Ointment with excellent formulation stability

摘要

Provided is an ointment which has excellent drug stability and excellent drug uniformity. The ointment, which comprises 1 to 5% by weight of 1-[2-[(4S)-4-hydroxy-1,2,3,4-tetrahydroquinolin-1-yl]-4-pyridyl]-2,3-bis(hydroxymethyl)-6,7-dimethoxynaphthalene·3/2 hydrate, 3 to 7% by weight of a separation inhibitor, 15 to 50% by weight of a hydrocarbon gel, a pH controller and 0.05 to 0.4% by weight of an antioxidant, has excellent drug stability and excellent drug dispersibility. In the present ointment, polyoxyethylene (196) polyoxypropylene (67) glycol is preferred as the separation inhibitor, diisopropanolamine is preferred as the pH controller, and dibutylhydroxytoluene is preferred as the antioxidant.

主权项

1. An ointment comprising:
(i) an oil phase containing: 3 to 7% by weight of a separation inhibitor selected from the group consisting of polyoxyethylene (196) polyoxypropylene (67) glycol, cetostearyl alcohol, behenyl alcohol, cetyl palmitate, polyoxyethylene (160) polyoxypropylene (30) glycol and polyoxyethylene (54) polyoxypropylene (39) glycol, and 15 to 50% by weight of a hydrocarbon gel, and (ii) a drug phase being a homogenous solution in which 1 to 5% by weight of 1-[2-[(4S)-4-hydroxy-1,2,3,4-tetrahydroquinolin-1-yl]-4-pyridyl]-2,3-bis(hydroxymethyl)-6,7-dimethoxynaphthalene×3/2hydrate, diisopropanolamine as a pH controller, and 0.05 to 0.4% by weight of an antioxidant selected from the group consisting of dibutylhydroxytoluene, butylhydroxyanisole, propyl gallate, tocopherol and pentaerythrityl-tetrakis[3-(3,5-di-t-butyl-4-hydroxyphenyl)propionate] are dissolved in an aqueous base, the pH of the drug phase being in the range of 8 to 10.5.