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目的探讨不同配方哌仑西平滴眼液的角膜通透性,为临床应用提供依据。方法配制2%哌仑西平滴眼液(单纯哌仑西平组)、2%哌仑西平+0.1%透明质酸钠滴眼液(透明质酸钠组)及2%哌仑西平+0.1%氮酮滴眼液(氮酮组)。将63只新西兰白兔分为3组,分别在各组兔双眼结膜囊内滴入上述眼液,滴眼6次,每次间隔5min。在最后1次滴眼后0.5、1·0、2·0、4·0、8·0、12·0、24·0h抽取前房水约0.2ml,使用高效液相色谱仪分析前房水中哌仑西平的浓度,并于每次滴眼前后和穿刺抽吸房水前用裂隙灯显微镜观察3组兔眼部的一般情况。结果最后1次滴眼后0.5、1·0、2·0、4·0h单纯哌仑西平组前房水中哌仑西平的浓度分别为(0.40±0.06)、(0.53±0.03)、(1.52±0.33)及(0.15±0.02)μg/ml,8·0h后高效液相色谱仪未能检测到哌仑西平。各时间点氮酮组和透明质酸钠组前房内哌仑西平浓度均明显高于单纯哌仑西平组(P<0.01),生物利用度分别约是其23·0倍和3.4倍。并且实验过程中各组兔眼部均无刺激症状。结论氮酮组的角膜通透性最好,透明质酸钠组次之,均显著高于单纯哌仑西平组,表明氮酮和透明质酸钠均可用于哌仑西平滴眼液中,为临床应用提供了新的思路。
Objective To investigate the corneal permeability of different formulations of pirenzepine eye drops and provide the basis for clinical application. Methods 2% pirenzepine eyedrops (pirenzepine alone), 2% pirenzepine + 0.1% sodium hyaluronate eye drops (sodium hyaluronate) and 2% pirenzepine + 0.1% nitrogen Ketone eye drops (Azone group). Sixty-three New Zealand white rabbits were divided into 3 groups, and the above eye drops were dripped into conjunctival sacs of rabbits in each group. The rabbits were dripped for 6 times at intervals of 5 minutes. 0.5ml · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · · + Pirenzepine concentration, and in each eye before and after puncture and atrial suction with a slit lamp microscope to observe the general situation of rabbit eyes. Results Pirenzepine concentrations in aqueous pirenzepine anterior chamber were (0.40 ± 0.06), (0.53 ± 0.03), (1.52 ± 0.33) and (0.15 ± 0.02) μg / ml, respectively. Pirenzepine could not be detected by HPLC after 8.0 h. The concentrations of pirenzepine in the atrial natriuretic group and sodium hyaluronate group at each time point were significantly higher than those in the pirenoxib group (P <0.01), and their bioavailability was about 23.0 times and 3.4 times, respectively. And the experimental group of rabbits eye irritation. Conclusion Adenone group had the best corneal permeability, followed by sodium hyaluronate group, which were significantly higher than that of Pirenzepine group. Both Azone and sodium hyaluronate could be used in pirenzepine eye drops and Clinical application provides a new idea.