Preparation of Sodium Polystyrene Sulfonate Suspension Enema for Treatment of Hyperkalemia.

K. Ohsawa, M. Ohtani, S. Kariya, Tohru Shinohara, K. Uchino, Kunji Mita, H. Matsuura, K. Akimoto, H. Kawahara, N. Hashimoto, K. Yakumaru, T. Rikihisa
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Abstract

Enemas of sodium polystyrene sulfonate (SPS) in 20% sorbitol (20% Sor) have regularly been administered by an irrigator for the treatment of hyperkalemia. However, intestinal necrosis, which may be caused by the high osmolality of Sor, has been reported in some patients who received enemas of SPS in Sor.We prepared several SPS suspensions using a 5% glucose solution containing methyl cellulose (MC), hydroxypropyl cellulose (HP) or Avicel RC 591 NF (AB) as a vehicle, and examined the physicochemical properties (dispersibility, osmotic pressure, viscosity and dropping time from irrigator) of each suspension. Among the suspensions tested, the 1% ABG suspension, which was prepared as follows; SPS was suspended in 5% glucose solution containing 1% AB by mixing at 5, 000 rpm for 3 min on a homo mixer, showed the best results. The 1% ABG suspension was isotonic with physiological fluid. A predominant dispersibility of SPS, a low viscosity and a short dropping time from the irrigator were all obtained using this-suspension. The suspension was quite stable for at least 90 days at room temperature.In uremic rats which were made by performing a bilateral nephrectomy, the occurrence of intestinal necrosis and the effect on the serum level of potassium were investigated after the rectal administration of SPS suspensions. No significant pathological changes were noted in rats receiving a 1% ABG suspension. In addition, the 1% ABG suspension caused a significant decrease in the serum level of potassium from the control level.These results suggest that the 1% ABG suspension for enemas of SPS can be useful in the treatment of hyperkalemia.
聚苯磺酸钠悬浮液灌肠治疗高钾血症的制备。
用20%山梨醇(20%山梨醇)中的聚苯乙烯磺酸钠(SPS)灌肠,定期用冲洗器进行高钾血症的治疗。然而,据报道,在一些接受SPS灌肠的患者中,肠坏死可能是由Sor的高渗透压引起的。以含有甲基纤维素(MC)、羟丙基纤维素(HP)或Avicel RC 591 NF (AB)的5%葡萄糖溶液为载体制备了几种SPS悬浮液,并检测了每种悬浮液的物理化学性质(分散性、渗透压、粘度和从灌溉器滴下时间)。在所测试的悬浮液中,1% ABG悬浮液,制备方法如下;将SPS悬浮于含有1% AB的5%葡萄糖溶液中,在同质搅拌器上以5000 rpm的转速搅拌3 min,效果最佳。1% ABG悬浮液与生理液等渗。该悬浮液具有良好的分散性、较低的粘度和较短的滴出时间。该悬浮液在室温下至少90天是相当稳定的。对双侧肾切除后的尿毒症大鼠,直肠给药SPS混悬液后,观察其肠坏死的发生情况及对血清钾水平的影响。接受1% ABG悬液的大鼠未见明显病理改变。此外,1% ABG悬浮液使血清钾水平较对照显著降低。这些结果表明,1% ABG悬浮液用于SPS灌肠可用于治疗高钾血症。
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