| 摘要 |
A formulation of solubilized lovastatin soft capsules and a manufacturing process thereof are provided, which formulation increases solubility and bioavailability of lovastatin which is a hardly soluble drug, and improves liquid stability of lovastatin. The formulation of solubilized lovastatin soft capsules comprises 1 to 20 wt.% of lovastatin, 10 to 70 wt.% of solubilizing agent, 10 to 70 wt.% of surfactant, 10 to 70 wt.% of co-surfactant, 1 to 20 wt.% of oils, 0.1 to 20 wt.% of antioxidant and 0.1 to 5 wt.% of pH regulating agent, wherein the solubilizing agent is selected from polyethyleneglycol, propyleneglycol, triacetin, glycerol, diethyleneglycol and monoethylether; the surfactant is selected from polyoxyethylene glycolated castor oil, mono- or tri-lauryl, palmityl, stearyl, or oleyl exter, polyoxyethylene stearic acid ester, polyoxyethylene-polyoxypropylene block copolymer, sodium dioctylsulfosuccinic acid or sodium lauryl sulfuric acid, phospholipid, propylene glycol dicaprylate, propyleneglycol dilaurate, propyleneglycol isostearate, propyleneglycol laurate, propyleneglycol caprilic-caprilic acid diester, mono-, capril/caprilic acid mono-or di-glyceride, sorbitan monolauryl, sorbitan monopalmityl or sorbitan monostearyl, cholesterol, pitosterol or cytosterol; the oil is selected from triglycerides of medium fatty acid, mono- or di-glycerides of oleic acid, isopropyl myristate, isopropyl palmitate, ethyl linolate or ethyl oliate, vegetable or animal oil, squalene or squalane, liquid oleic acid or linoleic acid, and dl-alpha-tocopheryl acetate; antioxidant is selected from tocopherol, dibutylhydroxytoluene, butylhydroxyanisol, ascorbic acid, sodium sulfite, sodium pyrosulfite and sodium hydrogen sulfite; and the pH regulating agent is selected from citric acid, succinic acid, stannic acid, formic acid, and maleic acid.
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