US4459295A
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Method of increasing oral absorption of glycosidic and related antibiotics
Assignee: Interx Research Corp
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Filing: 1982-06-11
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Granted: 1984-07-10
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Expires: 2002-06-11
Abstract
Abstract A method and drug form are provided for increasing the oral absorption of glycosidic and related antibiotics such as macrolide, aminoglycoside, lincomycin and anthracycline antibiotics and related chemical species by the oral administration of said glycosidic and related antibiotics in a suitable pharmaceutically accepted excipient to which has been added a hydroxyaryl or hydroxyaralkyl acid or salt thereof. The hydroxyaryl or hydroxyaralkyl acid or salt thereof is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of glycosidic and related antibiotic.
Inventors
- 👤 Takeru Higuchi
- 👤 Toshiaki Nishihata
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:41
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K45/00; A61K45/06; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K47/14; A61K47/16; A61K47/18; A61K9/00; A61K9/20; A61K9/2004; A61K9/2013; A61K9/48; A61K9/4841; A61K9/4858; A61K9/28; A61K9/2806; A61K9/2833; A61K9/286; A61K9/2866; A61K9/2886; A61K9/4891
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
140 words
A method for enhancing the rate of absorption of an orally administered glycosidic or related antibiotic into the bloodstream, said method comprising the steps of preparing a drug form capable of being orally absorbed, said drug form comprising a therapeutically effective dosage amount of the glycosidic or related antibiotics and an adjuvant of the Formula: ##STR3## wherein R 1 is --CO 2 H, --(CH 2 )--COOH, ##STR4## SO 3 H or a pharmaceutically acceptable salt thereof, wherein R 2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said oral absorption rate and administering said drug form orally to a warm-blooded animal.
Claim 2
Independent Claim
140 words
A method for enhancing the rate of absorption of an orally administered glycosidic or related antibiotic into the bloodstream, said method comprising the steps of preparing a drug form capable of being orally absorbed, said drug form comprising a therapeutically effective dosage amount of the glycosidic or related antibiotics and an adjuvant of the Formula: ##STR3## wherein R 1 is --CO 2 H, --(CH 2 )--COOH, ##STR4## SO 3 H or a pharmaceutically acceptable salt thereof, wherein R 2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said oral absorption rate and administering said drug form orally to a warm-blooded animal.
Claim 3
Dependent Claim
20 words
The method of claim 1 wherein said glycosidic or related antibiotic is a macrolide, an aminoglycoside, lincomycin, clindamycin or anthracycline.
Claim 4
Dependent Claim
10 words
The method of claim 2 wherein said macrolide is erythromycin.
Claim 5
Dependent Claim
10 words
The method of claim 2 wherein said aminoglycoside is gentamycin.
Claim 6
Dependent Claim
29 words
The method of claim 1 wherein said adjuvant comprises Sodium salicylate Sodium-5-methoxysalicylate 3-methylsalicylic acid Sodium-5-chlorosalicylate Sodium-5-bromosalicylate 5-trifluorosalicylic acid 3-t-butyl-5-methylsalicylic acid Sodium-5-t-octylsalicylate Sodium-3,5-diiodosalicylate 5-n-butoxysalicylic acid 5-methylsalicylic acid or 3-t-butyl-6-methylsalicylic acid
Claim 7
Dependent Claim
16 words
The method of claim 1 wherein the adjuvant is salicylic acid, sodium salicylate or sodium 5-methoxysalicylate.
Claim 8
Dependent Claim
104 words
An orally administered drug form comprising a therapeutically effective amount of glycosidic or related antibiotic and an adjuvant comprising a compound of the formula: ##STR5## wherein R 1 is --CO 2 H, --(CH 2 )--COOH, ##STR6## SO 3 H, or a pharmaceutically acceptable salt thereof wherein R 2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in sufficient amount to be effective in enhancing the oral absorption rate of said glycosidic or related antibiotic.
Claim 9
Dependent Claim
104 words
An orally administered drug form comprising a therapeutically effective amount of glycosidic or related antibiotic and an adjuvant comprising a compound of the formula: ##STR5## wherein R 1 is --CO 2 H, --(CH 2 )--COOH, ##STR6## SO 3 H, or a pharmaceutically acceptable salt thereof wherein R 2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in sufficient amount to be effective in enhancing the oral absorption rate of said glycosidic or related antibiotic.
Claim 10
Dependent Claim
19 words
The drug form of claim 7 wherein said glycosidic or related antibiotic is macrolide, aminoglycoside, lincomycin, clindamycin or anthracycline.
Claim 11
Dependent Claim
11 words
The drug form of claim 8 wherein said macrolide is erythromycin.
Claim 12
Dependent Claim
11 words
The drug form of claim 8 wherein said aminoglycoside is gentamicin.
Claim 13
Dependent Claim
30 words
The drug form of claim 7 wherein said adjuvant comprises: Sodium salicylate Sodium-5-methoxysalicylate 3-methylsalicylic acid Sodium-5-chlorosalicylate Sodium-5-bromosalicylate 5-trifluorosalicylic acid 3-t-butyl-5-methylsalicylic acid Sodium-5-t-octylsalicylate Sodium-3,5-diiodosalicylate 5-n-butoxysalicylic acid 5-methylsalicylic acid or 3-t-butyl-6-methylsalicylic acid
Claim 14
Dependent Claim
17 words
The drug form of claim 11 wherein the adjuvant is salicylic acid, sodium salicylate or sodium 5-methoxysalicylate.
References Cited (Backward Citations)
FR2258171A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-07-10 | 1988-01-09 | 1988-07-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-07-10 | 1992-01-09 | 1992-07-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-07-10 | 1996-01-09 | 1996-07-10 | $7700.00 | Window Closed / Lapsed |