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采用高分子魔芋葡甘聚糖的多潘立酮改良胃部靶向漂浮微球用于新兴健康病理

Ameliorated Stomach Specific Floating Microspheres for Emerging Health Pathologies Using Polymeric Konjac Glucomannan-Based Domperidone.

机构信息

Vaasudhara College of Pharmacy, Sante Circle, Chintamani Road, Hoskote, 562114 Karnataka, India.

Institute of Pharmaceutical Education and Research, Borgaon (Meghe), Wardha, Maharashtra 442 001, India.

出版信息

Biomed Res Int. 2022 Jul 13;2022:3670946. doi: 10.1155/2022/3670946. eCollection 2022.

Abstract

The goal of this study was to use polymeric konjac glucomannan (KGM), Kollidon VA 64 (KVA64), and glutaraldehyde to ameliorate stomach specific floating microspheres (SSFM) using domperidone (DoN) to increase bioavailability and emerging health pathologies. The SSFM were made using the emulsion cross-linking process, and the polymer was chosen based on its ability to get cross-linked. The thermodynamic parameters were used to determine the A classes of phase solubility curves using ideal complexes produced with KVA64. The optimal interaction constants at 25 and 37°C were found to be 116.14 and 128.05 M, respectively. The prepared SSFM had an average particle size (PS) of 163.71 ± 2.26 mm and a drug content of 96.66 ± 0.32%. It can be determined from drug release experiments that drug release is good in terms of regulated drug release after 12 h (92.62 ± 2.43%). The SSFMs were approximately sphere-shaped and had smooth surfaces, according to the morphological data. SSFMs were investigated using Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), and differential scanning calorimetry (DSC), and no chemical structural changes were identified. The SSFMs produces a considerable gastric residence time with optimal DoN release and absorption in stomach fluid, and the mean residence time (17.36 ± 1.4 h) and (10.47 ± 0.6 h) were considerably longer ( < 0.05) than those obtained following i.v. treatment (MRT = 8.42 ± 1.2 h; = 9.07 ± 0.7 h). The SSFMs maintained good physical stability for three months when stored at room temperature.

摘要

本研究的目的是使用聚合魔芋葡甘露聚糖(KGM)、共聚维酮(KVA64)和戊二醛来改善胃特定漂浮微球(SSFM),以提高多潘立酮(DoN)的生物利用度和新兴健康病理。SSFM 是通过乳液交联工艺制成的,选择聚合物是基于其交联能力。使用理想复合物测定热力学参数,确定 KVA64 产生的 A 类相溶解度曲线。在 25 和 37°C 下发现最佳相互作用常数分别为 116.14 和 128.05 M。制备的 SSFM 的平均粒径(PS)为 163.71 ± 2.26 mm,药物含量为 96.66 ± 0.32%。从药物释放实验可以看出,在 12 小时后(92.62 ± 2.43%),药物释放良好,符合调节药物释放的要求。根据形态学数据,SSFM 呈近似球状,表面光滑。通过傅里叶变换红外(FT-IR)光谱、X 射线衍射(XRD)和差示扫描量热法(DSC)对 SSFM 进行了研究,未发现化学结构发生变化。SSFM 在胃液中具有较长的胃滞留时间和最佳的多潘立酮释放和吸收,平均滞留时间(17.36 ± 1.4 h)和(10.47 ± 0.6 h)明显长于静脉注射治疗(MRT = 8.42 ± 1.2 h;= 9.07 ± 0.7 h)(<0.05)。SSFM 在室温下储存三个月时保持良好的物理稳定性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7963/9300317/58070fb0f64d/BMRI2022-3670946.001.jpg

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