Drug Formulation

Optimizing Drug Formulation for Enhanced Solubility, Stability, and Bioavailability

A good formulation is a key factor for drug success.

During the drug formulation phase, an active pharmaceutical ingredient (API) is combined with one or more excipients into a defined dosage form (liquid, tablet, capsules, etc.).

Advanced analytical technologies ensure that efficient and safe drugs are produced.

They provide high-quality reference data to formulation scientists on how the active pharmaceutical ingredients behave under predefined pH, temperature, and shear stress conditions and how compatible they are with the chosen excipients.

Selecting the correct analytical tools and instruments to characterize APIs, excipient, and final drug products is critical to formulation success.

METTLER TOLEDO instruments are the perfect fit for many analytical and characterization methods and product inspection tools used in drug formulation.

How to Choose a Formulation

Before formulation, scientists perform pre-formulation studies to characterize the chemical and physical properties of the APIs.

The acquired knowledge is then compared under different formulation conditions and used to choose an excipient compatible with the API.

Scientists also test excipient functionality and properties and evaluate how a formulation will behave under stress conditions - such as extreme pH and temperature, multiple cycles of freezing and thawing, or shear stress - and use the results to mitigate the damages.

During formulation studies, scientists focus on the chosen administration routes and optimize products regarding solubility, stability, bioavailability, ease of use, and administration, using methods such as:

freeze-drying
spray-drying
tableting
capsule development
enteric coating of tablets and capsules, or emulsion

This is done to modify drug substances' stability, bioavailability, and release profiles.

Ultimately, scientists cannot apply a one-size-fits-all approach when it comes to the formulation of APIs.

The intended formulation type and performance, as well as the API’s characteristics, influence the final solution.

Standard measurements in preformulation, formulation screening, and formulation quality control include:

pH and conductivity measurements
Karl Fisher water content determination
Thermal analysis (melting point, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), dynamic mechanical analyzer (DMA), etc.) of the API
Excipient and formulation concepts
Spectroscopic characterization (Fourier transformed infrared (FTIR) spectroscopy, Raman spectroscopy, UV-Vis spectrophotometry),
Bulk and tapped density of powders, particle size, and morphology monitoring during solubility and dissolution analysis, traceable, high-precision formulation weighing.

Once a formulation is refined and ready for production, industrial formulation management software provides complete control over formula management and material dispensing at scale.

Every action in production is automatically recorded, providing complete process transparency and automated batch evidence reporting.

Quality checks are enforced directly at the weighing stations and are electronically documented for complete track and trace, and full compliance with 21 CFR Part 11 is easily achieved.

METTLER TOLEDO solutions are an excellent fit for your drug formulation application.

Combined with METTLER TOLEDO laboratory software or industrial formulation software, they ensure traceability, facilitated scale-up, and compliance with FDA 21 CFR Part 11.

Solutions For Drug Formulation

Service For Your Solutions

METTLER TOLEDO Service is your one-stop shop for all your balance service, scale service, and inspection device service needs.

Our global network of factory-trained technicians is dedicated to providing expert care for your devices throughout the lifecycle.

From installation and initial calibration to preventive maintenance and timely upgrades, we ensure your operations run smoothly and efficiently.