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增稠剂格叶胶对布洛芬儿科制剂的影响。

Effect of grewia gum as a suspending agent on ibuprofen pediatric formulation.

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, 21201, USA.

出版信息

AAPS PharmSciTech. 2011 Jun;12(2):507-13. doi: 10.1208/s12249-011-9606-1. Epub 2011 Apr 14.

Abstract

The purpose of this work was to evaluate the potential of grewia gum (GG) as a suspending agent in pharmaceutical oral formulation using ibuprofen as model drug. Ibuprofen pediatric suspension (25 mg/5 mL) was formulated with grewia gum (0.5% w/v) as the suspending agent. Similar suspensions of Ibuprofen containing either sodium carboxymethylcellulose (Na-CMC) or hydroxymethylpropylcellulose (HPMC) were also produced. The suspensions were evaluated for ease of redispersion, sedimentation, rheological properties, and the effect of aging on the rheological properties at 25°C. The particle size and particle size distributions of the dispersed solute were determined. The redispersion time was 19, 11, and 0.5 min, respectively, for formulation containing Na-CMC, HPMC, and GG .The sedimentation volumes were 0.05, 0.05, and 0.125 mL, respectively, for Na-CMC, HPMC, and GG . Viscosities of suspensions at spindle speed of 25 rpm were of the order: GG > HPMC > Na-CMC when freshly prepared and of the order: HPMC > GG > Na-CMC within 6 months of storage. The particles size was 72.72, 73.82, 81.93, and 83.41 μm, respectively, for suspensions containing Na-CMC, ibuprofen alone, HPMC, and GG. Greatest hysteresis was observed in formulation containing HPMC. All the formulations were stable. It was our conclusion that the difference in the physicochemical properties of ibuprofen pediatric formulations was influenced more by the suspending agent used in the formulations than the drug. GG combined better redispersion with minimal changes in viscosity on storage compared to Na-CMC and HPMC as suspending agent. Thus GG may serve as a good suspending agent requiring no further aid in suspension redispersibility.

摘要

本工作旨在评估格罗娅胶(GG)作为药用口服制剂悬浮剂的潜力,以布洛芬为模型药物。将 GG(0.5%w/v)用作悬浮剂来制备布洛芬儿科混悬剂(25mg/5mL)。还制备了含有羧甲基纤维素钠(Na-CMC)或羟丙基甲基纤维素(HPMC)的类似布洛芬混悬剂。评估了混悬剂的再分散性、沉降性、流变学性质以及在 25°C 下老化对流变学性质的影响。测定了分散溶质的粒径和粒径分布。含 Na-CMC、HPMC 和 GG 的制剂的再分散时间分别为 19、11 和 0.5 分钟。Na-CMC、HPMC 和 GG 的沉降体积分别为 0.05、0.05 和 0.125mL。新鲜制备时,在转速为 25rpm 时悬浮液的粘度顺序为:GG>HPMC>Na-CMC,储存 6 个月时的粘度顺序为:HPMC>GG>Na-CMC。含 Na-CMC、布洛芬单独、HPMC 和 GG 的混悬剂的粒径分别为 72.72、73.82、81.93 和 83.41μm。含 HPMC 的制剂观察到最大滞后。所有配方均稳定。我们的结论是,布洛芬儿科制剂的物理化学性质差异更多地受到制剂中使用的悬浮剂的影响,而不是药物本身。与 Na-CMC 和 HPMC 相比,GG 作为悬浮剂在再分散时具有更好的分散性和最小的粘度变化。因此,GG 可以作为一种良好的悬浮剂,无需进一步辅助悬浮液再分散性。

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