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首页> 外文期刊>World Journal of Gastroenterology >Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs
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Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs

机译：盐酸青藤碱剂型释放特性对其比格犬药代动力学的影响

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AIM: To investigate the effect of release behavior of sustained-release dosage forms of sinomenine hydrochloride (SM·HCI) on its pharmacokinetics in beagle dogs. METHODS: The in vitro release behavior of two SM·HCI dosage forms, including commercial 12-h sustained-release tablets and 24-h sustained-release pellets prepared in our laboratory, was examined. The two dosage forms were orally administrated to beagle dogs, and then the in vivo SM·HCI pharmacokinetics was investigated and compared. RESULTS: The optimal SM·HCI sustained-release formulation was achieved by mixing slow- and rapid-release pellets (9:1, w/w). The SM·HCI release profiles of the sustained-release pellets were scarcely influenced by the pH of the dissolution medium. Release from the 12-h sustained-release tablets was markedly quicker than that from the 24-h sustained-release pellets, the cumulative release up to 12-h was 99.9% vs 68.7%. From a pharmacokinetic standpoint, the 24-h SM-HCI sustained-release pellets had longer t_(max) and lower C_(max) compared to the 12-h sustained-release tablets, the t_(max) being 2.67±0.52 h vs9.83±0.98 h and the C_(max) being 1 334.45±368.76 ng/mL vs893.12±292.55 ng/mL, respectively. However, the AUC_(0-tn) of two SM·HCI dosage forms was comparable and both preparations were statistically bioequivalent. Furthermore, the two preparations had good correlations between SM·HCI percentage absorption in vivo and the cumulative percentage release in vitro. CONCLUSION: The in vitro release properties of the dosage forms strongly affect their pharmacokinetic behavior in vivo. Therefore, managing the in vitro release behavior of dosage forms is a promising strategy for obtaining the optimal in vivo pharmacokinetic characteristics and safe therapeutic drug concentration-time curves.
机译：目的：探讨青藤碱盐酸盐（SM·HCI）缓释剂型的释放行为对其比格犬药代动力学的影响。方法：研究了两种SM·HCI剂型的体外释放行为，包括我们实验室制备的市售12小时缓释片剂和24小时缓释微丸。将两种剂型口服给予比格犬，然后研究并比较其体内SM·HCI药代动力学。结果：通过将缓释和速释微丸（9：1，w / w）混合，可获得最佳的SM·HCI缓释制剂。缓释微丸的SM·HCl释放曲线几乎不受溶解介质pH的影响。从12小时缓释片中释放的速度明显比从24小时缓释丸剂中释放的速度快，直到12小时的累积释放率为99.9％对68.7％。从药代动力学的角度来看，与12小时持续释放片剂相比，24小时SM-HCI持续释放微丸的t_（max）更长，C_（max）更低，t_（max）为2.67±0.52 h vs9 .83±0.98 h和C_（max）分别为1 334.45±368.76 ng / mL与893.12±292.55 ng / mL。但是，两种SM·HCI剂型的AUC_（0-tn）具有可比性，并且两种制剂在统计学上是生物等效的。此外，两种制剂在体内的SM·HCI吸收百分比与体外累积释放百分比之间具有良好的相关性。结论：剂型的体外释放特性强烈影响其体内药代动力学行为。因此，管理剂型的体外释放行为是获得最佳体内药代动力学特征和安全治疗药物浓度-时间曲线的有前途的策略。

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