Malipeddi Venkata Ramana, Awasthi Rajendra, Dua Kamal
Amity Institute of Pharmacy, Amity University, Lucknow, India.
NKBR College of Pharmacy & Research Centre, Phaphunda, India.
Polim Med. 2017 Jul-Dec;47(2):101-106. doi: 10.17219/pim/90020.
Ciprofloxacin is a broad-spectrum fluoroquinolone antibacterial drug to which most Gram-negative and many Gram-positive bacteria are highly susceptible. Fluoroquinolones are administered repeatedly, twice a day for 5 days, during the course of therapy. Hence, they require repeated administration. Ciprofloxacin qualifies as a drug candidate for a controlled-release drug delivery system.
The present work was aimed to develop ciprofloxacin hydrochloride-containing matrix tablets by the wet granulation method.
The tablets were prepared using EthocelTM 100 Premium and Eudragit® RS PO (Evonik Laboratory, Mumbai, India) as a rate-controlling polymer. Granular dioctyl phthalate (DCP) was used as a diluent. An isopropyl alcohol and dichloromethane (1:1) mixture was used as a granulating agent. The effect of the formulation variables on tablet performance was examined based on weight variation, hardness, friability, thickness, and drug release profiles. The results suggested that the tablets had good integrity.
The tablets were stable for 18 months. Formulation F7 gave a linear release pattern up to 12 h. The release of ciprofloxacin from formulation F7 followed zero-order kinetics. The release mechanism was found to be diffusion-controlled as the Higuchi equation was obeyed.
Ciprofloxacin hydrochloride-containing matrix tablets were prepared successfully. The tablets had good integrity and were found stable for 18 months.
环丙沙星是一种广谱氟喹诺酮类抗菌药物，大多数革兰氏阴性菌和许多革兰氏阳性菌对其高度敏感。在治疗过程中，氟喹诺酮类药物需每日给药两次，持续5天，因此需要重复给药。环丙沙星符合控释给药系统候选药物的条件。
本研究旨在通过湿法制粒法制备含盐酸环丙沙星的骨架片。
以乙基纤维素100 Premium和优特奇®RS PO（赢创实验室，印度孟买）作为控速聚合物制备片剂。使用邻苯二甲酸二辛酯（DCP）颗粒作为稀释剂。采用异丙醇和二氯甲烷（1:1）的混合物作为制粒剂。基于重量差异、硬度、脆碎度、厚度和药物释放曲线，考察了处方变量对片剂性能的影响。结果表明片剂具有良好的完整性。
片剂在18个月内稳定。处方F7在12小时内呈现线性释放模式。F7处方中环丙沙星的释放符合零级动力学。由于符合Higuchi方程，发现释放机制为扩散控制。
成功制备了含盐酸环丙沙星的骨架片。片剂具有良好的完整性，在18个月内稳定。
