Swain Ranjit Prasad, Elhassan Gamal Osman, Bhattacharjee Abhishek, Sahu Ram Kumar, Khan Jiyauddin
GITAM School of Pharmacy, GITAM (Deemed to be University), Visakhapatnam, Andhra Pradesh 530045, India.
School of Pharmaceutical Sciences, Siksha O Anusandhan (Deemed to be University), Bhubaneswar, Odisha 751003, India.
ACS Omega. 2024 Oct 8;9(42):42687-42697. doi: 10.1021/acsomega.3c09145. eCollection 2024 Oct 22.
In the current study, it was intended to prepare liquisolid tablets of pioglitazone HCl to improve the bioavailability and dissolution time of the drug, as it has low solubility in water. Mathematical formulas were adopted, and the quantities of the carrier (MCC), coating material (colloidal silicon dioxides), and nonvolatile liquid vehicle (Tween 80) were taken. Various ratios of the drug to liquid and carrier to coating had been used in the formulation of liquisolid compacts. The evaluation of the formulated liquisolid compacts was done by performing FTIR, DSC, XRD, and SEM studies. Postcompression parameters, dissolution, stability, and bioavailability were accessed for the optimized formulation. FTIR and DSC studies showed the compatibility of the drugs and excipients. XRD revealed the transition to the amorphous state. It was found that the properties of the newly manufactured liquisolid tablets were within the parameters of what is considered acceptable. The optimized formulation of LST10 showed 99.87 ± 0.19% ( < 0.05) pioglitazone released within 60 min of dissolution. Dissolution data treatments ( , IDR, RDR, %DE, MDT, , and ) resulted in better drug release than other drugs studied and marketed tablet formulations. The optimized formulation produced had been proven stable when it was subjected to accelerated stability testing. This suggested that the bioavailability of pioglitazone was enhanced, as indicated by the substantial increase in AUC (3.06-fold) and (4.18-fold). According to the findings, the selected combination and method significantly increased the dissolution time and bioavailability of pioglitazone. Moreover, this developed method can be used for other drugs with low water solubility.
在当前研究中,旨在制备盐酸吡格列酮液固分散体片以提高该药物的生物利用度和溶出时间,因为它在水中的溶解度较低。采用了数学公式,并确定了载体(微晶纤维素)、包衣材料(胶体二氧化硅)和非挥发性液体载体(吐温80)的用量。在液固分散体片的制剂中使用了药物与液体以及载体与包衣的各种比例。通过进行傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、X射线衍射(XRD)和扫描电子显微镜(SEM)研究对制备的液固分散体片进行评价。对优化后的制剂进行了压片后参数、溶出度、稳定性和生物利用度研究。FTIR和DSC研究表明药物与辅料具有相容性。XRD显示转变为无定形状态。发现新制备的液固分散体片的性质在可接受参数范围内。优化后的制剂LST10在60分钟溶出时间内释放出99.87±0.19%(<0.05)的吡格列酮。溶出数据处理( 、IDR、RDR、%DE、MDT、 和 )显示药物释放比其他研究药物和市售片剂制剂更好。所制备的优化制剂在进行加速稳定性试验时已证明是稳定的。这表明吡格列酮的生物利用度得到了提高,AUC(3.06倍)和 (4.18倍)显著增加即表明了这一点。根据研究结果,所选的组合和方法显著增加了吡格列酮的溶出时间和生物利用度。此外,这种开发的方法可用于其他低水溶性药物。