Method for the treatment of acne

Abstract

A method for treatment of acne with tetracyclines is provided. A lower sustained dose and no loading dose is employed, with an optional once-a-day dosing regimen.

1 . An oral dosage form comprising: 
 an antibiotically effective dose of an oral minocycline; and    a pharmaceutically suitable delivery vehicle having a fast dissolving carrier and a slow dissolving carrier, wherein said fast dissolving carrier and said slow dissolving carrier of said vehicle are at a weight ratio of about 0.3 to about 0.5;    wherein the oral dosage form for administration once a day provides a patient with about 0.5 mg/kg/day to about 1.5 mg/kg/day of said oral minocycline;    wherein said vehicle continuously releases, without an initial load dose, said oral minocycline at a rate so that C max  is reached at about 2.75 to about 4 hours after administration.    
     
     
         2 . The oral dosage form of  claim 1 , wherein said oral minocycline is minocycline as hydrochloride.  
     
     
         3 . The oral dosage form of  claim 1 , wherein the ratio of fast dissolving carrier to slow dissolving carrier is about 0.35 to about 0.45.  
     
     
         4 . The oral dosage form of  claim 1 , wherein the ratio of fast dissolving carrier to slow dissolving carrier is about 0.36 to about 0.40.  
     
     
         5 . The oral dosage form of  claim 1 , wherein said fast dissolving carrier comprises lactose monohydrate.  
     
     
         6 . The oral dosage form of  claim 1 , wherein said slow dissolving carrier is selected from the group consisting of polyvinyl pyrrolidone, polyvinyl acetate, microcrystalline cellulose, methyl cellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, magnesium stearate, and calcium stearate.  
     
     
         7 . The oral dosage form of  claim 1 , wherein said slow dissolving carrier comprises hydroxypropylmethyl cellulose.  
     
     
         8 . The oral dosage form of  claim 1 , wherein said slow dissolving carrier is present at about 23.5% to about 27.0% by weight of said oral dosage form.  
     
     
         9 . The oral dosage form of  claim 1 , wherein said slow dissolving carrier is present at: 
 23.5% by weight of said oral dosage form when said oral dosage form comprises 135 mg of said oral minocycline; or    27.0% by weight of said oral dosage form when said oral dosage form comprises 45 mg of said oral minocycline.    
     
     
         10 . The oral dosage form of  claim 1 , wherein said oral dosage form is formulated to release said oral minocycline at a rate so that C max  is reached at about 3.0 to about 3.75 hours after administration.  
     
     
         11 . The oral dosage form of  claim 1 , wherein said oral dosage form is a tablet or caplet comprising 45 mg or 135 mg of said oral minocycline.  
     
     
         12 . The oral dosage form of  claim 1 , further comprising an intragranular fast dissolving carrier.  
     
     
         13 . The oral dosage form of  claim 12 , wherein said slow dissolving carrier encapsulates said intragranular fast dissolving carrier.  
     
     
         14 . The oral dosage form of  claim 1 , further comprising a coating.  
     
     
         15 . An oral dosage form comprising: 
 an antibiotically effective dose of an oral minocycline; and    a pharmaceutically suitable delivery vehicle having a fast dissolving carrier and a slow dissolving carrier, wherein said fast dissolving carrier and said slow dissolving carrier of said vehicle are at a weight ratio of about 0.3 to about 0.5;    wherein the oral dosage form for administration once a day provides a patient with about 0.5 mg/kg/day to about 1.5 mg/kg/day of said oral minocycline;    wherein said vehicle continuously releases, without an initial load dose, said oral minocycline at a rate of either about 25 to about 52% within about 1 hour, about 53 to about 89% within about 2 hours, and at least about 90% within about 4 hours, or about 30 to about 52% within about 1 hour, about 53 to about 84% within about 2 hours, and at least about 85% within about 4 hours.