Pharmaceutical solid dosage form design

Zanowiak P. Lubrication in solid dosage form design and manufacture. In Swarbick J, Boylan JC, eds. Encyclopedia of Pharmaceutical Technology, vol. 9. New York Marcel Dekker, 1990 87-112. 

FROM MOLECULAR AND CRYSTALLOGRAPHIC STRUCTURE TO THE RATIONAL DESIGN OF PHARMACEUTICAL SOLID DOSAGE FORMS... 

A. Hlinak, K. Kuriyan, K. Morris, G. Reklaitis, P. Basu, Understanding critical material properties for solid dosage form design. Journal of Pharmaceutical Innovation, 1,12-17,2006. 

Buckton, G. (2002) Solid state properties, in Pharmaceutics The Science of Dosage Form Design (ed. M.E. Aulton), Churchill Livingstone, Edinburgh, pp. 141-151. 

In the preformulation study, the comprehension of physicochemical properties regarding water-solid surface interaction is beneficial to the handling, formulation, and manufacture of the finished products. Data on sorption/de-sorption isotherm, hydration of salts of drug product, water sorption of pharmaceutical excipients, and kinetics of water adsorption or desorption of a substance can be obtained effectively by the dynamic vapor sorption method. The knowledge may be utilized for dosage form design and supports the understanding of the mechanism of action. 

Since punch-and-die presses of various designs are widely used in the pharmaceutical industry and represent the most important equipment for the manufacturing of solid dosage forms, many books have been published on the subject in essentially all languages around the world. It exceeds the context of this book to go into more detail. Rather, the specialized literature should be sought and reviewed, which can be obtained from the pharmaceutical associations existing in all major countries, from international sellers of academic, scientific, and technical books that can be found on the Internet, and from vendors (Section 15.1). The books cited by the author [B.6, B.34, B.41, B.48, B.66, B.97, B.99, B.105] are those that are in his personal library. 

Many solid dosage forms are designed for controlled dissolution or liberation of the drug substance, controlled in the sense that its release is slow compared with the rate of systemic absorption. Dissolution testing using pharmacopoeia and other methods is an essential element of the pharmaceutical development process. There are still arguments about its relevance to the in vivo situation and there are still those who maintain that it cannot be anything other than a quality control tool to ensure batch to batch consistency. 

We have now examined what distinguishes experimental design problems involving mixtures and applied the simplex lattice and centroid designs to explore responses over the whole of the possible factor space. As we said earlier, it is hardly realistic to expect all components to be allowed to vary from zero to one hundred percent in a real system. That this should be so for solid pharmaceutical dosage formulation is especially evident - each component of a solid dosage form has its own function. 

However, its low solubility and chemical instability in water have limited the dosage form design and presented a substantial challenge to pharmaceutical scientists (3). Cyclodextrins (CyDs) have been successfully applied to improve the pharmaceutical properties of various drugs (4,5,6). In our preliminary study, it was found that HCFU forms solid complexes with a-, 3 and yCyDs. Thus, the present study dealt with the inclusion complexation of HCFU with three CyDs in an attempt to obtain improved solubility, dissolution rate, chemical stability, and bioavailability of HCFU. 

Hancock BC, ShambUn SL, Zografi G (1995) Molecular mobility of amorphous pharmaceutical solids below their glass-transition temperatures. Pharm Res 12(6) 799-806 Hancock BC, York P, Rowe RC (1997) The use of solubility parameters in pharmaceutical dosage form design. Int J Pharm 148(1) 1-21... 

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