In vivo absorption comparison of nanotechnology-based silybin tablets with its water-soluble derivative.
In this study, the in vivo oral absorption of a nanocrystal tablet formulation of a BCS II poorly water-soluble drug was compared with that of its water-soluble salt form. Silybin is used as the model drug, and its nanosuspension was prepared by high-pressure homogenization. Effect of process and formulation parameters on properties of the nansuspensions was investigated. Dried powder of the nanosuspension was prepared by spray drying and used for preparing tablets. A pharmacokinetic study was performed in Beagle dogs to compare the absorption for tablets of silybin nanocrystals and silybin meglumine. In vivo absorption of nanocrystal silybin tablet in Beagle dogs was determined. X-ray powder diffraction results indicated that silybin existed in a crystalline state after homogenization. In vivo absorption study in rats showed that the peroral absorption of silybin was enhanced remarkably by decreasing particle size. In vivo absorption of nanocrystal silybin tablet in Beagle dogs was comparable with that of the commercially available tablet of the water-soluble salt form of silybin. In conclusion, it is possible to increase the bioavailability of poorly soluble drugs by preparing its water-soluble derivative.
School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China and.
Di
D
Xu
Rui
R
Ni
Wei
W
Sun
Luk Chiu
LC
Li
Shirui
S
Mao
D000818:Animals; D017849:Animals, Inbred Strains; D000975:Antioxidants / Q000032:analysis / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D004285:Dogs; D004339:Drug Compounding; D065546:Drug Liberation; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D008297:Male; D008536:Meglumine / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D065568:Oral Mucosal Absorption; D010316:Particle Size; D011208:Powders; D017208:Rats, Wistar; D000077385:Silybin; D012838:Silymarin / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D013535:Suspensions; D013607:Tablets
D000975:Antioxidants; D005079:Excipients; D011208:Powders; D012838:Silymarin; D013535:Suspensions; D013607:Tablets; D000077385:Silybin; D008536:Meglumine
Dissolution rate; high-pressure homogenization; nanosuspensions; oral absorption; silybin; silybin meglumine