科研之友
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摘要
Andrographolide, a bioactive phytoconstituent, has a wider range of pharmacological action. However, due to the intestinal degradation, shows low oral bioavailability. The aim of the present work was to develop an excipients free delivery system using floating concept for andrographolide in order to enhance its site specific absorption and minimize pH dependent hydrolysis in alkaline environment. Andrographolide was adsorbed on the low-density porous Cavilink (TM) beads via solvent evaporation method. The 3(2) factorial design was used to study the effect of solvent volume and drug amount on characteristic of beads. Developed system were evaluated for yield, drug loading, differential scanning calorimetry, powder X-ray diffraction, fourier transform infrared, scanning electron microscopy, in-vitro buoyancy and drug release studies. Yield and drug loading were found in the range of 57 to 91% and 52 to 96%. DSC and PXRD revealed existence of drug in crystalline form. The obtained microparticles showed good in-vitro floating ability (82 +/- 4%) for more than 13 h using 0.1 N HCl as dissolution medium with initial burst release in the range of 7.13% to 22.63% followed by the controlled zero order drug release up to 10 h. Floating microparticulate system, could possibly be advantageous in terms of increased bioavailability of andrographolide.
- 出版日期2012-4
