Jain S K, Chourasia M K, Sabitha M, Jain R, Jain A K, Ashawat M, Jha A K
Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar, India.
Drug Deliv. 2003 Jul-Sep;10(3):169-77. doi: 10.1080/713840400.
Transdermal drug delivery system of diltiazem hydrochloride was developed to obtain a prolonged controlled drug delivery. Both the matrix diffusion controlled (MDC) and membrane permeation controlled (MPC) systems were developed. The matrix diffusion controlled systems used various combinations of hydrophilic and lipophillic polymers, whereas membrane permeation controlled systems were developed using the natural polymer chitosan. The MDC systems were prepared using the cast film method and the MPC systems by an adhesive sealing technique. Both the systems were characterized for in vitro and in vivo performance. The MDC systems were characterized for physicochemical properties such as tensile strength, moisture content, and water vapor transmission. The in vitro release studies showed that the release from the matrix diffusion controlled transdermal drug delivery systems follows a nonfickian pattern and that from the membrane permeation controlled transdermal drug delivery systems follow zero-order kinetics. The release from the matrix systems increased on increasing the hydrophilic polymer concentration, but the release from the membrane systems decrease on cross-linking of the rate controlling membrane and also on addition of citric acid to the chitosan drug reservoir gel. The in vivo studies of the selected systems showed that both systems are capable of achieving the effective plasma concentration for a prolonged period of time. The MPC system achieved effective plasma concentration a little more slowly than the MDC system, but it exhibited a more steady state plasma level for 24 hr.
开发了盐酸地尔硫䓬的透皮给药系统，以实现药物的长效控释。制备了基质扩散控制（MDC）系统和膜渗透控制（MPC）系统。基质扩散控制系统使用了亲水性和疏水性聚合物的各种组合，而膜渗透控制系统则使用天然聚合物壳聚糖开发。MDC系统采用流延膜法制备，MPC系统采用粘合剂密封技术制备。对这两种系统的体外和体内性能进行了表征。对MDC系统的物理化学性质进行了表征，如拉伸强度、水分含量和水蒸气透过率。体外释放研究表明，基质扩散控制的透皮给药系统的释放遵循非菲克扩散模式，而膜渗透控制的透皮给药系统的释放遵循零级动力学。随着亲水性聚合物浓度的增加，基质系统的释放增加，但膜系统的释放在控制速率的膜交联以及向壳聚糖药物储库凝胶中添加柠檬酸时会降低。所选系统的体内研究表明，这两种系统都能够在较长时间内达到有效的血浆浓度。MPC系统达到有效血浆浓度的速度比MDC系统稍慢，但在24小时内表现出更稳定的血浆水平。
