Bioavailability Enhancement: A Seamless Path to Clinical Success

Enhancing the bioavailability of poorly soluble drug candidates is a critical challenge in the pharmaceutical industry, with 70-90% of drugs exhibiting poor aqueous solubility.

At Almac, we understand the importance of overcoming this challenge to enhance Active Pharmaceutical Ingredient (API) solubility and drive bioavailability in the patient by bridging the gap between drug substance and drug product development and manufacture. By continually investing in advanced formulation technologies, state-of-the-art facilities and, most importantly, our people, we help our clients meet the demand of soluble and stable dosage forms.

From pre-formulation to GMP manufacture, we can transform your drug product’s potential into a clinical-ready solution.

Drug Product Testing

Before establishing a method for solubility enhancement, conducting physicochemical testing is essential to evaluate the API. This includes assessing:

• Solid form stability
• Dissolution rates
• Bulk density

As such, the physical property of the API is fundamental in helping us inform the most appropriate manufacturing process with the goal of developing a robust, scalable formulation tailored to the unique property of each molecule.

Due to the sensitive nature of APIs, our full suite of Drug Product Testing solutions from pre-formulation to process development and formulation development are designed to reduce the analytical challenges and streamline the path to improved bioavailability.

Bioavailability Enhancement Solutions

Advanced formulation technologies aim to improve the solubility and stability of poorly soluble APIs through Spray Dried Dispersions (SDDs) and Amorphous Solid Dispersions (ASDs) with the goal of maximising the therapeutic effect of the dosage form.

SDD occurs when the poorly soluble API and polymer is dissolved into a solvent and spray dried to prevent the API from reverting to its less soluble crystalline form, therefore enhancing solubility and bioavailability. At Almac, we offer spray drying solutions with batch sizes ranging 2g from 20kg+ from pre-formulation to early phase clinical trials.

In addition to SDD, micronisation often achieved from jet milling, works by reducing the particle size to improve dissolution properties of the API, thus speeding up dissolution rates.

Liquid fill also plays a pivotal role in developing lipid-based (solid & semi-solid) formulations for encapsulation. These formulations improve solubility and absorption of the drug product, making them ideal for oral delivery to maximise the therapeutic effect of the treatment.

Considerations for Bioavailability

Excipient selection

Selecting the right excipients is crucial. Our approach screens the API across a broad panel of excipients in parallel using high-throughput methods, evaluating solubility, dissolution and stability in various media, ensuring compatibility and scalability from early-phase development through to GMP manufacture.

Seamless Scale-up and Tech Transfer

Almac’s integrated, single-partner approach ensures a smooth transition from lab-scale innovation to GMP manufacturing. With equipment supporting batch sizes from grams to hundreds of kilos, and a collaborative approach, clients benefit from a seamless tech transfer process and consistent quality at every stage.

Improved patient outcomes

Although poorly soluble drug products are a persistent challenge, enhanced bioavailability creates opportunities for pharmaceutical companies to maximise the therapeutic impact of their unique treatments and deliver solutions to patients faster.

From pre-formulation development to GMP manufacture, trust Almac for a seamless path to clinical success.