Enhanced delivery epinephrine and prodrug compositions
Pharmaceutical compositions having enhanced active component permeation properties are described.
1. A pharmaceutical composition for oral delivery, comprising:
an oral mucoadhesive polymeric matrix in a film that is orally dissolvable;
a pharmaceutically active component including epinephrine or its prodrug in the polymeric matrix; and
an adrenergic receptor interacter that creates increased blood flow or enables a flushing of the tissue to modify transmucosal uptake of the pharmaceutically active component thereof through a mucosal barrier by utilizing at least a paracellular transport route or mechanism, wherein the pharmaceutical composition is a film, the pharmaceutically active component being contained in the polymeric matrix of the film.
2. The pharmaceutical composition according to claim 1 , further comprising a permeation enhancer.
3. The pharmaceutical composition according to claim 2 , wherein the permeation enhancer includes a phenylpropanoid.
4. The pharmaceutical composition according to claim 3 , wherein the phenylpropanoid is eugenol or eugenol acetate.
5. The pharmaceutical composition according to claim 3 , wherein the phenylpropanoid is a cinnamic acid, cinnamic acid ester, cinnamic aldehyde or hydrocinnamic acid.
6. The pharmaceutical composition according to claim 3 , wherein the phenylpropanoid is chavicol.
7. The pharmaceutical composition according to claim 3 , wherein the phenylpropanoid is safrole.
8. The pharmaceutical composition according to claim 2 , wherein the permeation enhancer includes farnesol or Labrasol.
9. The pharmaceutical composition according to claim 2 , wherein the permeation enhancer includes linoleic acid.
10. The pharmaceutical composition according to claim 1 , wherein the composition is a film further comprising a polymeric matrix, the pharmaceutically active component being contained in the polymeric matrix.
11. The pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition is a film further comprising a polymeric matrix, the pharmaceutically active component being contained in the polymeric matrix.
12. The pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition is a chewable or gelatin based dosage form, spray, gum, gel, cream, tablet, liquid or film.
13. The pharmaceutical composition according to claim 1 , wherein the adrenergic receptor interacter is a phytoextract.
14. The pharmaceutical composition according to claim 13 , wherein the phytoextract further includes an essential oil extract of a clove plant.
15. The pharmaceutical composition according to claim 13 , wherein the phytoextract further includes an essential oil extract of a leaf of a clove plant.
16. The pharmaceutical composition according to claim 13 , wherein the phytoextract further includes an essential oil extract of a flower bud of a clove plant.
17. The pharmaceutical composition according to claim 13 , wherein the phytoextract further includes an essential oil extract of a stem of a clove plant.
18. The pharmaceutical composition according to claim 13 , wherein the phytoextract is synthetic or biosynthetic.
19. The pharmaceutical composition according to claim 13 , wherein the phytoextract further includes 40-95% eugenol.
20. The pharmaceutical composition according to claim 1 , wherein the adrenergic receptor interacter includes a terpenoid, terpene or a sesquiterpene.
21. The pharmaceutical composition according to claim 1 , wherein the polymer matrix includes a polymer.
22. The pharmaceutical composition according to claim 21 , wherein the polymer is a water soluble polymer.
23. The pharmaceutical composition according to claim 21 , wherein the polymer includes a polyethylene oxide.
24. The pharmaceutical composition according to claim 21 , wherein the polymer includes a cellulosic polymer is selected from the group of: hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxyethylmethyl cellulose, hydroxypropyl cellulose, methylcellulose and carboxymethyl cellulose.
25. The pharmaceutical composition according to claim 21 , wherein the polymeric matrix comprises a cellulosic polymer, polyethylene oxide and polyvinyl pyrrolidone, polyethylene oxide and a polysaccharide, polyethylene oxide, hydroxypropyl methylcellulose and a polysaccharide, or polyethylene oxide, hydroxypropyl methylcellulose, polysaccharide and polyvinylpyrrolidone.
26. The pharmaceutical composition according to claim 21 , wherein the polymeric matrix comprises at least one polymer selected from the group of: pullulan, polyvinyl pyrrolidone, polyvinyl alcohol, sodium alginate, polyethylene glycol, xanthan gum, tragancanth gum, guar gum, acacia gum, arabic gum, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl copolymers, starch, gelatin, ethylene oxide-propylene oxide co-polymers, collagen, albumin, poly-amino acids, polyphosphazenes, polysaccharides, chitin, chitosan, and derivatives thereof.
27. The pharmaceutical composition according to claim 1 , further comprising a stabilizer.
28. The pharmaceutical composition according to claim 1 , wherein the polymeric matrix comprises a dendritic polymer or a hyperbranched polymer.
29. The pharmaceutical composition according to claim 1 , wherein the prodrug is dipivefrin.
30. A pharmaceutical composition for oral delivery, comprising:
an oral mucoadhesive polymeric matrix in a film that is orally dissolvable;
a pharmaceutically active component including dipivefrin in the polymeric matrix; and
an adrenergic receptor interacter that creates increased blood flow or enables a flushing of the tissue to enhance transmucosal uptake of epinephrine, wherein the pharmaceutical composition is a film, the pharmaceutically active component being contained in the polymeric matrix of the film.
31. The pharmaceutical composition of claim 30 , wherein the polymeric matrix is in a dosage having bioadhesion that forms a gel like structure when administered in the oral cavity of a user.
32. The pharmaceutical composition of claim 31 wherein the film is orally dissolvable between about 1 minute and about 20 minutes.
33. A pharmaceutical composition for oral delivery, comprising:
a mucoadhesive polymeric matrix;
a pharmaceutically active component including prodrug of epinephrine in the polymeric matrix; and
an adrenergic receptor interacter that creates increased blood flow or enables a flushing of the tissue to modify transmucosal uptake of the pharmaceutically active component, wherein the pharmaceutical composition is a film, the pharmaceutically active component being contained in the polymeric matrix of the film.
34. The pharmaceutical composition of claim 33 , wherein the polymeric matrix is a film that is orally dissolvable, and that is in a dosage having bioadhesion that forms a gel like structure when administered in the oral cavity of a user.
35. The pharmaceutical composition of claim 34 wherein the film is orally dissolvable between about 1 minute and about 20 minutes.
36. The pharmaceutical composition of claim 1 , wherein at least one adrenergic receptor interacter is an ester.
37. The pharmaceutical composition of claim 36 , wherein the ester is an ester of epinephrine.
38. The pharmaceutical composition of claim 1 , further comprising a surfactant.
39. The pharmaceutical composition of claim 1 , wherein the surfactant is a caprylocaproyl polyoxylglyceride.