微粒和纳米粒眼部给药系统

[5]Riz os I.Three 2year survival of patients with heart failure caused by dilat 2

ed cardiomy opathy and L 2carnitine adm inistration [J ].Am Heart J ,2000,139(2Pt3):s120.

[6]Sethi R ,Dhalla K S ,G anguly PK,et al .Beneficial effects of propionyl

L 2carnitine on sarcolemmal changes in congestive heart failure due to my 2ocardial in farction[J ].Cardiovasc Res ,1999,42(3):607.

[7]Eskandari G H ,K andem ir O ,P olat G,et al .Serum L 2carnitine levels

and lipoprotein com positions in chronic viral hepatitis patients[J ].Clin Biochem ,2001,34(5):431.

[8]Neri S ,Pistone G,Saraceno B ,et al .L 2carnitine decreases severity

and type of fatigue induced by interferon 2alpha in the treatment of pa 2tients with hepatitis C[J ].Neuro Psychobiology ,2003,47(2):94.[9]杨金龙,夏子禹,游龙英,等.复方卡尼汀治疗慢性病毒性肝炎

[J ].中国新药与临床杂志,2001,20(2):125.

[11]M alaguarnera M ,Pistone G,Astuto M ,et al .L 2carnitine in the treat 2

ment of m ild or m oderate hepatic encephalopathy[J ].Dig Dis ,2003,21(3):271.

[12]林修,叶榕,王耀新.卡尼汀治疗急性脑梗死[J ].中国新药与

临床杂志,2001,20(2):121.

[13]M ontg omery S A ,Thal LJ ,Amrein R ,et al .M eta 2analysis of double

blind random ized controlled clinical trials of acetyl 2L 2carnitine versus placebo in the treatment of m ild cognitive im pairment and m ild Alzheimer ’s disease [J ].Int Clin Psychopharmacol ,2003,18(2):61.

[14]Benvenga S ,Ruggeri RM ,Russ o A ,et al .Usefulness of L 2carnitine ,

a naturally accurally peripheral antag onist of thyroid horm one action in iatrogenic hyperthyroidism :a random ized ,double 2blind ,placebo 2con 2trolled clinical trial[J ].J Clin Endocrinol M eta

b ,2001,86(8):3579.[15]Benvenga S ,Lapa D ,Canav o S ,et al .Successive thyroid storms treat 2

ed with L 2carnitine and low doses of methimaz ole [J ].Am J M ed ,2003,115(5):417.

[16]M alone J I ,Schocken DD ,M orris on AD ,et al .Diabetic cardiomy opa 2

thy and carnitine deficiency[J ].J Diabetes C om plications ,1999,13(2):86.

[17]王咏梅,殷仁富,杜荣增,等.左旋卡尼汀对糖尿病伴高血压患

者血浆肉碱浓度及血糖的影响[J ].第二军医大学学报,2003,

24(4):425.

[18]Vestla E ,Racek J ,Irefil L ,et al .E ffect of L 2carnitine supplementa 2

tion in hem odialysis patients[J ].Nephron ,2001,88(1):218.[19]M atsumura M ,Hatakeyama S ,K oni I ,et al .C orrelation between

serum carnitine levels and erythrocyte osm otic fragility in hem odialysis patients[J ].Nephron ,1996,72(4):574.

[20]Labonia W D.L 2carnitine effects on anem ia in hem odialyzed patients

treated with erythropoietin[J ].Am J K idney Dis ,1995,26(5):757.[21]Boran M ,Dalva I ,G onenc F ,et al .Response to recombinant human

erythropoietin (r 2HuEPO )and L 2carnitine combination in patients with anem ia of end 2stage renal disease[J ].Nephron ,1996,73(2):314.

(2004201202收稿)

3

国家自然科学基金资助(30100204)

【作者简介】　胡 (1981-),男,在读硕士研究生。研究方向:药物新剂型与新技术。【通讯作者】　吴　伟。T el :021*********,E 2mail :wuwei @

微粒和纳米粒眼部给药系统3

胡 ,吴　伟　(复旦大学药学院药剂学教研室,上海200032)

【中图分类号】R944.9 【文献标识码】A 【文章编号】100724006(2005)022*******

眼部给药剂型最常见的是滴眼剂和眼膏剂。

这两种普通剂型使用方便,易于被患者接受。但眼膏剂容易引起雾视,滴眼剂则易从眼部流失,生物利用度很低。对于需要长期治疗的眼部疾病,即使反复使用,效果也不能维持,同时个别药物由于鼻泪管引流易引起全身不良反应。近年来,眼部给药系统的研究愈来愈受到关注,剂型的研究主要集中在延长药物与角膜上皮和结膜的接触时间,提高生物利用度,减少全身不良反应,局部定位给药和眼部的缓、控释给药系统。

微粒和纳米粒眼部给药系统是克服普通剂型缺

点的一种行之有效的方法。一般微粒粒径为1～500μm ,纳米粒粒径在10～1000nm ,可包裹一系列水溶性和难溶性药物。做成缓控释制剂,维持长时间的疗效,还具有一定的靶向作用。同时粒径<10μm 的微粒或纳米粒可以滴眼给药,克服了传统滴眼液易在角膜前消除的缺点,使用方便。现就微粒和纳米粒的眼部给药系统的研究进展作一综述。1　眼内分布和靶向性

粒径较大的微粒,眼内注射主要起缓释长效作