US 11,938,224 B1
Benzonatate modified release solid tablets and capsules
Andrea Nelson, Belle Mead, NJ (US); Sachin Chaudhari, Monmouth Junction, NJ (US); Nemichand B. Jain, Princeton Junction, NJ (US); and Shivanand Puthli, Monmouth Junction, NJ (US)
Assigned to TRIS PHARMA INC, Monmouth Junction, NJ (US)
Filed by Tris Pharma, Inc., Monmouth Junction, NJ (US)
Filed on Aug. 19, 2021, as Appl. No. 17/406,137.
Application 17/406,137 is a continuation of application No. 16/777,420, filed on Jan. 30, 2020, abandoned.
Application 16/777,420 is a continuation of application No. 15/482,201, filed on Apr. 7, 2017, abandoned.
Claims priority of provisional application 62/320,219, filed on Apr. 8, 2016.
Int. Cl. A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/24 (2006.01)
CPC A61K 9/28 (2013.01) [A61K 31/24 (2013.01)] 9 Claims
 
1. A modified release benzonatate composition comprising a tablet or multiple mini-tablets in a capsule, wherein each mini-tablet or the tablet comprises: (a) a homogenous solid dispersion comprising (i) benzonatate adsorbed onto a porous silicon dioxide having a surface area of about 300 m2g to 350 m2g to form a benzonatate adsorbate powder, wherein the ratio of benzonatate to the silicon dioxide is about 4:1 to about 1:1, based on the weight of the adsorbate, and (ii) 20% w/w to 40% w/w of a water-soluble polyethylene oxide resin having an average molecular weight of about 900,000 as determined in a rheological method, based on the total weight of the solid dispersion (a), wherein (i) and (ii) are in a tablet or mini-tablets and form a matrix, (b) a bucco-protective pH-dependent, reverse enteric coat over said homogenous solid dispersion matrix tablet or mini-tablets and (c) a non-functional outer coat,
wherein there is substantially no benzonatate release from the composition in a patient's buccal cavity post-dosing with the composition as assessed in simulated saliva,
wherein said composition has an extended release of benzonatate of about 8 to about 12 hours, wherein the extended release can be assessed in an in vitro dissolution assay,
and further
wherein the modified release benzonatate composition is resistant to dose-dumping in the presence of alcoholic beverages.