The invention relates to a
calcium heparin /
sodium salt nano-sized oral preparation and a preparation method thereof, and a
calcium heparin /
sodium salt nano-sized
liposome with high encapsulation rate for preparing the
calcium heparin /
sodium salt nano-sized oral preparation. The calcium heparin /
sodium salt nano-sized
liposome is obtained by the following steps: dissolving
chitosan in 1-10% dilutedsolution of
acetic acid (the usage amount of
chitosan is 0.5-5g per 100ml
acetic acid solution) to obtain an acidified
chitosan solution, filtering, collecting filtrate, adding dropwise 1-99% aqueoussolution of calcium heparin /
sodium salt into the filtrate under magnetic stirring until milk white precipitate occurs, centrifugating the resulating suspension, collecting precipitates, and freezes-
drying to obtain calcium heparin /
sodium salt nano-sized
liposome. The calcium heparin / sodium salt nano-sized oral preparation is characterized in that the preparation has good stability, high encapsulation rate (up to 98%), and high
in vitro release rate (up to 25% at hour 4); the preparation is absorbed in the intestinal tract with
high absorption rate and
high concentration; the
half life is prolonged upon the increase of oral dosage, showing zero-order
kinetics; the tissue concentration is larger than
blood concentration; the preparation is released sustainedly; and study in rabbits (20mg oral intake) shows that the
blood concentration in vivo is kept high for over 50 hours, thereby proving sustained release.