Univ. Bordeaux, EA 4575 Analytical and Pharmaceutical Developments Applied to Neglected Diseases and Counterfeits, Bordeaux, France.
Int J Pharm. 2012 Oct 15;436(1-2):624-30. doi: 10.1016/j.ijpharm.2012.07.030. Epub 2012 Jul 30.
The aim of this study was to identify a candidate formulation for further development of a home or near-home administrable paediatric rectal form of a broad-spectrum antibiotic - specially intended for (emergency) use in tropical rural settings, in particular for children who cannot take medications orally and far from health facilities where injectable treatments can be given. Azithromycin, a broad-spectrum macrolide used orally or intravenously for the treatment of respiratory tract, skin and soft tissue infections, was selected because of its pharmacokinetic and therapeutic properties. Azithromycin in vitro solubility and stability in physiologically relevant conditions were studied. Various pharmaceutical forms, i.e. rectal suspension, two different rectal gels, polyethylene glycol (PEG) suppository and hard gelatin capsule (HGC) were assessed for in vitro dissolution and in vivo bioavailability in the rabbit. Azithromycin PEG suppository appears to be a promising candidate.
本研究旨在确定一种候选制剂，以便进一步开发一种可在家中或接近家中使用的、针对广谱抗生素的直肠给药剂型，特别适用于（紧急）在热带农村环境中使用，特别是针对无法口服药物且远离可提供注射治疗的医疗机构的儿童。阿奇霉素是一种口服或静脉用的广谱大环内酯类药物，用于治疗呼吸道、皮肤和软组织感染，因其药代动力学和治疗特性而被选中。研究了阿奇霉素在生理相关条件下的体外溶解度和稳定性。评估了各种剂型，即直肠混悬剂、两种不同的直肠凝胶、聚乙二醇（PEG）栓剂和硬胶囊（HGC），以考察其在兔体内的体外溶解和体内生物利用度。阿奇霉素 PEG 栓剂似乎是一种很有前途的候选制剂。
