Pharmaceutica Analytica Acta

Considerations in pre-formulation stage of solid and semi-solid dosage forms

5^th International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems

March 16-18, 2015 Crowne Plaza, Dubai, UAE

Mustafa Hamido

Posters & Accepted Abstracts: Pharm Anal Acta

Abstract:

Solid and semi-solid dosage forms are the most widely marketed and administered drugs nowadays. Almost 70% of the administered drugs are in solid states. It is preferred by the pharmaceutical companies due to its high safety, low cost and marketing issues. Pre-formulation is a stage of development during which the physicochemical properties of drug substance are characterized. Before the formulation of a drug substance into a dosage form, it is essential that to be chemically and physically characterized. Pre- formulation begins with calculation/prediction ?in silico? of many of the important physicochemical characteristics of the API. Literature search of similar type of compounds is the second step of pre-formulation process. Pre-formulation influences on selection of the drug candidate itself, selection of formulation components, API & drug product manufacturing processes, determination of the most appropriate container closure system, development of analytical methods, assignment of API retest periods, the synthetic route of the API and toxicological strategy. The most important function of pre-formulation stage is solid state characterization which determines the next step in the formulation work of the studied API. Physical properties of the studied API influence on its physical and chemical stability. It influences on the rout of administration, delivery system and the drug activity. Moreover, Chemical stability of the drug is affected by the physical properties. Crystal morphology, polymorphism, amorphous forms and hygroscopicity are usually studied. In addition, solubility, salt form, melting point, dissolution of the API are also studied. Certain properties are studied in pre-formulation stage of the solid dosage forms. These properties relate mainly to the ability of the powder to flow in the compressing machine and subsequently its compressibility. They influence on the dissolution rate of the API, stability, bioavlaibility, degradation rate and purity. The studied properties include particle size, its distribution, its surface area and porosity. It includes also true density, flowability, API color, electrostaticity, caking and polymorphism.