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Modulating Gliclazide Release and Bioavailability Utilizing Multiparticulate Drug Delivery Systems
Journal of Pharmaceutical Innovation ( IF 2.7 ) Pub Date : 2021-03-10 , DOI: 10.1007/s12247-021-09542-9
Ebtesam W. Elsayed , Ahmed A. El-Ashmawy , Khaled M. Mahmoud , Nadia M. Mursi , Laila H. Emara

Purpose

To formulate multiparticulate controlled-release alginate-gelatin (AL-GL) beads in order to modify gliclazide (GLZ) release rate.

Methods

AL-GL beads were prepared using different glutaraldehyde concentrations and dried using either air or freeze-drying method. For comparison, calcium alginate beads (AL-beads) were prepared at different temperatures. Drug incorporation efficiency, beads swelling%, drug release rate, and kinetics in gradient conditions (USP Apparatus-4) were studied. Selected AL-GL beads, as a test formulation (T), were in-vivo compared with Diamicron® 80 mg conventional tablet (R).

Results

AL-beads curing temperature was inversely proportional to GLZ incorporation efficiency and directly proportional to beads swelling%. GLZ release from AL-beads was slow in 0.1 N HCl and very fast in pH 7.4. In case of AL-GL beads, GLZ incorporation efficiency and swelling% were inversely proportional to glutaraldehyde concentration. AL-GL beads showed zero-order release of GLZ for up to 11 h. Scanning electron microscope (SEM) images of the freeze-dried beads showed a highly porous surface. Differential scanning calorimetry (DSC) and Fourier transform infra-red (FT-IR) studies indicated an interaction between alginate and gelatin due to crosslinking, while FT-IR indicated the absence of chemical interaction with GLZ. The relative bioavailability (T/R) was 97.57, 138.34, and 143.53%, for Cmax, AUC0–72, and AUC0–∞, respectively. Tmax of T was significantly higher than R.

Conclusion

AL-GL beads could represent promising delivery systems for modulating GLZ release rate and minimizing the variation in its absorption.



中文翻译:

利用多颗粒药物传递系统调节格列齐特的释放和生物利用度

目的

配制多颗粒控释藻酸盐-明胶(AL-GL)珠粒,以改善格列齐特(GLZ)的释放速率。

方法

使用不同的戊二醛浓度制备AL-GL珠粒,并使用空气或冷冻干燥法进行干燥。为了比较,在不同温度下制备藻酸钙珠(AL-珠)。研究了药物掺入效率,珠溶胀%,药物释放速率和梯度条件下的动力学(USP Apparatus-4)。与80 mg常规片剂(R)相比,将选定的AL-GL珠作为测试制剂(T)进行了体内实验。

结果

AL珠的固化温度与GLZ的掺入效率成反比,与珠溶胀%成正比。在0.1 N HCl中,AL珠中的GLZ释放缓慢,而在pH 7.4中,释放非常快。对于AL-GL珠,GLZ的掺入效率和溶胀%与戊二醛浓度成反比。AL-GL珠粒显示GLZ零级释放长达11小时。冷冻干燥的珠的扫描电子显微镜(SEM)图像显示出高度多孔的表面。差示扫描量热法(DSC)和傅立叶变换红外(FT-IR)研究表明,由于交联,藻酸盐和明胶之间存在相互作用,而FT-IR表明与GLZ没有化学相互作用。对于C max,AUC ,相对生物利用度(T / R)为97.57、138.34和143.53%0–72和AUC 0–∞T的T max显着高于R。

结论

AL-GL磁珠可以代表有前途的传递系统,用于调节GLZ释放速率并最大程度地减少其吸收变化。

更新日期:2021-03-10
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