Topical delivery system of ophthalmic drugs by periocular injection with viscous solution.
Topical delivery system of ophthalmic drugs by periocular injection with viscous solution.
复制标题
通过眼周注射粘稠溶液的眼科药物局部给药系统。
DOI：
--
复制
发表时间：
1999
影响因子：
2
通讯作者：
M. Ichikawa
中科院分区：
文献类型：
--
作者：
H. Sasaki;S. Kashiwagi;T. Mukai;K. Nishida;J. Nakamura;M. Nakashima;M. Ichikawa
本研究的目的是评估眼周注射黏性溶液作为眼科药物的局部给药系统。Tilisolol和carboxymethylcellulose （CMC）分别作为模型β受体阻滞剂和粘性聚合物。采用高效液相色谱法（HPLC）测定兔泪液、血液、房水和玻璃体中含有3% CMC的替尼索罗50微l囊内、球后和眼睑结膜注射后的药物浓度。眼周注射替利索罗（50微l）， 3% CMC显示泪液中药物从注射部位轻微渗漏。与缓冲液相比，黏性载体降低了药物从注射部位到体循环的吸收速率常数。这表明，黏性溶液改善了药物在注射部位和眼周组织的滞留。虽然眼周注射黏性载体（3% CMC）在房水中的AUC低于注入时的AUC，但在玻璃体中的AUC相当。与眼周注射缓冲液后相比，CMC使玻璃体内auc分别增加了球后注射3.1倍和睑结膜注射1.4倍。结果，3% CMC眼周注射比滴注和眼周注射缓冲液能更好地将替利索罗输送到玻璃体。
The purpose of this study is to evaluate periocular injections with viscous solution as a topical delivery system of ophthalmic drugs. Tilisolol and carboxymethylcellulose (CMC) were used as a model beta-blocker and a viscous polymer, respectively. After intracapsular, retrobulbar and palpebral conjunctival injections (50 microl) of tilisolol with 3% CMC into rabbits, drug concentrations in the tear fluid, blood, aqueous humor and vitreous body were determined by HPLC. Periocular injection (50 microl) of tilisolol with 3% CMC showed slight leakage of the drug in the tear fluid from the injection site. The viscous vehicle decreased the absorption rate constant of the drug from the injection site to systemic circulation compared with the buffer solution. It suggests that the viscous solution improved the retention of drug at both the injection site and in periocular tissues. Although the periocular injections with viscous vehicle (3% CMC) showed lower AUC in the aqueous humor than that observed in instillation, they showed comparable AUC in the vitreous humor. Compared to the results after the periocular injections with buffer solution, CMC increased the AUCs in the vitreous body 3.1-fold with retrobulbar injection and 1.4-fold with palpebral conjunctival injection, respectively. As a result, periocular injections with 3% CMC showed higher delivery of tilisolol to the vitreous body against the aqueous humor than the instillation and periocular injections with buffer solution.