Dri-nasal sprays

Abstract

There is provided non-aqueous liquid spray compositions comprising a pharmacologically acceptable non aqueous liquid carrier in which said bioactive material is directly insoluble, a pharmacologically acceptable water insoluble ester of a water soluble acid soluble in said carrier, a pharmacologically acceptable water soluble glycol soluble in said ester and a pharmacologically acceptable water soluble bio-active material soluble in said glycol but not directly soluble in the carrier. There are also provided methods of producing and administering such compositions.

1 . A non-aqueous liquid spray composition for a bioactive material comprising 
 1) a pharmacologically acceptable non aqueous liquid carrier in which said bioactive material is directly insoluble,    b) a pharmacologically acceptable water insoluble ester of a water soluble acid soluble in said carrier,    c) a pharmacologically acceptable water soluble glycol soluble in said ester,    d) a pharmacologically acceptable water soluble bio-active material soluble in said glycol but directly insoluble in said carrier.    
     
     
         2 . The composition of  claim 1  wherein . the carrier is selected from the group consisting of a cyclopentasiloxane, an ethylene diglyceride, a propylene diglyceride, a propylene triglyceride and mixtures of said glycerides.  
     
     
         3 . The composition of  claim 2  wherein the cyclopentasiloxane is a polyalkylcyclopentasiloxane.  
     
     
         4 . The composition of  claim 3  wherein the carrier is selected from the group consisting of decamethylcyclopentylsiloxane, an ethylene diglyceride, a propylene diglyceride, a propylene triglyceride and mixtures of said glycerides, wherein the glyceride moieties are selected from the group consisting of cAprilic and capric glycerides.  
     
     
         5 . The composition of  claim 1  comprising 
 a) from about 50-about 90 wt. % of the carrier,  
 b) from about 1 0-about 40 wt % of the water insoluble ester,  
 c) from about 1-about 5 wt. % of the water soluble glycol,  
 d) from about 0-01-about 2 wt. % of the bio-active material.  
 
     
     
         6 . The composition of  claim 1  comprising 
 a) from about 60 about 90 wt. % of the carrier,  
 b) from about 10 about 20 wt % of the water insoluble ester,  
 c) from about 1 to about 3 wt. % of the water soluble glycol,  
 d) from about 0.01 to about 2 wt. % of the bio-active material.  
 
     
     
         7 . The composition of  claim 5  wherein the glycol is a C 3  to C 8  glycol.  
     
     
         8 . The composition of  claim 7  wherein the glycol is selected from the group consisting of polyethylene glycol and polypropylene glycol.  
     
     
         9 . The composition of  claim 5  wherein the ester is a lactate ester.  
     
     
         10 . The composition of  claim 9  wherein the lactate ester is a C 12 - C 15  alkyl lactate  
     
     
         11 . The composition of  claim 10  wherein the alkyl group is selected from the group consisting of cetyl, lauryl, isostearyl and myristyl and mixtures thereof  
     
     
         12 . The composition of  claim 5  wherein the bio-active material is selected from the group consisting of decongestants, antihistamines, antitussives, anticholinergics, steroids, antibiotics, analgesics, antispasmotics, brocho-dilators, vitamins, hormones, antihypertensives and antimicrobials.  
     
     
         13 . The composition of  claim 5  wherein the bio-active material is a decongestant.  
     
     
         14 . The composition of  claim 13  wherein the bio-active material is selected from the group consisting of oxymetazoline, xylometazoline, naphazoline, phenylephrine, ephedrine in water soluble form.  
     
     
         15 . The composition of  claim 14  wherein the bio-active material is in the form of a pharmacologically acceptable salt.  
     
     
         16 . The composition of  claim 15  wherein the salt is a hydrochloride or sulfate.  
     
     
         17 . A method of producing a spray composition of  claim 1  which comprises the sequential steps of dissolving the bio-active material of (d) in a glycol of (c), dissolving said solution of (d) in (c) in an ester of (b) and dissolving said solution of (d) in (c)) in (b) in a carrier of (a).  
     
     
         18 . The method of producing a spray composition of  claim 2  which comprises the sequential steps of dissolving the bio-active material of (d) in a glycol of (c), dissolving said solution of (d) in (c) in an ester of (b) and dissolving said solution of (d) in(c) ) in (b) in a carrier (a) as defined in  claim 2 .  
     
     
         19 . The method of producing a spray composition of  claim 5  which comprises the sequential steps of dissolving the bio-active material of (d) in a glycol of (c), dissolving said solution of (d) in (c) in an ester of (b) and dissolving said solution of (d) in (c) in (b) in a carrier of (a) selected from the group consisting of decamethylcyclopentylsiloxane, an ethylene diglyceride, a propylene diglyceride, a propylene triglyceride and mixtures of said glycerides, wherein the glyceride moieties are selected from the group consisting of cAprilic and capric glycerides.  
     
     
         20 . A method of administering a bio-active material to a subject in need of same which comprises spraying a pharmacologically effective amount of a composition of  claim 1  into the nasal cavity of said subject.  
     
     
         21 . The method of  claim 20 , wherein the bio-active material is selected from the group consisting of decongestants, antihistamines, antitussives, anticholinergics, steroids, analgesics antibiotics, antispasmotics, brochodilators, vitamins, hormones, antihypertensives and antimicrobials.  
     
     
         22 . The method of  claim 21 , wherein the bio-active material is a decongestant.  
     
     
         23 . The method of  claim 22 , wherein the bio-active material is selected from the group consisting of oxymetazoline, xylometazoline, naphazoline, phenylephrine, ephedrine in water soluble form.