遇见数据集

<p>DATASET.</p>

收藏
NIAID Data Ecosystem2026-05-10 收录
官方服务:

资源简介:

Gastroretentive drug delivery systems (GRDDS) are designed to prolong gastric residence time and improve drug bioavailability. Among these, swelling-based expandable films offer the dual advantage of increased gastric retention and controlled drug release. Metoprolol tartrate, a β1-receptor blocker with a short half-life and low oral bioavailability, was selected as the model drug. This study aimed to develop and evaluate a novel swelling-based expandable gastroretentive film of Metoprolol using a 4 × 4 full factorial design to systematically investigate the effects of HPMC and Carbopol 934 concentrations. Sixteen formulations (F1–F16) were prepared by solvent casting and swelling index (SI) and in vitro drug release were chosen as response variables. The optimized film (F14) exhibited a high SI and sustained drug release, delivering ≈86% of Metoprolol over 12 hours. Kinetic modeling demonstrated first-order and Higuchi release patterns with a non-Fickian mechanism, while model-independent parameters (AIC, MSC, similarity factors) supported these findings. Characterization studies confirmed the robustness of F14: FTIR and XRD revealed no drug–polymer interaction and an amorphous drug state, while SEM showed a uniform surface with interconnected pores. Mechanical testing confirmed desirable tensile strength and flexibility. Radiographic evaluation in rabbits demonstrated that F14 expanded and remained in the stomach for up to 12 hours, validating its gastroretentive capacity. Furthermore, short-term stability testing under accelerated ICH conditions confirmed the film’s physical and chemical stability and sustained-release performance for 6 weeks. In conclusion, the optimized expandable film (F14) combined swelling, gastric retention, and sustained drug release, highlighting its promise as a gastroretentive platform to enhance Metoprolol bioavailability and efficacy.

胃滞留型给药系统(Gastroretentive Drug Delivery Systems, GRDDS)旨在延长药物在胃内的滞留时间,提升药物生物利用度。其中,基于溶胀的可膨胀薄膜兼具增强胃滞留与可控释药的双重优势。本研究选用半衰期短、口服生物利用度低的β1受体阻滞剂酒石酸美托洛尔(Metoprolol Tartrate)作为模型药物,旨在开发并评价一款新型溶胀型可膨胀胃滞留薄膜。实验采用4×4全因子实验设计,系统考察羟丙基甲基纤维素(HPMC)与卡波姆934的浓度对制剂性能的影响。通过溶剂浇铸法制备了16组处方(F1~F16),并以溶胀指数(Swelling Index, SI)和体外药物释放度作为响应变量。优化处方薄膜(F14)表现出较高的溶胀指数与持续释药性能,12小时内累计释放约86%的酒石酸美托洛尔。释药动力学建模分析显示,其释药行为符合一级动力学与Higuchi释药模式,且为非菲克释药机制;非模型依赖参数(赤池信息准则(Akaike Information Criterion, AIC)、MSC与相似因子)进一步验证了上述结果。表征研究证实了F14的优异性能:傅里叶变换红外光谱(Fourier Transform Infrared Spectroscopy, FTIR)与X射线衍射(X-ray Diffraction, XRD)分析表明,薄膜中未发生药物-聚合物相互作用,药物以无定形态存在;扫描电子显微镜(Scanning Electron Microscopy, SEM)观测显示,薄膜表面均匀且具有相互连通的孔道结构。力学性能测试结果证实,该薄膜具备理想的抗拉强度与柔韧性。家兔放射成像评估结果显示,F14薄膜可发生膨胀并在胃内滞留长达12小时,验证了其胃滞留能力。此外,在加速国际人用药品注册技术协调会(International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use, ICH)规定的加速稳定性试验条件下开展的短期稳定性测试表明,该薄膜在6周内可保持良好的物理与化学稳定性,且持续释药性能无明显衰减。综上,优化后的可膨胀薄膜(F14)兼具溶胀、胃滞留与持续释药的多重优势,表明其作为胃滞留型给药平台在提升酒石酸美托洛尔生物利用度与治疗效果方面具有良好的应用前景。

创建时间:
2026-04-01
二维码
社区交流群
二维码
科研交流群
商业服务