Vieillard V, Eychenne N, Astier A, Yiou R, Deffaux C, Paul M
Service de pharmacie, hôpital Henri-Mondor, 51, avenue du Maréchal-de-Lattre-de-Tassigny, 94010 Créteil cedex, France.
Ann Pharm Fr. 2013 Sep;71(5):358-63. doi: 10.1016/j.pharma.2013.06.005. Epub 2013 Aug 21.
Currently, severe erectile dysfunction can be treated by intracavernous injections of solutions containing three active ingredients: prostaglandin E1 (PGE1), papaverine and urapidil. Very few data exist on this mixture where phentolamine has been replaced by Urapidil because Phentolamine is not used for this indication in France. The aim of our study was to assess the stability of this formulation and to extend its expiration to permit preparation of batches. Three batches of the preparation containing 15μg/mL PGE1, 15mg/mL of papaverine and 2mg/mL urapidil were made aseptically and then packed in polypropylene syringes stored at 4°C. The physico-chemical stability has been tested as follows: HPLC stability-indicating method, visual observation, measurement of pH and osmolarity. We found that the limiting factor was PGE1 and we exceeded the threshold of 10% loss after 55 days. Replacement of Urapidil by Phentolamine seems to have a slight detrimental effect on stability. Nevertheless, these results allow us to consider the advance preparation of this formulation and provide quality treatment to these patients by avoiding too frequent visits to the hospital.
目前，重度勃起功能障碍可通过海绵体内注射含有三种活性成分的溶液进行治疗：前列腺素E1（PGE1）、罂粟碱和乌拉地尔。关于用乌拉地尔替代酚妥拉明的这种混合物的数据非常少，因为在法国酚妥拉明不用于此适应症。我们研究的目的是评估该制剂的稳定性并延长其有效期以允许批量制备。无菌制备了三批含有15μg/mL PGE1、15mg/mL罂粟碱和2mg/mL乌拉地尔的制剂，然后包装在聚丙烯注射器中，储存在4°C。理化稳定性测试如下：HPLC稳定性指示方法、目视观察、pH值和渗透压测量。我们发现限制因素是PGE1，55天后我们超过了10%损失的阈值。用酚妥拉明替代乌拉地尔似乎对稳定性有轻微不利影响。尽管如此，这些结果使我们能够考虑提前制备该制剂，并通过避免患者过于频繁地前往医院就诊为这些患者提供优质治疗。
