Investigation on recombinant hirudin via oral route.
The possibility for oral administration of peptide recombinant hirudin variant (rHV2-K47) as an anticoagulant agent was evaluated in several aspects. The proteolytic properties of rHV2-K47 and its stability during storage were examined by in vitro experiments. Radiolabeled rHV2-K47 was infused into the duodenum of rats and rHV2-K47 absorbed into serum was shown to be intact by electrophoresis pattern. The in vivo coagulation time of blood from mouse was prolonged significantly after oral administration of rHV2-K47. The bioavailability (F) of rHV2-K47 via oral route reached 10.11% in comparison with intravenous administration as gold standard. All the results suggested that rHV2-K47 could be delivered successfully via the oral route.
Cen
Xiaodong
X
College of Life Sciences, Peking University, Yiheyuan Road 5, Box #20, 100871 Beijing, PR China.
Ni
Jianquan
J
Tan
Taochao
T
Liu
Xia
X
Li
Changling
C
Chen
Jiepeng
J
Huang
Yixiu
Y
Zhu
Shenggeng
S
Bi
Qun
Q
D000284:Administration, Oral; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage* / Q000494:pharmacology*; D001777:Blood Coagulation / Q000187:drug effects; D004355:Drug Stability; D004386:Duodenum; D006629:Hirudins / Q000008:administration & dosage* / Q000494:pharmacology*; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000187:drug effects; D008297:Male; D051379:Mice; D051381:Rats; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000494:pharmacology
D000925:Anticoagulants; D006629:Hirudins; D011994:Recombinant Proteins