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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

A Step Towards Excellence

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

ISSN
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

Current Issue
22nd NATIONAL CONVENTION

22nd National Convention of Society of Pharmacognosy & International Conference. For more details visit


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Article In Press
Biomechanical/biochemical factors contributing to cardiac fibrosis in the heart and engineered cardiac tissue
THE ASSOCIATION AND LINKGAGE OF VARIOUS RETROVIRUSES AND ITS PROGRESSION TOWARDS NEURODEGENERATION
Architecture of Viral RNA Helicases; HCV helicase as Antiviral Target
GC-MS analysis of rhizome extract by Cold maceration of Curcuma amada Roxb.
Development and Evaluation of Febuxostat Sublingual Tablet Formulation
Development and Evaluation of Febuxostat Sublingual Tablet Formulation
A comparative study of adaptogenic effect of Withania somnifera with Mifepristone (a GR antagonist) on chronic stress - induced perturbations in glucose metabolism
In Vitro Anticancer Activity Of Leaves Of Rumex Vesicarius Linn And Symplocos Racemosa Roxb By Trypan Blue Method
PREPARATION AND INVITRO CHARACTERISATION OF ANTIBACTERIAL NANOCAPSULES
Cytotoxic potential of the crude solvent extract of Botryodiplodia theobromae – an endophytic fungi isolated from Catharanthus roseus.
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IJPRT ISSUE

January - March 6 [1] 2014

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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Article Detail

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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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News & Events
22nd National Convention of Society of Pharmacognosy & International Conference. For more details visit https://ncsp.ganpatuniversity.ac.in
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)