Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, Hokkaido, Japan.
Drug Dev Ind Pharm. 2009 Jul;35(7):780-7. doi: 10.1080/03639040802592443.
Oral sustained release gel formulations may provide a means of administering drugs to dysphagic and geriatric patients who have difficulties with handling and taking oral dosage forms.
We have designed gel formulations for the oral administration of paracetamol with suitable rheological characteristics for ease of administration to patients with swallowing difficulties and sufficient integrity in the acidic environment of the stomach to achieve a sustained release of this drug.
Gels formed by gelatin, agar, gellan, pectin, and xyloglucan were assessed for suitable gel strength and in vitro and in vivo release characteristics.
Gellan (1.5% w/v) and xyloglucan gels (1.5% w/w) had acceptable gel strengths for ease of swallowing and retained their integrity in the rat stomach sufficiently well to sustain the release of paracetamol over a period of 6 hours. Comparison of 1.5% xyloglucan gels with a commercially available preparation with identical paracetamol concentrations demonstrated improved sustained release properties of the xyloglucan gels.
Gels formed by gellan and xyloglucan have suitable rheological and sustained release characteristics for potential use as vehicles for oral delivery of drugs to dysphagic patients.
口服缓释凝胶制剂可为吞咽困难和老年患者提供一种给药方式，这些患者在服用口服剂型方面存在困难。
我们设计了用于口服扑热息痛的凝胶制剂，其具有适合吞咽困难患者给药的适当流变学特性，并且在胃的酸性环境中有足够的完整性，以实现该药物的持续释放。
评估了明胶、琼脂、结冷胶、果胶和木葡聚糖形成的凝胶的适当凝胶强度以及体外和体内释放特性。
结冷胶（1.5%w/v）和木葡聚糖凝胶（1.5%w/w）具有可接受的吞咽凝胶强度，并在大鼠胃中保持足够的完整性，以在 6 小时内持续释放扑热息痛。将 1.5%木葡聚糖凝胶与具有相同扑热息痛浓度的市售制剂进行比较，表明木葡聚糖凝胶具有改善的持续释放特性。
结冷胶和木葡聚糖形成的凝胶具有适合的流变学和持续释放特性，可作为吞咽困难患者口服给药的药物载体。
