Classification of the ibuprofen active pharmaceutical ingredients by chemical patterns combining HPLC, 1H-NMR spectroscopy and chemometrics: traceability of legal medicines.

INTRODUCTION: Ibuprofen is one of the widespread used non-steroidal anti-inflammatory drugs. Ibuprofen active ingredient is manufactured in many sites located all around the world. The aim of this paper was to classify the geographical source of ibuprofen active pharmaceutical ingredients (APIs) from the legal market, based on chemical characteristics and its impurity pattern and to define a geographical fingerprint. METHODS: To classify ibuprofen in different geographical groups, the chemometrics by principal component analysis (PCA) and Cluster analysis was applied to HPLC, 1H-NMR data of twenty-four samples of APIs from approved manufacturers located in different European and Asian countries. RESULTS: The PCA showed clearly two different geographical groups, based on particular patterns of European or Indian samples; the cluster analysis showed the similarity of group. CONCLUSION: The chemometric analysis is an important tool for tracking the geographical origin of APIs. This could be useful to supplement the quality control ensuring safety of the medicinal products in legal market and dealing with the evolving changes of the illegal market.

Investigation on the possibility of biowaivers for ibuprofen.

The aim of the study was to investigate the ability of in vitro dissolution to ensure bioequivalence of ibuprofen products. Ibuprofen is a Biopharmaceutics Classification System (BCS) class II drug with low solubility at pH 1.2 and 4.5 and high solubility at pH 6.8. The possibility of extending the "BCS biowaivers" to weak acidic compounds has been suggested. Three ibuprofen formulations were compared in vitro and in vivo with the reference. Dissolution profiles in several pH buffers showed similarity at 75 and 50 rpm. However, the bioequivalence studies showed that two formulations were not equivalent in C(max) because of a statistically significant difference. Conversely, another formulation was bioequivalent both in AUC and C(max) in a pilot study (n = 10) and a final study (n = 18), demonstrating that the previous failures were not due to lack of statistical power, but due to a different absorption rate that cannot be detected in vitro. In conclusion, "biowaivers" for this type of class II drugs are not feasible because the dissolution tests do not detect differences in absorption rate. Differences in absorption rate cannot be neglected, not only because absorption rate has clinical relevance but also because the clinical importance of the differences cannot be assessed if they are not quantified.

Protective effects of NSAIDs on the development of Alzheimer disease.

BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) may protect against Alzheimer disease (AD), but observational studies and trials have offered contradictory results. Prior studies have also been relatively short and small. We examined the effects on AD risk of NSAID use for >5 years and of NSAIDs that suppress formation of A beta (1-42) amyloid in a large health care database. METHODS: Cases were veterans aged 55 years and older with incident AD using the US Veterans Affairs Health Care system. Matched controls were drawn from the same population. NSAID exposure was categorized into seven time periods: no use, 1 but 5 years of use (0.68-0.85). For users of ibuprofen, it decreased from 1.03 (1.00-1.06) to 0.56 (0.42-0.75). Effects of other NSAID classes and individual NSAIDs were inconsistent. There was no difference between a group of A beta (1-42)-suppressing NSAIDs and others. DISCUSSION: Long-term nonsteroidal anti-inflammatory drug (NSAID) use was protective against Alzheimer disease. Findings were clearest for ibuprofen. A beta (1-42)-suppressing NSAIDs did not differ from others.

Ibuprofen to rofecoxib: what does it all mean and what do I do now?

NSAIDs are used throughout the World Health Organization three-step analgesic ladder, and are indicated for pain in all stages of malignancy. Side-effects are common with NSAIDs. Much has been written about NSAIDs and COX, since the discovery of COX-1 and COX-2 isoforms. How do you choose the appropriate NSAID? The choice of NSAID continues to be dependent upon associated gastroduodenal toxicity and the related risk factors of individual patients. Choosing the appropriate NSAID should minimize the likelihood of needing additional medications to manage adverse effects and symptoms caused by the NSAID therapy itself.