Preformulation Studies: An Integral Part of Formulation Design

Abstract

When a promising new chemical entity is synthesized, it needs transformation to appropriate formulation in order to show a better and desirable action at appropriate site. Preformulation study is a phase which is initiated once the new molecule is seeded. In a broader way, it deals with studies of physical, chemical, analytical, and pharmaceutical properties related to molecule and provides idea about suitable modification in molecule to show a better performance. Study of these parameters and suitable molecular modification can be linked to generation of effective, safer, stable, and reliable pharmaceutical formulation. Therefore, preformulation study is an approach for generation of pharmaceutical formulation which utilizes knowledge and area application of toxicology, biochemistry, medicinal chemistry, and analytical chemistry. The highlighted chapter is framed with a vision to provide an in-depth knowledge about pharmaceutical formulation development.

Preformulation Studies: A Versatile Tool in Formulation Design

“…Preformulation studies are facilitated the right path of selecting the appropriate adjuvants and other formulation conditions required during manufacture. For example, the stability profile of a live attenuated Ty21a bacterial typhoid vaccine performed by spectroscopic techniques provides time-dependent real-time high throughput information at a broad range of temperatures (10-85°C) and pH (4)(5)(6)(7)(8). The above information is useful during preformulation studies of other similar type of peptide drugs.…”

“…These studies are most and much important before formulation development and they give us an idea about the stages of drug formulation development related to the physicochemical properties of new chemical entities (NCEs) or any drug substances [2][3][4]. During drug development stages, the physical and chemical properties are categorised and standardised to establish the optimum mark for formulation development and ensure that these properties are helpful for formulation development [5,6]. Key preformulation factors are thermal particle size, shape, dissociation and partition coefficient, drug/API stability, absorption behaviour, and solid-state characters like polymorphism.…”

“…Deep understanding and thorough information of physicochemical and related biopharmaceutical properties of the drug direct scientists to design optimum and appropriate formulation delivery methods to get strong proof of concept (POC) and pre-clinical studies to have a clear understanding of active pharmaceutical ingredients (API) characters and relevant additives that might affect the final formulation and drug performance [5].…”

Sustained release matrix tablet of 100 mg losartan potassium: Formulation development and in vitro characterization

“…Evaluation of pre-compression parameter, which involves bulk density, tapped density, compressibility index and angle of repose, is very important before compression (Mandal, Pal, 2008a;Patel, 2019). All these parameters were evaluated with a pre-defined method as mentioned below:…”

Application of Af4-Multidetection to Liraglutide in Its Formulation: Preserving and Representing Native Aggregation

“…Once the peptide Active Pharmaceutical Ingredient (API) is produced and purified, and usually lyophilized, it undergoes formulation to reach its Finished Dosage Form (FDF). This phase comprises a series of studies: pre-formulation (evaluation of physicochemical properties before and after combination to excipients), analytical profiling (structural characterization and impurity determination), and evaluation of pharmaceutical properties [ 11 , 12 ]. Commercialization of protein drug candidates has to further face many road barriers: changes in external and/or internal variables, including temperature, pH, and chemical environment, may lead to processes such as denaturation, aggregation, or precipitation, causing destabilization of the protein structure and affecting its functioning [ 13 ].…”