Moghimipour Eskandar, Rezaee Saeed, Salimi Anayatollah, Asadi Elham, Handali Somayeh
Cellular and Molecular Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
J Adv Pharm Technol Res. 2013 Jul;4(3):141-5. doi: 10.4103/2231-4040.116781.
Ciprofloxacin is a fluoroquinolone and is used against a broad spectrum of gram-negative and gram-positive bacteria. The aim of the study is to investigate the effect of structural vehicles and other formulating factors on physical stability and rheological behavior of ciprofloxacin suspension. To formulate the suspensions, the effect of glycerin and polysorbate 80 as wetting agents was evaluated. Then to achieve controlled flocculation, different concentrations of sodium chloride and calcium chloride were added. After choosing suitable wetting and flocculating agents, structural vehicles such as sodium carboxyl methyl cellulose (NaCMC), hydroxypropylmethylcellulose (HPMC) and Veegum were evaluated. Physical stability parameters such as sedimentation volume, the degree of flocculation and the ease of redispersion of the suspensions and growth of crystals were evaluated. After incorporation of structural vehicles, the rheological properties of formulations containing were also studied to find out their rheological behavior. According to the results, suspension containing glycerin (0.2% w/v) and sodium chloride (0.05% w/v) as wetting agent and flocculating agent, respectively, were the most stable formulations regarding their F and N. Microscopic observations showed the growth of crystals in ciprofloxacin suspension in formulation without excipients and the minimum amount of crystal growth was seen in suspension containing NaCMC (0.25% w/v), Veegum (0.1% w/v) and NaCl (0.05% w/v). Rheological studies showed that almost all of the formulations had psuedoplastic behavior with different degree of thixotropy. The formulation containing NaCMC (0.25% w/v), Veegum (0.1% w/v) and NaCl (0.05% w/v) was the most stable formulation. It may be concluded that by altering the amount ratios of formulation factors, the best rheological behavior and the most proper thixotropy may be achieved.
环丙沙星是一种氟喹诺酮类药物，可用于对抗多种革兰氏阴性菌和革兰氏阳性菌。本研究的目的是研究结构载体和其他制剂因素对环丙沙星混悬液物理稳定性和流变学行为的影响。为了制备混悬液，评估了甘油和聚山梨酯80作为润湿剂的效果。然后，为了实现可控絮凝，添加了不同浓度的氯化钠和氯化钙。在选择合适的润湿剂和絮凝剂后，评估了诸如羧甲基纤维素钠（NaCMC）、羟丙基甲基纤维素（HPMC）和硅酸镁铝等结构载体。评估了物理稳定性参数，如混悬液的沉降体积、絮凝程度、再分散难易程度以及晶体生长情况。加入结构载体后，还研究了含药制剂的流变学性质以了解其流变行为。根据结果，分别含有甘油（0.2% w/v）和氯化钠（0.05% w/v）作为润湿剂和絮凝剂的混悬液在F和N方面是最稳定的制剂。显微镜观察显示，在无辅料的环丙沙星混悬液制剂中有晶体生长，而在含有NaCMC（0.25% w/v）、硅酸镁铝（0.1% w/v）和氯化钠（0.05% w/v）的混悬液中晶体生长量最少。流变学研究表明，几乎所有制剂都具有不同程度触变性的假塑性行为。含有NaCMC（0.25% w/v）、硅酸镁铝（0.1% w/v）和氯化钠（0.05% w/v）的制剂是最稳定的制剂。可以得出结论，通过改变制剂因素的用量比例，可以实现最佳的流变行为和最适宜的触变性。
