Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth University, Erandwane, Pune, 411038, Maharashtra, India.
AAPS PharmSciTech. 2012 Sep;13(3):896-902. doi: 10.1208/s12249-012-9779-2. Epub 2012 Jun 19.
The purpose of this research was to address the utility of naproxen sodium-chitosan spray-dried complexes for antiulcer and antiarthritic activities. The cold stress technique was used to examine the ulcerogenic potential of naproxen sodium (NPX) and spray-dried formulations in the different doses. The ulcerations reduced with the dose of spray-dried complexes of naproxen sodium and chitosan. The conspicuous hemorrhagic lesions were visible in the morphological features of the animal treated with naproxen 50 mg/kg (p.o.). Thus, the results suggest that the spray-dried naproxen sodium-chitosan complex (NPXF) was not corrosive to the gastric mucosa at high doses of 50, 100, and 200 mg/kg (p.o.) under stressful conditions. It is evident from the present investigation that NPXF does not possess any ulcerogenic potential in comparison to naproxen which, under stressful conditions, led to the hypersecretion of HCl, culminating to petichial hemorrhages in the gastric mucosa of the animals. The biphasic pattern was observed in the various arthritic parameters. The rise in paw volume, joint diameter, WBC count, arthritis score, and fall in body weight was significantly ameliorated in the animals treated with NPXF (5, 10, and 20 mg/kg, p.o). At the end of the study, slight erythema was visible in the naproxen-treated animals. However, no erythema, redness, or ulcers were visible in the animals treated with NPXF. Thus, the direct compression properties and reduced ulcerogenic activity, combined with the demonstrated solubilizing power and analgesic effect enhancer ability toward the drug, make naproxen sodium-chitosan spray-dried complexes particularly suitable for developing a reduced-dose, fast-release, solid oral dosage form of naproxen.
本研究旨在探讨萘普生钠-壳聚糖喷雾干燥复合物在抗溃疡和抗关节炎活性方面的应用。采用冷应激技术研究不同剂量的萘普生钠（NPX）和喷雾干燥制剂的致溃疡潜力。与萘普生钠和壳聚糖的喷雾干燥复合物的剂量相比，溃疡减少。用 50mg/kg（po）的萘普生治疗的动物的形态特征中可见明显的出血性病变。因此，结果表明，在应激条件下，高剂量 50、100 和 200mg/kg（po）时，喷雾干燥的萘普生钠-壳聚糖复合物（NPXF）对胃黏膜没有腐蚀性。目前的研究表明，与在应激条件下导致胃酸分泌过多，导致动物胃黏膜出现小片状出血的萘普生相比，NPXF 没有任何致溃疡潜力。在各种关节炎参数中观察到双相模式。用 NPXF（5、10 和 20mg/kg，po）治疗的动物的爪体积、关节直径、白细胞计数、关节炎评分和体重下降均显著改善。研究结束时，在萘普生治疗的动物中可见轻微红斑。然而，在接受 NPXF 治疗的动物中未见红斑、发红或溃疡。因此，直接压缩性能和降低的致溃疡活性，加上显示的增溶能力和对药物的镇痛作用增强能力，使萘普生钠-壳聚糖喷雾干燥复合物特别适合开发低剂量、快速释放、固体口服萘普生剂型。
