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 retention in a stomach, comprising:
a hinge assembly, and
two parts connected together by the hinge assembly,
at least one part being an arm comprising a cavity engaging an insert comprising an active pharmaceutical ingredient (API) or diagnostic,
wherein the hinge assembly and the two parts are configured to transform between
a collapsed configuration for ingestion,
an expanded configuration for retention within the stomach, and
a third configuration wherein at least one of the two parts disengages from the hinge assembly,
wherein said disengagement is due to at least partial erosion of the insert, and
wherein the disengaged parts are sized for exiting the stomach through the pyloric valve.
2. The GRDF of claim 1 , wherein the two parts are two arms.
3. The GRDF of claim 1 , wherein the two parts are pivotably connected to each other by the hinge assembly.
4. The GRDF of claim 1 , wherein the two parts comprise a pH dependent polymer that erodes in a basic environment.
5. The GRDF of claim 1 , wherein the two parts are erodible at a pH of 5 to 7.5.
6. The GRDF of claim 1 , wherein the at least one of the two parts comprises a cellulose ester and a plasticizer.
7. The GRDF of claim 6 , wherein the cellulose ester is cellulose acetate, cellulose triacetate, hydroxypropylmethylcellulose acetate succinate, cellulose propionate, cellulose acetate propionate, cellulose acetate butyrate, or a combination thereof.
8. The GRDF of claim 6 , wherein the plasticizer is dibutyl sebacate, triethyl citrate, polyethylene glycol, polyethylene glycol monomethyl ether, acetyl tributyl citrate, triacetin, or a combination thereof.
9. The GRDF of claim 1 , wherein the cavity has a volume of about 100 mm 3 to about 2000 mm 3 .
10. The GRDF of claim 1 , wherein the partial erosion of the insert occurs after a predetermined time period of from four hours to 180 days has elapsed.
11. The GRDF of claim 1 , wherein the disengagement is due to erosion of greater than 50% of the API or the diagnostic from the GRDF.
12. The GRDF of claim 1 , wherein the API or the diagnostic erodes at a controlled rate over a period of 6 to 24 hours.
13. The GRDF of claim 1 , wherein the GRDF is maintained in the collapsed configuration by a retention mechanism that dissolves when introduced to a fluid environment and wherein said GRDF transitions to the expanded configuration upon at least partial dissolution of said retention mechanism in less than 5 minutes.
14. The GRDF of claim 1 , wherein the insert further comprises an excipient, and wherein a ratio of the weight of the excipient to the weight of the API or the diagnostic is from about 0.8 to about 0.05.
15. The GRDF of claim 1 , further comprising a second API or a second diagnostic.
16. The GRDF of claim 1 , wherein the parts are produced by injection molding or 3D printing.
17. The GRDF of claim 1 , wherein the insert is retained in the stomach for a time period of 6 hours to 180 days.
18. The GRDF of claim 1 , further comprising a biasing element configured to transition the GRDF from the collapsed configuration to the expanded configuration.
19. The GRDF of claim 1 , having a mechanical durability to remain intact under a repeated force of about 400 grF to about 3000 grF, for a time period of about 1 hour to 24 hours.