Back to results
US 5,674,533 AGranted
Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
AssigneeRecordati S.A., Chemical and Pharmaceutical Company
InventorsGiancarlo Santus, Ettore Bilato, Gabriele Lazzarini
Life of this patent
Estimating the term…
Abstract
Disclosed are compositions and dosage forms containing moguisteine and having controlled release properties, methods for using such compositions and dosage forms and methods for making them.
Claims34
A controlled-release pharmaceutical dosage form suitable for the administration of moguisteine in a liquid suspension, which controlled-release pharmaceutical dosage form comprises:
- microgranules containing moguisteine as an active ingredient, said microgranules before being coated having a smooth surface and substantially spherical shape and no controlled-release properties,
- said microgranules comprising a plurality of at least three coatings thereon, at least one of said coatings imparting controlled release properties to said microgranules, the first of said coatings thereon being pH sensitive,
- said at least three coatings comprising alternating hydrophilic and lipophilic layers applied to said microgranules, said coatings preventing tastable dissolution of said moguisteine upon ingestion and ensuring a predetermined sustained release profile of moguisteine and maintenance over time of said release profile, said lipophilic layer being free of organic solvent, wherein said dosage form when ingested does not result in immediately bioavailable extragranular moguisteine being released into the oral cavity.
A controlled release pharmaceutical dosage form suitable for the administration of moguisteine in a liquid suspension, which comprises:
- microgranules containing moguisteine as an active ingredient and polyethylene glycol as a plasticizer, said microgranules before coating having a smooth surface and substantially spherical shape and no controlled-release properties,
- said microgranules comprising a plurality of at least three coatings thereon, at least one of said coatings imparting controlled-release properties to said microgranules, wherein a first one of said coatings comprises cellulose acetate phthalate, a second one of said coatings applied successively on said first coating comprises a mixture of glyceryl monostearate and beeswax, and a third of said coatings applied successively on said second coating comprises cellulose acetate phthalate, said first coating being pH sensitive, said second coating being free of organic solvent,
- said coatings preventing tastable dissolution of said moguisteine upon ingestion and ensuring a predetermined sustained release profile of moguisteine and maintenance of said release profile, wherein said dosage form when ingested does not result in immediate bioavailable extragranular moguisteine being released into the oral cavity.
A method for preparing a palatable controlled-release pharmaceutical dosage form for the administration of moguisteine in a liquid suspension, which comprises:
- (a) mixing moguisteine and at least one plasticizer to form micro-granules;
- and
- (b) coating the microgranules with a first, hydrophilic, coating layer comprising a polymer selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate and combinations thereof, said first coating being pH sensitive;
- (c) coating the microgranules formed in (b) with a second, lipophilic, coating comprising a waxy material selected from the group of mono-, di- tri-glycerides of C.sub.6 -C.sub.36 fatty acids, carnauba wax, beeswax, and candelilla wax, alcohols, fatty acids, and combinations thereof, wherein said waxy material is applied in its melted state using heated compressed air as a spray medium, said second coating being free of organic solvent;
- and
- (d) coating the microgranules formed in (c) with a third, hydrophilic coating comprising a polymer selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate and combinations thereof.
3 more elements
A composition for use in the symptomatic treatment of coughing, said composition comprising:
- microgranules containing moguisteine as an active ingredient, said microgranules before being coated having a smooth surface and substantially spherical shape and no controlled-release properties,
- said microgranules comprising a plurality of at least three coatings thereon, at least one of said coatings imparting controlled release properties to said microgranules, the fist of said coatings thereon being pH sensitive,
- said at least three coatings comprising alternating hydrophilic and lipophilic layers applied to said microgranules, said coatings preventing tastable dissolution of said moguisteine upon ingestion and ensuring a predetermined sustained release profile of moguisteine and maintenance over time of said release profile, said lipophilic layer being free of organic solvent, wherein the composition when ingested does not result in immediately bioavailable moguisteine being released into the oral cavity.
A composition for use in the symptomatic treatment of coughing, said composition comprising:
- microgranules containing moguisteine as an active ingredient and polyethylene glycol as a plasticizer, said microgranules before coating having a smooth surface and substantially spherical shape and no controlled-release properties,
- said microgranules comprising a plurality of at least three coatings thereon, at least one of said coatings imparting controlled-release properties to said microgranules, the first of said coatings thereon being pH sensitive,
- a first one of said coatings comprising cellulose acetate phthalate, a second one of said coatings applied successively on said first coating comprising a mixture of glyceryl monostearate and beeswax, and a third one of said coatings applied successively on said second coating comprising cellulose acetate phthalate,
- said coatings preventing testable dissolution of said moguisteine upon ingestion and ensuring a predetermined sustained release profile of moguisteine and maintenance of said release profile, said second coating being free of organic solvent;
- and
- a vehicle for the administration of said coated microgranules, wherein said composition when ingested does not result in immediately bioavailable extragranular moguisteine being released into the oral cavity.
3 more elements
A controlled-release pharmaceutical dosage form suitable for the administration of moguisteine in a liquid suspension, which comprises:
- microgranules containing moguisteine as an active ingredient, said microgranules before being coated having a smooth surface and substantially spherical shape and no controlled-release properties,
- said microgranules comprising a plurality of at least three coatings thereon, at least one of said coatings imparting controlled release properties to said microgranules,
- said at least three coatings comprising alternating hydrophilic and lipophilic layers applied to said microgranules, said coatings preventing tastable dissolution of said moguisteine upon ingestion and ensuring a predetermined sustained release profile of moguisteine and maintenance over time of said release profile, at least one of said lipophilic layers comprising a waxy material selected from the group of mono-, di- tri-glycerides of C.sub.6 -C.sub.36 fatty acids, carnauba wax, beeswax, and candelilla wax, alcohols, and fatty acids,
- wherein said waxy material is free of organic solvents.
1 more element
Dependencies are inferred from the claim text.