Stable loratadine spill resistant formulation

Abstract

The present invention provides for a storage stable pharmaceutical liquid suspension for oral administration having a pharmaceutically effective amount of an antihistamine. The storage stable suspension preferably contains loratadine. The present invention further provides a process of preparing the storage stable pharmaceutical liquid suspension as well as a method of treating a mammal with a therapeutically effective amount of loratadine in the stable pharmaceutical liquid suspension.

1 . A storage stable pharmaceutical liquid suspension for oral administration, comprising a pharmaceutically effective amount of an antihistamine selected from the group consisting of loratadine, descarboxethoxyloratadine, azatadine and pharmaceutically acceptable salts thereof, and a surfactant. 
     
     
         2 . The storage stable pharmaceutical suspension of  claim 1 , having a pH of between about 6.4 to about 7.3. 
     
     
         3 . The storage stable pharmaceutical suspension of  claim 1 , wherein the suspension comprises from about 0.01% up to about 0.10% of an antihistamine (w/w), sorbitol in an amount up to about 20% (w/w), propylene glycol in an amount up to about 10% (w/w), surfactant in an amount up to about 3% (w/w), a thickening agent in an amount up to about 1% (w/w), and water. 
     
     
         4 . The storage stable pharmaceutical suspension of  claim 3 , wherein the thickening agent is a carbomer. 
     
     
         5 . The storage stable pharmaceutical suspension of  claim 4 , wherein the carbomer is Carbomer 934P. 
     
     
         6 . The storage stable pharmaceutical suspension of  claim 1 , wherein the surfactant ranges from about 0.01% to about 2.5% (w/w). 
     
     
         7 . The storage stable pharmaceutical suspension of  claim 1 , wherein the surfactant is Poloxamer 188. 
     
     
         8 . The storage stable pharmaceutical suspension of  claim 1 , further comprising at least one organoleptic agent. 
     
     
         9 . The storage stable pharmaceutical suspension of  claim 1 , wherein the antihistamine is loratadine. 
     
     
         10 . The storage stable pharmaceutical suspension of  claim 9 , wherein the concentration of loratadine is about 0.088% (w/w). 
     
     
         11 . The storage stable pharmaceutical suspension of  claim 1 , further comprising a decongestant, an analgesic, an antitussive, an expectorant, or any combination of two or more thereof. 
     
     
         12 . A method for treating a human in need of an antihistamine, comprising the step of administering a therapeutically effective amount of the storage stable pharmaceutical liquid suspension of  claim 1 . 
     
     
         13 - 17 . (canceled) 
     
     
         18 . The storage stable pharmaceutical suspension of  claim 1 , wherein there is no crystalline growth during a heat-cool study for three days at 45° C. 
     
     
         19 . (canceled) 
     
     
         20 . A pharmaceutical suspension, wherein loratadine at a concentration of about 0.088% (w/w) is suspended in a uniformly dispersed manner in an aqueous suspension without agitation during the product shelf-life and wherein the pharmaceutical suspension has the following properties:
 antimicrobial activity;   a viscosity of between about 5,000 cps to about 15,000 cps;   a product shelf-life of up to about six months;   no crystalline growth during a heat-cool study for three days at 45° C.;   no oxidation of the loratadine; and   an acceptable palatability.   
     
     
         21 . The pharmaceutical suspension of  claim 20 , wherein the pharmaceutical suspension has a yield value of between about 0.3 to about 200 D/cm 2 . 
     
     
         22 . (canceled) 
     
     
         23 . The pharmaceutical suspension of  claim 20 , wherein the shelf-life is up to about twelve months. 
     
     
         24 . The pharmaceutical suspension of  claim 20 , wherein the shelf-life is up to about eighteen months. 
     
     
         25 . A method for treating a human in need of loratadine, comprising the step of administering a therapeutically effective amount of the pharmaceutical suspension of  claim 20 . 
     
     
         26 - 29 . (canceled) 
     
     
         30 . A method for preparing a stable pharmaceutical formulation of loratadine, comprising the steps of:
 a. dispersing carbomer in water;   b. adding glycerin, sucralose, masking agent and peach flavor to the carbomer slurry;   c. dissolving sodium hydroxide in water and adding to the slurry of step (b);   d. dissolving a surfactant in water;   e. adding a preservative, a propylene glycol, and a glycerin to the surfactant to form a mixture;   f. dispersing loratadine into the mixture of (e);   g. adding (f) to the slurry of (c);   h. adjusting the pH with the sodium hydroxide solution to obtain a pH of between 6.4 to 7.3.