| 摘要 |
PURPOSE: A composition containing zwitterionic phospholipid and bisphosphonate and having reduced gastrointestinal(GI) toxicity and improved bio-availability and methods for treating osteoporosis using the composition are provided. The zwitterionic phospholipids exist in a sufficient amount to improve the bio-availability of bisphonates, the bisphosphonates exist in a sufficient amount to reduce bone resorption, increase bone density and/or reduce bone fracture when administered with food. CONSTITUTION: A pharmaceutical composition for treating osteoporosis contains one or more zwitterionic phospholipids of formula 2 and one or more bisphosphonates of formula 1. In formula 1, R1 is H, OH or Cl; R is (a)C1-6 alkyl group optionally substituted by amino, alkylamino, dialkylamino or heterocyclyl, (b)halogen, (c)arylthio, preferably chloro-substituted arylthio, (d)C5-7 cycloalkylamino, or (e)5- or 6-membered saturated heterocyclyl containing N having one or two hetero atoms. In formula 2, R1 and R2 are C8-32 saturated or unsaturated substitutes; R3 is H or CH3; X is H or COOH; and R4 is =O or H2.
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