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首页> 外文期刊>International Journal of Pharmacy and Pharmaceutical Sciences >PREFORMULATION STUDY OF POLOXAMER 407 GELS: EFFECT OF ADDITIVE
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PREFORMULATION STUDY OF POLOXAMER 407 GELS: EFFECT OF ADDITIVE

机译：POLOXAMER 407凝胶的预成型研究：添加剂的作用

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Objective: Present work was aimed to observe effect of additives normally used in thermoreversible gel formulation. As, the formulation is temperature sensitive, it seems gelling is likely be additives dependent. Thermoreversible gels for nasal administration of sumatriptan succinate were prepared to improve bioavailability and patient compliance. Methods: In this, effect of concentrations of various additives on that is enthalpy of gelation and enthalpy of gel melting were observed. These include poloxamer 407 (thermoreversible polymer), sorbitol (osmotic agent), carbopol 934 P (mucoadhesive agent), benzalkonium chloride (preservative) and sumatriptan succinate. Aqueous gels containing poloxamer 407 (16%, 18%, 20%, 22%, 24% w/w) were prepared. Gels of all above additives were prepared separately by cold method with a concentration of sorbitol (0.5 M, 1M, 1.5M), carbopol 934 P (0.25%, 0.5%, 0.75%, 1% w/w), sodium chloride (0.45%, 0.90 %, 1.5% w/w) benzalkonium chloride (0.02, 0.04, 0.06% w/w) and sumatriptan succinate 25mg/100 g. Results: For plain poloxamer gels, as T1 decreases and T2 increases with increase in poloxamer 407 concentrations, enthalpy of gelation was reduced and enthalpy of gel melting increased. Decrease in T1 and T2 was found with sorbitol and extent of decrease in T2 was significant. Carbopol 934 P and sodium chloride was shown to decrease T1and T2with increase in their concentration. No effect of benzalkonium chloride and sumatriptan succinate was observed on T1 and T2. Conclusion: There are considerable thermodynamic effects of additives on thermoreversible gelation. It is essential to consider this in formulation development of thermoreversible gel
机译：目的：目前的工作旨在观察通常用于热可逆凝胶制剂的添加剂的效果。由于该制剂对温度敏感，因此胶凝似乎可能取决于添加剂。鼻腔给予舒马曲坦琥珀酸酯的热可逆性凝胶的制备可提高生物利用度和患者依从性。方法：在这种方法中，观察到各种添加剂的浓度对凝胶化焓和凝胶熔化焓的影响。这些包括泊洛沙姆407（热可逆性聚合物），山梨糖醇（渗透剂），卡波普934 P（粘膜粘附剂），苯扎氯铵（防腐剂）和舒马普坦琥珀酸酯。制备含有泊洛沙姆407（16％，18％，20％，22％，24％w / w）的水凝胶。所有上述添加剂的凝胶均通过冷法分别制备，其浓度为山梨糖醇（0.5 M，1M，1.5M），Carbopol 934 P（0.25％，0.5％，0.75％，1％w / w），氯化钠（0.45） ％，0.90％，1.5％w / w）的苯扎氯铵（0.02、0.04、0.06％w / w）和舒马曲坦琥珀酸盐25mg / 100g。结果：对于普通泊洛沙姆凝胶，随着泊洛沙姆407浓度的增加，随着T1的降低和T2的增加，凝胶的焓降低并且凝胶的熔融焓增加。发现山梨糖醇降低了T1和T2，并且T2的降低程度很明显。结果表明，Carbopol 934 P和氯化钠会随着浓度的增加而降低T1和T2。没有观察到苯扎氯铵和舒马曲坦琥珀酸酯对T1和T2有影响。结论：添加剂对热可逆凝胶化具有相当大的热力学作用。在热可逆凝胶的配方开发中必须考虑到这一点

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