Department of Quality Control & Quality Assurance, Holding Company for Biological Products and Vaccines, Cairo, Egypt.
Department of Pharmaceutics, College of Pharmacy, AL-Qassim University, Al-Qassim, Kingdom of Saudi Arabia.
Drug Des Devel Ther. 2022 Dec 13;16:4235-4250. doi: 10.2147/DDDT.S394523. eCollection 2022.
Development and evaluation of bucco-adhesive films of Gliclazide for pediatric use.
Sixteen films were formulated using a different combination of Gelatin, Hydroxy propyl methyl cellulose (HPMC), polyvinyl alcohol, Hydroxy propyl cellulose (HPC), chitosan, polyethylene glycol, sodium alginate, and carbopol. Compatibility study for drug and polymers was conducted using differential scanning calorimetry method and Fourier transform infrared spectroscopy. All films were examined for drug content, weight variation, thickness, swelling index, muco-adhesion and folding endurance. In vitro drug release has been completed for two hours. Stability studies were conducted at 4°C, 25°C, and 40°C for selected films. The optimized formulation based on in vitro data was selected for a bioavailability study in rabbits.
The selected film formula (carbopol 2%, HPMC 2%) did not demonstrate interactions between the drug and polymers, while it showed accepted content, muco-adhesion, and mechanical properties. The in vitro release study showed rapid and complete release of drug from films. Stability studies confirmed accepted stability of the selected film at 4°C and 25°C, but the film get hard with few particles at 40°C. The bioavailability studies conducted showed that there was 2.1 fold increase in the AUC of selected film compared with oral tablets.
Bucco adhesive films of Gliclazide is a promising dosage form for the treatment of diabetes in children.
开发和评估适合儿科使用的格列齐特颊膜。
使用不同组合的明胶、羟丙基甲基纤维素（HPMC）、聚乙烯醇、羟丙基纤维素（HPC）、壳聚糖、聚乙二醇、海藻酸钠和卡波姆，共配制了 16 种膜剂。采用差示扫描量热法和傅里叶变换红外光谱法对药物和聚合物进行相容性研究。对所有膜剂进行药物含量、重量变化、厚度、溶胀指数、黏膜黏附性和耐折性检测。体外药物释放完成 2 小时。对选定的膜剂在 4°C、25°C 和 40°C 下进行稳定性研究。根据体外数据，选择优化的配方进行兔体内生物利用度研究。
所选膜剂配方（卡波姆 2%、HPMC 2%）未显示药物与聚合物之间存在相互作用，同时表现出可接受的药物含量、黏膜黏附性和机械性能。体外释放研究显示药物从膜剂中快速完全释放。稳定性研究证实所选膜剂在 4°C 和 25°C 下具有可接受的稳定性，但在 40°C 下膜剂会变硬并出现少量颗粒。进行的生物利用度研究表明，与口服片剂相比，所选膜剂的 AUC 增加了 2.1 倍。
格列齐特颊膜是一种有前途的儿童糖尿病治疗剂型。
