Patent US4425337A successfully refreshed from Google Patents.
US4425337A
Expired / Lapsed
US
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Adjuvants for rectal delivery of drug
Assignee: Merck and Co Inc
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Filing: 1981-12-30
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Granted: 1984-01-10
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Expires: 2001-12-30
Abstract
Abstract A method and drug form enhancing the rate of absorption of a rectally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps of preparing a drug form capable of being rectally administered. The drug form comprises a therapeutically effective unit dosage amount of a selected drug of the type which is capable of being absorbed into the blood stream from the rectal compartment and phenothiazines or salts thereof being present in the drug form in a sufficient amount to be effective in enhancing the drug absorption rate, when rectally administering the drug form to warm blooded animals.
Inventors
- 👤 Jose Alexander
- 👤 Joseph A. Fix
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 06:24
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/22; A61K31/00; A61K31/33; A61K31/395; A61K31/54; A61K9/00; A61K9/02
Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
170 words
A method for enhancing the rate of absorption of a rectally administered drug from a rectal compartment into the blood stream, said method comprising the steps of preparing a drug form capable of being rectally administered, said drug form comprising a therapeutically effective dosage amount of a β-lactam antibiotic capable of being absorbed into the blood stream from the rectal compartment, and a phenothiazine of the formula: ##STR2## and the pharmaceutically acceptable acid addition salts thereof, wherein: X is hydrogen, alkyl, halo, trihaloalkyl, thioalkyl, alkylsulfoxide or ketoalkyl; and R is dialkylaminoalkyl, N-alkylpiperazinoalkyl, N-alkylpiperazinoalkyl or N-alkylpiperidinoalkyl wherein additionally the piperazino group can be substituted with hydroxyalkyl thereof as adjuvant, said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said absorption rate and said adjuvant being present in the drug form at from 10-500 mg in each unit dose and being present in a ratio of 5% to 50% of adjuvant to adjuvant plus drug, and administering said drug form into said rectal compartment.
Claim 2
Independent Claim
170 words
A method for enhancing the rate of absorption of a rectally administered drug from a rectal compartment into the blood stream, said method comprising the steps of preparing a drug form capable of being rectally administered, said drug form comprising a therapeutically effective dosage amount of a β-lactam antibiotic capable of being absorbed into the blood stream from the rectal compartment, and a phenothiazine of the formula: ##STR2## and the pharmaceutically acceptable acid addition salts thereof, wherein: X is hydrogen, alkyl, halo, trihaloalkyl, thioalkyl, alkylsulfoxide or ketoalkyl; and R is dialkylaminoalkyl, N-alkylpiperazinoalkyl, N-alkylpiperazinoalkyl or N-alkylpiperidinoalkyl wherein additionally the piperazino group can be substituted with hydroxyalkyl thereof as adjuvant, said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said absorption rate and said adjuvant being present in the drug form at from 10-500 mg in each unit dose and being present in a ratio of 5% to 50% of adjuvant to adjuvant plus drug, and administering said drug form into said rectal compartment.
Claim 3
Dependent Claim
15 words
The method of claim 1 wherein said β-lactam antibiotic comprises cefoxitin, cefmetzole, cephamandole or amoxicillin.
Claim 4
Dependent Claim
10 words
The method of claim 1 wherein said drug comprises cefoxitin.
Claim 5
Dependent Claim
35 words
The method of claim 1 wherein said adjuvant comprises: ______________________________________
chlorpromazine mesoridazine
perphenazine piperacetazine
thioridazine acetophenazine
triflupromazine butoperazine
fluphenazine carphenazine
promazine methophenazine
trifluoperazine propionazine
prochlorperazine thiopropazate
______________________________________ or a pharmaceutically acceptable acid addition salt thereof.
References Cited (Backward Citations)
US3689646A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-01-09 | 1987-07-11 | 1988-01-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-01-09 | 1991-07-11 | 1992-01-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-01-09 | 1995-07-11 | 1996-01-10 | $7700.00 | Window Closed / Lapsed |