格列美脲分散片与传统片剂在兔子体内的药代动力学比较评估

IF 2.4 4区 医学 Q3 CHEMISTRY, MEDICINAL
Altaf Ur Rahman, Fazli Nasir, Muzna Ali Khattak, Talaya Hidayatullah, Sadia Pervez, Syeda Rabqa Zainab, Arbab Tahir Ali, Shazma Gohar, Gul E Maryam, Waleed H Almalki
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引用次数: 0

摘要

目标:制备格列美脲口服分散片(ODT)的目的是使其起效迅速、生物利用度更高,同时便于吞咽困难患者服用,以改善患者的依从性:格列美脲是一种当代降糖药物,属于磺酰脲类衍生物。它适用于 2 型糖尿病。遵医嘱用药仍然是传统给药系统的局限性之一,尤其是在儿科、老年病、精神病和旅行患者中,与商业片剂相比,ODT 为这类人群提供了一种良好的替代剂型:方法:使用动物模型评估了制备的 ODT 和传统片剂(CT)的体内药代动力学参数比较。采用高效液相色谱法测定口服单剂量格列美脲后在预定时间间隔内的血浆浓度。药代动力学参数使用 Summit PK® 软件的 PK Solutions 2.0 进行计算:ODT的Cmax(22.08微克/毫升)明显较高(p= 0.006),而口服分散制剂的tmax较低,为3.0小时。与 CT 相比,ODT 的相对生物利用度为 104.34%,tmax 也向左移动:根据体内研究结果,格列美脲 ODT 在患者依从性、快速起效和提高生物利用度方面均有益处。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comparative pharmacokinetic evaluation of glimepiride orodispersable and conventional tablets in rabbits.

Objectives: Glimepiride Orodispersable Tablets (ODT) were prepared with the goal to have rapid onset of action and higher bioavailability with ease administration to individuals with swallowing difficulty to ameliorate patient compliance.

Significance: Glimepiride is a contemporary hypoglycemic medication that belongs to the family of sulfonylurea derivatives. It is used in type 2 diabetes mellitus. Compliance adherence remains one of the limitations with the conventional drug delivery system especially in pediatric, geriatric, psychiatric, and traveling patients, for such population ODT provides a good alternate dosage form compared with Commercial Tablets.

Method: The Comparative in vivo pharmacokinetic parameters of the prepared ODT and conventional tablets (CT) were evaluated using an animal model. The plasma concentration of Glimepiride after oral administration of a single dose was determined at predetermined time intervals with HPLC. The pharmacokinetic parameters were calculated using PK Solutions 2.0 from Summit PK® software.

Results: The Cmax obtained with ODT (22.08 µg/ml) was significantly (p= 0.006) high, a lower tmax of 3.0 hr was achieved with the orodispersable formulation of the drug. The ODT showed 104.34% relative bioavailability as compared to CT and left shift of tmax as well.

Conclusion: As per findings of the in vivo investigation, the Glimepiride ODT would be beneficial in terms of patient compliance, quick onset of action, and increased bioavailability.

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来源期刊
CiteScore
6.80
自引率
0.00%
发文量
82
审稿时长
4.5 months
期刊介绍: The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.
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