ABSTRACT
Phospholipid concentrates in a water miscible solvent were explored as injectable formulations for the poorly water-soluble drugs, using the anti-infective PHA 244 as model substance. Formulations containing up to 70% w/v phospholipid could dissolve 15% PHA 244. The formulations showed excellent syringe-ability and no precipitation of the drug after dilution in an excess of water. The local tolerability and pharmacokinetics of the formulations were explored after subcutaneous injection into cattle. A slow release pattern over a 2-week period and excellent local tolerability at the injection site were observed. Considering the low manufacturing costs, related to the production of solutions, this SupraVail MLM (Membrane Lipid Matrix) technology is a cost-effective alternative to more expensive depot technologies for poorly water-soluble drugs with similar release characteristics, like sterile aqueous and oily drug substance suspensions, as cited in the literature.
