Effect of sodium caprate on the oral absorptions of danshensu and salvianolic acid B.
The current study aims to investigate the effect of sodium caprate on the intestinal absorption and bioavailabilities of danshensu and salvianolic acid B, the major active components in Salvia miltiorrhiza Bge (Danshen). Biopharmaceutics and pharmacokinetics properties of the two compounds have been characterized by in vitro, in situ models as well as in vivo in rats. Based on the identified biopharmaceutics characteristics of the two compounds, effect of sodium carparate as absorption enhancer on the intestinal absorption and pharmacokinetics of danshensu and salvianolic acid B in pure compound form as well as extract form were investigated both in vitro and in vivo. Both danshensu and salvianolic acid B demonstrated very limited intestinal permeabilities, leading to oral bioavailabilities of only 11.09% and 3.90% in rats, respectively. Results from both in vitro and in vivo studies consistently indicated that sodium caprate could significantly enhance intestinal permeabilities as well as the in vivo bioavailabilities of both danshensu and salvianolic acid B. The current findings not only identified the usefulness of sodium caprate for the improved delivery of Danshen product but also demonstrated the importance of biopharmaceutics characterization in the dosage form development of traditional Chinese medicine.
Zhou
Limin
L
School of Pharmacy, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, PR China.
Chow
Moses S S
MS
Zuo
Zhong
Z
D000284:Administration, Oral; D000818:Animals; D001572:Benzofurans / Q000493:pharmacokinetics*; D001682:Biological Availability; D018938:Caco-2 Cells; D003652:Decanoic Acids / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D007408:Intestinal Absorption; D007773:Lactates / Q000493:pharmacokinetics*; D008297:Male; D010539:Permeability; D051381:Rats; D017207:Rats, Sprague-Dawley; D027561:Salvia miltiorrhiza / Q000737:chemistry; D053630:Depsides
D001572:Benzofurans; D003652:Decanoic Acids; D005079:Excipients; D007773:Lactates; C031071:decanoic acid; C035055:3,4-dihydroxyphenyllactic acid; C076944:salvianolic acid B; D053630:Depsides