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肠外营养乳剂与长春西汀联合应用的可能性:配伍研究与展望

Potential Use of Common Administration of Emulsion for Parenteral Nutrition and Vinpocetine: Compatibility Study and Prospect.

作者信息

Tomczak Szymon, Kaszuba Kornelia, Szkudlarek Jagoda, Piwowarczyk Ludwika, Jelińska Anna

机构信息

Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, 3 Rokietnicka, 60-806 Poznań, Poland.

出版信息

Metabolites. 2024 Aug 7;14(8):439. doi: 10.3390/metabo14080439.

Abstract

Vinpocetine (VP) is distributed after oral and intravenous administration, and its uptake in the thalamus, basal ganglia, and visual cortex. Due to poor bioavailability (7%) and marked first-pass effect (75%), including a short half-life (2-3 h), oral administration of VP is limited. It requires frequent administration of the drug to obtain a therapeutic effect. Attempts to overcome these difficulties include the use of new drug delivery systems and/or alternative routes of drug administration. One possibility is the common administration of lipid emulsion and drug using the same catheter. However, this procedure is not recommended due to potential interaction and lack of safety data. For this purpose, we checked the compatibility of VP solutions with eight commercially available parenteral nutrition admixtures, i.e., Lipoflex special, Omegaflex special, Lipoflex peri, Omegaflex peri, Kabiven, SmofKabiven, Kabiven Peripheral, and Olimel Peri N4E. Coadministration is only possible if the stability of the drug and the lipid emulsion is confirmed. The available data are scarce and only concern the incompatibility of VP with ibuprofen. Compatibility tests were carried out in simulated administration through a Y-site connector using clinical flow rates. The stability of the drug and lipid emulsion was assessed by visual inspection and measurement of pH, osmolality, particle size as mean droplet diameter (MDD) and percentage of lipids residing in globules larger than 5 µm (PFAT5), zeta potential, polydispersity index, and lipid-free parenteral nutrition admixture(PNA) turbidity. The results of the compatibility of VP with eight commercial PN admixtures showed that all lipid emulsions show different signs of destabilization. In the studied samples, particles larger than 1000 nm, a significant increase in MDD, zeta potential, and loss of homogeneity visible as an increase in the polydispersity index were observed. Most of the samples had PFAT5 above the USP limit (0.05%). Taking into account the obtained data, VP should not be administered with the studied lipid emulsions for parenteral nutrition.

摘要

长春西汀(VP)经口服和静脉给药后会进行分布,并在丘脑、基底神经节和视觉皮层中摄取。由于生物利用度低(约7%)和明显的首过效应(约75%),包括半衰期短(2 - 3小时),口服VP受到限制。需要频繁给药才能获得治疗效果。克服这些困难的尝试包括使用新的药物递送系统和/或替代给药途径。一种可能性是使用同一根导管同时给予脂质乳剂和药物。然而,由于存在潜在相互作用且缺乏安全数据,不建议采用此方法。为此,我们检查了VP溶液与八种市售肠外营养混合制剂的相容性,即特殊Lipoflex、特殊Omegaflex、围手术期Lipoflex、围手术期Omegaflex、卡文、SmofKabiven、外周卡文和Olimel Peri N4E。只有在确认药物和脂质乳剂的稳定性后才可能联合给药。现有数据稀少,且仅涉及VP与布洛芬的不相容性。相容性测试是通过使用临床流速经Y型接口连接器进行模拟给药来进行的。通过目视检查以及测量pH值、渗透压、粒径(以平均液滴直径(MDD)表示)、大于5 µm的球粒中脂质所占百分比(PFAT5)、zeta电位、多分散指数以及无脂质肠外营养混合制剂(PNA)的浊度来评估药物和脂质乳剂的稳定性。VP与八种市售肠外营养混合制剂的相容性结果表明,所有脂质乳剂均呈现出不同程度的不稳定迹象。在所研究的样品中,观察到粒径大于1000 nm、MDD显著增加、zeta电位以及多分散指数增加所显示的均一性丧失。大多数样品的PFAT5高于美国药典规定的限度(0.05%)。考虑到所获得的数据,不应将VP与所研究的用于肠外营养的脂质乳剂一起给药。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1cb/11356329/93ab6aec5772/metabolites-14-00439-g001.jpg

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