Giammaria Daniele, Cinque Benedetta, Di Lodovico Domenico, Savastano Maria Cristina, Cifone Maria Grazia, Spadea Leopoldo
Department of Surgical Sciences, Eye Clinic, University of L'Aquila, L'Aquila - Italy.
Eur J Ophthalmol. 2009 Sep-Oct;19(5):842-7. doi: 10.1177/112067210901900525.
To find out if the combination for intravitreal use of the antibody bevacizumab (AvastinTM; Genentech, Inc., San Francisco, CA) and triamcinolone acetonide (TA) (Kenacort; Bristol-Myers Squibb, Anagni, Italy) could affect over time the anti -vascular endothelial growth factor (VEGF) activity of bevacizumab.
Two different combined preparations were obtained, drawing up together 1.25 mg/0.05 mL of bevacizumab and 2 mg/0.05 mL (B+TA(2mg)) or 4 mg/0.05 mL (B+TA(4mg)) of TA into insulin syringes with 29-G needle. Control preparations were obtained with bevacizumab and an injectable solution (B). The syringes were stored refrigerated at 4 degrees C. The bevacizumab concentration was measured, through its binding to VEGF-165 isoform, at 48 hours and at 1 week.
No preparations showed statistically significant changes in bevacizumab concentration with time (p=0.74 for B+T(2mg), p=0.92 for B+T(4mg), p=0.57 for B). The B+TA(2mg) preparations showed a larger percentage of degradation of bevacizumab than the B+TA(4mg) preparations (28.4% versus 17.6% at 48 hours; 26.4% versus 18% at 1 week). The B control preparations showed the lowest drug degradation: 9.6% at 48 hours and 14.8% at 1 week.
After storage at 4 degrees C for 48 hours and 1 week, the combined preparations showed a larger reduction in bevacizumab concentration than the control preparations. No significant change was observed with the length of storage. The preparations obtained mixing 4 mg/0.05 mL of TA and 1.25 mg/0.05 mL of bevacizumab maintained the highest anti-VEGF activity over time.
探究玻璃体内联合使用抗体贝伐单抗（阿瓦斯汀；基因泰克公司，加利福尼亚州旧金山）和曲安奈德（TA）（康宁克通；百时美施贵宝公司，意大利阿纳尼）是否会随时间影响贝伐单抗的抗血管内皮生长因子（VEGF）活性。
制备两种不同的联合制剂，将1.25mg/0.05mL的贝伐单抗与2mg/0.05mL（B + TA(2mg)）或4mg/0.05mL（B + TA(4mg)）的TA一起吸入带有29G针头的胰岛素注射器中。对照制剂由贝伐单抗和一种可注射溶液（B）制成。注射器在4℃冷藏保存。在48小时和1周时，通过贝伐单抗与VEGF - 165异构体的结合来测量其浓度。
没有制剂显示贝伐单抗浓度随时间有统计学显著变化（B + T(2mg)的p = 0.74，B + T(4mg)的p = 0.92，B的p = 0.57）。B + TA(2mg)制剂中贝伐单抗的降解百分比高于B + TA(4mg)制剂（48小时时为28.4%对17.6%；1周时为26.4%对18%）。B对照制剂显示出最低的药物降解：48小时时为9.6%，1周时为14.8%。
在4℃保存48小时和1周后，联合制剂中贝伐单抗浓度的降低幅度大于对照制剂。储存时间长短未观察到显著变化。混合4mg/0.05mL的TA和1.25mg/0.05mL的贝伐单抗制成的制剂随时间保持了最高的抗VEGF活性。
