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Metoclopramide hydrochloride thermally sensitive rectal in situ gelling system, a novel out-patient treatment for vomiting in pediatric age

机译:盐酸甲丙烷酰胺盐酸盐热敏感直肠原位胶凝系统,一种新型外科治疗呕吐在儿科时代

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摘要

Vomiting is a common symptom of pediatric illness. Rectal route can be considered as an alternative route for antiemetic drugs that complains from difficulty of oral therapy with vomiting and the undesirability of parenteral route due to pain and the need for emergency unit admission. In this study, we attempted to find an alternative and efficient route for Metoclopramide HCL (MET HCL) via its formulation in an in situ gelling system to avoid the limitations of solid suppositories. MET HCL loaded liquid suppositories (LSs) were prepared using Poloxamer 407 (P407) with one of the following mucoadhesive polymers; HPMC, HEC or PVP at different concentrations. Gelation temperature, mucoadhesiveness, pH, drug content and viscosity of the prepared LSs were estimated. All the formulations showed sustained release of MET HCL over 8?h. F15 batch was selected for further investigations due to its higher mucoadhesive force, viscosity and slower drug release. The pharmacokinetic data showed that AUC0-24, Tmax and MRT were significantly higher (p?
机译:呕吐是小儿疾病的常见症状。直肠途径可以被认为是抑制药物的替代途径,其涉及口服治疗呕吐的难度和由于疼痛和急诊单位入院的需要和肠胃外途径的不良性。在这项研究中,我们试图通过其制剂在原位胶凝系统中找到替代和有效的途径,以避免固体栓剂的局限性。 Met HCl负载液栓栓剂(LSS)使用泊洛沙姆407(P407)用以下粘膜粘附聚合物之一制备; HPMC,HEC或PVP,不同浓度。估计凝胶化温度,粘膜粘附性,pH,药物含量和粘度。所有配方均显示出8μlMetHcl的持续释放。选择F15批次因其较高的粘膜粘附力,粘度和较慢的药物释放而进一步研究。药代动力学数据表明,与口腔形式以LS形式施用HCl以LS形式施用时,AUC0-24,Tmax和MRT显着更高(P?<β05)。本研究表明,AS HCL作为LS的给药可能代表口服潜在的替代,具有卓越的治疗益处。

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