眼用制剂的前药及其药动学研究进展

前药是自身无活性,在体内经化学或酶代谢后释放出有药效活性的原药或代谢物的化合物。前药设计是一种改善眼用制剂不良性质,如水溶性差、生物利用度低、半衰期短和眼部刺激性的重要手段。眼用制剂的药动学主要研究眼对药物的吸收、分布、代谢和排泄的规律。笔者将按照结构修饰类型综述眼用前药的药动学研究进展,从而指导临床合理用药、减少不良反应、提高疗效。

Research Progress of Ocular prodrug and Its Pharmacokinetics

Prodrugs are inactive drug molecules, which needs to be chemical or enzymatic bio-transformed in vivo, and to release the therapeutically active parent drug or metabolite. Prodrug design can be used to improve pharmaceutical properties of ophthalmic drug such as poor aqueous solubility, low bioavailability, short half-life and irritation to the eye. Ocular pharmacokinetics is the processes of absorption, distribution, metabolism and elimination of drugs in the eyes. This review aims to discuss pharmacokinetic research progress of ocular prodrug according to their structural modification, and to provide evidences for clinical rational drug use, reducing side effects and improving efficacy.