US4478822A
Expired / Lapsed
US
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Drug delivery system utilizing thermosetting gels
Assignee: Merck and Co Inc
•
Filing: 1983-05-16
•
Granted: 1984-10-23
•
Expires: 2003-05-16
Abstract
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.
Inventors
- 👤 John L. Haslam
- 👤 Takeru Higuchi
- 👤 Arthur R. Mlodozeniec
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:07
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K47/00; A61K47/06; A61K47/16; A61K47/18
Claims Analysis
Total Claims: 57
Claim 1
Independent Claim
163 words
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.
Claim 2
Dependent Claim
163 words
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.
Claim 3
Dependent Claim
14 words
The composition of claim 1 wherein the polymer is one wherein w is 2.
Claim 4
Dependent Claim
10 words
The composition of claim 1 wherein the polymer is Tetronic®1307.
Claim 5
Dependent Claim
26 words
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.
Claim 6
Dependent Claim
38 words
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.
Claim 7
Dependent Claim
22 words
The composition of claim 1 wherein the antihistaminics and decongestants are selected from the group consisting of perilamine, chlorpheneramine, tetrahydrozaline and antazoline.
Claim 8
Dependent Claim
31 words
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.
Claim 9
Dependent Claim
11 words
A composition of claim 1 wherein the antiparasitic compound is ivermectin.
Claim 10
Dependent Claim
20 words
The composition of claim 1 wherein the antiviral effective compounds are selected from the group consisting of acyclovir and interferon.
Claim 11
Dependent Claim
20 words
A composition of claim 1 wherein the local anesthetics are selected from the group consisting of benzocaine, lidocaine and procaine.
Claim 12
Dependent Claim
39 words
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.
Claim 13
Dependent Claim
20 words
The composition of claim 1 wherein the analgesic drug is selected from the group consisting of diflunisal, aspirin or acetaminophen.
Claim 14
Dependent Claim
24 words
The composition of claim 1 wherein the antiarthritics are selected from the group consisting of phenylbutazone, indomethacin, sulindac, dexamethasone, ibuprofen, allopurinol, oxyphenbutazone or probenecid.
Claim 15
Dependent Claim
22 words
The composition of claim 1 wherein the antiasthma drugs are selected from the group consisting of theophylline, ephedrine, beclomethasone diproprionate and epinephrine.
Claim 16
Dependent Claim
19 words
The composition of claim 1 wherein the anticoagulants are selected from the group consisting of heparin, bishydroxycoumarin, and warfarin.
Claim 17
Dependent Claim
18 words
The composition of claim 1 wherein the anticonvulsants are selected from the group consisting of diphenylhydantoin and diazepam.
Claim 18
Dependent Claim
22 words
The composition of claim 1 wherein the antidepressants are selected from the group consisting of amitriptyline, chlordiazepoxide perphenazine, protriptyline, imipramine and doxepin.
Claim 19
Dependent Claim
21 words
The composition of claim 1 wherein the antidiabetics are selected from the group consisting of insulin, tolbutamide, tolazamide, acetohexamide and chlorpropamide.
Claim 20
Dependent Claim
20 words
The composition of claim 1 wherein the antineoplastics are selected from the group consisting of adriamycin, flurouracil, methotrexate and asparaginase.
Claim 21
Dependent Claim
28 words
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.
Claim 22
Dependent Claim
28 words
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.
Claim 23
Dependent Claim
22 words
The composition of claim 1 wherein the muscle relaxants are selected from the group consisting of melphalan, danbrolene, cyclobenzoprine, methocarbamol and diazepam.
Claim 24
Dependent Claim
22 words
The composition of claim 1 which includes a buffering agent or salt of from 0 to 5% by weight of the composition.
Claim 25
Dependent Claim
32 words
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.
Claim 26
Dependent Claim
19 words
The composition of claim 1 which includes from 0.001% to 5% by weight of the composition of a preservative.
Claim 27
Dependent Claim
30 words
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.
Claim 28
Dependent Claim
22 words
The composition of claim 1 wherein the acid or base is selected from the group consisting of hydrochloric acid or sodium hydroxide.
Claim 29
Independent Claim
166 words
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.
Claim 30
Independent Claim
166 words
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.
Claim 31
Dependent Claim
17 words
A method of treatment according to claim 28 wherein the polymer is one wherein w is 2.
Claim 32
Dependent Claim
13 words
A method of treatment according to claim 23 wherein the polymer is Tetronic®1307.
Claim 33
Dependent Claim
29 words
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.
Claim 34
Dependent Claim
24 words
A method of treatment of claim 28 wherein said pharmaceutical composition is administered rectally, urethrally, nasally, vaginally, otically or orally within the buccal pouch.
Claim 35
Dependent Claim
41 words
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.
Claim 36
Dependent Claim
25 words
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.
Claim 37
Dependent Claim
33 words
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.
Claim 38
Dependent Claim
13 words
A method of treatment of claim 28 wherein the antiparasitic compound is ivermectin.
Claim 39
Dependent Claim
23 words
A method of treatment according to claim 28 wherein the antiviral effective compounds are selected from the group consisting of acyclovir and interferon.
Claim 40
Dependent Claim
23 words
A method of treatment according to claim 28 wherein the local anesthetics are selected from the group consisting of benzocaine, lidocaine and procaine.
Claim 41
Dependent Claim
42 words
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.
Claim 42
Dependent Claim
23 words
A method of treatment according to claim 28 wherein the analgesic drug is selected from the group consisting of diflunisal, aspirin or acetaminophen.
Claim 43
Dependent Claim
33 words
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.
Claim 44
Dependent Claim
25 words
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.
Claim 45
Dependent Claim
22 words
A method of treatment according to claim 28 wherein the anticoagulants are selected from the group consisting of heparin, bishydroxycoumarin, and warfarin.
Claim 46
Dependent Claim
21 words
A method of treatment according to claim 28 wherein the anticonvulsants are selected from the group consisting of diphenylhydantoin and diazepam.
Claim 47
Dependent Claim
25 words
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.
Claim 48
Dependent Claim
24 words
A method of treatment according to claim 28 wherein the antidiabetics are selected from the group consisting of insulin, tolbutamide, tolazamide, acetohexamide and chlorpropamide.
Claim 49
Dependent Claim
23 words
A method of treatment according to claim 28 wherein the antineoplastics are selected from the group consisting of adriamycin, flurouracil, methotrexate and asparaginase.
Claim 50
Dependent Claim
31 words
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.
Claim 51
Dependent Claim
31 words
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.
Claim 52
Dependent Claim
25 words
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.
Claim 53
Dependent Claim
27 words
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.
Claim 54
Dependent Claim
35 words
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.
Claim 55
Dependent Claim
24 words
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.
Claim 56
Dependent Claim
33 words
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.
Claim 57
Dependent Claim
25 words
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.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-10-23 | 1988-04-23 | 1988-10-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-10-23 | 1992-04-23 | 1992-10-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-10-23 | 1996-04-23 | 1996-10-23 | $7700.00 | Window Closed / Lapsed |