SELFEMULSIFIABLE FORMULATION HAVING ENHANCED BIOABSORPTION AND IMMUNOSUPPRESSION ACTIVITIES AND METHOD OF PREPARATION THEREOF

摘要

Abstract A selfemulsifiable formulation for oral administration essentially comprising of immunosuppression agent, hydrophilic agent, lipophilic agent, surfactants, antioxidant and preservative is disclosed, wherein immunosuppression agent is lactam macrolide having immunosuppression activity and present in an amount of about 2 to 10% by weight of the formulation; hydrophilic agent is ethanol present in a weight ratio of about 1:0.5 to about 1:2.5 with respect to immunosuppression agent; lipophilic agent is medium chain triglycerides of caprylic and/or capric acids; surfactants are the combination of transesterified caprylic and capric glycerides, polysorbate 80, and cremophor RH 40; antioxidant is selected from a group consisting of alpha-tocopherol, ascorbyl palmitate, butyl hydroxy anisole, butyl hydroxy toluene, propyl gallate; and preservative is selected from a group consisting of ethanol and benzyl alcohol.