Mustafa Hamido
UAE
Title: Considerations in pre-formulation stage of solid and semi-solid dosage forms
Biography
Biography: Mustafa Hamido
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 infl uences 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. Th e 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 infl uence on its physical and chemical stability. It infl uences on the rout of administration, delivery system and the drug activity. Moreover, Chemical stability of the drug is aff ected 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. Th ese properties relate mainly to the ability of the powder to fl ow in the compressing machine and subsequently its compressibility. Th ey infl uence on the dissolution rate of the API, stability, bioavlaibility, degradation rate and purity. Th e studied properties include particle size, its distribution, its surface area and porosity. It includes also true density, fl owability, API color, electrostaticity, caking and polymorphism.