Drug Formulation Development: A Quick Guide | Rondaxe CMC Consulting

Pharmaceutical formulation is a significant hurdle for biotech firms researching novel medications for first-in-human (FIH) clinical trials. In the early phases of drug research, and in the future commercial success of a potential exploratory medicinal product, formulation development is critical.

This article gives a practical introduction to drug formulation development elements (in the context of early phase clinical trials) to assist biotechnology businesses with this vital step in the drug development process.

What Is Drug Formulation?

Medicine formulation, also known as “pharmaceutical”l formulation, combines a range of ingredients with the medicinal’s active pharmaceutical ingredient (API) in order to create a drug product that can be delivered to patients effectively.

Why Is Drug Formulation Development Important?

Formulation development is critical because it entails creating an appropriate medicinal preparation with a form that is both stable and suitable.

What Factors Should Be Considered When Starting The Formulation Development Process?

Choosing which physical shape the medicinal product should assume is an important component of the drug formulation design step. Undoubtedly, simplicity and convenience of administration must be the top goals when selecting the form of a drug, to assure effective use by patients in early phase clinical trials (and subsequently in the clinical situation). Biotech businesses must examine which medicinal form will be the least disruptive; not surprisingly, patients must be included in the drug development process.

What Are Drug Preformulation Studies?

Preformulation is a set of research that focuses on the physicochemical qualities of a novel drug candidate – and how they may impact medication performance along with the creation of a dosage form.

This can be useful for formulation design, or to justify the necessity for molecular change. Every medicine has inherent chemical and physical features which must be considered when developing a pharmaceutical formulation. These attributes provide the foundation for combining pharmaceuticals with pharmaceutical substances in preparing a dosage form.

The goal of preformulation research is to create an elegant, stable, effective and safe dosage form by defining a kinetic rate profile, compatibility with other components and physicochemical properties of novel medicinal compounds. Drug solubility, partition coefficient, dissolving rate, polymorphic forms, and stability are all significant factors to consider in preformulation research.

Examples Of Medication Formulation Issues Encountered In Early Stages

Early-stage drug development programs often confront issues with stability and bioavailability. The capacity of a certain formulation to stay within its physical, chemical, microbiological, therapeutic and toxicological criteria is referred to as “drug product stability”.

The percentage of a given medicinal dosage which enters the systemic circulation as an intact drug (and the pace at which this happens) is referred to as “bioavailability”.

A chemical may be unstable in a solution and must be mixed with another substance before being administered to a patient. Inadequate solubility can also affect bioavailability. More than 40% of new chemical entities (and a significant proportion of APIs) in development are poorly soluble.

One of the major challenges confronting the biopharmaceutical industry today is optimizing drug solubility and bioavailability. Due to poor bioavailability, several new compounds in clinical development encounter difficulties in late-stage clinical trials.

2. Formulation Drug Development - A Quick GuideWhy Is It Critical To Consider Late-stage Clinical Trials?

It is critical to keep late-stage development in mind while developing a medication formulation. Relevant stability and bioavailability data can be used to influence the creation of formulations for subsequent phase investigations (and improve production once the chemical enters the clinic).

Because liquid formulations of drug candidates are both quicker and less expensive to produce, they are used in many first-in-human clinical studies. Furthermore, liquid formulations are often seen as a means of increasing oral bioavailability.

However, throughout the creation of formulations for early phase clinical research, the possibility of ultimately developing a future solid product should be carefully evaluated. Solubility and bioavailability may be challenging to recreate in increasingly complicated dosage forms which are utilized in late-phase clinical studies and in the clinical environment.

More information on drug formulation development can be found online at rondaxe.com or by calling us at (315) 469-2800.