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

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

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ECO-FRIENDLY SYNTHESIS OF SILVER NANOPARTICLES USING AQUEOUS LEAVES EXTRACT OF CLOME GYNANDRA AND THEIR ANTIBACTERIAL ACTIVITY”
Synthesis, characterization, augmentation of iron oxide nanoparticles from Musa paradisaca peel extract and its antibacterial activity
Antianaphylactic Activity Polyherbal Formulation Against Systemic, Cutaneous And Compound 48/80 Induced Invitro Anaphylaxis
A study on an autoimmune disease-PSORIASIS
EFFICACY OF EMBLICA OFFICINALIS ON SERUM ENZYMES AGAINST AIR POLLUTANTS EXPOSED ALBINO RATS.
Formulation and Evaluation of Buccal Drug Delivery System of Ketorolac Tromethamine Using Mucoadhesive Polymers
Signaling pathways associated with liver cancer stem cell therapy
PHARMACOLOGICAL ACTIVITIES OF ASTAXANTHIN
A review on ethnobotany, phytochemistry and pharmacology of Plantago major L. – nature's treasure
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IJPRT ISSUE

January - March 6 [1] 2014

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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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Scopus (Elsevier)
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Ulrich's International Periodical Dictionary
Indian Science Abstract
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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)