Recent Advances in the Characterization of Solid State Pharmaceuticals

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The farewell speaker at Pharma LabNext Conclave 2021 was Dr Raj Suryanarayanan, Professor and William & Mildred Peters Endowed Chair, Department of Pharmaceutics, College of Pharmacy, University of Minnesota. His research focuses on how to apply principles of pharmaceutical materials science to the design of robust pharmaceutical dosage forms with reproducible and predictable properties. At the event, he spoke about recent advances in the characterization of solid state pharmaceuticals.

He gave a technical presentation on the different classes of drugs on the market and pointed out that there is a challenge with solubility that needs to be addressed. He gave details about the different types of compounds and their characteristics. He said that by changing crystalline compounds to amorphous, you can achieve better solubility and bioavailability. However, switching from the amorphous to the crystalline form of drugs results in a loss of bioavailability. He warned that if sufficient precautions are not taken, amorphous drugs will turn into crystalline and products may have to be taken off the market. He also explained the limitation of the amorphous form and said that it is inherently unstable.

He said about 50 percent of all drug molecules are administered as salts. The rate of dissolution, bioavailability and solubility are some of the advantages of salt formation. He explained the factors causing drug disproportion including excipients, humidity, temperature, and mechanical activation / processing parameters, citing examples of several drugs and their compositions to explain his points.

He then explained various analytical methods used in the pharmaceutical industry such as HPLC, X-ray powder diffractometry, spectroscopic techniques like IR, RAMAN and solid state NMR, calorimetry, etc.

Thus, the presentation examined phase transformation in situ to provide critical spatial information and offer a mechanistic overview of phase transformation for rational selection of excipients. A key takeaway from the session was that since the surface of a tablet is in contact with the outside environment, the formulator must be very careful. Surface composition and microstructure can play a disproportionate role in product properties and performance.

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