Enhancing the bioavailability of magnolol in rabbits using melting solid dispersion with polyvinylpyrrolidone.
OBJECTIVE
Preparation of magnolol-loaded amorphous solid dispersion was investigated for improving the bioavailability.


METHODS
A solid dispersion of magnolol was prepared with polyvinylpyrrolidone K-30 (PVP) by melting method, and the physical properties were characterized by using differential scanning calorimetry, powder X-ray diffractometry, Fourier transformation-infrared spectroscopy and scanning electron microscope. In addition, dissolution test was also performed. Subsequently, the bioavailability of magnolol pure compound, its physical mixture and solid dispersion were compared in rabbits. The blood samples withdrawn via marginal ear vein at specific time points were assayed by HPLC method.


RESULTS
Oral administration of the solid dispersion of magnolol with PVP significantly increased the systemic exposures of magnolol and magnolol sulfates/glucuronides by 80.1% and 142.8%, respectively, compared to those given with magnolol pure compound.


CONCLUSIONS
Magnolol-loaded amorphous solid dispersion with PVP has demonstrated enhanced bioavailability of magnolol in rabbits.
School of Pharmacy, China Medical University , Taichung , Taiwan.
Shiuan-Pey
SP
Lin
Yu-Chi
YC
Hou
Tzu-Yun
TY
Liao
Shang-Yuan
SY
Tsai
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D017705:Lignans / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D011205:Povidone / Q000737:chemistry*; D011817:Rabbits; D012995:Solubility
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001713:Biphenyl Compounds; D004337:Drug Carriers; D017705:Lignans; C005498:magnolol; D011205:Povidone