JPS6416716A - Production of emulsion pharmaceutical containing sparingly soluble drug sealed therein - Google Patents

Abstract

PURPOSE:To obtain a pharmaceutical, forming a fine emulsion and capable of being parenterally, especially intraveously administered, by kneading a sparingly soluble drug with an oily ingredient in the coexistence of a phospholipid, adding an aqueous solution and emulsifying the resultant kneaded blend. CONSTITUTION:A sparingly soluble drug hardly soluble in water and oils is sufficiently kneaded and blended with an adequate amount of an oily ingredient (preferably an oil, derived from a plant and purified to a high purity) and a phospholipid to form a homogeneous dispersion system, which is then mixed with a solution prepared by dissolving the residual phospholipid in the residual oily ingredient while heating and homogenized using a homomixer. An aqueous solution containing required additives, such as emulsification adjuvant, isotonizing agent, antioxidant, dissolved therein is then added to emulsify the obtained blend and afford the aimed emulsion pharmaceutical. The above- mentioned pharmaceutical preferably consists of 0.001-30wt./vol.% sparingly soluble drug, 1-30wt./vol.%, especially 5-20wt./vol.% oily ingredient, the phospholipid in an amount of 1-50pts.wt., especially 5-35pts.wt. based on 100pts.wt. oily ingredient and water in an adequate amount.