A rectally administered suppository comprising a drug and an adjuvant

Claim 2

A rectally administered drug form comprising a therapeutically effective dosage amount of a drug capable of being absorbed into the blood stream from a rectal compartment and an adjuvant of hydroxy aryl or hydroxy aralkyl acids or salts, amides or esters thereof, said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing the absorption rate of said drug from from said rectal compartment into the bloodstream.

Claim 3

The drug form of Claim 1 wherein said drug comprises xanthines, anticancer agents, antibiotics, polypeptides, antiarrythmics, other cardiovascular agents, antidiabetics, antiulcers, antigungals, antinauseants, sedatives, diuretics, antihypertensives, and drugs for treatment of Parkinson's disease.

Claim 4

The drug form of Claim 1 wherein said drug comprises chloramphenicol, penicillin, or cephalosporin.

Claim 5

The drug form of Claim 1 wherein said drug comprises quinidine, lidocaine, theophylline, L-dopa, cefmetazole, insulin, cefoxitin, heparin, phenol red, pencillin G, or gentamycin.

Claim 6

The drug form of Claim 1 wherein said drug comprises amiloride, hydrochlorothiazide, moduretic, carbidopa, levodopa, cefoxitin, cefmetzole, cyclobenzaprine, diflunisal, indomethacin, methyldopa, sulindac, timolol, (-)-l-(cyclopropylmethyl) 4-[3-(trifluoro- methylthio)5H-dibenzo(a,d)cyclohepten-5-ylidene]-piperidine hydrochloride, N-[(S)-l-(ethoxycarbonyl)-3-phenylpropyl]-L-alanyl-L-proline maleate, (+)10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine oxalate, 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline-carboxylic acid, 3-fluoro-D-alanine and D-4-(1-methyl-3-oxo- l-butenylamino)-3-isoxazolidinone sodium salt hemihydrate, L-N-(2-oxopiperidin-6- ylcarbonyl)-histidyl-L-thiazolidine-4-carboxamide, N-formimidoyl thienamycin monohydrate, (6,7-dichloro-2-methyl-2-phenyl-l-oxo-5-indanyloxy)acetic acid, ibuprofen, naproxen, 5-(4-chlorobenzoyl)-1,4-dimethyl-lH-hyrrole-2-acetic acid, phenylbutazone, dexamethasone, prednisolone, clonidine, propranolol, diazepam, chlorodiazeproxide, furosemide, cephamandole, nalidixic acid, amoxicillin, haloperidol, and captopril.

Claim 7

The drug form of any one of Claims . 1 to 5 wherein said adjuvant comprises wherein R 1 is a radical selected from -C0 2 H, -(CH2)n-COOH, -CH = CH-CO 2H , -SO 3 H, -CH 2 SO 3 H, X(CH 2 ) n CO 2 H, SO 2 NHR 4 , PO(OH)N(OH) 2 , PO(OH)OR 4 , or a pharmaceutically acceptable salt thereof wherein R 2 is a radical selected from OH, H, a lower alkoxy radical having 1-10 carbon atoms, a lower alkyl radical having 1-10 carbon atoms, a lower akenyl radical having 2-5 carbon atoms, a lower alkanoyl radical having 1-5 carbon atoms, a lower alkanoyloxy radical having 1-5 carbon atoms, a carboxy radical, a carbo-lower alkoxy radical having 1-5 carbon atoms, a halo radical, a mono-, di-, or tri-halo lower alkyl radical having 1-5 carbon atoms, an amino radical, a mono- or di-lower alkyl amino radical having 1-5 carbon atoms, a carbamyl radical, a lower mono- or di-alkyl carbamyl radical wherein the alkyl group has 1-5 carbon atoms, a thio radical, a lower alkyl thio radical wherein the aklyl group has 1-5 carbon atoms, a cyano radical, a lower alkyl sulfone radical wherein the alkyl group has 1-5 carbon atoms, a lower alkyl sulfoxide radical wherein the alkyl group has 1-5 carbon atoms, a nitro radical, N(CN Z ) 2 , C(CN) 3 , an alkynyl radical having 2-6 carbon atoms, a cycloaklyl radical having 3-10 carbon atoms, a cycloalkenyl radical having 3-10 carbon atoms, an aryl radical, a hetroaryl radical including thiophenyl and imadazoalyl, or a heterocycloalkyl radical, wherein R 3 is a straight or branched alkyl radical having 1-6 carbon atoms or a hydroxy radical, wherein R 4 is H or a lower alkyl radical having 1-5 carbon atoms, wherein X is 0 or S, wherein n is an integer of 0-5, wherein y is 1 or 2, and when y is 2, both the R 2 radicals, taken together, can form a ring containing O, N or S.

Claim 8

The drug form of any one of Claims 1 to 5 wherein said adjuvant comprises wherein R 1 is a radical selected from -C0 2 H, -(CH 2 ) -COOH, -CH=CH-CO 2 H, -SO 3 H, -CH 2 SO 3 H, O(CH 2 ) CO 2 H or a pharmaceutically acceptable salt thereof wherein R 2 is selected from OH, H, a lower alkoxy radical having 1-10 carbon atoms, a lower alkyl radical having 1-10 carbon atoms, a halo radical, a mono-, di-, or tri- halo lower alkyl radical wherein the alkyl group has 1-5 carbon atoms, a lower alkyl thio radical wherein the alkyl radical has 1-5 carbon atoms, a cyloalkyl radical having 3-10 carbon atoms, or a cycloalkenyl radical having 3-10 carbon atoms and wherein y is an integer of 1 or 2.

Claim 9

The drug form of any one of Claims 1 to 5 wherein said adjuvant comprises wherein R 1 is C0 2 H, (CH 2 )COOH, S0 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.

Claim 10

The drug form of any one of Claims 1 to 5 wherein said adjuvant is 5-methoxysalicylic acid, salicylic acid, homovanillic acid; 2,5-dihydroxybenzoic acid; 2,4-dihydroxybenzoic acid; 3,4-dihydroxymandelic acid; 3-methoxy-4-hydroxy-cinnamic acid; 5-methoxy-2-hydroxyphenylsulfonic acid; 3-methylsalicylic acid; ; 5-methylsalicylic acid; S-tert-octylsalicylic acid; 3-tert-butyl-6-methylsalicylic acid; 3,5-diisopropylsalicylic acid; 3-tert-butyl-5-methylsalicylic acid; guaicolsulfonic acid; 5-bromosalicylic acid; 3,5-dibroamosalicylic acid; 5-iodosalicylic acid; 3,5-diiodosalicylic acid; 3,5-diiodosalicylic acid; 2-hydroxyphenylacetic acid; 3-hydroxy-2-naphthoic acid; mandelic acid; phenyllactic acid; 2-hydroxyphenylmethanesulfonic acid; 5-trifluoro-methyl-2-hydroxybenzoic acid; 4-hydroxy-3-hydroxyphenylmethanesulfonic acid; 3-methoxy-salicylic acid; 5-octyloxysalicylic acid; 5-butoxy-salicylic acid; p-hydroxyphenoxyacetic acid; 3,4-dihydroxyphenylacetic acid; 5-chlorosalicylic acid; 3,4 dihydroxycinnamic acid; 3,5-dihydroxybenzoic acid; 2-hydroxy-3-methoxybenzoic acid; 1-hydroxy-2-naphthoic acid; salicyluric acid; or the sodium salts thereof.

Claim 11

The drug form of any one of Claims 1 to 9 wherein said drug form is a suppository, especially comprising a soft elastic gelatin capsule containing said drug and said adjuvant.