- Synthesis, characterization and biological activity of hydroxyl- bisphosphonic analogs of bile acids
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Bisphosphonates (BPs) are now the most widely used drugs for diseases associated with increased bone resorption, such as osteoporosis, and tumor bone diseases. A significant drawback of the BPs is their poor oral absorption that is enhanced by the presence of bile acid substituents in the bisphosphonate framework, with no toxic effects. A straightforward synthesis of bile acid-containing hydroxy-bisphosphonates and a full characterization of these pharmaceutically important molecules, including an evaluation of affinity and the mechanism of binding to hydroxyapatite, is presented. The biological activity of bile acid-containing bisphosphonate salts was determined using the neutral-red assay on the L929 cell line and primary cultures of osteoclasts. The bioactivity of the new compounds was found superior than bisphosphonates of established activity.
- Bortolini, Olga,Fantin, Giancarlo,Fogagnolo, Marco,Rossetti, Stefano,Maiuolo, Loredana,Di Pompo, Gemma,Avnet, Sofia,Granchi, Donatella
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experimental part
p. 221 - 229
(2012/07/28)
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- Method for virus inactivation in the presence of polyalkylene glycol as well as the pharmaceutical preparation obtained therewith
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The invention relates to a pharmaceutical preparation comprising a plasma protein wherein said preparation is free of infectious agents as well as essentially free of denaturation products and is obtainable by a method that encompasses the following steps: a) addition of a polyether and a chaotropic agent to a solution comprising the plasma protein, optional lyophilization of the solution; b) inactivation of infectious agents in the presence of the polyether by a physio-chemical or chemical treatment, and c) removal of the polyether and the chaotropic agent.
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