Abstract：
The buccal route has great prospects and possible benefits for the administration of drugs systemically. The present study involves designing, developing and optimising the buccal tablet formulation of Enalapril Maleate (EM) by using the QbD approach. We prepared the EM buccal tablets using the dry granulation method. In the QTPP profile, the CQAs for EM buccal tablets are Mucoadhesive strength, swelling index and drug release (dependent variables); the CMAs identified for EM buccal tablets were Carbopol 934P, HPMC-K100M and chitosan (independent variables). Diluent quantity, blending time and compression force were selected as CPPs; the Box-Behnkentdesign was used to evaluate the relationship between the CMAs and CPPs. Based on the DoE, the composition of the optimised formulation of EM BT-18 consists of 20mg of EM, 15 mg of carbopol 934p, 17 mg of HPMC-K100M, 10mg of chitosan, 30 mg of PVP K-30, 1 mg of magnesium stearate, 16 mg of Mannitol, 1 mg of aspartame, and 50 mg of Ethyl cellulose. The optimised formulation of EM BT 18 was found to have a Mucoadhesive strength of 24.32±0.30g. The swelling index was 90.74±0.25% and drug release was sustained up to 10 hours 98.4±3.62% compared to the marketed product, whose release was up to 8 hours. We attempted to design a buccal tablet of Enalapril Maleate for sustained drug release in the treatment of hypertension. Patients who cannot take oral medication due to trauma or unconscious conditions could receive the formulation. Development of a newly P.ceutical product is very time-consuming, extremely costly and high-risk, with very little chance of a successful outcome. Hence, this study showed EM tablets are already available on the market but we have chosen a buccal drug delivery system using a novel approach using QbD tools to target the quality of the product accurately.
摘要：
口腔途径对于全身给药具有很大的前景和可能的益处。本研究涉及设计，通过使用QbD方法开发和优化马来酸依那普利（EM）的口腔片剂配方。我们使用干法制粒方法制备EM口腔片剂。在QTPP配置文件中，EM口腔片剂的CQAs是粘膜粘附强度，肿胀指数和药物释放(因变量)；EM含片的CMA为Carbopol934P，HPMC-K100M和壳聚糖(独立变量)。稀释剂数量,选择混合时间和压缩力作为CPPs；Box-Behnkentdesign用于评估CMA和CPPs之间的关系。基于DoE,EMBT-18的优化配方的组成由20mgEM组成，15毫克卡波姆934p，17毫克HPMC-K100M，10mg的壳聚糖，30毫克PVPK-30，1毫克硬脂酸镁，16毫克甘露醇,1毫克阿斯巴甜,和50mg乙基纤维素。发现EMBT18的优化配方具有24.32±0.30g的粘膜粘合强度。与市售产品相比，溶胀指数为90.74±0.25％，药物释放持续10小时98.4±3.62％。释放时间长达8小时。我们试图设计一种马来酸依那普利的口腔片剂，用于治疗高血压的持续药物释放。由于创伤或无意识状况而不能服用口服药物的患者可以接受该制剂。开发一种新的医疗产品非常耗时，极其昂贵和高风险，成功的机会很小。因此，这项研究表明，EM片剂已经在市场上出售，但我们选择了口腔给药系统，使用QbD工具的新方法来准确地定位产品的质量。
