Pisal Sambhaji, Zainnuddin Rana, Nalawade Pradeep, Mahadik Kakasaheb, Kadam Shivajirao
Poona College of Pharmacy and Research Center, Bharati Vidyapeeth Deemed University, Pune-411 038, Maharashtra, India.
AAPS PharmSciTech. 2004 Sep 17;5(4):e64. doi: 10.1208/pt050464.
The polyethylene glycol (PEG) treatment of ciprofloxacin-Indion 234 complex was aimed to retard rapid ion exchange drug release at gastric pH. Ciprofloxacin loading on Indion 234 was performed in a batch process, and the amount of K(+) in Indion 234 displaced by drug with time was studied as equilibrium constant K(DM). Drug-resin complex (DRC) was treated with aqueous PEG solution (0.5%-2% wt/vol) of different molecular weights (MWs) for 2 to 30 minutes. The PEG-treated ciprofloxacin-Indion 234 complex was evaluated for particle size, water absorption time, and drug release at gastric pH. During drug loading on Indion 234, the equilibrium constant (K(DM)) increased rapidly up to 20 minutes with efficient drug loading. Increased time of immersion of the drug resinate in PEG solutions significantly retained higher size particles upon dehydration. The larger DRC particles showed longer water absorption times owing to compromised hydrating power. The untreated DRC showed insignificant drug release in deionized water; while at gastric pH, ciprofloxacin release was complete in 90 minutes. A trend of increased residual particle size, proportionate increase in water absorption time, and hence the retardation of release with time of immersion was evident in PEG-treated DRC. The time of immersion of DRC in PEG solution had predominant release retardant effect, while the effect of molecular weight of PEG was insignificant. Thus, PEG treatment of DRC successfully retards ciprofloxacin ion exchange release in acidic pH.
聚乙二醇(PEG)处理环丙沙星 - 离子交换树脂Indion 234复合物的目的是减缓在胃酸pH值下药物的快速离子交换释放。环丙沙星在Indion 234上的负载采用分批法进行,并研究了随着时间推移药物取代Indion 234中K(+)的量作为平衡常数K(DM)。用不同分子量(MW)的PEG水溶液(0.5%-2% wt/vol)处理药物 - 树脂复合物(DRC)2至30分钟。对PEG处理后的环丙沙星 - Indion 234复合物进行粒径、吸水时间和胃酸pH值下药物释放的评估。在环丙沙星负载到Indion 234的过程中,随着有效药物负载,平衡常数(K(DM))在20分钟内迅速增加。药物树脂酸盐在PEG溶液中浸泡时间增加,脱水后显著保留了更大尺寸的颗粒。较大的DRC颗粒由于水合能力受损,吸水时间更长。未处理的DRC在去离子水中药物释放不明显;而在胃酸pH值下,环丙沙星在90分钟内释放完全。在PEG处理的DRC中,残余粒径增加、吸水时间成比例增加以及释放随浸泡时间延迟的趋势明显。DRC在PEG溶液中的浸泡时间具有主要的释放延迟作用,而PEG分子量的影响不显著。因此,PEG处理DRC成功地减缓了环丙沙星在酸性pH值下的离子交换释放。