Pharmaceutical composition for piperidinoalkanol compounds

Abstract

The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.

1 . A pharmaceutical composition in solid dosage form comprising, 
 a) a therapeutically effective amount of a piperidinoalkanol compound of formula                          wherein X is a number ranging from about zero to 5, or an optical isomer of the piperidinoalkanol compound, wherein the piperidinoalkanol compound has a particle surface area of greater than about 1.0 m 2 /g; and    b) at least one inert ingredient.    
   
   
       2 . The pharmaceutical composition according to  claim 1 , wherein the inert ingredient is a disintegrant.  
   
   
       3 . The pharmaceutical composition according to  claim 1 , wherein X is zero.  
   
   
       4 . The pharmaceutical composition according to  claim 1  wherein at least one inert ingredient is selected from the group consisting of croscarmellose sodium, lactose, microcrystalline cellulose, pregelatinized starch, gelatin, calcium carbonate, magnesium stearate and sodium starch glycolate.  
   
   
       5 . A pharmaceutical composition according to  claim 1  wherein the particle surface area of the piperidinoalkanol compound is about 2 to 10 m 2 /g.  
   
   
       6 . A pharmaceutical composition according to  claim 5  wherein the particle surface area of the piperidinoalkanol compound is about 2 to 6 mg 2 /g.  
   
   
       7 . A pharmaceutical composition according to  claim 6  wherein the particle surface area of the piperidinoalkanol compound is about 2 to 4 mg 2 /g.  
   
   
       8 . A pharmaceutical composition in solid dosage form comprising: 
 a) a therapeutically effective amount of a piperidinoalkanol compound of the formula:                        wherein x is a number ranging from about zero to 5, or an optical isomer of the piperidinoalkanol compound;      b) a first inert ingredient selected from the group consisting of pregelatinized starch, gelatin, povidone and a cellulose derivative; and    c) a second inert ingredient selected from the group consisting of methacrylic acid DVB, cross-linked polyvinylpyrrolidone, croscarmellose sodium, crospovidone and polacrilin potassium.    
   
   
       9 . The pharmaceutical composition of  claim 8 , further comprising a third inert ingredient selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, stearic acid, talc and hydrogenated vegetable oil.  
   
   
       10 . The pharmaceutical composition of  claim 9 , further comprising a fourth inert ingredient selected from the group consisting of lactose, starch, microcrystalline cellulose, powdered cellulose and mannitol.  
   
   
       11 . A pharmaceutical composition in solid dosage form comprising: 
 a) a therapeutically effective amount of a piperidinoalkanol compound of the formula:                        wherein x is a number ranging from about zero to 5, or an optical isomer of the piperidinoalkanol compound;      b) a first inert ingredient selected from the group consisting of pregelatinized starch, gelatin, povidone and a cellulose derivative; and    c) a second inert ingredient selected from the group consisting of methacrylic acid DVB, cross-linked polyvinylpyrrolidone, croscarmellose sodium, sodium starch glycolate, crospovidone and polacrilin potassium; provided that the pharmaceutical composition does not include a carbonate salt in an amount of more than 1% by weight of the pharmaceutical composition.    
   
   
       12 . The pharmaceutical composition of  claim 11 , wherein no carbonate salt is present.  
   
   
       13 . The pharmaceutical composition of  claim 11 , further comprising a third inert ingredient selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, stearic acid, talc and hydrogenated vegetable oil.  
   
   
       14 . The pharmaceutical composition of  claim 13 , further comprising a fourth inert ingredient selected from the group consisting of lactose, starch and inicrocrystalline cellulose.  
   
   
       15 . A pharmaceutical composition in solid dosage form comprising: 
 a) a therapeutically effective amount of a piperidinoalkanol compound of the formula:                        wherein x is a number ranging from about zero to 5, or an optical isomer of the piperidinoalkanol compound;      b) a first inert ingredient selected from the group consisting of pregelatinized starch, gelatin, povidone and a cellulose derivative; and    c) a second inert ingredient selected from the group consisting of methacrylic acid DVB, cross-linked polyvinylpyltolidone, croscarmellose sodium, sodium starch glycolate, crospovidone and polacrilin potassium; provided that the pharmaceutical composition does not include concurrently a carbonate salt in an amount of more than 1% by weight of the pharmaceutical composition and a pharmaceutically acceptable nonionic surfactant.    
   
   
       16 . The pharmaceutical composition of  claim 15 , further comprising a third inert ingredient selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, stearic acid, talc and hydrogenated vegetable oil.  
   
   
       17 . The pharmaceutical composition of  claim 16 , further comprising a fourth inert ingredient selected from the group consisting of lactose, starch and microcrystalline cellulose.  
   
   
       18 . A pharmaceutical composition in solid dosage form comprising: 
 a) a therapeutically effective amount of a piperidinoalkanol compound of the formula:                        wherein x is a number ranging from about zero to 5, or an optical isomer of the piperidinoalkanol compound;      b) a first inert ingredient selected from the group consisting of pregelatinized starch, gelatin, povidone and a cellulose derivative; and    c) a second inert ingredient selected from the group consisting of methacrylic acid DVB, cross-linked polyvinylpyrrolidone, croscarmellose sodium, sodium starch glycolate, crospovidone and polacrilin potassium; provided that the pharmaceutical composition does not include concurrently a carbonate salt in an amount of more than 1% by weight of the pharmaceutical composition and a pharmaceutically acceptable cationic surfactant.    
   
   
       19 . The pharmaceutical composition of  claim 18 , further comprising a third inert ingredient selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, stearic acid, talc and hydrogenated vegetable oil.  
   
   
       20 . The pharmaceutical composition of  claim 19 , further comprising a fourth inert ingredient selected from the group consisting of lactose, starch and inicrocrystalline cellulose.  
   
   
       21 . A pharmaceutical composition in solid dosage form consisting essentially of: 
 a) a therapeutically effective amount of a piperidinoalkanol compound of the formula:                          wherein x is a number ranging from about zero to 5, or an optical isomer of the piperidinoalkanol compound;    b) a first inert ingredient selected from the group consisting of pregelatinized starch, gelatin, povidone and a cellulose derivative; and    c) a second inert ingredient selected from the group consisting of methacrylic acid DVB, cross-linked polyvinylpyrrolidone, croscarmellose sodium, sodium starch glycolate, crospovidone and polacrilin potassium.    
   
   
       22 . The pharmaceutical composition of  claim 21 , further consisting essentially of a third inert ingredient selected from the group consisting of magnesium stearate, calcium stearate, zinc stearate, stearic acid, talc and hydrogenated vegetable oil.  
   
   
       23 . The pharmaceutical composition of  claim 22 , further consisting essentially of a fourth inert ingredient selected from the group consisting of lactose, starch and microcrystalline cellulose.