Characteristics of a novel phospholipid-based depot injectable technology for poorly water-soluble drugs

Eur J Pharm Biopharm. 2004 Nov;58(3):587-93. doi: 10.1016/j.ejpb.2004.04.002.

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.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Cattle
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / metabolism
  • Injections, Subcutaneous
  • Male
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / chemistry
  • Pharmaceutical Preparations / metabolism
  • Phospholipids / administration & dosage*
  • Phospholipids / blood
  • Phospholipids / chemistry
  • Solubility / drug effects
  • Water / administration & dosage*
  • Water / chemistry
  • Water / metabolism

Substances

  • Delayed-Action Preparations
  • Pharmaceutical Preparations
  • Phospholipids
  • Water