Formulation and Evaluation of Linagliptin Buccal Films

H. Ahad, Suprith Doijode, Hindustan K. Mahalingan, Abdul Ahad, Pavan Kumar, Pawan Dhamala
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Abstract

Achieving steady concentration levels of drugs in the plasma for diabetics is important for an extended period. Thestudy focussed on developing mucoadhesive buccal films incorporating linagliptin, aiming to achieve controlled drug delivery foreffective type 2 diabetes management towards steady level plasma concentration. The research utilizes various mucoadhesivepolymers, specifically HPMC K100, HPMC E5LV, and Eudragit RL100, exploring their potential in formulating optimized filmsthrough solvent casting technique. Our primary aim was to identify the most effective formulation, that would ensure controlleddrug release over an extended period. We formulated various formulations and evaluated drug content, swelling index, in-vitrodrug discharge, and ex-vivo mucoadhesive strength. The formulation, incorporated linagliptin, HPMC E5LV, HPMC K100,Eudragit RL100, glycerol, and polyethylene glycol. Results from our comprehensive evaluations showcased favorable dissolutiontime, robust mechanical properties, and impressive mucoadhesive characteristics in the buccal films. The sustained drugdischarge and mucoadhesive strength exhibited by formulation F7 indicate its potential for effective type 2 diabetes managementwith a single film administration lasting up to 8 hours. This research represents a significant step forward in the field ofpharmaceuticals, offering a promising avenue for developing mucoadhesive buccal films to control drug delivery precisely forenhanced therapeutic outcomes in the management of type 2 diabetes.
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利拉利汀颊黏膜的制备与评估
使糖尿病患者血浆中的药物浓度长期保持在稳定水平非常重要。这项研究的重点是开发含有利拉利汀的粘液黏附性口腔黏膜,旨在实现控制性给药,从而有效控制 2 型糖尿病患者的血浆浓度达到稳定水平。研究采用了多种粘液黏性聚合物,特别是 HPMC K100、HPMC E5LV 和 Eudragit RL100,通过溶剂浇铸技术探索它们在配制优化薄膜方面的潜力。我们的主要目的是确定最有效的配方,以确保在较长时间内控制药物的释放。我们配制了多种配方,并对药物含量、膨胀指数、体内药物释放量和体外粘附强度进行了评估。配方中加入了利拉利汀、HPMC E5LV、HPMC K100、Eudragit RL100、甘油和聚乙二醇。我们的综合评估结果表明,颊黏膜具有良好的溶解时间、坚固的机械性能和令人印象深刻的黏附特性。配方 F7 所表现出的持续药物排出和粘附强度表明,它具有单次用药长达 8 小时的潜力,可有效控制 2 型糖尿病。这项研究标志着在制药领域向前迈出了重要一步,为开发粘液黏附性口腔薄膜提供了一条大有可为的途径,可精确控制药物输送,提高 2 型糖尿病的治疗效果。
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