The in vitro transdermal delivery study of Buspirone hydrochloride

• Main Authors: Jung-Tzu Chang, 張容慈
• Other Authors: Pao-Chu Wu
• Format: Others
• Language: zh-TW
• Published: 2010
• Online Access: http://ndltd.ncl.edu.tw/handle/09831402423813965631

碩士 === 高雄醫學大學 === 藥學研究所 === 98 === Buspirone hydrochloride (BH) is a structurally and pharmaco- logically unique anxiolytic that is used to treat a variety of different anxiety conditions. The in vitro delivery of BH through rat skin was investigated in order to evaluate the feasibility of delivering a therapeutic dose of BH by this route. We also examined the influence of chemical and physical enhancer on BH permeation. The enhancer that we used is the microemulsion as a chemical method. Microemulsions are clear, stable, isotropic mixtures of oil, water and surfactant, frequently in combination with a cosurfactant. And we applied iontophoresis and eletroporation as physical enhancer. In vitro permeation studies, the microemulsion (F1, containing 12% surfactant, 3% oil phase, 85% liquid phase) formulation in the flux and cumulative amounts of BH was 5 times flod higher than its solubility in the water, so we choose the formulation to permeate with iontophoresis and eletroporation. By applying iontophoresis for 12 hours, it was possible to achieve a BH cumulative amount of approximately 2236.74?b386.05 ?慊/cm2 , which would be 2-fold higher than passive diffusion. It is noteworthy that when the current was on and off in turn. Significantly, the effect was particularly prominent for the 2-h on/2-h off application mode that has 7-fold higher of cumulative amounts than BH permeation without iontophoresis. The influence of BH transdermal delivery with eletroporation is positive, the observed cumulative amounts was 1995.29?b568.41?慊/cm2 , that has 1.73-fold higher of cumulative amounts than control mode.