US4474753A
Expired / Lapsed
US
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Topical drug delivery system utilizing thermosetting gels
Assignee: Merck and Co Inc
•
Filing: 1983-05-16
•
Granted: 1984-10-02
•
Expires: 2003-05-16
Abstract
Abstract This invention relates to a unique drug delivery system for application to the skin which drug delivery system is a liquid at room temperature, but when administered topically to the skin becomes a semi-solid or gel when warmed by the body.
Inventors
- 👤 John L. Haslam
- 👤 Takeru Higuchi
- 👤 Arthur R. Mlodozeniec
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 23:15
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0014; A61K47/00; A61K47/06; A61K47/16; A61K47/18
Claims Analysis
Total Claims: 51
Claim 1
Independent Claim
128 words
An aqueous pharmaceutical composition for administration to the skin comprising a. 10% to 50% by weight to a polyoxamine polymer of the formula ##STR2## wherein w is an integer of from 2 to 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 contraints; and b. a pharmacologically effective amount of drug selected from the group consisting of antibacterial substances, anti-infectives, anesthetics, anti-inflammatories, anti-parasitics, antivirals, antifungals, analgesics; and diagnostics; 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
128 words
An aqueous pharmaceutical composition for administration to the skin comprising a. 10% to 50% by weight to a polyoxamine polymer of the formula ##STR2## wherein w is an integer of from 2 to 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 contraints; and b. a pharmacologically effective amount of drug selected from the group consisting of antibacterial substances, anti-infectives, anesthetics, anti-inflammatories, anti-parasitics, antivirals, antifungals, analgesics; and diagnostics; 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
11 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
39 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, the antimicrobial combination of fludalanine/pentizidone and nitrofurazone.
Claim 7
Dependent Claim
22 words
The composition of claim 5 wherein the β-lactam antibiotics are selected from the group consisting of cefoxitin, n-formamidoyl thienamycin, and thienamycin derivatives.
Claim 8
Dependent Claim
21 words
The composition of claim 1 wherein the anti-infectives are selected from the group consisting of iodine, chloramines, benzalkonium chloride and phenol.
Claim 9
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, triamcinalone, indomethacin, sulindac and its salts and corresponding sulfide.
Claim 10
Dependent Claim
11 words
A composition of claim 1 wherein the antiparasitic compound is ivermectin.
Claim 11
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 12
Dependent Claim
19 words
A composition of claim 1 wherein the anesthetics are selected from the group consisting of benzocaine, lidocaine and dibucaine.
Claim 13
Dependent Claim
25 words
The composition of claim 1 wherein the antifungal agent is selected from the group consisting of tolnaftate, undecylenic acid, salicylic acid, zinc undecylenate and thiabendazole.
Claim 14
Dependent Claim
26 words
The composition of claim 1 wherein the analgesic drug is selected from the group consisting of methylsalicylate, menthol, camphor, methylnicotinate, triethanolamine salicylate, glycol salicylate and salicylamine.
Claim 15
Dependent Claim
35 words
The composition of claim 1 wherein the diagnostic compound is selected from the group consisting of n-alkyl carbonates, cholesteryl oleyl carbonate, cholesteryl nonanoate or cholesteryl benzoate all in proper proportions to effect liquid crystal responses.
Claim 16
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 17
Dependent Claim
32 words
The composition of claim 15 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 18
Dependent Claim
18 words
The composition of claim 1 which includes from 0.001% to 5% weight of the composition of a preservative.
Claim 19
Dependent Claim
30 words
The composition of claim 17 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 20
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 21
Independent Claim
139 words
A method of treating a condition requiring pharmacological treatment which comprises administering to the skin of a patient a liquid drug delivery vehicle 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, anti-infectives, anesthetics, anti-inflammatories, anti-parasitics, antivirals, antifungals, analgesics; and diagnostics; 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 22
Independent Claim
139 words
A method of treating a condition requiring pharmacological treatment which comprises administering to the skin of a patient a liquid drug delivery vehicle 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, anti-infectives, anesthetics, anti-inflammatories, anti-parasitics, antivirals, antifungals, analgesics; and diagnostics; 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 23
Dependent Claim
17 words
A method of treatment according to claim 19 wherein the polymer is one wherein w is 2.
Claim 24
Dependent Claim
14 words
A method of treatment according to claim 20 wherein the polymer is Tetronic® 1307.
Claim 25
Dependent Claim
29 words
A method of treatment according to claim 20 wherein the gel-sol transition temperature of the composition is room temperature or below and said composition is liquid at this temperature.
Claim 26
Dependent Claim
23 words
A method of treatment according to claim 20 wherein the mechanical properties of the skin are restored to a flexible and emollient condition.
Claim 27
Dependent Claim
42 words
A method of treatment according to claim 20 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, the antimicrobial combination of fludalanine/pentizidone and nitrofurazone.
Claim 28
Dependent Claim
25 words
A method of treatment according to claim 25 wherein the β-lactam antibiotics are selected from the group consisting of cefoxitin, n-formamidoyl thienamycin and thienamycin derivatives.
Claim 29
Dependent Claim
24 words
The method of treatment according to claim 20 wherein the anti-infectives are selected from the group consisting of iodine, chloramines, benzalkonium chloride and phenol.
Claim 30
Dependent Claim
33 words
A method of treatment according to claim 20 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 31
Dependent Claim
13 words
A method of treatment of claim 20 wherein the antiparasitic compound is ivermectin.
Claim 32
Dependent Claim
24 words
A method of treatment according to claim 20 wherein the antiviral effective compounds are selected from the group consisting of acyclovir, idoxuridine and interferon.
Claim 33
Dependent Claim
22 words
A method of treatment according to claim 20 wherein the anesthetics are selected from the group consisting of benzocaine, lidocaine and dibucaine.
Claim 34
Dependent Claim
28 words
A method of treatment according to claim 20 wherein the antifungal agent is selected from the group consisting of tolnaftate, undecylenic acid, salicylic acid, zinc undecylenate and thiabendazole.
Claim 35
Dependent Claim
29 words
A method of treatment according to claim 20 wherein the analgesic drug is selected from the group consisting of methylsalicylate, menthol, camphor, methylnicotinate, triethanolamine salicylate, glycol salicylate and salicylamine.
Claim 36
Dependent Claim
40 words
A method of treatment according to claim 20 wherein the diagnostic compound is selected from the group consisting of cholesteryl n-alkyl carbonates, cholesteryl oleyl carbonate, cholesteryl nonanoate or cholesteryl benzoate all in proper proportions to effect a liquid crystal response.
Claim 37
Dependent Claim
27 words
A method of treatment according to claim 20 wherein the composition includes a buffering agent or salt of from 0% to 5% by weight of the composition.
Claim 38
Dependent Claim
35 words
A method of treatment according to claim 35 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 39
Dependent Claim
24 words
A method of treatment according to claim 20 wherein the composition includes from 0.001% to 5% by weight of the composition of a preservative.
Claim 40
Dependent Claim
33 words
A method of treatment according to claim 37 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 41
Dependent Claim
25 words
A method of treatment according to claim 19 wherein the acid or base is selected from the group consisting of hydrochloric acid or sodium hydroxide.
Claim 42
Dependent Claim
136 words
An aqueous pharmaceutical composition for administration to the skin of a patient as a protective covering thereof comprising: a. 10% to 50% by weight to a polyoxamine polymer of the formula ##STR4## wherein w is an integer of from 2 to 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 antibacterial substances, anti-infectives, anesthetics, anti-inflammatories, anti-parasitics, antivirals, antifungals, analgesics; and diagnostics; 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 43
Dependent Claim
136 words
An aqueous pharmaceutical composition for administration to the skin of a patient as a protective covering thereof comprising: a. 10% to 50% by weight to a polyoxamine polymer of the formula ##STR4## wherein w is an integer of from 2 to 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 antibacterial substances, anti-infectives, anesthetics, anti-inflammatories, anti-parasitics, antivirals, antifungals, analgesics; and diagnostics; 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 44
Dependent Claim
14 words
The composition of claim 40 wherein the polymer is one where w is 2.
Claim 45
Dependent Claim
11 words
The composition of claim 40 wherein the polymer is Tetronic® 1307.
Claim 46
Dependent Claim
26 words
The composition of claim 40 wherein the gel-sol transition temperature of the composition is room temperature or below and said composition is liquid at this temperature.
Claim 47
Dependent Claim
22 words
The composition of claim 40 which includes a buffering agent or salt of from 0 to 5% by weight of the composition.
Claim 48
Dependent Claim
32 words
The composition of claim 44 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 49
Dependent Claim
19 words
The composition of claim 40 which includes from 0.001% to 5% by weight of the composition of a preservative.
Claim 50
Dependent Claim
30 words
The composition of claim 46 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 51
Dependent Claim
22 words
The composition of claim 40 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) | 1987-10-02 | 1988-04-02 | 1988-10-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-10-02 | 1992-04-02 | 1992-10-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-10-02 | 1996-04-02 | 1996-10-02 | $7700.00 | Window Closed / Lapsed |