Formulating Liquid Filled Capsules To Enhance The Solubility And In-Vitro Dissolution

Approximately 40% of new drug candidates have poor water solubility and the oral delivery of such drugs is frequently associated with implications of low bioavailability, high intra and inter-subject variability, and lack of dose proportionality1. Potential drug candidates with promising pharmacodynamics may be rejected at an early stage during the lead molecule selection stage itself. Liquid filled hard capsule offers a platform for managing successful transition from “to be abandoned molecule” to a potent bioactive drug product. However, the means of doing so is restricted by physicochemical properties of the Active Pharmaceutical Ingredient (API).

The formulator’s arsenal typically consists of a wide ranging array of solubilizers, co-solvents, surfactants & emulsifying agents to achieve favorable pharmacokinetics. Their generous use is limited by permissible daily intake levels, individual solubilizing capacities & compatibility with the gelatin shell. An excipient mixture approach helps judicious selection of type and concentration of each excipient. Here, the same approach aided in achieving target in-vitro dissolution (75%Q in 45 min) of a poorly soluble API.

To enhance the solubility and in-vitro dissolution/bioavailability of a low soluble (0.5 mg/mL) BCS Class II compound (API).