OA10517A - Azathioprine compositions for colonic administration - Google Patents

Azathioprine compositions for colonic administration Download PDF

Info

Publication number: OA10517A
Authority: OA; OAPI
Prior art keywords: azathioprine; unit dosage; aza; dosage form; pharmaceutical composition
Prior art date: 1995-03-30

Application number

OA70090A

Other languages

English (en)

Inventor

William J Sandborn

Original Assignee

Mayo Foundation

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1995-03-30

Filing date

1997-09-30

Publication date

2002-04-24

1997-09-30 Application filed by Mayo Foundation filed Critical Mayo Foundation

2002-04-24 Publication of OA10517A publication Critical patent/OA10517A/en

Links

LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 title claims abstract description 65
229960002170 azathioprine Drugs 0.000 title claims abstract description 63
239000000203 mixture Substances 0.000 title claims abstract description 23
230000000112 colonic effect Effects 0.000 title description 2
210000001072 colon Anatomy 0.000 claims abstract description 12
238000000034 method Methods 0.000 claims abstract description 11
208000022559 Inflammatory bowel disease Diseases 0.000 claims abstract 5
239000002552 dosage form Substances 0.000 claims description 12
238000009505 enteric coating Methods 0.000 claims description 9
239000002702 enteric coating Substances 0.000 claims description 9
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 9
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
241000792859 Enema Species 0.000 claims description 5
201000010099 disease Diseases 0.000 claims description 5
239000007920 enema Substances 0.000 claims description 5
229940095399 enema Drugs 0.000 claims description 4
229920002678 cellulose Polymers 0.000 claims description 3
239000007788 liquid Substances 0.000 claims description 3
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims description 2
239000002736 nonionic surfactant Substances 0.000 claims description 2
208000024891 symptom Diseases 0.000 claims description 2
238000011200 topical administration Methods 0.000 claims description 2
239000008194 pharmaceutical composition Substances 0.000 claims 6
SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical compound [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 5
GAMPNQJDUFQVQO-UHFFFAOYSA-N acetic acid;phthalic acid Chemical compound CC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O GAMPNQJDUFQVQO-UHFFFAOYSA-N 0.000 claims 2
239000001913 cellulose Substances 0.000 claims 2
NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims 1
206010009887 colitis Diseases 0.000 claims 1
239000000463 material Substances 0.000 claims 1
229920000609 methyl cellulose Polymers 0.000 claims 1
239000001923 methylcellulose Substances 0.000 claims 1
XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 claims 1
239000002562 thickening agent Substances 0.000 claims 1
238000009472 formulation Methods 0.000 abstract description 13
230000003111 delayed effect Effects 0.000 abstract description 6
150000003839 salts Chemical class 0.000 abstract description 2
GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 description 58
229960001428 mercaptopurine Drugs 0.000 description 29
239000006260 foam Substances 0.000 description 17
238000001990 intravenous administration Methods 0.000 description 10
239000012141 concentrate Substances 0.000 description 7
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
206010053317 Hydrophobia Diseases 0.000 description 6
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 6
229920000642 polymer Polymers 0.000 description 6
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239000003826 tablet Substances 0.000 description 6
210000001035 gastrointestinal tract Anatomy 0.000 description 5
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
201000006704 Ulcerative Colitis Diseases 0.000 description 4
210000004369 blood Anatomy 0.000 description 4
239000008280 blood Substances 0.000 description 4
239000002775 capsule Substances 0.000 description 4
IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 4
LXCFILQKKLGQFO-UHFFFAOYSA-N p-hydroxybenzoic acid methyl ester Natural products COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 4
WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 3
206010009900 Colitis ulcerative Diseases 0.000 description 3
KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 3
229920003134 Eudragit® polymer Polymers 0.000 description 3
108010024636 Glutathione Proteins 0.000 description 3
VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 3
229920002125 Sokalan® Polymers 0.000 description 3
102000004377 Thiopurine S-methyltransferases Human genes 0.000 description 3
108090000958 Thiopurine S-methyltransferases Proteins 0.000 description 3
ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
238000010521 absorption reaction Methods 0.000 description 3
229960001631 carbomer Drugs 0.000 description 3
150000001875 compounds Chemical class 0.000 description 3
VHJLVAABSRFDPM-QWWZWVQMSA-N dithiothreitol Chemical compound SC[C@@H](O)[C@H](O)CS VHJLVAABSRFDPM-QWWZWVQMSA-N 0.000 description 3
229940079593 drug Drugs 0.000 description 3
239000003814 drug Substances 0.000 description 3
239000004088 foaming agent Substances 0.000 description 3
229960003180 glutathione Drugs 0.000 description 3
238000004128 high performance liquid chromatography Methods 0.000 description 3
210000003405 ileum Anatomy 0.000 description 3
210000004698 lymphocyte Anatomy 0.000 description 3
239000006187 pill Substances 0.000 description 3
239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 3
235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 3
229940068968 polysorbate 80 Drugs 0.000 description 3
229920000053 polysorbate 80 Polymers 0.000 description 3
229920002744 polyvinyl acetate phthalate Polymers 0.000 description 3
229940100467 polyvinyl acetate phthalate Drugs 0.000 description 3
231100000419 toxicity Toxicity 0.000 description 3
230000001988 toxicity Effects 0.000 description 3
WLAMNBDJUVNPJU-UHFFFAOYSA-N 2-methylbutyric acid Chemical compound CCC(C)C(O)=O WLAMNBDJUVNPJU-UHFFFAOYSA-N 0.000 description 2
208000011231 Crohn disease Diseases 0.000 description 2
229920003141 Eudragit® S 100 Polymers 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
235000011054 acetic acid Nutrition 0.000 description 2
229960000583 acetic acid Drugs 0.000 description 2
238000004458 analytical method Methods 0.000 description 2
210000004027 cell Anatomy 0.000 description 2
239000003795 chemical substances by application Substances 0.000 description 2
239000012153 distilled water Substances 0.000 description 2
230000000694 effects Effects 0.000 description 2
239000003995 emulsifying agent Substances 0.000 description 2
239000012530 fluid Substances 0.000 description 2
230000002496 gastric effect Effects 0.000 description 2
125000002883 imidazolyl group Chemical group 0.000 description 2
KBOPZPXVLCULAV-UHFFFAOYSA-M mesalaminate(1-) Chemical compound NC1=CC=C(O)C(C([O-])=O)=C1 KBOPZPXVLCULAV-UHFFFAOYSA-M 0.000 description 2
235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
239000004292 methyl p-hydroxybenzoate Substances 0.000 description 2
229960002216 methylparaben Drugs 0.000 description 2
238000012986 modification Methods 0.000 description 2
230000004048 modification Effects 0.000 description 2
210000004877 mucosa Anatomy 0.000 description 2
229910052757 nitrogen Inorganic materials 0.000 description 2
231100000252 nontoxic Toxicity 0.000 description 2
230000003000 nontoxic effect Effects 0.000 description 2
239000007935 oral tablet Substances 0.000 description 2
229940096978 oral tablet Drugs 0.000 description 2
239000002304 perfume Substances 0.000 description 2
239000012071 phase Substances 0.000 description 2
239000000843 powder Substances 0.000 description 2
229940002612 prodrug Drugs 0.000 description 2
239000000651 prodrug Substances 0.000 description 2
235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 2
239000004405 propyl p-hydroxybenzoate Substances 0.000 description 2
229960003415 propylparaben Drugs 0.000 description 2
239000000243 solution Substances 0.000 description 2
239000008347 soybean phospholipid Substances 0.000 description 2
210000002784 stomach Anatomy 0.000 description 2
239000004094 surface-active agent Substances 0.000 description 2
239000000375 suspending agent Substances 0.000 description 2
210000001519 tissue Anatomy 0.000 description 2
230000000699 topical effect Effects 0.000 description 2
239000000230 xanthan gum Substances 0.000 description 2
229920001285 xanthan gum Polymers 0.000 description 2
229940082509 xanthan gum Drugs 0.000 description 2
235000010493 xanthan gum Nutrition 0.000 description 2
IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 1
BVZWTQCTAVYACS-UGLFOIIFSA-N Azaspiracid Chemical compound C[C@H]1C[C@@H](C)CN[C@@]11O[C@@H]2[C@@H](O3)C[C@H](C)C[C@]3(CC(=C)[C@@H]3[C@H](C[C@@H](C)[C@](O)([C@H](O)[C@H]4O[C@@H]5C[C@@H](C)[C@@]6(O[C@]7(O[C@@H](C=CC7)\C=C\CCC(O)=O)CC6)O[C@@H]5C4)O3)C)O[C@@H]2C1 BVZWTQCTAVYACS-UGLFOIIFSA-N 0.000 description 1
229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
WTEVQBCEXWBHNA-UHFFFAOYSA-N Citral Natural products CC(C)=CCCC(C)=CC=O WTEVQBCEXWBHNA-UHFFFAOYSA-N 0.000 description 1
208000030453 Drug-Related Side Effects and Adverse reaction Diseases 0.000 description 1
208000004232 Enteritis Diseases 0.000 description 1
206010058838 Enterocolitis infectious Diseases 0.000 description 1
102000004190 Enzymes Human genes 0.000 description 1
108090000790 Enzymes Proteins 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
206010067482 No adverse event Diseases 0.000 description 1
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
241000906446 Theraps Species 0.000 description 1
206010070863 Toxicity to various agents Diseases 0.000 description 1
238000002835 absorbance Methods 0.000 description 1
150000001252 acrylic acid derivatives Chemical class 0.000 description 1
239000002671 adjuvant Substances 0.000 description 1
XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
229910052782 aluminium Inorganic materials 0.000 description 1
229910000147 aluminium phosphate Inorganic materials 0.000 description 1
235000011114 ammonium hydroxide Nutrition 0.000 description 1
239000007864 aqueous solution Substances 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
238000004820 blood count Methods 0.000 description 1
244000309464 bull Species 0.000 description 1
239000001273 butane Substances 0.000 description 1
235000010980 cellulose Nutrition 0.000 description 1
229940081734 cellulose acetate phthalate Drugs 0.000 description 1
238000006243 chemical reaction Methods 0.000 description 1
208000037976 chronic inflammation Diseases 0.000 description 1
230000006020 chronic inflammation Effects 0.000 description 1
229940043350 citral Drugs 0.000 description 1
239000011248 coating agent Substances 0.000 description 1
238000000576 coating method Methods 0.000 description 1
229920001577 copolymer Polymers 0.000 description 1
239000003246 corticosteroid Substances 0.000 description 1
229960001334 corticosteroids Drugs 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
238000013461 design Methods 0.000 description 1
235000005911 diet Nutrition 0.000 description 1
230000000378 dietary effect Effects 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
239000002270 dispersing agent Substances 0.000 description 1
239000006185 dispersion Substances 0.000 description 1
238000012377 drug delivery Methods 0.000 description 1
229940088679 drug related substance Drugs 0.000 description 1
239000008387 emulsifying waxe Substances 0.000 description 1
229940079360 enema for constipation Drugs 0.000 description 1
230000002255 enzymatic effect Effects 0.000 description 1
230000002550 fecal effect Effects 0.000 description 1
239000007888 film coating Substances 0.000 description 1
238000009501 film coating Methods 0.000 description 1
229940042555 fleet enema Drugs 0.000 description 1
230000009969 flowable effect Effects 0.000 description 1
230000037406 food intake Effects 0.000 description 1
235000011389 fruit/vegetable juice Nutrition 0.000 description 1
210000004051 gastric juice Anatomy 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
239000007903 gelatin capsule Substances 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
WTEVQBCEXWBHNA-JXMROGBWSA-N geranial Chemical compound CC(C)=CCC\C(C)=C\C=O WTEVQBCEXWBHNA-JXMROGBWSA-N 0.000 description 1
229940116364 hard fat Drugs 0.000 description 1
230000007062 hydrolysis Effects 0.000 description 1
238000006460 hydrolysis reaction Methods 0.000 description 1
229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 1
239000005457 ice water Substances 0.000 description 1
230000002519 immonomodulatory effect Effects 0.000 description 1
230000001506 immunosuppresive effect Effects 0.000 description 1
229940073062 imuran Drugs 0.000 description 1
230000001939 inductive effect Effects 0.000 description 1
208000027139 infectious colitis Diseases 0.000 description 1
208000015181 infectious disease Diseases 0.000 description 1
230000002458 infectious effect Effects 0.000 description 1
238000001802 infusion Methods 0.000 description 1
230000000977 initiatory effect Effects 0.000 description 1
238000002347 injection Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
210000004347 intestinal mucosa Anatomy 0.000 description 1
239000000787 lecithin Substances 0.000 description 1
235000010445 lecithin Nutrition 0.000 description 1
229940067606 lecithin Drugs 0.000 description 1
201000002364 leukopenia Diseases 0.000 description 1
231100001022 leukopenia Toxicity 0.000 description 1
230000007774 longterm Effects 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
238000010197 meta-analysis Methods 0.000 description 1
230000004060 metabolic process Effects 0.000 description 1
229940117841 methacrylic acid copolymer Drugs 0.000 description 1
229920003145 methacrylic acid copolymer Polymers 0.000 description 1
239000011859 microparticle Substances 0.000 description 1
239000004570 mortar (masonry) Substances 0.000 description 1
210000004400 mucous membrane Anatomy 0.000 description 1
238000002414 normal-phase solid-phase extraction Methods 0.000 description 1
YTJSFYQNRXLOIC-UHFFFAOYSA-N octadecylsilane Chemical compound CCCCCCCCCCCCCCCCCC[SiH3] YTJSFYQNRXLOIC-UHFFFAOYSA-N 0.000 description 1
239000002245 particle Substances 0.000 description 1
230000008506 pathogenesis Effects 0.000 description 1
229940023488 pill Drugs 0.000 description 1
229920003023 plastic Polymers 0.000 description 1
239000004033 plastic Substances 0.000 description 1
238000010149 post-hoc-test Methods 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
206010036784 proctocolitis Diseases 0.000 description 1
239000001294 propane Substances 0.000 description 1
239000003380 propellant Substances 0.000 description 1
239000008213 purified water Substances 0.000 description 1
238000011160 research Methods 0.000 description 1
QEVHRUUCFGRFIF-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C(C5=CC=C(OC)C=C5N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 QEVHRUUCFGRFIF-MDEJGZGSSA-N 0.000 description 1
230000000717 retained effect Effects 0.000 description 1
238000012216 screening Methods 0.000 description 1
239000002002 slurry Substances 0.000 description 1
210000000813 small intestine Anatomy 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
239000007909 solid dosage form Substances 0.000 description 1
239000007892 solid unit dosage form Substances 0.000 description 1
238000001228 spectrum Methods 0.000 description 1
230000009885 systemic effect Effects 0.000 description 1
231100000057 systemic toxicity Toxicity 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
230000007723 transport mechanism Effects 0.000 description 1
238000002562 urinalysis Methods 0.000 description 1
239000003643 water by type Substances 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4891—Coated capsules; Multilayered drug free capsule shells
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0031—Rectum, anus
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
- A61K9/122—Foams; Dry foams
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Epidemiology (AREA)
Dispersion Chemistry (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

OA70090A 1995-03-30 1997-09-30 Azathioprine compositions for colonic administration OA10517A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US08/413,505 US5691343A (en)	1995-03-30	1995-03-30	Use of topical azathioprine to treat inflammatory bowel disorders

Publications (1)

Publication Number	Publication Date
OA10517A true OA10517A (en)	2002-04-24

Family

ID=23637470

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA70090A OA10517A (en)	1995-03-30	1997-09-30	Azathioprine compositions for colonic administration

Country Status (18)

Country	Link
US (2)	US5691343A (ja)
EP (1)	EP0817634A1 (ja)
JP (1)	JPH11502842A (ja)
KR (1)	KR19980703423A (ja)
AP (1)	AP727A (ja)
AU (1)	AU707168B2 (ja)
BR (1)	BR9607964A (ja)
CA (1)	CA2216728A1 (ja)
CZ (1)	CZ290428B6 (ja)
EA (1)	EA199700282A1 (ja)
HU (1)	HUP9801241A3 (ja)
IS (1)	IS4561A (ja)
NO (2)	NO311491B1 (ja)
NZ (1)	NZ306062A (ja)
OA (1)	OA10517A (ja)
PL (1)	PL322526A1 (ja)
TR (1)	TR199701079T1 (ja)
WO (1)	WO1996030021A1 (ja)

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US7048906B2 (en)	1995-05-17	2006-05-23	Cedars-Sinai Medical Center	Methods of diagnosing and treating small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions
ES2224428T3 (es)	1997-09-26	2005-03-01	Celltech Pharma Europe Limited	Composicion farmnaceutica para el tratamiento de la enfermedad inflmatoria intestinal.
US6355623B2 (en)	1998-09-24	2002-03-12	Hopital-Sainte-Justine	Method of treating IBD/Crohn's disease and related conditions wherein drug metabolite levels in host blood cells determine subsequent dosage
US7323471B1 (en)	1999-08-13	2008-01-29	Dor Biopharma, Inc.	Topical azathioprine for the treatment of oral autoimmune diseases
US6689788B1 (en) *	2000-08-25	2004-02-10	University Of Florida	Method and composition for treatment of inflammatory bowel disease
US6946258B2 (en)	2002-03-04	2005-09-20	Biologix Diagnostics, Llc	Rapid, immunochemical process for measuring thiopurine methyltransferase
IL152127A0 (en) *	2002-10-06	2003-05-29	Bio Balance Corp	Probiotic compositions for the treatment of inflammatory bowel disease
US7067460B2 (en)	2002-11-14	2006-06-27	Baker Hughes Incorporated	Organofunctional compounds for shale stabilization of the aqueous dispersed phase of non-aqueous based invert emulsion drilling system fluids
CA2560654A1 (en) *	2004-04-01	2006-09-20	Teva Pharmaceutical Industries Ltd.	Imroved formulations of 6-mercaptopurine
US8188067B2 (en)	2004-04-01	2012-05-29	Teva Pharmaceutical Industries Ltd.	Formulations of 6-mercaptopurine
US7923014B2 (en) *	2007-02-12	2011-04-12	The Board Of Regents Of The University Of Texas System	Expression and purification of HIP/PAP and uses therefor
US7919251B2 (en) *	2007-10-12	2011-04-05	Guy's And St. Thomas' Nhs Foundation Trust	Non-thiopurine methyltransferase related effects in 6-mercaptopurine therapy
EP2110130A1 (en) *	2008-04-18	2009-10-21	Teva Pharmaceutical Industries Ltd.	Pharmaceutical use of 6-mercaptopurine
CA3038602C (en)	2015-09-29	2023-12-05	ProdrugXtend Pty Ltd	Extended-release formulations comprising 6-thioguanine
US20170105996A1 (en)	2015-10-16	2017-04-20	Teva Pharmaceutical Industries, Ltd.	Treatment of non-alcoholic fatty liver disease or non-alcoholic steatohepatitis with delayed-release 6-mercaptopurine

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JPS6272618A (ja) *	1985-09-27	1987-04-03	Kanji Takada	アザチオプリン製剤
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1995
- 1995-03-30 US US08/413,505 patent/US5691343A/en not_active Expired - Fee Related
1996
- 1996-03-12 TR TR97/01079T patent/TR199701079T1/xx unknown
- 1996-03-12 CZ CZ19973092A patent/CZ290428B6/cs not_active IP Right Cessation
- 1996-03-12 AP APAP/P/1997/001098A patent/AP727A/en active
- 1996-03-12 BR BR9607964-9A patent/BR9607964A/pt not_active Application Discontinuation
- 1996-03-12 HU HU9801241A patent/HUP9801241A3/hu unknown
- 1996-03-12 NZ NZ306062A patent/NZ306062A/xx unknown
- 1996-03-12 JP JP8529440A patent/JPH11502842A/ja active Pending
- 1996-03-12 WO PCT/US1996/003383 patent/WO1996030021A1/en not_active Ceased
- 1996-03-12 AU AU54218/96A patent/AU707168B2/en not_active Ceased
- 1996-03-12 CA CA002216728A patent/CA2216728A1/en not_active Abandoned
- 1996-03-12 PL PL96322526A patent/PL322526A1/xx unknown
- 1996-03-12 KR KR1019970706827A patent/KR19980703423A/ko not_active Ceased
- 1996-03-12 EA EA199700282A patent/EA199700282A1/ru unknown
- 1996-03-12 EP EP96911292A patent/EP0817634A1/en not_active Withdrawn
1997
- 1997-08-01 US US08/905,490 patent/US5905081A/en not_active Expired - Fee Related
- 1997-09-18 IS IS4561A patent/IS4561A/is unknown
- 1997-09-25 NO NO19974440A patent/NO311491B1/no not_active IP Right Cessation
- 1997-09-30 OA OA70090A patent/OA10517A/en unknown
2001
- 2001-06-13 NO NO20012930A patent/NO20012930D0/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
AU707168B2 (en)	1999-07-01
HUP9801241A3 (en)	2000-06-28
CA2216728A1 (en)	1996-10-03
NO311491B1 (no)	2001-12-03
NZ306062A (en)	1998-10-28
US5691343A (en)	1997-11-25
EA199700282A1 (ru)	1998-04-30
IS4561A (is)	1997-09-18
NO974440D0 (no)	1997-09-25
MX9707391A (es)	1997-11-29
EP0817634A1 (en)	1998-01-14
AP727A (en)	1999-01-29
KR19980703423A (ko)	1998-11-05
JPH11502842A (ja)	1999-03-09
CZ309297A3 (cs)	1998-03-18
NO20012930L (no)	1997-09-25
AU5421896A (en)	1996-10-16
HUP9801241A2 (hu)	1998-09-28
BR9607964A (pt)	1999-11-30
US5905081A (en)	1999-05-18
CZ290428B6 (cs)	2002-07-17
NO20012930D0 (no)	2001-06-13
AP9701098A0 (en)	1997-10-31
TR199701079T1 (xx)	1998-01-21
NO974440L (no)	1997-09-25
WO1996030021A1 (en)	1996-10-03
PL322526A1 (en)	1998-02-02

Publication	Publication Date	Title
US5905081A (en)	1999-05-18	Topical formulations of azathioprine to treat inflammatory bowel disorders
AU718971C (en)	2008-01-31	Colonic delivery of nicotine to treat inflammatory bowel disease
US6306434B1 (en)	2001-10-23	Pharmaceutical composition comprising cyclosporin solid-state microemulsion
Takaya et al.	1998	Importance of dissolution process on systemic availability of drugs delivered by colon delivery system
AU679852B2 (en)	1997-07-10	Stabilized composition for oral administration of peptides
AU2006233567A1 (en)	2006-10-19	Therapeutic combination in case of benign prostate hyperplasia
RS57881B1 (sr)	2019-01-31	Formulacija solubilizovane kapsule 1,1-dimetiletil [(1s)-1-{[(2s,4r)-4-(7-hloro-4metoksiizohinolin-1-iloksi)-2-({(1r,2s)-1-[(ciklopropilsulfonil)karbamoil]-2-etenilciklopropil}karbamoil)pirolidin-1-il]karbonil}-2,2-dimetilpropil]karbamata
US6166024A (en)	2000-12-26	Use of topical azathioprine and thioguanine to treat colorectal adenomas
JPH0451528B2 (ja)	1992-08-19
CA2290973C (en)	2003-06-17	Encapsulated solution dosage forms of sertraline
MXPA97007391A (es)	1998-07-03	Composiciones de azatioprina para administracion colonica
CN1179719A (zh)	1998-04-22	用于结肠给药的硫唑嘌呤组合物
Luong et al.	0	Formulation and in vivo study of capsules containing lansoprazole enteric-coated pellets
HK1019043B (en)	2003-08-01	Colonic delivery of nicotine to treat inflammatory bowel disease
MXPA98009708A (en)	1999-09-01	Stabilized composition for the oral administration of pepti
MXPA99012099A (en)	2000-09-04	Gelatine encapsulated solution dosage forms of sertraline