抗坏血酸亚铁浮片治疗贫血的处方及评价

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2019-11-30 DOI:10.2174/2210303109666190708151137
Kuldeep Singh, S. Jain, K. Razdan, Harmanpreet Singh, N. Sahajpal, Harjeet Singh, Amrinder Singh, Shubham Thakur
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引用次数: 1

摘要

抗坏血酸亚铁(FA)优先从上消化道吸收,由于其在上消化道停留时间短,生物利用度较低。此外,FA在高ph下具有低溶解度和稳定性。本研究的目的是制备FA的胃保留片,以增加其在胃中的停留时间,从而提高生物利用度。以聚维酮K30为粘结剂,碳酸氢钠为泡腾剂,采用不同的缓凝聚合物,采用湿造粒法制备FA漂浮片。将所制浮片与立即释放片进行了比较,并对其进行了体外和体内研究。体外释药试验表明,该优化批在0.1 NHCl条件下12 h释药率为96%。该浮片的释药机制无波动,释药动力学最符合peppas模型。与IR片(15-30%)相比,优化后的胃保留时间(6 h)比IR片(70%)显著增加。对健康家兔进行的x射线研究表明,优化后的批剂在胃内容物中保持浮力长达6 h,药代动力学研究表明,与常规IR片相比,优化后的批剂具有缓释行为。FA漂浮片通过增加其胃停留时间来提高铁的生物利用度,因此它可能是治疗铁缺乏症的更好方法,并有助于提高患者的依从性。
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Formulation and Evaluation of Ferrous Ascorbate Floating Tablets for the Treatment of Anaemia
Ferrous ascorbate (FA) is preferentially absorbed from the upper gastrointestinal (GI) track, and has low bioavailability due to less residence time of FA in upper GI track. In addition, FA has low solubility and stability at higher pH. The aim of this study was to prepare gastro-retentive tablets of FA in order to increase its gastric residence time and hence, bioavailability. Floating tablets of FA were prepared by wet granulation method using different retarding polymers, Povidone K30 as binder and sodium bicarbonate as effervescent agent. The prepared floating tablets were compared with immediate release (IR) tablets and characterized in detail for in vitro and in vivo studies. In-vitro drug release study of the optimized batch showed 96% drug release in 12 h in 0.1 N HCl. The mechanism of drug release from the floating tablets was non-fickian and release kinetics was best fit in peppas model. The gastric retention time of optimized was found to be significantly increased (6 h) in comparison with IR tablet (<1h). Further, bioavailability was also found significantly increased (>70%) in comparison with IR tablet (15-30%). X-ray studies carried on healthy rabbits suggested that the optimized batch remained buoyant in gastric contents up to 6 h and pharmacokinetic study showed sustained released behaviour of optimized batch in comparison to conventional IR tablet. Floating tablet of FA improved the bioavailability of iron by increasing its gastric residence time, hence it could be a better approach for treating iron deficiency and help in improving the patient compliance than IR tablets.
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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