Nanoparticle containing prostaglandin I₂derivative

摘要

There is provided a beraprost sodium-containing nanoparticle that contains beraprost sodium among other prostaglandin I2 (prostacyclin) derivatives, which are therapeutic agents for pulmonary hypertension. The beraprost sodium-containing nanoparticle is obtained by making beraprost sodium hydrophobic using a metal ion and allowing the hydrophobic beraprost sodium to react with poly-L-lactic acid or a poly(L-lactic acid/glycolic acid) copolymer, and a poly-DL- or L-lactic acid-polyethylene glycol block copolymer or a poly(DL- or L-lactic acid/glycolic acid)-polyethylene glycol block copolymer. The beraprost sodium-containing nanoparticle excels in sustained release of an active ingredient, reduces a side effect, and furthermore, has an excellent drug retention in the blood. Therefore, the beraprost sodium-containing nanoparticle is quite outstanding particularly regarding the sustainability of the medicinal effect.

主权项

1. A beraprost sodium-containing nanoparticle for treatment of pulmonary hypertension obtained by:
(a) converting beraprost sodium represented by the following formula (I): to a hydrophobicized beraprost sodium using a metal ion; and (b) allowing the hydrophobicized beraprost sodium to react with poly-L-lactic acid or a poly(L-lactic acid/glycolic acid) copolymer, and a poly-DL- or L-lactic acid-polyethylene glycol block copolymer or a poly(DL- or L-lactic acid/glycolic acid)-polyethylene glycol block copolymer to obtain a beraprost sodium-containing nanoparticle.