The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inser...The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac.The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose(HPMC,3% to 5%),chitosan(3% to 5%),poly vinyle alcohol(PVA,3% to 5%),methyl cellulose(MC,3% to 5%) as drug reservoir and ethyl cellulose(EC) polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time,achieving controlled release and greater therapeutic efficiency.The prepared ocular insert were then evaluated for physical appearances tensile strength,elongation at break(%),weight variation,uniformity of thickness,moisture absorption(%),pH,folding endurance,Fourier Transform Infrared spectroscopy,differential scanning calorimetry.Physicochemical characterization and in vitro transcorneal permeation studies reveals that,the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content,98.54% and 96.24%,respectively,over an extended period of 24 h.Hence these formulations were selected as best optimized formulations.It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system.Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release,proving a promising controlled release delivery system.展开更多
目的:制备并表征局部用咪喹莫特泡囊凝胶剂,考察药物皮内滞留效应。方法:制备并表征咪喹莫特泡囊凝胶剂,离体鼠皮透皮实验考察药物皮内滞留量和透过量,切片观察药物皮内分布。结果:泡囊的平均粒径197.2 nm,Zeta电位-42.97 m V,包封率27....目的:制备并表征局部用咪喹莫特泡囊凝胶剂,考察药物皮内滞留效应。方法:制备并表征咪喹莫特泡囊凝胶剂,离体鼠皮透皮实验考察药物皮内滞留量和透过量,切片观察药物皮内分布。结果:泡囊的平均粒径197.2 nm,Zeta电位-42.97 m V,包封率27.44%;泡囊凝胶剂体外释放t1/2与泡囊相似,但为凝胶剂的4.94倍和市售乳膏的3.83倍,12 h透过药量均比凝胶剂和市售乳膏小一半,单位面积皮内药物滞留量约为它们的2倍,切片显示药库效应显著。结论:泡囊凝胶剂具缓释作用和药库效应,可增加皮内滞留,减少角质层拦截和透过皮肤的药量,将有利于皮肤病的治疗,并可降低局部刺激性和全身毒性的风险。展开更多
文摘The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac.The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose(HPMC,3% to 5%),chitosan(3% to 5%),poly vinyle alcohol(PVA,3% to 5%),methyl cellulose(MC,3% to 5%) as drug reservoir and ethyl cellulose(EC) polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time,achieving controlled release and greater therapeutic efficiency.The prepared ocular insert were then evaluated for physical appearances tensile strength,elongation at break(%),weight variation,uniformity of thickness,moisture absorption(%),pH,folding endurance,Fourier Transform Infrared spectroscopy,differential scanning calorimetry.Physicochemical characterization and in vitro transcorneal permeation studies reveals that,the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content,98.54% and 96.24%,respectively,over an extended period of 24 h.Hence these formulations were selected as best optimized formulations.It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system.Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release,proving a promising controlled release delivery system.
文摘目的:制备并表征局部用咪喹莫特泡囊凝胶剂,考察药物皮内滞留效应。方法:制备并表征咪喹莫特泡囊凝胶剂,离体鼠皮透皮实验考察药物皮内滞留量和透过量,切片观察药物皮内分布。结果:泡囊的平均粒径197.2 nm,Zeta电位-42.97 m V,包封率27.44%;泡囊凝胶剂体外释放t1/2与泡囊相似,但为凝胶剂的4.94倍和市售乳膏的3.83倍,12 h透过药量均比凝胶剂和市售乳膏小一半,单位面积皮内药物滞留量约为它们的2倍,切片显示药库效应显著。结论:泡囊凝胶剂具缓释作用和药库效应,可增加皮内滞留,减少角质层拦截和透过皮肤的药量,将有利于皮肤病的治疗,并可降低局部刺激性和全身毒性的风险。
