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液体载体的流变学性质对固体口服剂型体外吞咽的影响。

Effect of the rheological properties of the liquid carrier on the in vitro swallowing of solid oral dosage forms.

作者信息

Lavoisier Anaïs, Shreeram Sathyavageeswaran, Jedwab Michael, Ramaioli Marco

机构信息

Paris-Saclay Food and Bioproduct Engineering research unit, INRAE, AgroParisTech, Massy, France.

Nestlé Health Science, Singapore, Singapore.

出版信息

J Texture Stud. 2021 Dec;52(5-6):623-637. doi: 10.1111/jtxs.12618. Epub 2021 Jun 23.

DOI:10.1111/jtxs.12618
PMID:34118071
Abstract

Solid oral dosage forms (SODF) are the most popular oral drug delivery forms, but they can be difficult to swallow, especially for patients suffering from swallowing disorders. This study investigated the dynamics of different combinations of liquid carriers and SODF during the oral phase of swallowing using an in vitro model. The rheological properties of the carriers were characterized using shear and extensional rheometry, and their effect on bolus velocity, bolus shape, post-swallow residues, and SODF position within the bolus was evaluated. The latter has been identified as a novel and promising variable to discriminate between alternative formulations. When swallowed with water, capsules and tablets did not impact significantly the velocity of the bolus, but they lagged behind the liquid bolus, suggesting that low viscosity Newtonian fluids are not efficient carriers for SODF. Increasing the viscosity of the carrier at high shear rates improved the ability of the liquid to transport the SODF but also increased the amount of post-swallow residues. At equivalent shear viscosity, elastic and extensional properties of carriers influenced positively the position of the SODF in the bolus. Capsules and tablets were transported toward the front of these boluses, during the oral phase of swallowing, which is considered beneficial to avoid SODF sticking to the mucosa in the following stages of swallowing. Thin elastic liquids appear as an interesting option to promote safe swallowing of capsules and tablets. Clinical studies are, however, necessary to confirm this positive effect in healthy and dysphagic patients.

摘要

固体口服剂型(SODF)是最常见的口服给药形式,但它们可能难以吞咽,尤其是对于患有吞咽障碍的患者。本研究使用体外模型研究了吞咽口腔期不同液体载体与SODF组合的动力学。通过剪切流变仪和拉伸流变仪对载体的流变学特性进行了表征,并评估了它们对团块速度、团块形状、吞咽后残留物以及团块内SODF位置的影响。后者已被确定为区分替代制剂的一个新的且有前景的变量。与水一起吞咽时,胶囊和片剂对团块速度没有显著影响,但它们落后于液体团块,这表明低粘度牛顿流体不是SODF的有效载体。在高剪切速率下增加载体的粘度提高了液体运输SODF的能力,但也增加了吞咽后残留物的量。在等效剪切粘度下,载体的弹性和拉伸特性对SODF在团块中的位置有积极影响。在吞咽口腔期,胶囊和片剂被运输到这些团块的前端,这被认为有利于在吞咽的后续阶段避免SODF粘附在粘膜上。薄弹性液体似乎是促进胶囊和片剂安全吞咽的一个有趣选择。然而,需要进行临床研究以证实这种积极作用在健康和吞咽困难患者中的效果。

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