Crystalline drugs

McFarland, J. W. Du, C. M. Avdeef, A., Factors influencing the water solubility of crystalline drugs, in van de Waterbeemd, H. Lennemas, H. Artursson, P. (eds.), Drug Bioavailability. Estimation of Solubility, Permeability, Absorption and Bioavailability, Wiley-VCH, Weinheim, 2003 (in press). 

Factors Influencing the Water Solubilities of Crystalline Drugs... 

We report here studies conducted with 58 crystalline drug-like compounds. The solubilities are of high quality, having been determined in only three laboratories using the same automated potentiometric method. However, the set is too small to... 

When formulating with crystalline drugs that have received a Biopharmaceutical classification system (BCS) ranking as being either... 

When the excipient matrix in a formulation is largely amorphous, similar XRPD methods can be used to determine the amount of crystalline drug substance present in a drug product. The principles were established in a study that included a number of solid dose forms [40],... 

The synthesis of letrozole (3) is quite simple (Scheme 3.5). An Sn2 displacement of 4-bromomethyl-benzonitrile (25) with imidazole was carried out in methylene chloride at room temperature to produce adduct 26. Deprotonation of 26 in DMF using potassium t-butoxide was followed by addition of para-fluorobenzonitrile. The S Ar reaction afforded letrozole (3) as an oil. In order to make the crystalline drug, a hemisuccinate was prepared, which has a melting point of 149-150°C. 

Everz, L. and Mielck, J. (1992). V feter-induced physical transformation of a crystalline drug in a uidized bed pseudopolymorphism-polymorphism of carbamazepiBa/ J. Pharm. Biopharm., 38 28S. 

Comparison of Drug Release from an Osmotic CR Tablet Containing Solid Dispersion as Compared to that from an Osmotic CR Tablet with Crystalline Drug that had not been Manipulated... 

Markovich RJ, Anderson Evans C, Coscolluela CB, Zibas SA, Rosen J. Spectroscopic identification of an amorphous-to-crystalline drug transition in a solid dispersion SCH-48461 capsule formulation. J Pharm Biomed Anal 1997 19 661-673. 

Molar Volume and Solubility Parameters for Some Liquid Compounds and Crystalline Drug Compounds... 

Saklatvala, R., Royall, P. G. and Craig, D. Q. M. (1999). The detection of amorphous material in a nominally crystalline drug using modulated temperature DSC—a case smdy. Int. J. Pharm., 192, 55-62. [255]... 

PROBLEMS IN THE FREEZING PROCESS OF CRYSTALLINE DRUGS AND THEIR SOLUTIONS... 

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