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首页> 外文期刊>European journal of pharmaceutics and biopharmaceutics: official journal of Arbeitsgemeinschaft fuer Pharmazeutische Verfahrenstechnik e.V >Release characteristics and in vitro-in vivo correlation of pulsatile pattern for a pulsatile drug delivery system activated by membrane rupture via osmotic pressure and swelling.
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Release characteristics and in vitro-in vivo correlation of pulsatile pattern for a pulsatile drug delivery system activated by membrane rupture via osmotic pressure and swelling.

机译：经由渗透压和溶胀引起的膜破裂激活的搏动性药物传递系统的搏动性模式的释放特征和体内外相关性。

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摘要

This study attempted to characterize the influence of core and coating formulations on the release profiles to establish in vitro/in vivo correlations of pulsatile pattern for a pulsatile drug delivery system activated by membrane rupture based on three core tablet formulations (A-core: HPMC 50+4000 cps, B-core: E10M, and C-core: K100M) coated with various thicknesses of a semipermeable ethylcellulose membrane plasticized with HPMC 606 (Pharmacoat 606) at different ratios with/without adding various amounts of water to dissolve it in the coating solution. Drug release behaviors were investigated using apparatus II in four media of pH 1.2 solution, pH 6.8 buffer, deionized water, and a NaCl solution rotated at 75, 100, and 150 rpm. Pilot studies of the in vivo pharmacokinetics were conducted as well for comparison with the in vitro results. Results demonstrated that drug release from the three kinds of core tablets in deionized water increased with an increasing stirring rate, and decreased with an increasing viscosity grade of HPMC used in the core formulations. A significant promotion of drug release from core tablets was observed for the three levels of NaCl media in comparison with that in deionized water. Results further demonstrated that a slightly slower release rate in pH 1.2 solution and a faster release rate in pH 6.8 buffer than that in deionized water were observed for the A-core and B-core tablets, with the former being slower than the latter. However, similar release rates in the three kinds of media were observed for C-core tablets, but they were slower than those for the A- and B-core tablets. Dissolution of coated tablets showed that the controlling membrane was ruptured by osmotic pressure and swelling which activated drug release with a lag time. The lag time was not influenced by the pH value of the release medium or by the rotation speeds. The lag time increased with a higher coating level, but decreased with the addition of the hydrophilic plasticizer, Pharmacoat 606, and of the water amount in the coating solution. The lag time also increased with a higher concentration of NaCl in the medium. The release rate after the lag time was determined by the extent of retardation of gelation of HPMC in the core tablet based on the ionic strength of the medium. Results of the three pilot crossover studies for the exemplified pulsatile systems indicated that the lag time for the in vivo plasma profile was well correlated with that determined from the in vitro release profile in pH 1.2 solution and the in vivo release rate was better reflected by that performed in pH 6.8 buffer.
机译：这项研究试图表征核心和包衣制剂对释放曲线的影响，以建立基于三种核心片剂的膜破裂激活的脉冲药物传递系统的脉冲模式的体外/体内相关性（A核心：HPMC 50 +4000 cps，B核：E10M和C核：K100M）涂有各种厚度的，以不同比例用HPMC 606（Pharmacoat 606）增塑的半透性乙基纤维素膜，有/没有添加各种量的水将其溶解在涂料溶液。使用装置II在pH 1.2溶液，pH 6.8缓冲液，去离子水和以75、100和150 rpm旋转的NaCl溶液的四种介质中研究了药物的释放行为。还进行了体内药代动力学的初步研究，以与体外结果进行比较。结果表明，在去离子水中，三种核心片中的药物释放随搅拌速率的增加而增加，而随着核心制剂中使用的HPMC粘度等级的增加而降低。与去离子水相比，三种水平的NaCl介质均能显着促进药物从核心片剂释放。结果进一步表明，对于A核和B核片剂，在pH 1.2溶液中的释放速率和在去离子水中的pH 6.8缓冲剂的释放速率都比去离子水中的释放速率稍快，而前者要慢于后者。但是，C核片剂在三种介质中的释放速率相似，但比A核和B核片剂慢。包衣片剂的溶解表明，控制膜由于渗透压和溶胀而破裂，其活化药物的释放具有滞后时间。滞后时间不受释放介质的pH值或转速影响。滞后时间随着涂层水平的提高而增加，但随着亲水性增塑剂Pharmacoat 606的加入和涂层溶液中水量的增加而减少。滞后时间也随着培养基中NaCl浓度的增加而增加。滞后时间后的释放速率由核心片剂中HPMC凝胶化的阻滞程度（基于介质的离子强度）确定。对示例性搏动系统进行的三项交叉试验的结果表明，体内血浆曲线的滞后时间与根据pH 1.2溶液中体外释放曲线确定的滞后时间高度相关，并且体内滞后时间更好地反映了这一点。在pH 6.8缓冲液中进行。

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