| 摘要 |
PURPOSE: Provided are liquid pharmaceutical formulations of alendronic acid or a pharmaceutically acceptable salt thereof, and in particular, those containing a buffer which can control gastric pH. CONSTITUTION: Provided is a liquid pharmaceutical formulation comprising: alendronic acid or a pharmaceutically acceptable salt as an active ingredient; a sufficient amount of buffer such that: A) the pH of the formulation is between approximately 3.5 and approximately 7.5; and B) 15 ml of the formulation is able to raise the pH of 50 ml of 0.1 N HCl (pH approximately 1) to a pH of at least 3.0; and optionally, one or more additional agents including those selected from the group consisting of: preservatives, flavoring agents, colorants, and sweeteners. Another aspect of this invention is a pharmaceutical formulation made by mixing the aforementioned active ingredients, buffer and optional agent(s). Buffering systems include those selected from the group consisting of citrate, tartrate, fumarate, phosphate, acetate, and mixtures thereof. Typically, 0.2 to 3 g of a salt or free acid and base will be used to make a buffer salt combination (per 15 ml dose). Generally, a 15 ml dose of the formulation of this invention will contain between 0.2 to 3 g of at least one of the following: disodium phosphate, trisodium citrate dihydrate, disodium tartrate dihydrate, or di sodium formate. For example a useful buffering system is a citrate buffer comprising anhydrous citric acid and trisodium citrate dihydrate, present in a molar ratio of about 1:1-350, preferably about 1:50-150, and more preferably about 1:81.
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