PHARMACEUTICAL PREPARATION FOR CONTROLLING WATER-SOLUBLE DRUG RELEASE
A solid formulation comprising a water-soluble drug and a hardly water-soluble pharmaceutically-acceptable solid substance, which comprises silicone as a carrier, wherein the silicone formulation can exhibit an excellent controlled-release of the water-soluble drug.
1 . A parenteral solid formulation comprising a water-soluble drug and a hardly water-soluble pharmaceutically-acceptable solid substance, which comprises silicone as a carrier.
2 . The parenteral solid formulation of claim 1 wherein the hardly water-soluble substance is low substituted hydroxypropylcellulose, partly pregelatinized starch, crospovidone, croscarmellose sodium, myristic acid, cholesterol and/or saccharin.
3 . The parenteral solid formulation of claim 1 wherein the hardly water-soluble substance is low substituted hydroxypropylcellulose and/or cholesterol.
4 . The parenteral solid formulation of claim 1 wherein the hardly water-soluble substance is contained in 3 to 35% by weight per the whole weight of the formulation.
5 . The parenteral solid formulation of claim 1 wherein the silicone is contained in 55% or more by weight per the whole weight of the formulation.
6 . The parenteral solid formulation of claim 1 further comprising a water-soluble additive agent.
7 . The parenteral solid formulation of claim 6 wherein the water-soluble additive agent is sodium chloride, glucose, mannitol, lactose, glycine, sodium cholate, sodium desoxycholate and/or sodium glycocholate.
8 . The parenteral solid formulation of claim 6 wherein the water-soluble additive agent is sodium chloride and/or sodium desoxycholate.
9 . The parenteral solid formulation of claim 8 wherein the hardly water-soluble substance is low substituted hydroxypropylcellulose, and the water-soluble additive agent is sodium chloride.
10 . The parenteral solid formulation of claim 8 wherein the hardly water-soluble substance is cholesterol, and the water-soluble additive agent is sodium chloride and sodium desoxycholate.
11 . The parenteral solid formulation of claim 1 wherein the total weight of the water-soluble drug, the hardly water-soluble substance and the optional water-soluble additive agent is 10 to 40% per the whole weight of the formulation, provided that the total weight of the water-soluble drug and the water-soluble additive agent is not more than 35% per the whole weight of the formulation.
12 . The parenteral solid formulation of claim 1 comprising essentially a water-soluble drug, a pharmaceutically acceptable hardly water-soluble solid substance, and an optional water-soluble additive agent, and which comprises silicone as a carrier.
13 . The parenteral solid formulation of claim 1 which is a matrix formulation.
14 . The parenteral solid formulation of claim 1 which is an implantable formulation.