Alshora Doaa H, Ibrahim Mohamed A, Zayed Gamal, Al Rwashed Mohammed A, Abou-Taleb Heba A, Ali Marwa F
Department of Pharmaceutics, College of Pharmacy, King Saud University, Saudi Arabia.
Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Assiut, Egypt.
Saudi Pharm J. 2022 May;30(5):635-645. doi: 10.1016/j.jsps.2022.02.006. Epub 2022 Feb 14.
According to the American College of Cardiology/American Heart Association (ACC/AHA), both aspirin and statin are used in the primary prevention of cardiovascular diseases. Aspirin (ASA) is contraindicated if there is gastrointestinal bleeding because it will exaggerate the condition. In this study, the effect of surfactant; sodium lauryl sulfate (SLS), in enhancing the dissolution of simvastatin (SIM) and ASA, as well as gastric irritation and upset, was studied. Oral tablets containing both ASA and SIM with and without the SLS were manufactured using the direct compression technique. The prepared tablets were characterized with respect to hardness, friability, uniformity of dosage units, disintegration, and dissolution The effect of the addition of SLS in reducing the irritation and protection of gastric mucosa were also investigated. The results showed that the compressed tablets possessed sufficient hardness, acceptable friability, and are uniform with respect to disintegration, drugs contents, and tablet weight. The results showed that SIM alone exhibited a gastroprotective effect on the induced irritation. In addition, the incorporation of the SLS in the tablets containing SIM and ASA significantly enhanced the dissolution rates of both drugs and significantly decreased the gastric irritation and the ulcer index. The ulcer index of aspirin was decreased from 2.3 for tablets manufactured without SLS to 0.8 for tablets containing SLS. In a conclusion, the addition of pH modifier surfactant; SLS could enhance the dissolution rate of poorly soluble acidic drugs, reduce gastric upset and irritation without any effect on the main characters of the tablets. Moreover, the addition of SLS is very useful in improving the therapeutic activities and reducing the side effects of ASA and SIM for patients who require long-term administration of these drugs.
根据美国心脏病学会/美国心脏协会（ACC/AHA）的建议，阿司匹林和他汀类药物均用于心血管疾病的一级预防。如果存在胃肠道出血，则禁用阿司匹林（ASA），因为它会使病情加重。在本研究中，研究了表面活性剂月桂醇硫酸酯钠（SLS）对辛伐他汀（SIM）和ASA溶出度的增强作用，以及对胃部刺激和不适的影响。采用直接压片技术制备了含或不含SLS的ASA和SIM口服片剂。对制备的片剂进行了硬度、脆碎度、剂量单位均匀性、崩解度和溶出度等方面的表征。还研究了添加SLS对减轻刺激和保护胃黏膜的作用。结果表明，压制片剂具有足够的硬度、可接受的脆碎度，在崩解度、药物含量和片剂重量方面均均匀。结果表明，单独的SIM对诱导的刺激具有胃保护作用。此外，在含有SIM和ASA的片剂中加入SLS显著提高了两种药物的溶出速率，并显著降低了胃部刺激和溃疡指数。阿司匹林的溃疡指数从不含SLS的片剂的2.3降至含SLS的片剂的0.8。总之，添加pH调节剂表面活性剂SLS可以提高难溶性酸性药物的溶出速率，减少胃部不适和刺激，而对片剂的主要特性没有任何影响。此外，对于需要长期服用这些药物的患者，添加SLS在改善治疗效果和降低ASA和SIM的副作用方面非常有用。
