Loperamide Hydrochloride → Loperamide
Reaction equation
[CH3:1][N:2]([C:4]([C:6]([C:29]1[CH:30]=[CH:31][CH:32]=[CH:33][CH:34]=1)([C:23]1[CH:24]=[CH:25][CH:26]=[CH:27][CH:28]=1)[CH2:7][CH2:8][N:9]1[CH2:14][CH2:13][C:12]([OH:22])([C:15]2[CH:16]=[CH:17][C:18]([Cl:21])=[CH:19][CH:20]=2)[CH2:11][CH2:10]1)=[O:5])[CH3:3].Cl>O>[CH3:1][N:2]([C:4]([C:6]([C:29]1[CH:34]=[CH:33][CH:32]=[CH:31][CH:30]=1)([C:23]1[CH:24]=[CH:25][CH:26]=[CH:27][CH:28]=1)[CH2:7][CH2:8][N:9]1[CH2:14][CH2:13][C:12]([OH:22])([C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][CH:16]=2)[CH2:11][CH2:10]1)=[O:5])[CH3:3]Participants
3
Reactant 1
Product 1
Reagents, catalysts & solvents 1
Procedure
Octreotide was provided as a sterile lyophilisate and reconstituted with sterile water for injection to yield a stock solution (10 mg/mL). The stock solution was stored refrigerated (2 to 8° C.). On each day of dosing, the stock solution is diluted with sterile water for injection to a final concentration of 0.1 mg/mL. Loperamide hydrochloride was dissolved in saline for injection to yield a final concentration of loperamide base of 0.1 mg/mL (Note: 1 g of loperamide hydrochloride=0.929 g of loperamide base. A correction factor of 1.076 was used for formulation preparation). Loperamide hydrochloride solution is prepared weekly. Compound 552 was formulated as a solution with 10% hydroxypropyl-β-cyclodextrin (97%) in water. In order to verify the concentration of the test articles in the formulations, representative samples (1.0 mL in duplicate, except for octreotide, where only 0.1 mL each will be collected) were collected at appropriate intervals during the study.