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Ex-vivo evaluation of crab shell chitosan as absorption enhancer in ciprofloxacin tablet formulation

机译:蟹壳壳聚糖作为环丙沙星片制剂吸收促进剂的离体评价

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This study was aimed at evaluating crab shell chitosan as absorption enhancer in ciprofloxacin tablet formulation using the ex-vivo model. Six batches of ciprofloxacin tablets containing varying concentrations of crab shell-derived chitosan ranging from 0 to 5% w/w at 1% w/w intervals were produced. Batch CTS-0 containing no chitosan served as the control. The crushing strength, friability, disintegration time, dissolution profile and permeation profile of all the batches were determined. Friability was not significantly affected but the crushing strength and disintegration time of tablets decreased with increase in concentration of chitosan. There was no significant difference in the cumulative percent drug released in 1 h but the cumulative percent drug permeated in 4 h increased with increase in the concentration of chitosan. It increased from 68% (when no chitosan was added) to 81.8% (when 5% w/w chitosan was incorporated). The polymer caused a faster onset of drug release but the eventual total drug released was not significantly influenced. It also improved the permeation of the released drug. This study correlates with in-vivo bioavailability study because the usual oral bioavailability of ciprofloxacin without absorption enhancer is 70%. Hence, crab shell chitosan at concentration of 5% w/w could increase the absorption of ciprofloxacin from 70 to 82%. The study suggests the use of the chitosan at this concentration to improve the absorption of ciprofloxacin.
机译:这项研究旨在使用离体模型评估蟹壳壳聚糖作为环丙沙星片剂中吸收增强剂的作用。制备了六批环丙沙星片剂,它们含有不同浓度的蟹壳衍生的壳聚糖,浓度范围为0%至5%w / w,间隔为1%w / w。不含壳聚糖的批号CTS-0用作对照。测定所有批次的抗碎强度,易碎性,崩解时间,溶解曲线和渗透曲线。脆性没有受到显着影响,但是随着壳聚糖浓度的增加,片剂的抗碎强度和崩解时间降低。 1小时内释放的累积百分数没有显着差异,但随着壳聚糖浓度的增加,在4小时内渗透的累积百分数增加。它从68%(当不添加壳聚糖时)增加到81.8%(当掺入5%w / w壳聚糖时)。聚合物引起药物释放的更快开始,但是最终释放的总药物没有受到显着影响。它还改善了释放药物的渗透性。该研究与体内生物利用度研究相关,因为没有吸收促进剂的环丙沙星的常规口服生物利用度为70%。因此,浓度为5%w / w的蟹壳壳聚糖可以将环丙沙星的吸收率从70%增加到82%。研究表明,以这种浓度使用壳聚糖可改善环丙沙星的吸收。

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