PHARMACEUTICAL COMPOSITION AND PROCESS FOR MONTELUKAST TABLETS
The manufacture of compositions containing montelukast and to stable tablet compositions resulting thereof are disclosed, which include a first compaction step of a dry blend including, montelukast or a pharmaceutically acceptable salt thereof, and microcrystalline cellulose, and a further compression step into tablets.
1 . A process for the preparation of tablets comprising a first compaction step of a dry blend comprising montelukast or a pharmaceutically acceptable salt thereof and microcrystalline cellulose and a further compression step into tablets.
2 . The process according to claim 1 , wherein the compacted blend is granulated and the resulting granules are compressed into tablets.
3 . The process according to claim 1 , wherein additional excipients are added to the compacted blend before compression.
4 . The process according to claim 1 , wherein the tablets are further coated.
5 . The process according to claim 3 , wherein the additional excipients are selected from the group consisting of disintegrants, lubricants, glidants, binders, diluents, and combinations thereof.
6 . The process according to claim 1 , wherein the additional excipients are selected among colloidal silicon dioxide, starch, magnesium stearate, sodium stearyl fumarate, croscarmellose sodium, crospovidone, sodium starch glycolate and talc.
7 . The process according to claim 1 , wherein the dry blend further comprises sucralose.
8 . The process according to claim 1 , wherein the compaction step is performed using a roll compactor.
9 . The process according to claim 1 , wherein the compression step is performed suing a rotating press.
10 . The process according to claim 1 , wherein the compaction step is performed at a pressure within the range of 2 to 4 Mpa.
11 . The process according to claim 1 , wherein the compaction is performed at a powder flow of 5 to 20 g/min.
12 - 21 . (canceled)
22 . The process according to claim 1 , wherein the tablets are of a chewable type.
23 . The process according to claim 1 , wherein the tablets comprise 1 to 20 mg of montelukast or a pharmaceutically acceptable salt thereof.
24 . The process according to claim 5 , wherein:
the binder are any selected among acacia, alginic acid, carbomer, sodium carboxymethylcellulose, dextrin, ethylcellulose, gelatine, glucose, guar gum, hydroxypropylcellulose, maltose, methylcellulose, povidone, polyvinylpyrrolidone, starch, methylcellulose or polyethylene oxide;
the diluents are any selected among microcrystalline cellulose, calcium, phosphate or sulfate carbonates, dextrates, dextrins, dextrose excipients, fructose, kaolin, lactitol, anhydrous lactose, lactose monohydrate, maltose, mannitol, sorbitol, sucrose, starch, pregelatinized starch, or talc;
the glidants are any selected among: colloidal silicon, magnesium trisilicate, starch, talc or tribasic calcium phosphate; and
the disintegrants are any selected among: alginic acid, croscarmellose sodium, crospovidone, potassium polacrilin, sodium starch glycolate, and starch.
25 . The process according to claim 1 , wherein the tablet has the following composition:
Montelukast sodium
5.20
mg
Hydroxypropyl cellulose
35.00
mg
Microcrystalline cellulose
10.00
mg
Mannitol
195.00
mg
Flavour
3.60
mg
Iron oxide red
0.10
mg
Sodium stearyl fumarate
3.50
mg
Sucralose
0.50
mg
Aerosil
0.90
mg
(AcDiSol) Crossed linked sodium
10.00
mg
carboxymethyl cellulose
Sodium stearyl fumarate
2.80
mg
Total
266.60
mg
26 . The process according to claim 1 , wherein the tablet has the following composition:
Tablet
Montelukast sodium
10.40
mg
Hydroxypropyl cellulose
20.00
mg
Microcrystalline cellulose
10.00
mg
Mannitol
120.00
mg
Aerosil
0.80
mg
(AcDiSol) Crossed linked sodium
20.00
mg
carboxymethyl cellulose
Sodium stearyl fumarate
1.80
mg
Total
185.00
mg
Coating
Opadry II 85 F white
5.50
mg
Total
190.50
27 . The process of claim 1 , wherein the tablet comprises montelukast or a salt thereof, microcrystalline cellulose and sucralose, wherein the amount of impurity does not increase by more than 0.4% by weight from the initial amount of montelukast after storage at about 40° C. and about 75% relative humidity for 1 month.
28 . The process of claim 27 , wherein the amount of impurity does not increase by more than 0.2%.
29 . The process of claim 1 for preparing a medicament for treating or preventing a leukotriene induced condition.
30 . The process according to claim 28 , wherein the leukotriene induced condition is asthma or chronic bronchitis.