Modified release composition of highly soluble drugs
A novel modified release dosage form comprising of a high solubility active ingredient, which utilizes dual retard technique to effectively reduce the quantity of release controlling agents. Present invention can optionally comprise additionally another active ingredient as an immediate release form or modified release form. Present invention also relates to a process for preparing the said formulation.
1. A process for the preparation of a modified release dosage form comprising metformin hydrochloride prepared by using dual retard technique to control the release of metformin, wherein the said dual retard technique is a combination of a matrix formulation and a reservoir formulation, said process comprising:
a) preparing micro matrix particles consisting of metformin hydrochloride and one or more hydrophobic release controlling agents consisting of poly(ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate chloride) 1:2:O.1; poly(ethyl acrylate, methyl methacrylate, trimethylamonioethyl methacrylate chloride) 1:2:0.2; and poly(ethyl acrylate, methyl methacrylate) 2:1; and
b) coating said micro matrix articles with one or more hydrophobic release controlling agents selected from the group consisting of waxes selected from the group consisting of beeswax, carnauba wax, microcrystalline wax, and ozokerite; fatty alcohols selected from the group consisting of cetostearyl alcohol, stearyl alcohol; cetyl alcohol and myristyl alcohol; and fatty acid esters selected from the group consisting of glyceryl monostearate; glycerol monooleate, acetylated monoglycerides, tristearin, tripalmitin, cetyl esters wax, glyceryl palmitostearate, glyceryl behenate and hydrogenated castor oil.
2. A process according to claim 1 , wherein said micro matrix particles contain metformin hydrochloride and one or more hydrophobic release controlling agents are present in a weight ratio of from 100:2.5 to 100:30.
3. A process according to claim 1 wherein in said micro matrix particles, metformin hydrochloride can be less than or equal to 1500 mg.
4. A process according to claim 1 , wherein said micro matrix particles and coating of one or more of said hydrophobic release controlling agents are present in a weight ratio of from 100:1 to 100:30.