US2003068378A1PendingUtilityA1

Compositions and methods for mucosal delivery

45
Assignee: LAVIPHARM LAB INCPriority: Jan 21, 1999Filed: Mar 5, 2002Published: Apr 10, 2003
Est. expiryJan 21, 2019(expired)· nominal 20-yr term from priority
Inventors:Li-Lan ChenWilliam R. PfisterDonald W. RennThitiwan BuranachokpaisanJames OsborneHock S. TanLi Tao
A61P 31/04A61P 31/10A61P 43/00A61P 31/12A61P 1/02A61P 15/10A61P 15/18A61K 31/505A61K 9/7015A61K 9/145A61K 9/0043A61K 31/495A61K 9/0007A61K 9/0031A61K 9/0056A61K 9/006A61K 9/1623A61K 9/7007A61K 9/0034A61K 9/70
45
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References
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Claims

Abstract

Mucosal surface-coat-forming film dosage units containing a water-soluble hydrocolloid, an effective dose of a sexual dysfunction active agent and a mucosal adhesion enhancer, wherein the mucosal adhesion enhancer is a starch graft copolymer.

Claims

exact text as granted — not AI-modified
What is claimed:  
     
         1 . A dosage unit comprising a mucosal surface-coat-forming film, wherein the mucosal surface-coat-forming film comprises a water-soluble hydrocolloid, an effective dose of a sexual dysfunction active agent and a mucosal adhesion enhancer, wherein the mucosal adhesion enhancer is a starch graft copolymer.  
     
     
         2 . The dosage unit of  claim 1 , wherein the mucosal adhesion enhancer is a copolymer of starch and acrylic acid.  
     
     
         3 . The dosage unit of  claim 1 , wherein the film exhibits a dry tack value of less than 3.5 g.  
     
     
         4 . The dosage unit of  claim 1 , wherein the film exhibits a dry tack value of less than 2.0 g.  
     
     
         5 . The dosage unit of  claim 1 , wherein the film exhibits a wet tack value of greater than 35 g.  
     
     
         6 . The dosage unit of  claim 1 , wherein the water-soluble hydrocolloid exhibits a gelation temperature that is greater than 70° C. for a 2% polymer solution.  
     
     
         7 . The dosage unit of  claim 1 , wherein the water-soluble hydrocolloid exhibits a hydration rate in 24 hours of 5-20% at 75% humidity at room temperature.  
     
     
         8 . The dosage unit of  claim 1 , wherein the water-soluble hydrocolloid is a polymer selected from the group consisting of a natural, semi-natural and synthetic biopolymer.  
     
     
         9 . The dosage unit of  claim 8 , wherein the water-soluble hydrocolloid is selected from the group consisting of a polysaccharade and a polypeptide.  
     
     
         10 . The dosage unit of  claim 8 , wherein the water-soluble hydrocolloid comprises a hydroxypropylmethylcellulose polymer.  
     
     
         11 . The dosage unit of  claim 10 , wherein the hydroxypropylmethylcellulose polymer has a molecular weight of less than 200,000 Daltons.  
     
     
         12 . The dosage unit of  claim 1 , wherein the film further comprises at least one of an emulsifier, a plasticizer, a taste modifying agent, a water soluble inert filler, a preservative, a coloring agent, a stabilizer and a buffering agent.  
     
     
         13 . The dosage unit of  claim 1 , wherein the film further comprises an emulsifier present at a concentration in the range of 0.1 to 10 wt % of the dosage unit.  
     
     
         14 . The dosage unit of  claim 1 , wherein the film further comprises a taste modifying agent comprising at least one of a sweetening agent, a flavoring agent and a taste masking agent.  
     
     
         15 . The dosage unit of  claim 1 , wherein the film further comprises a water soluble inert filler present at a concentration in the range of 0.5 to 50 wt % of the dosage unit.  
     
     
         16 . The dosage unit of  claim 1 , wherein the film further comprises a preservative present at a concentration in the range of 0.01 to 10 wt % of the dosage unit.  
     
     
         17 . The dosage unit of  claim 1 , wherein the active agent is present at a concentration in the range of 0.01 to 75 wt % of the dosage unit.  
     
     
         19 . The dosage unit of  claim 1 , wherein the sexual dysfunction active agent is sildenafil citrate.  
     
     
         20 . The dosage unit of  claim 1 , wherein the film has a dry film thickness in the range of 1 to 20 mil.  
     
     
         21 . The dosage unit of  claim 20 , wherein the film has a dry film thickness of less than 10 mils.  
     
     
         22 . The dosage unit of  claim 1 , wherein the film exhibits a tensile strength greater than 1500 psi.  
     
     
         23 . The dosage unit of  claim 1 , wherein the film exhibits a % elongation of less than 20%.  
     
     
         24 . The dosage unit of  claim 1 , wherein the film exhibits a modulus in the range of 35,000 to 300,000 psi.  
     
     
         24 . The dosage unit of  claim 1 , wherein the film exhibits a dissolution time in the range of 10 to 600 seconds upon application to an oral mucosal surface.  
     
     
         25 . The dosage unit of  claim 1 , wherein the film exhibits a dissolution time in the range of 1 to 300 seconds upon application to an oral mucosal surface.  
     
     
         26 . The dosage unit of  claim 24 , wherein the film exhibits a tensile strength greater than 1,500 psi, a % elongation of less than 20% and a disintegration time in the range from 1 to 300 seconds upon application to an oral mucosal surface.  
     
     
         27 . The dosage unit of  claim 1 , wherein the active agent is encapsulated within a polymer, wherein the polymer is chemically or physically distinct from the hydrocolloid.  
     
     
         28 . The dosage unit of  claim 1 , wherein the dosage unit comprises at least two active agents.  
     
     
         29 . The dosage unit of  claim 1 , wherein the mucosal adhesion enhancer is present at a concentration of up to 50%.  
     
     
         30 . A dosage unit comprising a mucosal surface-coat-forming film, wherein the mucosal surface-coat-forming film comprises a water-soluble hydrocolloid, an effective dose of a sexual dysfunction active agent and a mucosal adhesion enhancer; wherein the active agent is encapsulated within a polymer which is chemically or physically distinct from the hydrocolloid; wherein the mucosal adhesion enhancer is a starch graft copolymer; wherein the film exhibits a dry tack value of less than 3.5 g, a wet tack of greater than 35 g, a gelation temperature that is greater than 70° C. for a 2% polymer solution, a dry film thickness of not more than 20 mil, a water content of 0.5 to 10%, a tensile strength greater than 1500 psi, a modulus in the range of 35,000 to 300,000 psi, a % elongation of less than 20%, a tear propagation resistance of 0.001 to 1 N, and a dissolution time on not more than 600 seconds upon application to an oral mucosal surface.  
     
     
         31 . The dosage unit of  claim 30 , wherein the mucosal adhesion enhancer is a copolymer of starch and acrylic acid.  
     
     
         32 . The dosage unit of  claim 30 , wherein the film exhibits a dry tack value of less than 2.0 g.  
     
     
         33 . The dosage unit of  claim 30 , wherein the water-soluble hydrocolloid exhibits a hydration rate in 24 hours of 5-20% at 75% humidity at room temperature.  
     
     
         34 . The dosage unit of  claim 30 , wherein the water-soluble hydrocolloid is a polymer selected from the group consisting of a natural, semi-natural and synthetic biopolymer.  
     
     
         35 . The dosage unit of  claim 34 , wherein the water-soluble hydrocolloid is selected from the group consisting of a polysaccharade and a polypeptide.  
     
     
         36 . The dosage unit of  claim 34 , wherein the water-soluble hydrocolloid comprises a hydroxypropylmethylcellulose polymer.  
     
     
         37 . The dosage unit of  claim 36 , wherein the hydroxypropylmethylcellulose polymer has a molecular weight of less than 200,000 Daltons.  
     
     
         38 . The dosage unit of  claim 30 , wherein the film further comprises at least one of an emulsifier, a plasticizer, a taste modifying agent, a water soluble inert filler, a preservative, a coloring agent, a stabilizer and a buffering agent.  
     
     
         39 . The dosage unit of  claim 30 , wherein the film further comprises an emulsifier present at a concentration in the range of 0.1 to 10 wt % of the dosage unit.  
     
     
         40 . The dosage unit of  claim 30 , wherein the film further comprises a taste modifying agent comprising at least one of a sweetening agent, a flavoring agent and a taste masking agent.  
     
     
         41 . The dosage unit of  claim 30 , wherein the film further comprises a water soluble inert filler present at a concentration in the range of 0.5 to 50 wt % of the dosage unit.  
     
     
         42 . The dosage unit of  claim 30 , wherein the film further comprises a preservative present at a concentration in the range of 0.01 to 10 wt % of the dosage unit.  
     
     
         43 . The dosage unit of  claim 30 , wherein the active agent is present at a concentration in the range of 0.01 to 75 wt % of the dosage unit.  
     
     
         44 . The dosage unit of  claim 30 , wherein the sexual dysfunction active agent is sildenafil citrate.  
     
     
         45 . The dosage unit of  claim 30 , wherein the film has a dry film thickness in the range of 1 to 20 mil.  
     
     
         46 . The dosage unit of  claim 45 , wherein the film has a dry film thickness of less than 10 mils.  
     
     
         47 . The dosage unit of  claim 30 , wherein the film exhibits a dissolution time in the range of 10 to 600 seconds upon application to an oral mucosal surface.  
     
     
         48 . The dosage unit of  claim 30 , wherein the film further exhibits a dissintegration time in the range of 1 to 300 seconds upon application to an oral mucosal surface.  
     
     
         49 . The dosage unit of  claim 30 , wherein the active agent is encapsulated within a polymer, wherein the polymer is chemically or physically distinct from the hydrocolloid.  
     
     
         50 . The dosage unit of  claim 30 , wherein the dosage unit comprises at least two active agents.  
     
     
         51 . The dosage unit of  claim 30 , wherein the mucosal adhesion enhancer is present at a concentration of up to 50%.

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