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Last Updated: September 23, 2021

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Claims for Patent: 4,478,822

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Summary for Patent: 4,478,822
Title: Drug delivery system utilizing thermosetting gels
Abstract:This invention relates to a unique drug delivery system for delivering drugs to a body cavity. The drug delivery system comprises a medicament and a polymer such that the drug delivery system is a liquid at room temperature but forms a semi-solid or gel at the body temperature in the body cavity.
Inventor(s): Haslam; John L. (Lawrence, KS), Higuchi; Takeru (Lawrence, KS), Mlodozeniec; Arthur R. (Lawrence, KS)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:06/495,239
Patent Claims:1. An aqueous pharmaceutical composition for rectal, urethral, nasal, vaginal, optical or oral in the buccal pourch administration to a body cavity to treat a condition requiring pharmacological treatment comprising

a. 10% to 50% by weight of a polymer of the formula: ##STR2## wherein w is an integer of from 2-6 containing approximately 40% to 80% poly(oxyethylene) and approximately 20 to 60% poly(oxypropylene) and having a molecular weight of 7,000 to 50,000; and x and y are any integers within the above constraints; and

b. a pharmacologically effective amount of drug selected from the group consisting of anti-bacterial substances, antihistamines and decongestants, anti-inflammatories, anti-parasitics, antiviral, local anesthetics, antifungal, amebecidal, or trichomonocidal agents, analgesics, antiarthritics, antiasthmatics, anticoagulants, anticonvulsants, antidepressants, antidiabetics, antineoplastics, antipsychotics, antihypertensives, and muscle relaxants and anti-protozoals; and

c. a pharmaceutically acceptable acid or base being in sufficient quantity to adjust the pH of the composition to range from 2 to 9 and wherein the composition is liquid at about room temperature or below.

2. The composition of claim 1 wherein the polymer is one wherein w is 2.

3. The composition of claim 1 wherein the polymer is Tetronic.RTM.1307.

4. The composition of claim 1 wherein the gel-sol transition temperature of the composition is room temperature or below and said composition is liquid at this temperature.

5. The composition of claim 1 wherein the antibacterial substances are selected from the group consisting of beta-lactam antibiotics, tetracyclines, chloramphenicol, neomycin, gramicidin, bacitracin, sulfonamides, aminoglycoside antibiotics, tobramycin, nitrofurazone, nalidixic acid and analogs and the antimicrobial combination of fludalanine/pentizidone.

6. The composition of claim 1 wherein the antihistaminics and decongestants are selected from the group consisting of perilamine, chlorpheneramine, tetrahydrozaline and antazoline.

7. The composition of claim 1 wherein the anti-inflammatory drugs are selected from the group consisting of cortisone, hydrocortisone, betamethasone, dexamethasone, fluocortolone, prednisolone, triamcinolone, indomethacin, sulindac and its salts and corresponding sulfide.

8. A composition of claim 1 wherein the antiparasitic compound is ivermectin.

9. The composition of claim 1 wherein the antiviral effective compounds are selected from the group consisting of acyclovir and interferon.

10. A composition of claim 1 wherein the local anesthetics are selected from the group consisting of benzocaine, lidocaine and procaine.

11. The composition of claim 1 wherein the antifungal, antiprotozoal, amebecidal or trichomonacidal agent is selected from the group consisting of polyoxyethylene nonylphenol, alkylaryl sulfonate, oxyquinoline sulfate, miconazole nitrate, sulfanilamide, condicidin, sulfisoxazole, nystatin, clotrimazole, metronidazole, chloramphenicol, chloroquine, trimethoprim or sulfamethoxazole.

12. The composition of claim 1 wherein the analgesic drug is selected from the group consisting of diflunisal, aspirin or acetaminophen.

13. The composition of claim 1 wherein the antiarthritics are selected from the group consisting of phenylbutazone, indomethacin, sulindac, dexamethasone, ibuprofen, allopurinol, oxyphenbutazone or probenecid.

14. The composition of claim 1 wherein the antiasthma drugs are selected from the group consisting of theophylline, ephedrine, beclomethasone diproprionate and epinephrine.

15. The composition of claim 1 wherein the anticoagulants are selected from the group consisting of heparin, bishydroxycoumarin, and warfarin.

16. The composition of claim 1 wherein the anticonvulsants are selected from the group consisting of diphenylhydantoin and diazepam.

17. The composition of claim 1 wherein the antidepressants are selected from the group consisting of amitriptyline, chlordiazepoxide perphenazine, protriptyline, imipramine and doxepin.

18. The composition of claim 1 wherein the antidiabetics are selected from the group consisting of insulin, tolbutamide, tolazamide, acetohexamide and chlorpropamide.

19. The composition of claim 1 wherein the antineoplastics are selected from the group consisting of adriamycin, flurouracil, methotrexate and asparaginase.

20. The composition of claim 1 wherein the antipsychotics are selected from the group consisting of prochlorperazine lithium carbonate, lithium citrate, thioridazine, molindone, fluphenazine, trifluoperazine, perphenazine, amitriptyline and triflupromazine.

21. The composition of claim 1 wherein the antihypertensives are selected from the group consisting of spironolactone, methyldopa, hydralazine, clonidine, chlorothiazide, deserpidine, timolol, propranolol, metoprolol, prazosin hydrochloride and reserpine.

22. The composition of claim 1 wherein the muscle relaxants are selected from the group consisting of melphalan, danbrolene, cyclobenzoprine, methocarbamol and diazepam.

23. The composition of claim 1 which includes a buffering agent or salt of from 0 to 5% by weight of the composition.

24. The composition of claim 23 wherein the buffering agent or salt is selected from the group consisting of alkali or alkali earth carbonates, chlorides, sulfates, phosphates, bicarbonates, citrates, borates, acetates and succinates.

25. The composition of claim 1 which includes from 0.001% to 5% by weight of the composition of a preservative.

26. The composition of claim 25 wherein the preservatives are selected from the group consisting of sodium bisulfite, sodium thiosulfate, ascorbate, benzalkonium chloride, chlorobutanol, thimerosal, phenylmercuric borate, parabens, benzylalcohol and phenylethanol.

27. The composition of claim 1 wherein the acid or base is selected from the group consisting of hydrochloric acid or sodium hydroxide.

28. A method of treating a condition requiring pharmacological treatment which comprises administering rectal, urethral, nasal, vaginal, optical or oral in the buccal pourch to a body cavity a liquid drug delivery device comprising:

a. 10% to 50% by weight of a polymer of the formula ##STR3## wherein w is an integer of from 2 to 6 containing approximately 40% to 80% poly(oxyethylene) and approximately 20-60% poly(oxypropylene) and having a molecular weight of 7,000 to 50,000; and x and y are any integers within the above constraints; and

b. a pharmacologically effective amount of drug selected from the group consisting of antibacterial substances, antihistamines and decongestants, anti-inflammatories, antiparasitics, antivirals, local anesthetics, antifungal, amebecidal, or trichomonocidal agents, analgesics, antiarthritics, antiasthmatics, anticoagulants, anticonvulsants, antidepressants, antidiabetics, antineoplastics, antipsychotics, antihypertensives, muscle relaxants and antiprotozoals; and

c. a pharmaceutically acceptable acid or base being in sufficient quantity to adjust the pH of the composition to range from 2 to 9 and wherein the composition is liquid at about room temperature or below.

29. A method of treatment according to claim 28 wherein the polymer is one wherein w is 2.

30. A method of treatment according to claim 23 wherein the polymer is Tetronic.RTM.1307.

31. A method of treatment according to claim 28 wherein the gel-sol transition temperature of the composition is room temperature or below and said composition is liquid at this temperature.

32. A method of treatment of claim 28 wherein said pharmaceutical composition is administered rectally, urethrally, nasally, vaginally, otically or orally within the buccal pouch.

33. A method of treatment according to claim 28 wherein the antibacterial substances are selected from the group consisting of beta-lactam antibiotics, tetracyclines, chloroamphenicol, neomycin, gramicidin, bacitracin, sulfonamides, aminoglycoside antibiotics, tobramycin, nitrofurazone, nalidixic acid and analogs and the antimicrobial combination of fludalanine/pentizidone.

34. A method of treatment according to claim 28 wherein the antihistaminics and decongestants are selected from the group consisting of perilamine, chlorpheniramine, tetrahydrozaline and antazoline.

35. A method of treatment according to claim 28 wherein the anti-inflammatory drugs are selected from the group consisting of cortisone, hydrocortisone, betamethasone, dexamethasone, fluocortolone, prednisolone, triamcinalone, sulindac and its salts and corresponding sulfide.

36. A method of treatment of claim 28 wherein the antiparasitic compound is ivermectin.

37. A method of treatment according to claim 28 wherein the antiviral effective compounds are selected from the group consisting of acyclovir and interferon.

38. A method of treatment according to claim 28 wherein the local anesthetics are selected from the group consisting of benzocaine, lidocaine and procaine.

39. A method of treatment according to claim 28 wherein the antifungal, antiprotozoal, amebecidal or trichomonacidal agent is selected from the group consisting of polyoxyethylene nonylphenol, alkylaryl sulfonate, oxyquinoline sulfate, miconazole nitrate, sulfonilamide, condicidin, sulfisoxazole, nystatin, clotrimazole metronidazole, chloramphenicol, chloroquine, trimethoprim or sulfamethoxazole.

40. A method of treatment according to claim 28 wherein the analgesic drug is selected from the group consisting of diflunisal, aspirin or acetaminophen.

41. A method of treatment according to claim 28 wherein the antiarthritics are selected from the group consisting of phenylbutazone, indomethacin, sulindac and its salts and corresponding sulfide, dexamethasone, ibuprofen, allopurinol, oxyphenbutazone or probenecid.

42. A method of treatment according to claim 28 wherein the antiasthma drugs are selected from the group consisting of theophylline, ephedrine, beclomethasone diproprionate and epinephrine.

43. A method of treatment according to claim 28 wherein the anticoagulants are selected from the group consisting of heparin, bishydroxycoumarin, and warfarin.

44. A method of treatment according to claim 28 wherein the anticonvulsants are selected from the group consisting of diphenylhydantoin and diazepam.

45. A method of treatment according to claim 28 wherein the antidepressants are selected from the group consisting of amitriptyline, chlordiazepoxide perphenazine, protriptyline, imipramine and doxepin.

46. A method of treatment according to claim 28 wherein the antidiabetics are selected from the group consisting of insulin, tolbutamide, tolazamide, acetohexamide and chlorpropamide.

47. A method of treatment according to claim 28 wherein the antineoplastics are selected from the group consisting of adriamycin, flurouracil, methotrexate and asparaginase.

48. A method of treatment according to claim 28 wherein the antipsychotics are selected from the group consisting of prochlorperazine lithium carbonate, lithium citrate, thioridazine, molindone, fluphenazine, trifluoperazine, perphenazine, amitriptyline and triflupromazine.

49. A method of treatment according to claim 28 wherein the antihypertensives are selected from the group consisting of spironolactone, methyldopa, hydralazine, clonidine, chlorothiazide, deserpidine, timolol, propranolol, metoprolol, prazosin hydrochloride and reserpine.

50. A method of treatment according to claim 28 wherein the muscle relaxants are selected from the group consisting of melphalan, danbrolene, cyclobenzaprine, methocarbamol and diazepam.

51. A method of treatment according to claim 28 wherein the composition includes a buffering agent or salt of from 0% to 5% by weight of the composition.

52. A method of treatment according to claim 51 wherein the buffering agent or salt is selected from the group consisting of alkali or alkali earth carbonates, chlorides, sulfates, phosphates, bicarbonates, citrates, borates, acetates and succinates.

53. A method of treatment according to claim 28 wherein the composition includes from 0.001% to 5% by weight of the composition of a preservative.

54. A method of treatment according to claim 53 wherein the preservatives are selected from the group consisting of sodium bisulfite, sodium thiosulfate, ascorbate, benzalkonium chloride, chlorobutanol, thimerosal, phenylmercuric borate, parabens, benzylalcohol and phenylethanol.

55. A method of treatment according to claim 28 wherein the acid or base is selected from the group consisting of hydrochloric acid or sodium hydroxide.

Details for Patent 4,478,822

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck ELSPAR asparaginase VIAL 101063 001 1978-01-10 ⤷  Try it Free Merck & Co., Inc. (Rahway, NJ) 2039-03-29 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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