Amaral M H, Lobo J M, Ferreira D C
Centro de Tecnologia do Medicamento, Faculty of Pharmacy, University of Oporto, Rua Aníbal Cunha, 164, 4050-Porto, Portugal.
AAPS PharmSciTech. 2001 Apr 9;2(2):E6. doi: 10.1208/pt020206.
The effect of the concentration of hydrophilic (hydroxypropyl methylcellulose [HPMC]) and hydrophobic (hydrogenated castor oil [HCO]) products, fillers (lactose and dibasic calcium phosphate), and buffers (sodium bicarbonate, calcium carbonate, and sodium citrate) on naproxen release rate was studied. Matrix tablets were prepared by double compression, and in vitro dissolution tests were performed. The dissolution results showed that an increased amount of HPMC or hydrogenated castor oil resulted in reduced drug release. The inclusion of buffers in the HPMC matrix tablets enhanced naproxen release. For HCO tablets, only sodium bicarbonate enhanced naproxen release. The presence of lactose on HPMC matrix tablets did not show a significantly different result from that obtained with the formulation containing dibasic calcium phosphate as a filler. However, for the tablets containing HCO, the presence of lactose significantly enhanced the naproxen release rate. The matrix-forming materials in this study were suitable for use in sustained-release tablets containing naproxen. The drug release can be modulated by adding suitable amounts of diluents and buffers.
研究了亲水性(羟丙基甲基纤维素 [HPMC])和疏水性(氢化蓖麻油 [HCO])产品、填充剂(乳糖和磷酸氢钙)以及缓冲剂(碳酸氢钠、碳酸钙和柠檬酸钠)的浓度对萘普生释放速率的影响。通过二次压制制备了骨架片,并进行了体外溶出试验。溶出结果表明,HPMC 或氢化蓖麻油用量增加会导致药物释放减少。在 HPMC 骨架片中加入缓冲剂可增强萘普生的释放。对于 HCO 片,只有碳酸氢钠能增强萘普生的释放。HPMC 骨架片上乳糖的存在与以磷酸氢钙作为填充剂的制剂相比,未显示出显著不同的结果。然而,对于含有 HCO 的片剂,乳糖的存在显著提高了萘普生的释放速率。本研究中的骨架形成材料适用于含萘普生的缓释片。通过添加适量的稀释剂和缓冲剂可以调节药物释放。