Hanaee J, Javadzadeh Y, Taftachi S, Farid D, Nokhodchi A
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran.
Farmaco. 2004 Nov;59(11):903-6. doi: 10.1016/j.farmac.2004.07.006.
Salbutamol is a selective beta(2)-adrenoreceptor agonist with different pharmacological effects. In this research because of the simplicity of suppository application in elderly and its higher plasma concentration than tablets as well as its particular indication in premature labour, salbutamol suppositories were prepared. The suppositories were formulated containing 10 mg of the drug and Witepsol H15, the oleaginous soluble base using melting method. To optimize the release rate of drug, different surfactants namely, sodium lauryl sulphate (SLS) as an ionic surfactant and Tween 80 as well as Arlacel 60 as non-ionic surfactants with different HLBs were chosen. The effect of surfactant concentration on the release rate of salbutamol from suppositories were also investigated. All prepared formulations fulfilled the specifications set down in British Pharmacopoeia. The results showed that Tween 80 (2%w/w) and SLS (0.75%w/w) caused an increase in dissolution rate of salbutamol from suppositories. As anionic surfactants, such as SLS, cause greater damage on mucosa than non-ionic surfactant, such as Tween 80, this study recommended that Tween 80 could be added in suppository formulation in order to increase the dissolution rate of salbutamol. It was also shown that the release rate of salbutamol altered linearly with the amount of Tween 80 in suppository formulations.
沙丁胺醇是一种具有不同药理作用的选择性β₂肾上腺素受体激动剂。在本研究中,由于栓剂应用于老年人较为简便,且其血浆浓度高于片剂,以及在早产方面有特定适应症,因此制备了沙丁胺醇栓剂。这些栓剂采用热熔法制备,含有10毫克药物和油溶性基质Witepsol H15。为了优化药物释放速率,选择了不同的表面活性剂,即离子型表面活性剂十二烷基硫酸钠(SLS)以及具有不同亲水亲油平衡值(HLB)的非离子型表面活性剂吐温80和司盘60。还研究了表面活性剂浓度对沙丁胺醇从栓剂中释放速率的影响。所有制备的制剂均符合英国药典规定的规格。结果表明,吐温80(2%w/w)和十二烷基硫酸钠(0.75%w/w)可提高沙丁胺醇从栓剂中的溶出速率。由于阴离子表面活性剂(如十二烷基硫酸钠)对黏膜的损伤比非离子表面活性剂(如吐温80)更大,本研究建议在栓剂配方中添加吐温80以提高沙丁胺醇的溶出速率。研究还表明,沙丁胺醇的释放速率与栓剂配方中吐温80的用量呈线性变化。