CA2624110A1

CA2624110A1 - A rapidly-dissolving orally administrable wafer formulation

Info

Publication number: CA2624110A1
Application number: CA 2624110
Authority: CA
Inventors: Pankaj Modi
Original assignee: Individual
Current assignee: Individual
Priority date: 2008-03-27
Filing date: 2008-03-27
Publication date: 2008-11-14
Anticipated expiration: 2028-03-27
Also published as: CA2624110C

Abstract

An orally administrable wafer is provided comprising at least one physiologically acceptable film forming agent. The wafer is formed by mixing the film-forming agent with an aqueous solution to form a gel and exposing the gel to a plurality of heating and cooling cycles. The wafer is rapidly dissolving and suitable for administration of pharmaceutical agents.

Claims

1. An orally administrable wafer comprising at least one physiologically acceptable film forming agent, wherein the film forming agent is dissolved in an aqueous solution and treated with heat to form a wafer that exhibits a dissolution rate of at least about 2 milligrams/sec in an aqueous environment.

2. A wafer as defined in claim 1, wherein the film forming agent is selected from the group consisting of pullulan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, carboxymethyl cellulose, polyvinyl alcohol, sodium alginate, polyethylene glycol, glycolide, polylactide, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl polymer, amylose, high amylose starch, hydroxypropylated high amylose starch, dextrin, pectin, chitin, chitosan, levan, elsinan and mixtures thereof.

3. A wafer as defined in claim 2, comprising the film forming agents pullalan, PEG, polyvinyl alcohol and carrageenan.

4. A wafer as defined in claim 1, additionally comprising a pharmaceutical agent.

5. A wafer as defined in claim 4, wherein the pharmaceutical agent is an analgesic.

6. A wafer as defined in claim 5, wherein the pharmaceutical agent is selected from the group consisting of morphine, heroin, hydromorphone, metophon, oxymorphone, levorphanol, codeine, hydrocodone, xycodone, nalorphine, naloxone, naltrexone and fentanyl.

7. A wafer as defined in claim 4, wherein the pharmaceutical agent is an anti-microbial agent.

8. A wafer as defined in claim 1, additionally comprising one or more compounds selected from the group consisting of: a plasticizing agent, a flavoring agent, a sulfur precipitating agent, a saliva stimulating agent, a cooling agent, a surfactant, a stabilizing agent, an emulsifying agent, a thickening agent, a binding agents, a coloring agent, a sweetener, and a fragrance.

9. An orally administrable wafer comprising at least one physiologically acceptable film forming agent, wherein said wafer is formed by mixing the film forming agent with an aqueous solution to form a gel and exposing the gel to a plurality of heating and cooling cycles.

10. A wafer as defined in claim 4, that exhibits a T max, of the agent on administration of the wafer to a patient of less than about 7 minutes.

11. A method of preparing an orally administrable wafer comprising the steps of:
1) mixing at least one physiologically acceptable film forming agent with an aqueous solution to form a gel; and 2) exposing the gel to a plurality of cycles, each cycle comprising heating and cooling, to transform the gel into a wafer.

12. A method as defined in claim 11, wherein each cycle comprises a period of heating up to a temperature within the range of 60 - 90 °C.

13. A method as defined in claim 11, wherein each cycle comprises a period of heating and a period of cooling, and each of said periods lasts about 5 - 15 s.

14. A method as defined in claim 11, comprising at least 3 cycles of heating and cooling.

15. A method as defined in claim 14, wherein the total time of the cycles is between about 1 and 2 minutes.

16. A method as defined in claim 11, comprising the additional step of adding a pharmaceutical agent dissolved in an aqueous solution to the gel prior to heating.

17. A method as defined in claim 16, wherein a measured amount of pharmaceutical agent is added to the gel to yield a wafer with a defined quantity of pharmaceutical agent therein.

18. A method as defined in claim 11, wherein the heating is achieved by exposure to microwaves.

19. An orally administrable wafer comprising a pharmaceutical agent and at least one physiologically acceptable film forming agent, wherein the pharmaceutical agent is present in a pre-defined quantity.

20. A wafer as defined in claim 19, having a dissolution rate of at least about 2 milligrams/sec in an aqueous environment.

21. A wafer as defined in claim 4, wherein the C max of the agent attained on administration of the wafer to a patient is at least about 25%.

22. A method of administering a pharmaceutical agent to a mammal comprising the step of orally administering to the mammal a wafer comprising the pharmaceutical agent, wherein said wafer comprises at least one physiologically acceptable film forming agent and the pharmaceutical agent and the wafer is characterized by a dissolution rate of at least about 2 mg/s in an aqueous environment.

23. A method as defined in claim 22, wherein the pharmaceutical agent treats pain.

24. A method as defined in claim 22, wherein the wafer is prepared by mixing at least one physiologically acceptable film forming agent with an aqueous solution to form a gel;
and exposing the gel to a plurality of cycles, each cycle comprising heating and cooling, to transform the gel into a wafer.