Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Cyberjaya, Selangor, Malaysia.
Department of Pharmaceutical Technology, Faculty of Pharmacy, UCSI University, Cheras, Wilayah Persekutuan Kuala Lumpur, Malaysia.
Int J Pharm Compd. 2023 Nov-Dec;27(6):512-521.
Memantine hydrochloride is commonly prescribed for Alzheimer's disease and vascular dementia. However, the drug is only available in tablet form, a dosage form which is difficult for geriatrics to swallow. This problem is especially difficult for those patients diagnosed with Alzheimer's. This study was therefore aimed to develop and characterize an oral disintegrating film containing memantine hydrochloride using different types and concentrations of polymers. Using the solvent casting method, twelve formulations were developed, which involved manipulations on the type and concentration of the polymer. Afterwards, six formulations were selected to undergo characterization tests. These tests evaluated the films' tensile strength, Young's Modulus, percent elongation, folding endurance, disintegration and dissolution time, content uniformity, moisture loss, and moisture uptake. Polymers such as polyvinyl alcohol, hydroxypropyl methylcellulose, polyvinyl pyrrolidone, and pullulan gum were respectively incorporated at different concentrations. The study found that only hydroxypropyl methylcellulose and polyvinyl alcohol formulations developed into acceptable oral disintegrating films. Formulation E (hydroxypropyl methylcellulose 50-mg/film), which exhibited optimal mechanical strength, fast disintegration and dissolution, and excellent content uniformity, was identified as the best formula. Although polyvinyl alcohol showed higher mechanical strength, hydroxypropyl methylcellulose films were better at fulfilling the optimal characteristics of an oral disintegrating film. The study showed that the mechanical strength increased proportionally to the polymer concentration in the polyvinyl alcohol film. However, for the hydroxypropyl methylcellulose film, the mechanical strength increased only when hydroxypropyl methylcellulose's concentration was increased from a 40-mg/film to a 50-mg/film but decreased with a 60-mg/film. To summarize, orally disintegrating films containing memantine hydrochloride was developed, characterized, and reasoned to have high potential to be marketed and to increase medication compliance among geriatrics suffering from Alzheimer's disease.
盐酸美金刚通常用于治疗阿尔茨海默病和血管性痴呆。然而,这种药物只有片剂形式,对于老年人来说,这种剂型很难吞咽。对于那些被诊断患有阿尔茨海默病的患者来说,这个问题尤其困难。因此,本研究旨在开发并描述一种含有盐酸美金刚的口服崩解膜,使用不同类型和浓度的聚合物。通过溶剂浇铸法,开发了 12 种配方,涉及聚合物类型和浓度的操作。然后,选择了 6 种配方进行特征测试。这些测试评估了薄膜的拉伸强度、杨氏模量、伸长率、耐折性、崩解和溶解时间、含量均匀性、水分损失和水分吸收。分别使用了聚乙烯醇、羟丙基甲基纤维素、聚乙烯吡咯烷酮和普鲁兰胶等聚合物,并在不同浓度下进行了操作。研究发现,只有羟丙基甲基纤维素和聚乙烯醇配方制成了可接受的口服崩解膜。E 配方(每片含羟丙基甲基纤维素 50 毫克)表现出最佳的机械强度、快速崩解和溶解,以及出色的含量均匀性,被确定为最佳配方。虽然聚乙烯醇表现出更高的机械强度,但羟丙基甲基纤维素薄膜在满足口服崩解膜的最佳特性方面表现更好。研究表明,聚乙烯醇薄膜的机械强度与聚合物浓度成正比增加。然而,对于羟丙基甲基纤维素薄膜,机械强度仅在羟丙基甲基纤维素浓度从 40 毫克/片增加到 50 毫克/片时增加,但在 60 毫克/片时降低。综上所述,开发了含有盐酸美金刚的口服崩解膜,并对其进行了特征描述,认为其具有很高的市场潜力,可以提高患有阿尔茨海默病的老年人的用药依从性。