Oral Solid Dosage Forms Fact Sheet

Offering Expert Preclinical and Clinical Formulation Development of Oral Solid Dosage Forms

Oral administration remains the most widely used route for the successful delivery of active pharmaceuticals to patients. Dosage form design will be driven by a combination of factors
including:

Speed of development (fast into clinic)
Anticipated dose
Excipients required to improve API stability or enhance bioavailability
Targeted (enteric) or modified (delayed) release profile requirement

Developing Oral Dosage Forms

Upperton can offer clients expert preclinical and clinical formulation development of oral solid dosage (OSD) forms; from early feasibility, right through to clinical manufacture. Formulations can range from simple powder in bottle/sachet for reconstitution to more complex capsules and tablets.

Typical Development Pathway

Capsule Formulations

Capsule formulations are often the favoured dosage form for initial clinical studies as they offer a fast, convenient way to deliver the API to the pharmacy. Capsules may contain simple unformulated API or more advanced formulations, such as amorphous spray-dried dispersions designed to enhance bioavailability.

Tablet Formulations

Whilst capsule delivery represents the faster route into the clinic, tablets give more flexibility in the formulation and offer a more cost-effective solution for products entering later stages of development or commercial manufacture, as well as being a more established approach for targeted delivery.

Analytical and Stability Testing

Phase-appropriate methods are developed for analysis of OSDs from early-stage development, through to GMP manufacture.

Characterisation of OSDs Typically Includes:

Appearance – visual and
microscopic
Material identification
- FTIR
Assay and related
substances – HPLC, UV, GC
Water content – Karl
Fischer
Residual solvents – GC
Blend homogeneity
Blend density/
compressibility
Content uniformity/
weight uniformity
Tablet hardness/
friability
USP disintegration and
dissolution
Discriminating/
clinically relevant
dissolution
Microbial limits
(outsourced)

Stability

During the preclinical stage, accelerated stability studies focus on excipient compatibility, where API and excipients are blended together and stability assessed with ASAPprime®. More formal ICH stability studies are used during development to determine product stability/shelf life on technical and clinical batches manufactured under GMP conditions.