Extended release pharmaceutical compositions
Inventors
Jaiswal, Sunil Beharilal • Shah, Vaibhavi Ankur • Tiwari, Sunil Deviprasad
Assignees
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Publication Number
US-10517829-B2
Publication Date
2019-12-31
Expiration Date
Abstract
The present invention provides extended release pharmaceutical compositions structured for once a day administration comprising skeletal muscle relaxant such as cyclobenzaprine or its pharmaceutically acceptable salt thereof that extends the release of the drug under in-vitro conditions for at least 8 to 12 hours. The invention also provides process for the preparation of such structured compositions.
Core Innovation
The invention relates to once-daily extended release pharmaceutical compositions of cyclobenzaprine or cyclobenzaprine hydrochloride that are capable of being filled into capsules. The composition is an extended release pellet having an inert core and a matrix coating on the inert core, where the matrix coating comprises cyclobenzaprine or a pharmaceutically acceptable salt and one or more extended release agents. The pellets are designed to provide an extended release profile over an 8 to 12 h range for once a day administration.
A key aspect is the placement and composition of drug and extended release components within the pellet structure. Cyclobenzaprine or cyclobenzaprine hydrochloride is included in the extended-release layer and/or positioned between the inert core and the matrix layer and/or included in the inert core, while the matrix coating contains one or more extended release agents. The extended release agents include ethyl cellulose, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate, polyvinyl alcohol, polyvinyl acetate, waxes and fatty alcohols, vinyl pyrrolidone-vinyl acetate copolymer, dimethylaminoethyl methacrylate and neutral methacrylic acid esters, methacrylic acid copolymers, ammoniomethacrylate copolymers, and neutral copolymer of polymethacrylic acid ester.
The formulation defines quantitative composition ranges for the pellet. The inert core comprises 30 weight percent to 60 weight percent of the pellet composition, and the extended release agent comprises from 5 weight percent to 50 weight percent of the pellet composition, and from about 50 weight percent to about 90 weight percent of the matrix coating. Cyclobenzaprine hydrochloride is recited as the pharmaceutically acceptable cyclobenzaprine salt and is from 0.01% to 50% by weight of the pellet composition. The disclosed embodiments include optional plasticizer-containing matrix embodiments and plasticizer-free embodiments, with extended-release performance described using dissolution profiles.
Claims Coverage
The independent claim covers 3 inventive features in an extended release pellet composition capable of being filled into capsules, with a defined inert core, a matrix coating containing cyclobenzaprine or a pharmaceutically acceptable salt plus selected extended release agents, and specified weight-percent ranges.
Inert core and matrix coating for capsule-fillable extended release pellets
An extended release pellet composition, capable of being filled into capsules, comprising an inert core and a matrix coating on said inert core, said matrix coating comprising cyclobenzaprine or a pharmaceutically acceptable salt thereof, and one or more extended release agents.
Selected extended release agents for the matrix coating
The one or more extended release agents is selected from the group consisting of one or more of ethyl cellulose, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate, polyvinyl alcohol, polyvinyl acetate, cetyl alcohol, stearyl alcohol, bees wax, carnauba wax, stearic acid, vinyl pyrrolidone-vinyl acetate copolymer, dimethylaminoethyl methacrylate and other neutral methacrylic acid esters, methacrylic acid copolymers type A, methacrylic acid copolymers type B, methacrylic acid copolymers type C, ammoniomethacrvlate copolymers, and neutral copolymer of polvmethacrylic acid ester.
Defined pellet weight-percent relationships for core, matrix, and drug salt
The inert core comprises 30 weight percent to 60 weight percent of the pellet composition and the extended release agent comprises from 5 weight percent to 50 weight percent of the pellet composition and from about 50 weight percent to about 90 weight percent of the matrix coating; the pharmaceutically acceptable cyclobenzaprine salt is cyclobenzaprine hydrochloride and is from 0.01% to 50% by weight of the pellet composition.
Overall, the claim coverage is directed to a capsule-fillable extended release pellet with a defined inert core and a matrix coating that includes cyclobenzaprine, together with specifically selected extended release agents and defined weight-percent ranges for the core, matrix coating, extended release agent, and drug salt.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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