Gurny R, Ryser J E, Tabatabay C, Martenet M, Edman P, Camber O
Department of Pharmaceutical Technology, University of Geneva, Switzerland.
Graefes Arch Clin Exp Ophthalmol. 1990;228(6):510-2. doi: 10.1007/BF00918481.
The aim of the present study was to quantify in man the distribution and clearance of two aqueous sodium hyaluronate (SH) solutions of 0.125% and 0.250% after the administration of 25 microliters onto the cornea. Isotonic phosphate buffer (PB) was used as a reference instillation. No systemic or local medication was given to the seven 18- to 30-year-old, healthy male volunteers. A detailed evaluation of the anterior segment of the eye, as well as a Schirmer test and a break-up time measurement, yielded results within the normal range. The clearance of 0.125% and 0.250% SH solutions radiolabelled with sodium pertechnetate Tc-99m was measured by gamma scintigraphy and compared with that of a PB solution tagged with the same radiolabel. There was no statistically significant difference between the quantities of 0.125% SH and PB solutions remaining in the precorneal space at 20 min (paired t-test, P = 0.78, n = 7). However, in comparing the 0.250% SH with the PB solution, we observed a statistically significant difference (P = 0.01, n = 7) in the amount remaining in the precorneal space after the same interval. Actually, 53% of the radiolabelled 0.250% SH solution remained on the cornea as compared with 30% for the 0.125% SH solution and 18.3% for the PB solution. These results suggest that an SH solution of 0.250% might have a prolonged residence time on the precorneal surface, and that SH could therefore be used as an additive in various drug-release systems for the eye.
本研究的目的是在人体中定量检测25微升0.125%和0.250%的两种透明质酸钠（SH）水溶液滴入角膜后的分布和清除情况。使用等渗磷酸盐缓冲液（PB）作为对照滴注液。7名年龄在18至30岁的健康男性志愿者未接受全身或局部用药。对眼前节进行详细评估以及进行泪液分泌试验和泪膜破裂时间测量，结果均在正常范围内。通过γ闪烁显像法测量用高锝酸钠Tc-99m放射性标记的0.125%和0.250% SH溶液的清除情况，并与标记有相同放射性核素的PB溶液进行比较。20分钟时，角膜前间隙中剩余的0.125% SH溶液和PB溶液的量之间无统计学显著差异（配对t检验，P = 0.78，n = 7）。然而，将0.250% SH与PB溶液进行比较时，我们观察到相同时间间隔后角膜前间隙中剩余量存在统计学显著差异（P = 0.01，n = 7）。实际上，放射性标记的0.250% SH溶液有53%留在角膜上，而0.125% SH溶液为30%，PB溶液为18.3%。这些结果表明，0.250%的SH溶液可能在角膜前表面具有延长的停留时间，因此SH可作为眼部各种药物释放系统的添加剂。
