Solid dispersion tablets of breviscapine with polyvinylpyrrolidone K30 for improved dissolution and bioavailability to commercial breviscapine tablets in beagle dogs.
Breviscapine, one of cardiovascular drugs extracted from a Chinese herb Erigeron breviscapinus, has been frequently used to treat cardiovascular diseases such as hypertension, angina pectoris, coronary heart disease and stroke. However, its poor water solubility and low bioavailability in vivo severely restrict the clinical application. To overcome these drawbacks, breviscapine solid dispersion tablets consisting of breviscapine, polyvinylpyrrolidone K30 (PVP K30), microcrystalline cellulose and crospovidone were appropriately prepared. In vitro dissolution profiles showed that breviscapine released percentage of solid dispersion tablets reached 90 %, whereas it was only 40 % for commercial breviscapine tablets. Comparative pharmacokinetic study between solid dispersion tablets and commercial products was investigated on the normal beagle dogs after oral administration. Results showed that the bioavailability of breviscapine was greatly increased by 3.45-fold for solid dispersion tablets. The greatly improved dissolution rate and bioavailability might be attributed to intermolecular hydrogen bonding reactions between PVP K30 and scutellarin. These findings suggest that our solid dispersion tablets can greatly improve the bioavailability as well as the dissolution rate of breviscapine.
Engineering Research Center of Modern Preparation Technology of TCM, Ministry of Education, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, People's Republic of China, wendycong@126.com.
Wenjuan
W
Cong
Lan
L
Shen
Desheng
D
Xu
Lijie
L
Zhao
Kefeng
K
Ruan
Yi
Y
Feng
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D004285:Dogs; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D005079:Excipients / Q000737:chemistry*; D005419:Flavonoids / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D006860:Hydrogen Bonding; D008297:Male; D008954:Models, Biological; D011205:Povidone / Q000737:chemistry*; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods
D004365:Drugs, Chinese Herbal; D005079:Excipients; D005419:Flavonoids; D013607:Tablets; C061097:breviscapine; D002482:Cellulose; D011205:Povidone; C109691:microcrystalline cellulose