Pharmaceutical evaluation of hospital-prepared, ulinastatin-containing vaginal suppositories

Abstract

Ulinastatin (UTI) is a trypsin inhibitor derived from human urine. UTI has inhibitory activities against many enzymes, and is clinically effective and safe for the treatment of acute pancreatitis. Administration of UTI into the vagina is an effective treatment for threatened premature delivery. Traditional UTI-containing vaginal suppositories may have adverse effects on the stability and quality of UTI because of the properties of Witepsol® W-35. Therefore, we sought to develop UTI-containing vaginal suppositories with good UTI uniformity using a UTI injection solution and Witepsol® S-55. We investigated the influence of moisture content and hardness on the quality of UTI-containing vaginal suppositories. The residual moisture content of vaginal suppositories using S-55 decreased as mixing time increased. In addition, suppository hardness increased as mixing time increased because moisture content decreased. The water phase, which contains UTI, was dispersed uniformly by mixing for 5 h, and prepared vaginal suppositories had uniform UTI content. These results suggest that we can prepare UTI-containing vaginal suppositories with good quality control, and this will be beneficial for patients.