Compressed tablet formulation
AssigneeMerck & Co., Inc.
InventorsUdit Batra, Raymond Higgins, Karen Thompson, Ashok Katdare
Life of this patent
Estimating the term…
Abstract
This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the treatment of HIV infections and AIDS.
Claims13
-16. (canceled)
A process for the preparation of a 50% drug loaded compressed tablet comprising the following steps:
- (a) blending efavirenz with a filler/disintegrant, super-disintegrant, binder and surfactant;
- (b) adding at least 1.1% by weight of water per weight of efavirenz to wet granulate the blended mixture to agglomerate the mixture;
- (c) drying the granulated mixture to a moisture content of about 0% to about 10%;
- (d) milling the dried mixture to granulate to a uniform size;
- (e) blending the milled mixture with a filler/compression aid;
- (f) lubricating the blended mixture with a lubricant;
- and
- (g) compressing the lubricated mixture to a compressed tablet of the desired shape.
A process for the preparation of a 50% drug loaded film coated compressed tablet comprising the following steps:
- (a) blending efavirenz with microcrystalline cellulose, sodium lauryl sulfate, hydroxypropyl cellulose and croscarmellose sodium;
- (b) adding at least 1.1 weight % water per weight of efavirenz to wet granulate the blended mixture for about 3 minutes to about 8 minutes to agglomerate the mixture;
- (c) drying the granulated mixture to a moisture content of about 2% to about 5%;
- (d) milling the dried mixture to a granulate of about 250μ to about 75μ;
- (e) blending the milled mixture with lactose;
- (f) lubricating the blended mixture with magnesium stearate;
- (g) compressing the lubricated mixture to a compressed tablet of the desired shape;
- and
- (h) film coating the compressed tablet with a film coating suspension to about 1% to about 10% by weight of the weight of compressed tablet.
A process for preparing a compressed tablet comprising crystalline efavirenz, filler/disintegrant, superdisintegrant, binder, surfactant, diluent/compression aid, and lubricant, which comprises:
- (a) blending a mixture of the crystalline efavirenz, filler/disintegrant, superdisintegrant, binder and surfactant;
- (b) adding water to the blended mixture to obtain a wet granulate;
- (c) drying the wet granulate;
- (d) milling the dried granulate;
- (d) blending the milled granulate with a filler/compression aid;
- (e) lubricating the blend;
- and
- (f) compressing the lubricated blend to obtain the compressed tablet.
Dependencies are inferred from the claim text.