Zaid Abdel Naser, Assali Mohyeddin, Zalmout Samah, Basheer Aseel
Department of Pharmacy, An Najah National University, Nablus, Palestine.
Sama Pharmaceuticals Co. Ltd., Nablus, Palestine.
Eur J Hosp Pharm. 2017 May;24(3):157-161. doi: 10.1136/ejhpharm-2016-000913. Epub 2016 Jun 15.
Statins are the first-line therapy for lowering high lipid levels. Atorvastatin calcium (AtC) is the most commonly prescribed statin. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which converts HMG-CoA into mevalonic acid, a cholesterol precursor.
To compound and evaluate the stability of AtC suspension (0.4% w/v) using commercial tablets or pure AtC powder as the source of the active pharmaceutical ingredient.
Several AtC suspension formulations were produced using commercial AtC tablets or AtC pure powder as the source of the active ingredient. The most suitable one in terms of general organoleptic properties and dissolution was selected for stability studies. For this purpose, samples of final suspensions were stored at room temperature and in the refrigerator. Assay, pH, organoleptic properties and microbial contamination were evaluated according to the USP specifications. High performance liquid chromatography was used for the analysis and quantification of AtC in the studied samples.
The obtained suspension (S4) had good organoleptic properties. It showed complete dissolution of AtC within 30 min. However, the suspension prepared from crushed tablet (S4) showed a better dissolution profile than that prepared from pure powder (S4). The prepared formula had unchanged pH, which remained around 9.9. S and S formulas were both free from microbial contamination. Both products showed good stability within at least the period of use of the 100 mL AtC bottles.
AtC extemporaneous suspension was successfully prepared using tablets as a source of AtC or pure AtC powder. However, S4 had a better dissolution profile than S4. This study provides a solution for patients with swallowing difficulties or feeding tubes who are unable to take medicines in solid oral dosage forms. Community pharmacists can prepare the suspension using AtC tablets as the source of the active ingredient.
他汀类药物是降低高血脂水平的一线治疗药物。阿托伐他汀钙（AtC）是最常用的他汀类药物。它抑制3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶，该酶将HMG-CoA转化为甲羟戊酸，一种胆固醇前体。
以市售片剂或纯AtC粉末作为活性药物成分的来源，制备并评估AtC混悬液（0.4% w/v）的稳定性。
以市售AtC片剂或AtC纯粉末作为活性成分的来源，制备了几种AtC混悬液制剂。根据一般感官性质和溶出度选择最适合的制剂进行稳定性研究。为此，将最终混悬液的样品分别储存在室温下和冰箱中。根据美国药典规范评估含量测定、pH值、感官性质和微生物污染情况。采用高效液相色谱法对研究样品中的AtC进行分析和定量。
所得混悬液（S4）具有良好的感官性质。AtC在30分钟内完全溶解。然而，由压碎片剂制备的混悬液（S4）比由纯粉末制备的混悬液（S4）具有更好的溶出曲线。制备的制剂pH值不变，保持在9.9左右。S4和S4制剂均无微生物污染。两种产品在至少100 mL AtC瓶的使用期内均表现出良好的稳定性。
以片剂或纯AtC粉末作为AtC的来源，成功制备了AtC临时混悬液。然而，S4的溶出曲线比S4更好。本研究为吞咽困难或使用饲管而无法服用固体口服剂型药物的患者提供了一种解决方案。社区药剂师可以使用AtC片剂作为活性成分的来源制备混悬液。
