Journal of Pharmacy and Pharmaceutical Sciences 

About: Journal of Pharmacy and Pharmaceutical Sciences is an academic journal published by Canadian Society for Pharmaceutical Sciences. The journal publishes majorly in the area(s): Pharmacokinetics & Cmax. It has an ISSN identifier of 1482-1826. It is also open access. Over the lifetime, 375 publications have been published receiving 12125 citations. The journal is also known as: JPPS & Journal of Pharmacy & Pharmaceutical Sciences.

Evolution of nonsteroidal anti-inflammatory drugs (NSAIDs): cyclooxygenase (COX) inhibition and beyond

Abstract: Purpose. NSAIDs constitute an important class of drugs with therapeutic applications that have spanned several centuries. Treatment of inflammatory conditions such as rheumatoid arthritis (RA) and osteoarthritis (OA) starting from the classic drug aspirin to the recent rise and fall of selective COX-2 inhibitors has provided an enthralling evolution. Efforts to discover an ultimate magic bullet to treat inflammation continues to be an important drug design challenge. This review traces the origins of NSAIDs, their mechanism of action at the molecular level such as cyclooxygenase (COX) inhibition, development of selective COX-2 inhibitors, their adverse cardiovascular effects, and some recent developments targeted to the design of effective anti-inflammatory agents with reduced side effects. Methods. Literature data is presented describing important discoveries pertaining to the sequential development of classical NSAIDs and then selective COX-2 inhibitors, their mechanism of action, the structural basis for COX inhibition, and recent discoveries. Results. A brief history of the development of NSAIDs and the market withdrawal of selective COX-2 inhibitors is explained, followed by the description of prostaglandin biosynthesis, COX isoforms, structure and function. The structural basis for COX-1 and COX-2 inhibition is described along with methods used to evaluate COX-1/COX-2 inhibition. This is followed by a section that encompasses the major chemical classes of selective COX-2 inhibitors. The final section describes briefly some of the recent advances toward developing effective anti-inflammatory agents such as nitric oxide donor NO-NSAIDs, dual COX/LOX inhibitors and anti-TNF therapy. Conclusions. A great deal of progress has been made toward developing novel anti-inflammatory agents. In spite of the tremendous advances in the last decade, the design and development of a safe, effective and economical therapy for treating inflammatory conditions still presents a major challenge.

Review of the cosolvency models for predicting solubility of drugs in water-cosolvent mixtures

Abstract: The cosolvency models presented from 1960 to 2007 were reviewed and their accuracies for correlating and/or predicting the solubility of drugs in water-cosolvent mixtures were discussed. The cosolvency models could be divided into theoretical, semi-empirical and empirical models, the first group of models provide basic information from the solution, while the last group of models are good suitable for solubility correlation studies. The simplest cosolvency model, i.e. the log-linear model of Yalkowsky, provides an estimate of drug solubility in water-cosolvent mixtures using aqueous solubility of the drug, whereas the Jouyban-Acree model predicts the solubility with an acceptable error with the cost of one more data point (the solubility in neat cosolvent) which is required as input value in the prediction process. A number of error terms used in the literature was also discussed with a brief comments on the acceptable prediction error for pharmaceutical applications.

Adverse effects of nonsteroidal antiinflammatory drugs: an update of gastrointestinal, cardiovascular and renal complications.

Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are used chronically to reduce pain and inflammation in patients with arthritic conditions, and also acutely as analgesics by many patients Both therapeutic and adverse effects of NSAIDs are due to inhibition of cyclooxygenase (COX) enzyme NSAIDs are classified as non-selective and COX-2-selective inhibitors (COXIBS) based on their extent of selectivity for COX inhibition However, regardless of their COX selectivity, reports are still appearing on the GI side effect of NSAIDs particularly on the lower gastrointestinal (GI) tract and the harmful role of their controlled release formulations In addition, previously unpublished data stored in the sponsor’s files, question the GI sparing properties of rofecoxib, a COXIB that has been withdrawn due to cardiovascular (CV) side effects Presently, the major side effects of NSAIDs are the GI complications, renal disturbances and CV events There is a tendency to believe that all NSAIDs are associated with renal and CV side effects, a belief that is not supported by solid evidence Indeed, lower but still therapeutics doses of some NSAIDs may be cardioprotective In this review, we briefly discuss the GI toxicity of the NSAIDs and assess their renal and CV adverse effects in more detail This article is open to POST-PUBLICATION REVIEW Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page

Intranasal Drug Delivery: How, Why and What for?

Abstract: Over the last decade the interest in intranasal delivery as a non-invasive route for drug administration has been exponentially increased. Since the nasal mucosa offers numerous benefits as a target issue for drug delivery, a wide variety of therapeutic compounds may be administered intranasally for topic, systemic and central nervous system action. The present paper reviews the relevant aspects of nasal anatomy, physiology and histology, and refers to the biological, physicochemical and pharmaceutical factors that must be considered during the process of discovery and development of nasal drugs as well as in their incorporation in appropriate nasal pharmaceutical formulations.

α-Amylase inhibitors: a review of raw material and isolated compounds from plant source.

Abstract: - Inhibition of α-amylase, enzyme that plays a role in digestion of starch and glycogen, is considered a strategy for the treatment of disorders in carbohydrate uptake, such as diabetes and obesity, as well as, dental caries and periodontal diseases. Plants are an important source of chemical constituents with potential for inhibition of α-amylase and can be used as therapeutic or functional food sources. A review about crude extracts and isolated compounds from plant source that have been tested for α-amylase inhibitory activity has been done. The analysis of the results shows a variety of crude extracts that present α-amylase inhibitory activity and some of them had relevant activity when compared with controls used in the studies. Amongst the phyto-constituents that have been investigated, flavonoids are one of them that demonstrated the highest inhibitory activities with the potential of inhibition related to number of hydroxyl groups in the molecule of the compound. Several phyto-constituents and plant species as α-amylase inhibitors are being reported in this article. Majority of studies have focused on the anti-amylase phenolic compounds. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on on the issue’s contents page.