VALSARTAN SOLID ORAL DOSAGE FORMS AND METHODS OF MAKING SUCH FORMULATIONS
The invention relates to melt granulation processes for preparing immediate release and sustained release pharmaceutical formulations comprising valsartan.
1 . A process for preparing a MR pharmaceutical formulation of valsartan, which comprises the steps of (a) preparing a blend by combining valsartan, a hydrophobic component and, optionally, an hydrophilic component; and (b) compressing the blend into a solid oral dosage form tablet.
2 . The process of claim 1 wherein the solid oral dosage form is a tablet.
3 . A process according to claim 1 further comprising mixing an optional lubricant with the blend prior to compressing the blend into a tablet.
4 . A process according to claim 1 , wherein the process is carried out under substantially anhydrous conditions.
5 . A process according to claim 1 , wherein the hydrophilic erodible component is selected from the group consisting of hydroxypropyl methylcellulose, lactose, croscarmellose sodium, polyvinylpyrrolidone, guar and xanthan gums, polyethylene glycol (MW>400), celluloses, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, sodium carboxymethyl cellulose, sodium alginate, methyl cellulose, carboxypolymethylene, acacia gum, tragencanth gum and polyethylene oxide.
6 . A process according to claim 7 , wherein the hydrophilic erodible component is hydroxypropyl methylcellulose.
7 . A process according to claim 1 , wherein the hydrophobic component is selected from the group consisting of ethyl cellulose, methacrylic acid polymers and copolymers, fatty acids and esters thereof, waxes and high molecular weight fatty alcohols.
8 . A process according to claim 1 , wherein the hydrophobic component is selected from the group consisting of EUDRAGIT NE 30 D from Rohm and Haas, stearic acid, behenic acid, glyceryl monostearate, glyceryl palmitostearate, glyceryl behenate, carbuna wax and cetyl alcohol.
9 . A process according to claim 8 , wherein the hydrophobic component is selected from the group consisting of cetyl alcohol and stearyl alcohol.
10 . A process according to claim 1 , wherein the valsartan comprises from about 0.1% to about 99% by weight of the formulation.
11 . A process according to claim 1 , wherein the hydrophilic erodible component comprises from about 10% to about 90% by weight of the formulation.
12 . A process according to claim 1 , wherein the hydrophobic component comprises from about 10% to about 30% by weight of the formulation.
13 . A process according to claim 1 , wherein the ratio of hydrophilic erodible component to hydrophobic component is 9:1 to 1:1.
14 . (canceled)
15 . (canceled)
16 . A process for preparing an immediate-release pharmaceutical formulation of valsartan, which comprises the steps of: (a) mixing valsartan with a diluent to form a pre-mix; (b) melting wax in a pre-heated jacket vessel and adding the pre-mix to the vessel to obtain uniform granulation; (c) cooling the granulation; and (d) compressing the blend into a solid oral dosage form.
17 . The process of claim 16 wherein the solid oral dosage form is a tablet.
18 - 23 . (canceled)