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Effect of physicochemical nature of suspending agents on neutralization capacity of alumina and magnesia suspension and functionality testing of hydroxypropyl cellulose.

机译:悬浮剂的理化性质对氧化铝和氧化镁悬浮液的中和能力以及羟丙基纤维素的功能测试的影响。

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摘要

This research deals with the physicochemical effects of ionic and non ionic suspending agents, additives (citrate and tartrate ions) on the in vitro activity of liquid antacid suspensions. Functionality testing of Nisso HPC-L and Klucel-EF in alumina and magnesia suspension was also carried out.;Antacid suspensions were manufactured using Silverson homogenizer. Each suspension contained 200 mg/5 mL of the antacid each of aluminum hydroxide and magnesium hydroxide as the active ingredients, 1% suspending agent, 10% sorbo, 0.2% methylparaben, 0.02% propylparaben, 0.1% sodium saccharin, 0.1% peppermint flavor and purified water q.s. to 100%. Fordtran's in vitro test which simulates the hydrodynamic condition of the stomach has been established as a method with in vivo correlation. And this method was used. In this test 1 mL of the test antacid suspensions was dispersed in 100 mL of purified water at 37°C and agitated with a magnetic bar at 60 rpm. And this was titrated by pH-stat method maintaining pH at 3 by the addition of 0.1 N HCL at specified time interval up to 2 hr. The amount of 0.1 N HCL consumed at the end of 2 hr was converted to milliequivalents of HCL which was taken as a neutralization/buffering capacity of the antacid.;The nature of suspending agents strongly affected the neutralization capacity of the antacid. Suspensions containing Nisso HPC-L, Klucel-EF, sodium carboxymethyl cellulose and sodium alginate showed neutralization capacity of 10.0, 9.87, 5.63 and 4.80 mEq per 5 mL of antacid respectively. This clearly demonstrated superiority of non ionic hydroxypropyl cellulose over ionic sodium carboxymethyl cellulose and sodium alginate and there was no significant difference in buffering capacity of the antacid using Nisso HPC-L and Klucel-EF. It was observed that antacid suspensions containing sodium carboxymethyl cellulose and sodium alginate showed fibrous precipitous mass during neutralization study indicating the incompatibility of the suspending agents with hydrochloric acid. Inclusion of the citrate ions increased the activity of antacids containing Nisso HPC-L, Klucel-EF, sodium carboxymethyl cellulose and sodium alginate up to 12.42, 12.40, 8.43 and 7.75 mEq/5 mL respectively. Inclusion of citrate ion decreased the stability, after 6 months suspensions were hard to re-disperse.;Nisso HPC-L and Klucel-EF containing suspensions had neutralization capacity of 12.42 and 12.40 mEq/5 mL antacid respectively. In a tartrate containing antacids Nisso HPC-L and Klucel-EF showed neutralization capacity of 11.60 and 11.55 mEq/5 mL respectively. Nisso HPC-L and Klucel-EF containing suspensions after 6 months yielded the sedimentation 63% and 60% respectively. Similar sedimentation values for the antacid containing additive potassium citrate were 33% and 35% respectively. They were for potassium sodium tartrate 52% and 50% respectively. Viscosity values for Nisso HPC-L and Klucel-EF containing suspensions were 50 cps and 45 cps respectively showing no significant difference.;Two different grades of Nisso HPC (HPC-SL and HPC-L) had similar in vitro neutralization activity. Antacid suspensions containing aluminum hydroxide gel LV-9 USP and aluminum hydroxide gel Visco-9 USP had no significant difference in neutralization capacity. Neutralization capacity of Maalox, Mylanta and Goldline were 13.0, 12.08 and 11.68 mEq/5 mL respectively. Antacids containing hydroxypropyl cellulose demonstrated comparable results with those of Maalox.
机译:这项研究涉及离子和非离子悬浮剂,添加剂(柠檬酸和酒石酸根离子)对液体抗酸剂悬浮液体外活性的物理化学作用。还对Nisso HPC-L和Klucel-EF在氧化铝和氧化镁悬浮液中的功能进行了测试。每个悬浮液含有200 mg / 5 mL的抗酸剂,分别为氢氧化铝和氢氧化镁作为有效成分,1%悬浮剂,10%山梨醇,0.2%对羟基苯甲酸甲酯,0.02%对羟基苯甲酸丙酯,0.1%糖精钠,0.1%薄荷味和纯净水到100%作为一种具有体内相关性的方法,已经建立了Fordtran的模拟胃水动力状况的体外测试。并且使用了这种方法。在该试验中,将1mL的试验抗酸剂悬浮液在37℃下分散在100mL的纯净水中,并用磁棒以60rpm的速度搅拌。然后通过pH-stat方法滴定,通过在指定的时间间隔(最多2小时)添加0.1 N HCl来保持pH为3。将2小时结束时消耗的0.1 N盐酸转化为毫克当量的盐酸,作为抗酸剂的中和/缓冲能力。悬浮剂的性质强烈影响抗酸剂的中和能力。含有Nisso HPC-L,Klucel-EF,羧甲基纤维素钠和藻酸钠的悬浮液的中和能力分别为每5 mL抗酸剂10.0、9.87、5.63和4.80 mEq。这清楚地证明了非离子羟丙基纤维素优于离子羧甲基纤维素钠和藻酸钠,并且使用Nisso HPC-L和Klucel-EF的抗酸剂的缓冲能力没有显着差异。观察到,在中和研究期间,包含羧甲基纤维素钠和藻酸钠的抗酸剂悬浮液显示出纤维状沉淀,表明悬浮剂与盐酸不相容。包含柠檬酸根离子可分别提高包含Nisso HPC-L,Klucel-EF,羧甲基纤维素钠和藻酸钠的抗酸剂的活性,分别高达12.42、12.40、8.43和7.75 mEq / 5 mL。六个月后,悬浮液难以再分散,柠檬酸离子的加入降低了稳定性。含Nisso HPC-L和Klucel-EF的悬浮液的中和能力分别为12.42和12.40 mEq / 5 mL抗酸剂。 Nisso HPC-L和Klucel-EF在含有抗酸剂的酒石酸盐中的中和能力分别为11.60和11.55 mEq / 5 mL。 6个月后,含有Nisso HPC-L和Klucel-EF的悬浮液分别产生了63%和60%的沉降。含抗酸剂添加剂柠檬酸钾的相似沉降值分别为33%和35%。它们分别是酒石酸钾钠的52%和50%。含Nisso HPC-L和Klucel-EF的悬浮液的粘度值分别为50 cps和45 cps,无显着差异。两种不同等级的Nisso HPC(HPC-SL和HPC-L)具有相似的体外中和活性。包含氢氧化铝凝胶LV-9 USP和氢氧化铝凝胶Visco-9 USP的抗酸悬浮液的中和能力无明显差异。 Maalox,Mylanta和Goldline的中和能力分别为13.0、12.08和11.68 mEq / 5 mL。含有羟丙基纤维素的抗酸剂显示了与Maalox相当的结果。

著录项

  • 作者

    Patel, Zalak H.;

  • 作者单位

    Long Island University, The Brooklyn Center.;

  • 授予单位 Long Island University, The Brooklyn Center.;
  • 学科 Pharmaceutical sciences.
  • 学位 M.S.
  • 年度 2009
  • 页码 74 p.
  • 总页数 74
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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