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首页> 美国卫生研究院文献>AAPS PharmSciTech >Controlled Release of Ropinirole Hydrochloride from a Multiple Barrier Layer Tablet Dosage Form: Effect of Polymer Type on Pharmacokinetics and IVIVC
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Controlled Release of Ropinirole Hydrochloride from a Multiple Barrier Layer Tablet Dosage Form: Effect of Polymer Type on Pharmacokinetics and IVIVC

机译：从多阻隔层片剂剂型中控释盐酸罗匹尼罗：聚合物类型对药代动力学和IVIVC的影响

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摘要

The purpose of the present study was to control in vitro burst effect of the highly water-soluble drug, ropinirole hydrochloride to reduce in vivo dose dumping and to establish in vitro–in vivo correlation. The pharmacokinetics of two entirely different tablet formulation technologies is also explored in this study. For pharmacokinetics study, FDA recommends at least 10% difference in drug release for formulations to be studied but here a different approach was adopted. The formulations F8A and F9A having similar dissolution profiles among themselves and with Requip® XL™ (f2 value 72, 77, 71 respectively) were evaluated. The Cmax of formulation F8A comprising hypromellose 100,000 cP was 1005.16 pg/ml as compared to 973.70 pg/ml of formulation F9A comprising hypromellose 4000 cP irrespective of Tmax of 5 and 5.75 h, respectively. The difference in release and extent of absorption in vivo was due to synergistic effect of complex RH release mechanism; however, AUC0–t and AUC0–∞ values were comparable. The level A correlation using the Wagner–Nelson method supported the findings where R2 was 0.7597 and 0.9675 respectively for formulation F8A and F9A. Thus, in vivo studies are required for proving the therapeutic equivalency of different formulation technologies even though f2 ≥ 50. The technology was demonstrated effectively at industrial manufacturing scale of 200,000 tablets.
机译：本研究的目的是控制高度水溶性药物罗匹尼罗盐酸盐的体外猝发效应，以减少体内剂量倾销并建立体内外相关性。在这项研究中还探讨了两种完全不同的片剂配方技术的药代动力学。对于药代动力学研究，FDA建议要研究的制剂在药物释放方面至少相差10％，但此处采用了不同的方法。评价了制剂F8A和F9A之间具有相似的溶出曲线，并且具有XL TM（分别具有f 2值72、77、71）。包含羟丙甲纤维素100,000 cP的制剂F8A的Cmax为1005.16 pg / ml，而包含羟丙甲纤维素4000 cP的F9A制剂973.70 pg / ml则不考虑Tmax分别为5和5.75 h。体内释放和吸收程度的差异是由于复杂的RH释放机制的协同作用所致。但是，AUC0–t和AUC0–∞的值是可比较的。使用Wagner-Nelson方法的A级相关性支持了以下发现：配方F8A和F9A的R 2 分别为0.7597和0.9675。因此，即使f2≥≥50，也需要进行体内研究以证明不同制剂技术的治疗等效性，该技术已在工业生产规模为200,000片的情况下得到了有效证明。

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