title: A new formulation concept for drugs with poor water solubility for parenteral application.
abstract: The parenteral application of active substances with poor solubility in water is often bound to the use of stabilizing excipients or surfactants with serious undesired side effects. A new concept is introduced based on a drug concentrate, comprising the active substance dissolved in parenterally acceptable organic solvents, and an aqueous dilution medium, which are mixed in a special mixing device immediately prior to application and thus generating the applicable formulation directly prior to administration. Due to the requirement of formulation stability for only a few minutes, the amount of stabilizing agents can be reduced significantly. It can be shown that model drugs dissolved in a mixture of polyoxyethylen glycol, ethanol and soya lecithin as stabilizer may be mixed to an aqueous glucose solution resulting in a parenterally acceptable and administerable dispersion which is physically stable for several minutes. First in vivo data show good tolerability and blood plasma levels which are comparable to conventional solutions.
authors.affiliation: Department for Pharmaceutics and Biopharmaceutics, Christian-Albrecht-University Kiel, Germany.
authors.forename: K
authors.initials: K
authors.lastname: Jürgens
authors.forename: B W
authors.initials: BW
authors.lastname: Müller
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D004355:Drug Stability; D064420:Drug-Related Side Effects and Adverse Reactions; D000431:Ethanol; D007267:Injections; D009391:Nephelometry and Turbidimetry; D019999:Pharmaceutical Solutions; D010713:Phosphatidylcholines; D011092:Polyethylene Glycols; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D012997:Solvents; D014867:Water / Q000737:chemistry
chemical_list: D019999:Pharmaceutical Solutions; D010713:Phosphatidylcholines; D012997:Solvents; D014867:Water; D000431:Ethanol; D011092:Polyethylene Glycols