Yousaf Abid Mehmood, Naheed Faiza, Shahzad Yasser, Hussain Talib, Mahmood Tariq
Department of Pharmacy, COMSATS University Islamabad, Lahore Campus, Pakistan.
Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan.
Polim Med. 2019 Jan-Jun;49(1):19-26. doi: 10.17219/pim/111516.
Sugar substitutes are used by diabetic, obese and calorie-conscious people. As artificial sweeteners are harmful to the body, natural sweeteners are more suitable. Sugar substitutes are available on the market in tablet forms, which are added to hot or cold drinks. Rapid disintegration and dissolution of sugar substitute-loaded tablet is desired. However, the tablets should be hard enough to maintain their integrity during mechanical shocks.
The objective of this research was to develop rapidly disintegrating and dissolving stevia-loaded tablets with appropriate wetting, hardness and friability.
Several tablets were prepared using different superdisintegrants using the direct compression method. Flowability tests of the powder blends were performed before compression; these test took into account such physical parameters as bulk density, tapped density, angle of repose, compressibility index, and Hausner's ratio. Evaluation of the compressed cores was accomplished with weight variation, hardness, thickness, friability, disintegration time, wetting time, and dissolution.
The disintegration time and wetting time of the tablets were in the following order: sodium starch glycolate > croscarmellose sodium > crospovidone containing tablets. A powder blend consisting of stevia extract, crospovidone, lactose, and magnesium stearate at the optimized ratio of 15/2.5/32/0.5 (w/w/w/w) showed the best flow, rapid disintegration (38 ±0.894 s), wetting (30 ±1 s), and dissolution (~ 95% in 1 min). Moreover, this formulation showed more rapid wetting (30 ±1 s vs 91 ±1.9 s), disintegration (38 ±0.894 s vs 143 ±1.276 s) and dissolution (~ 95% vs 60% in 1 min) than a commercial product.
The tablet consisting of stevia, crospovidone, lactose, and magnesium stearate at the weight ratio of 15/2.5/32/0.5 showed excellent results with regards to dissolution and disintegration; accordingly, this formulation could be a potential sugar substitute for diabetic, obese and/or calorie-conscious individuals.
糖尿病患者、肥胖者以及关注热量摄入的人群会使用糖替代品。由于人工甜味剂对身体有害,天然甜味剂更为适宜。糖替代品在市场上以片剂形式出售,可添加到热饮或冷饮中。人们期望载有糖替代品的片剂能迅速崩解和溶解。然而,片剂应具有足够的硬度,以便在机械冲击过程中保持其完整性。
本研究的目的是开发具有适当润湿性、硬度和脆碎度的速崩速溶甜菊糖苷片。
采用直接压片法,使用不同的超级崩解剂制备了几种片剂。在压片前对混合粉末进行流动性测试;这些测试考虑了诸如堆密度、振实密度、休止角、压缩指数和豪斯纳比等物理参数。通过重量差异、硬度、厚度、脆碎度、崩解时间、润湿时间和溶出度对压制片芯进行评价。
片剂的崩解时间和润湿时间顺序如下:羟丙甲纤维素钠>交联羧甲基纤维素钠>含交联聚维酮的片剂。由甜菊提取物、交联聚维酮、乳糖和硬脂酸镁按15/2.5/32/0.5(w/w/w/w)的优化比例组成的混合粉末表现出最佳的流动性、快速崩解(38±0.894秒)、润湿(30±1秒)和溶出(1分钟内约95%)。此外,该制剂比市售产品表现出更快的润湿(30±1秒对91±1.9秒)、崩解(38±0.894秒对143±1.276秒)和溶出(1分钟内约95%对60%)。
由甜菊糖苷、交联聚维酮、乳糖和硬脂酸镁按重量比15/2.5/32/0.5组成的片剂在溶出和崩解方面表现出色;因此,该制剂可能成为糖尿病患者、肥胖者和/或关注热量摄入人群的潜在糖替代品。