Increasing the Effectiveness of Slurry Experiments to Confirm the Relative Stability of Polymorphs

Thermodynamic stability and form selection. Form selection of active pharmaceutical ingredients is regarded as an essential part of drug development. The goal of form selection is to identify the most suitable solid form for toxicological studies, drug product development, and eventually commercialization. Determining the order in which solid forms exhibit physical stability is one Read more

Increasing the Effectiveness of Slurry Experiments to Confirm the Relative Stability of Polymorphs2022-05-03T20:03:00+00:00

Determining the Transition Temperature of Enantiotropic Polymorphs with Slow Transformation Kinetics

Select the polymorph with attributes fit for development. It is well established that polymorphism is common in pharmaceutical active ingredients.1 Bernstein and others present statistics that, when they are appropriately screened up to three in four compounds display polymorphism.2 Because of their distinct physical and chemical property differences, polymorph control becomes an essential task Read more

Determining the Transition Temperature of Enantiotropic Polymorphs with Slow Transformation Kinetics2022-04-11T15:46:52+00:00

Detecting Small Amounts of a Polymorph or Solid Form in Drug Product

How to quantitate a solid form in your drug product. A very important aspect of pharmaceutical mixture analysis is detecting and possibly quantitating a specific solid form in a drug product, especially tablets. Chapter 22 of Solid-State Properties of Pharmaceutical Materials by Byrn, Zografi, and Chen (Wiley, 2017) outlines several approaches to mixture analysis. Read more

Detecting Small Amounts of a Polymorph or Solid Form in Drug Product2022-04-01T20:44:24+00:00

Control of Nitrosamine Impurities in Human Drugs

In February 2021, the FDA issued a guidance aimed at preventing unacceptable levels of nitrosamine impurities in pharmaceutical products.  This guidance required a risk assessment to be completed by March 31, 2021.  This is because nitrosamines are genotoxic and are classified as possible or probable carcinogens. The guidance also described conditions under which nitrosamines Read more

Control of Nitrosamine Impurities in Human Drugs2022-01-17T20:27:49+00:00

Excipient Effects on Drug Product Performance

Traditionally, excipients utilized for the development of pharmaceutically-marketed drug products have been considered largely inert. Excipients are added to formulations for a variety of reasons that may include assisting processability of the drug product formulation, controlling the disintegration rate to facilitate regional dissolution along the gastrointestinal tract (GIT), bulking up the dosage form to enable Read more

Excipient Effects on Drug Product Performance2020-09-21T19:19:30+00:00

Are Polymorphs Obvious?

Not according to the United States Court of Appeals, citing Improved Pharma’s CSO Steve Byrn’s early paper on polymorph screening. The United States Court of Appeals for the Federal Circuit is known as the Supreme Court of patents, and its rulings are typically considered as significant landmarks in the patent and innovation field.  In Read more

Are Polymorphs Obvious?2022-01-17T20:30:49+00:00

Solving Difficult Polymorph Mixture Problems Using Synchrotron X-Ray Diffraction

A recent paper by Testa et al., Int. J. Pharm., 556 (2019) 125, investigated the mixture analysis of Olanzapine, which crystallizes in more than 60 solid forms, using synchrotron X-ray diffraction. They suggested that synchrotron techniques could help guide the discovery of methods to prepare and analyze pure polymorphs. Their observations and suggestions are consistent Read more

Solving Difficult Polymorph Mixture Problems Using Synchrotron X-Ray Diffraction2020-04-30T19:02:00+00:00

New Excipients for Solving Amorphous Formulation Problems – Part 2

At AAPS PharmSci 360, Improved Pharma found another exciting excipient for use in formulation. Like when SSCI was started, Improved Pharma was able to make several contacts at the AAPS meeting that will advance its problem-solving capabilities. One such advanced strategy is the utilization of calcium carbonate as an excipient to enhance dissolution. The excipient Read more

New Excipients for Solving Amorphous Formulation Problems – Part 22020-04-30T18:58:09+00:00

New Excipients for Solving Amorphous Formulation Problems – Part 1

At AAPS PharmSci 360 it was clear that new excipients could be utilized to innovatively solve a range of amorphous dispersion/formulation problems. These new excipients provide significant strategy advances over conventional approaches and although our Improved Pharma scientists utilized a number of novel approaches to prepare amorphous dispersions while at SSCI, these new excipients provide Read more

New Excipients for Solving Amorphous Formulation Problems – Part 12020-04-30T18:58:41+00:00

Detecting Differences In Formulations

As changes are made to the manufacturing process during drug development, it is often necessary to ensure that a drug or drug product made in a new way is the same as the material produced using the original methods. These equivalence studies often focus on chemical or physical properties and are relatively straight-forward for well-defined, Read more

Detecting Differences In Formulations2020-04-30T19:09:57+00:00
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