Abstract: The present invention relates to a pharmaceutical composition containing leuprolide acetate and having both immediate and sustained release properties and, more specifically, to a pharmaceutical composition in which, on the basis of the total weight of active ingredients, leuprolide as an immediate release preparation is contained in 0.001 wt % to 25 wt %; and leuprolide contained in microspheres of a sustained release preparation is contained in 75 wt % to 99.999 wt %. The pharmaceutical composition of the present invention is characterized by satisfying both a drug immediate release property so as to realize the prompt exposure to a sufficient amount of drug at the early stage for expression of medicinal effects and a drug sustained release property for four weeks or longer, and the pharmaceutical composition is effective in the prevention and treatment of sex hormone-dependent positive or malignant diseases.

Abstract: The present invention relates to a pharmaceutical composition containing leuprolide acetate and having both immediate and sustained release properties and, more specifically, to a pharmaceutical composition in which, on the basis of the total weight of active ingredients, leuprolide as an immediate release preparation is contained in 0.001 wt % to 25 wt %; and leuprolide contained in microspheres of a sustained release preparation is contained in 75 wt % to 99.999 wt %. The pharmaceutical composition of the present invention is characterized by satisfying both a drug immediate release property so as to realize the prompt exposure to a sufficient amount of drug at the early stage for expression of medicinal effects and a drug sustained release property for four weeks or longer, and the pharmaceutical composition is effective in the prevention and treatment of sex hormone-dependent positive or malignant diseases.

Abstract: The present invention relates to a method for preparing polymeric microspheres to improve the drug encapsulating efficiency and, more specifically, to a method for preparing polymeric microspheres, the method comprising the steps of: preparing an internal water phase (w1) and an oil phase (0); mixing the internal water phase and the oil phase to prepare a W1/0 emulsion, followed by cooling; mixing the W1/0 emulsion with an external water phase (W2) to prepare a W1/0/W2 emulsion; and drying the prepared W1/0/W2 emulsion, followed by collection. The method of the present invention can increase the drug encapsulating efficiency and manufacture polymeric microspheres having high drug contents through a procedure of maintaining the step of solidifying the oil phase at a particular temperature for a particular period of time, and thus the method of the present invention is effective in the preparation of sustained release-type drugs.