Casiraghi Antonella, Centin Giorgio, Selmin Francesca, Picozzi Claudia, Minghetti Paola, Zanon Davide
Department of Pharmaceutical Sciences, Università degli Studi di Milano, 20133 Milan, Italy.
Pharmacy and Clinical Pharmacology Department, Institute for Maternal and Child Health IRCCS Burlo Garofolo, 34137 Trieste, Italy.
Pharmaceutics. 2021 Nov 19;13(11):1963. doi: 10.3390/pharmaceutics13111963.
The availability of liquid oral preparations compounded by pharmacists is essential to meet paediatric needs which remain unanswered by the pharmaceutical industry. Unfortunately, compendial monographs are often not available and, in many cases, pre-formulation studies (e.g., compatibility with other excipients and solubility evaluations) are not performed in-depth, leading, in some rare cases, to the inadvertent administration of a toxic dose. In this study, the preparation of an oral liquid formulation for paediatric use, containing flecainide acetate at different strengths, was considered, taking into account the possible effects of conventionally used excipients. First, the optimal vehicle was selected based on a solubility study, evidencing some unexpected formations of precipitates. As a matter of fact, the buffers commonly used for oral solutions significantly reduced flecainide solubility, and the concomitant presence of citrate buffer and methylparaben even caused the formation of non-resuspendable crystals. Then, chemical, physical, and microbiological stability were assessed. Solutions at strengths of 10 and 20 mg/mL flecainide acetate were stable up to 8 weeks when compounded by using a 40% sucrose solution as a vehicle. Microbiological data showed that the use of methylparaben was not necessary over this time period.
药剂师配制的液体口服制剂对于满足制药行业尚未解决的儿科需求至关重要。不幸的是,通常没有药典专论,而且在许多情况下,预制剂研究(例如,与其他辅料的相容性和溶解度评估)没有深入进行,在一些罕见的情况下,会导致意外给予有毒剂量。在本研究中,考虑到传统使用辅料的可能影响,研究了含不同浓度醋酸氟卡尼的儿科用口服液体制剂的制备。首先,基于溶解度研究选择了最佳载体,发现有一些意外的沉淀形成。事实上,口服溶液常用的缓冲剂显著降低了氟卡尼的溶解度,柠檬酸盐缓冲剂和对羟基苯甲酸甲酯同时存在甚至导致形成不可再悬浮的晶体。然后,评估了化学、物理和微生物稳定性。当使用40%蔗糖溶液作为载体配制时,浓度为10和20mg/mL醋酸氟卡尼的溶液在长达8周的时间内是稳定的。微生物学数据表明,在此时间段内没有必要使用对羟基苯甲酸甲酯。