure Activity Relationship Study of Pyrazolothiazol-4-(5H)-One Derivatives as Epidermal Growth Factor Receptor Inhibitors
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IJPRT ISSUE

January - March 6 [1] 2014

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Exploring self- immolative prodrugs of hydroxychloroquine with aryl propionic acid NSAIDs for dual drug release in rheumatoid arthritis: Synthesis and pharmacokinetics

Author: SUNEELA DHANESHWAR, POORVASHREE JOSHI
Abstract: Incomplete absorption and poor oral bioavailability of hydroxychloroquine (HCQ) as well as gastrointestinal erosions of NSAIDs have attributed to major hurdles in the treatment of rheumatoid arthritis. To overcome these hurdles, we designed self- immolative dual delivery approach for disease modifying antirheumatic hydroxychloroquine and propionic acid derivatives of NSAIDs. Here, we report synthesis, stability, bio-conversion and pharmacokinetics of hydroxychloroquine esters with flurbiprofen (HF), zaltoprofen (HZ) and ketoprofen (HK). Chemical tethering was accomplished by CDI coupling. Characteristic C=O stretch of newly formed ester in IR, absence of singlet of HCQ–OH in NMR, molecular ion peaks of desired molecular weights in mass spectra, accurate percentage of C, H, N analysis in elemental analysis confirmed synthesis of projected structures. Bulky NSAIDs imparted higher lipophilicity. Stability of prodrugs in acidic pH (1.2) and stomach environment supported the reported mechanism of inhibition of gastrointestinal disturbances to minimize local gastrointestinal irritation. Our study elucidated pH (7.4) and intestinal esterases responsive hydrolysis of prodrugs. In vivo pharmacokinetic studies proved improvement in oral absorption (75-84%) and pharmacokinetic parameters like C max, T max, and AUC0-24 than parent HCQ. So, overall pharmacokinetics data implies that these self-immolative prodrugs can be ideal alternatives for extended release of HCQ and NSAIDs for management of RA. Extensive pre- clinical studies are underway to establish their utility in RA.
Keyword: Prodrugs; Hydroxychloroquine; NSAIDs; Arthritis; Disease modifying agent; CDI coupling, Absorption
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Ulrich's International Periodical Dictionary
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News & Events
Impact Factor for five years is 1.55 (2012 - 2016)
Year 2011 - 2015 Impact Factor - 1.46 Total Publications - 326 Total Citations - 477
Impact Factor for five years is 1.3 (2010 - 2014)