Isotopic ratios to detect infringements of patents or proprietary processes of pharmaceuticals: Two case studies

Process Patent Protection via Analysis of Stable Isotope Ratios

“…2 However, to our knowledge, few reviews address the possibilities afforded by stable isotope analysis for improving process patent protection in relation to pharmaceutical and other value-added products. 3,4 Recent work in pharmaceutical forensics demonstrates the sensitivity and applicability of stable isotope approaches. Early applications from our own work largely focused on batch manufacturing, in which we established that batches of pharmaceutical materials have distinctive ratios (or "fingerprints") of the stable isotopes of each element present in the final product.…”

“…The analysis of stable isotope ratios is a well-established strategy in forensic biochemistry and geochemistry, with legal criteria and guidelines for its applicability . However, to our knowledge, few reviews address the possibilities afforded by stable isotope analysis for improving process patent protection in relation to pharmaceutical and other value-added products. , …”

C & N Isotope Analysis of Diclofenac to Distinguish Oxidative and Reductive Transformation and to Track Commercial Products

“…Moreover, it was shown that especially N-isotope analysis of micropollutants has the potential for source appointment in the environment. Specifically, for pharmaceutical products such as aspirin, ibuprofen, or naproxen, it has been shown that the analysis of stable isotope ratios can be used as a fingerprint for product authentication and to track sources. − In one case, it was even possible to determine the location of an illegal production site by evidence from isotope analysis …”

A NIR, 1H-NMR, LC-MS and chemometrics pilot study on the origin of carvedilol drug substances: a tool for discovering falsified active pharmaceutical ingredients

“…5 In such a context, the use of chemometric analysis of APIs and medicinal products intended for characterisation of physicalchemical properties and impurity prole represents a valid tool for tracing the source and authenticity of APIs as well as nished products. [6][7][8][9][10][11][12][13] The nature and quantity of residual solvents, 14,15 proles of impurities, 6,16 heavy metal residues, isotopic ngerprinting [17][18][19][20][21][22] and polymorphic forms are features closely related to the synthetic route and manufacturing. The combination of analytical methods and chemometric analysis could provide deep knowledge of the characteristics of an API.…”