Parasrampuria J, Das Gupta V
Department of Pharmaceutics, University of Houston, TX 77030.
J Pharm Sci. 1990 Sep;79(9):835-6. doi: 10.1002/jps.2600790919.
Two oral liquid dosage forms of acetazolamide have been developed. Using the solubility profiles, polyethylene glycol 400 (7%, v/v) was used as the solubilizing agent and propylene glycol (53%, v/v) as the cosolvent to keep acetazolamide in solution. Because of the bitter taste of acetazolamide, sweetening agents (simple syrup, sorbitol solution, and artificial sweeteners) and flavors (raspberry, sweet, and menthol) were added to the final formulations. A buffer (either phosphate or citrate) solution was used to maintain a pH value of 4 (pH of maximum stability as reported earlier) to minimize hydrolysis. The final dosage forms were stable for at least 90 days at 37 degrees C (loss of potency of 5%). According to FDA guidelines, a tentative expiry date of 2 years at 25 degrees C is justifiable.
已开发出两种乙酰唑胺口服液体制剂。根据溶解度曲线，使用聚乙二醇400（7%，v/v）作为增溶剂，丙二醇（53%，v/v）作为助溶剂，以使乙酰唑胺保持在溶液中。由于乙酰唑胺有苦味，在最终制剂中添加了甜味剂（单糖浆、山梨醇溶液和人工甜味剂）和香料（覆盆子味、甜味和薄荷味）。使用缓冲液（磷酸盐或柠檬酸盐）将pH值维持在4（如先前报道的最大稳定性pH值），以尽量减少水解。最终剂型在37℃下至少稳定90天（效价损失5%）。根据美国食品药品监督管理局的指导原则，在25℃下暂定有效期为2年是合理的。
