Expandable gastroretentive dosage form
An oral gastro-retentive delivery device is provided which unfolds rapidly upon contact with gastric juice. The device is configured in a collapsed configuration for oral intake and unfolding for gastric retention for a predetermined period of time and eventually reducing in size for passage through the rest of the GI track.
1. A gastroretentive dosage form (GRDF) for extended retention in a stomach comprising a body made from a pharmaceutically acceptable material, comprising at least two arms and an active pharmaceutical ingredient (API) or diagnostic, and configured to transform between a collapsed configuration for ingestion, an expanded configuration for retention within the stomach for a predetermined time period, and a third configuration wherein the GRDF disassembles such that each of the disassembled parts of the GRDF is sized for exiting the stomach and wherein at least one of the at least two arms is configured to disassemble as an individual part from the body for exiting the stomach at a pH higher than about 5,
wherein in the expanded configuration, the at least two arms and the body each have a center axis, all center axes lying in a single plane, and the at least two arms define an interior angle between adjacent arms from about 45 degrees to about 90 degrees.
2. The GRDF of claim 1 , wherein the detachment of at least one of the at least two arms from the body for exiting the stomach is due to erosion of a pH sensitive material at a pH higher than about 5.
3. The GRDF of claim 2 , wherein the pH sensitive material erodes at a pH of no more than about 7.5.
4. The GRDF of claim 2 , wherein the pH sensitive material erodes in a basic environment.
5. The GRDF of claim 2 , wherein the pH sensitive material comprises a polymer.
6. The GRDF of claim 2 , wherein the pH sensitive material comprises a polyacrylamide, an acid phthalate of carbohydrate, an amylase acetate phthalate, a cellulose acetate phthalate, a hydroxypropyl cellulose phthalate, a hydroxypropyl ethylcellulose phthalate, a hydroxypropyl methyl cellulose phthalate, a methyl cellulose phthalate, a polyvinyl acetate phthalate, a polyvinyl acetate hydrogen phthalate, a sodium cellulose acetate phthalate, a starch acid phthalate, a styrene-maleic acid dibutyl phthalate copolymer, a styrene-maleic acid polyvinyl acetate phthalate copolymer, a styrene and maleic acid copolymer, a formalized gelatin, gluten, shellac, salol, keratin, a keratin sandarac-tolu, ammoniated shellac, benzophenyl salicylate, cellulose acetate trimellitate, a cellulose acetate blended with shellac, hydroxypropylmethyl cellulose acetate succinate, oxidized cellulose, a polyacrylic acid derivative, acrylic acid, an acrylic ester copolymer, methacrylic acid or an ester thereof, vinyl acetate, or a crotonic acid copolymer.
7. The GRDF of claim 2 , wherein the pH sensitive material represents less than 20% of the total weight of the body of the GRDF.
8. The GRDF of claim 7 , wherein the pH sensitive material represents less than 10% of the total weight of the body of the GRDF.
9. The GRDF of claim 2 , wherein the erosion of the pH sensitive material results in a partial degradation of at least one of the at least two arms and/or body.
10. The GRDF of claim 2 , wherein the body transitions from the collapsed configuration to the expanded configuration upon contact with gastric fluid in the stomach for less than 5 minutes.
11. The GRDF of claim 2 , wherein the predetermined time period is 18 hours to 180 days.
12. The GRDF of claim 2 , configured for the controlled release of the API in the stomach over a period of 24 hours to 180 days.
13. A gastroretentive dosage form (GRDF) for extended retention in a stomach comprising a body made from a pharmaceutically acceptable material, comprising at least two arms and an active pharmaceutical ingredient (API) or diagnostic, and configured to transform between a collapsed configuration for ingestion, an expanded configuration for retention within the stomach for a predetermined time period, and a third configuration wherein the GRDF disassembles such that each of the disassembled parts of the GRDF is sized for exiting the stomach and wherein at least one of the at least two arms is configured to disassemble as an individual part from the body for exiting the stomach at a pH higher than about 5,
wherein in the expanded configuration, the at least two arms and the body each have a center axis, all center axes lying in a single plane, and the at least two arms define an interior angle of between about 45 degrees and about 90 degrees.
14. A method of treating a patient with an API or diagnostic comprising orally administering to the patient the GRDF of claim 1 .
15. The method of claim 14 , further comprising orally administering an antidote to the patient, wherein the antidote increases the pH of the patient's stomach to higher than 5 so as to achieve erosion of the pH sensitive material and wherein the erosion of the pH sensitive material results in the disassembly and exiting from the stomach of pieces of sufficient size to evacuate the stomach.