反应详情

During several preclinical studies concerning a GHRP-1/ATRIGEL formulation, it was noted that commercial scale manufacture necessitated the standing of the citrate formulation which resulted in some precipitation of GHRP-1 from the GHRP-1/Citrate solution. When citric acid was added to the bulk solution, GHRP-1 tended to precipitate out of the solution over a couple of hours and made syringe filling difficult. Subsequent re-formulation studies showed that addition of a small amount of a solubilizing agent such as acetic acid to the bulk GHRP-1 citrate solution largely ameliorated this precipitation. This formulation was identified as AL3922.02. Subsequently, this formulation (AL3922.02) was found also to exhibit partial precipitation so as to enable commercial manufacture. Consequently, a fourth formulation (AL3922.04) was developed. The new formulation did not exhibit partial precipitation over the time needed for commercial formulation and exhibited similar in vivo release characteristics as the original formulation. Subsequently, the new formulation was slightly altered to produce version 2. Bulk version 2 was stable and did not exhibit precipitation. Version 2 was loaded into a syringe and the syringe contents lyophilized to remove water and acetic acid.