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75 Formulation Properties of Long-acting Injectable Antipsychotics and the Impact on Administration: Focus on Aripiprazole Lauroxil

机译：75长效可注射抗精神病药的配方特性及对管理的影响：专注于阿里普哌唑的Lauroxil

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Clinicians using long-acting injectable (LAI) antipsychotics may assume that there is uniformity in the injection technique for all LAIs. However, because LAIs have significant differences in their formulation, each requires a specific administration procedure. Here, we focus on how the formulation properties of the atypical LAI aripiprazole lauroxil impact its administration.The history of LAI formulations is presented as a background to recent advances in formulation technology. A shared challenge for new LAIs is to adapt the formulation of insoluble drugs to aqueous-based suspensions.The early LAIs kept the drug product dissolved as oil-based solutions, which were stable and did not require mixing prior to injection. However, oil-based solutions tend to be viscous and cause injection-site reactions (ISRs).New LAI formulations tend to be aqueous-based suspensions and need to be resuspended or reconstituted before injection. Beyond this common element, formulation properties lead to differences in administration for each of the available LAIs.We reviewed the formulations of LAIs indicated for the treatment of schizophrenia and how they impact instructions for use, with a focus on aripiprazole lauroxil.Aripiprazole monohydrate and olanzapine pamoate are lyophilized powders that require reconstitution before administration and should be injected slowly. Risperidone is formulated as microspheres in powder form that require reconstitution before injection, although the injection speed is not specified. Paliperidone palmitate is a ready-to-use aqueous suspension of crystalline particles and should be injected slowly. Aripiprazole lauroxil is an aqueous-based, ready-to-use suspension of crystalline particles. Unlike other LAIs, the formulation of aripiprazole lauroxil contains particles that are loosely associated to facilitate resuspension. Because loosely associated suspensions are shear-thinning, meaning the viscosity of the formulation decreases with higher injection force, the injection must be given rapidly. Vigorous shaking and rapid injection are key aspects of administration and have been accepted by patients and investigators in clinical trials. In a pivotal phase 3 study of aripiprazole lauroxil, the incidence of ISRs was low (3.9% and 5.8% for aripiprazole lauroxil 441mg and 882mg , respectively) and mostly associated with the first injection.Advances in formulation technology have increased LAI options for patients with schizophrenia. The aripiprazole lauroxil formulation differs from other LAIs in that the particles are loosely associated to support use as a ready-to-use pre-filled syringe. Because the suspension is shear-thinning, aripiprazole lauroxil requires rapid injection, which is not required when using other LAIs. An understanding of the differences in formulation design and how they impact the specific techniques associated with an LAI is essential for successful administration.Funding Acknowledgements: This study was funded by Alkermes, Inc.
机译：使用长效注射的临床医生（LAI）抗精神病药物可能假设所有LAIS的注射技术都存在均匀性。但是，由于LaIs在其制定中具有显着差异，因此每个都需要特定的管理程序。在这里，我们专注于如何如何对其给药的非典型赖阿里普哌唑的配方性质。赖索制剂的历史作为近期配方技术进步的背景。新LAI的共同挑战是使不溶性药物的制剂适应基于水性的悬浮液。LAIS早期使药物产品溶解为油基溶液，其稳定，并且在注射之前不需要混合。然而，油基溶液倾向于是粘性的并且导致注射部位反应（ISR）。新型配方往往是基于水性的悬浮液，并且需要在注射之前重新悬浮或重构。除了这种共同的元素之外，配方性质导致适用于每个可用的Lais.WE的给药差异，该次审查了Lais的配方，表明为治疗精神分裂症以及它们如何影响使用指令，重点是AripiPrazole Lauroxil.AripiPrazole单水合物和奥氮藻酰胺是在给药前需要重建的冻干粉末，并且应该缓慢注射。在注射前以在注射前进行粉末形式的粉末形式配制成酮酮，尽管未指定注射速度。 Paliperidone Palmitate是一种结晶颗粒的即用含水悬浮液，应该缓慢注射。阿里普哌唑桂罗唑是一种基于含水的即用常用的结晶颗粒的悬浮液。与其他LAIS不同，阿里普哌唑的制剂含有松散地相关的颗粒以促进重悬浮。由于松散相关的悬浮液是剪切变薄，因此意味着配方的粘度随着更高的喷射力而降低，必须快速给出注射。剧烈摇晃和快速注射是给药的关键方面，临床试验中的患者和调查人员已接受。在枢轴相3研究中，ISRS的发病率低（AripiPrazole Lauroxil 441mg和882mg的3.9％和5.8％），主要与第一次注射相关。配方技术中的载体增加了患者的选择精神分裂症。阿里普哌唑的Lauroxil配方与其他LaIs的不同之处在于，颗粒松散地与支撑用作用途预填充注射器的用途相关。由于悬浮液是剪切稀释，因此AripiPrazole Lauroxil需要快速注射，而使用其他Lais时不需要。理解配方设计的差异以及它们如何影响与LAI相关的具体技术对于成功的管理至关重要。文件致谢：本研究由Akalmes，Inc。资助

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