CN115209910A - 口服药物组合物 - Google Patents
口服药物组合物 Download PDFInfo
- Publication number
- CN115209910A CN115209910A CN202180017925.5A CN202180017925A CN115209910A CN 115209910 A CN115209910 A CN 115209910A CN 202180017925 A CN202180017925 A CN 202180017925A CN 115209910 A CN115209910 A CN 115209910A
- Authority
- CN
- China
- Prior art keywords
- compound
- pharmaceutical composition
- oral pharmaceutical
- acid
- cellulose
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 239000008203 oral pharmaceutical composition Substances 0.000 title claims abstract description 85
- 229940126062 Compound A Drugs 0.000 claims abstract description 117
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims abstract description 117
- 239000003814 drug Substances 0.000 claims abstract description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 11
- 201000010099 disease Diseases 0.000 claims abstract description 9
- 102000048260 kappa Opioid Receptors Human genes 0.000 claims abstract description 7
- 108020001588 κ-opioid receptors Proteins 0.000 claims abstract description 7
- 150000001875 compounds Chemical class 0.000 claims description 111
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 68
- 150000003839 salts Chemical class 0.000 claims description 59
- 238000010521 absorption reaction Methods 0.000 claims description 56
- 239000002775 capsule Substances 0.000 claims description 55
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims description 48
- 239000003623 enhancer Substances 0.000 claims description 42
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 42
- 239000002202 Polyethylene glycol Substances 0.000 claims description 40
- 229920001223 polyethylene glycol Polymers 0.000 claims description 40
- 125000005456 glyceride group Chemical group 0.000 claims description 38
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical class C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 34
- 235000019359 magnesium stearate Nutrition 0.000 claims description 34
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 32
- 239000000945 filler Substances 0.000 claims description 31
- 239000004094 surface-active agent Substances 0.000 claims description 31
- FUJLYHJROOYKRA-QGZVFWFLSA-N O-lauroyl-L-carnitine Chemical compound CCCCCCCCCCCC(=O)O[C@H](CC([O-])=O)C[N+](C)(C)C FUJLYHJROOYKRA-QGZVFWFLSA-N 0.000 claims description 30
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 30
- 239000005414 inactive ingredient Substances 0.000 claims description 29
- 239000000314 lubricant Substances 0.000 claims description 29
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 27
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 25
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 25
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 25
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 25
- 229940069328 povidone Drugs 0.000 claims description 25
- GCVGCXMTCJMBHY-UHFFFAOYSA-N 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoic acid Chemical compound OC(=O)CCCNC(=O)C1=CC=C(Cl)C=C1O GCVGCXMTCJMBHY-UHFFFAOYSA-N 0.000 claims description 23
- FIWQZURFGYXCEO-UHFFFAOYSA-M sodium;decanoate Chemical compound [Na+].CCCCCCCCCC([O-])=O FIWQZURFGYXCEO-UHFFFAOYSA-M 0.000 claims description 23
- 229920002678 cellulose Chemical class 0.000 claims description 20
- 239000001913 cellulose Chemical class 0.000 claims description 20
- 235000010980 cellulose Nutrition 0.000 claims description 20
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 20
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 20
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 20
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 20
- BHIZVZJETFVJMJ-UHFFFAOYSA-N 2-hydroxypropyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OCC(C)O BHIZVZJETFVJMJ-UHFFFAOYSA-N 0.000 claims description 18
- 239000011230 binding agent Substances 0.000 claims description 18
- 239000007884 disintegrant Substances 0.000 claims description 18
- 229940026235 propylene glycol monolaurate Drugs 0.000 claims description 18
- 208000002193 Pain Diseases 0.000 claims description 17
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
- 125000003816 2-hydroxybenzoyl group Chemical group OC1=C(C(=O)*)C=CC=C1 0.000 claims description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 15
- 239000008213 purified water Substances 0.000 claims description 14
- GHBFNMLVSPCDGN-UHFFFAOYSA-N rac-1-monooctanoylglycerol Chemical compound CCCCCCCC(=O)OCC(O)CO GHBFNMLVSPCDGN-UHFFFAOYSA-N 0.000 claims description 14
- RCEAADKTGXTDOA-UHFFFAOYSA-N OS(O)(=O)=O.CCCCCCCCCCCC[Na] Chemical compound OS(O)(=O)=O.CCCCCCCCCCCC[Na] RCEAADKTGXTDOA-UHFFFAOYSA-N 0.000 claims description 13
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 13
- IYFATESGLOUGBX-YVNJGZBMSA-N Sorbitan monopalmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O IYFATESGLOUGBX-YVNJGZBMSA-N 0.000 claims description 13
- 150000003904 phospholipids Chemical class 0.000 claims description 13
- 229960000502 poloxamer Drugs 0.000 claims description 13
- 229920001983 poloxamer Polymers 0.000 claims description 13
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 13
- 229920000053 polysorbate 80 Polymers 0.000 claims description 13
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 12
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 12
- 239000011734 sodium Substances 0.000 claims description 12
- 229910052708 sodium Inorganic materials 0.000 claims description 12
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 11
- FBUKVWPVBMHYJY-UHFFFAOYSA-N nonanoic acid Chemical compound CCCCCCCCC(O)=O FBUKVWPVBMHYJY-UHFFFAOYSA-N 0.000 claims description 11
- 229960002446 octanoic acid Drugs 0.000 claims description 11
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 10
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 10
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 claims description 10
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 10
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 10
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 10
- 229930195725 Mannitol Natural products 0.000 claims description 10
- 229920000881 Modified starch Polymers 0.000 claims description 10
- XAAHAAMILDNBPS-UHFFFAOYSA-L calcium hydrogenphosphate dihydrate Chemical compound O.O.[Ca+2].OP([O-])([O-])=O XAAHAAMILDNBPS-UHFFFAOYSA-L 0.000 claims description 10
- 229920001531 copovidone Chemical class 0.000 claims description 10
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 10
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 10
- 239000008101 lactose Substances 0.000 claims description 10
- 239000000594 mannitol Substances 0.000 claims description 10
- 235000010355 mannitol Nutrition 0.000 claims description 10
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims description 9
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 9
- 229920002472 Starch Polymers 0.000 claims description 9
- 235000021355 Stearic acid Nutrition 0.000 claims description 9
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 9
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 9
- 229960000913 crospovidone Drugs 0.000 claims description 9
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 9
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 9
- 229940049654 glyceryl behenate Drugs 0.000 claims description 9
- 230000002209 hydrophobic effect Effects 0.000 claims description 9
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 9
- 229940057948 magnesium stearate Drugs 0.000 claims description 9
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 9
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 9
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 9
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 9
- 229940083542 sodium Drugs 0.000 claims description 9
- 235000015424 sodium Nutrition 0.000 claims description 9
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 9
- 239000008107 starch Substances 0.000 claims description 9
- 235000019698 starch Nutrition 0.000 claims description 9
- 239000008117 stearic acid Substances 0.000 claims description 9
- 229960004274 stearic acid Drugs 0.000 claims description 9
- 239000000853 adhesive Substances 0.000 claims description 8
- 230000001070 adhesive effect Effects 0.000 claims description 8
- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 claims description 7
- 229940087068 glyceryl caprylate Drugs 0.000 claims description 7
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 claims description 7
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 6
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 6
- 229960004543 anhydrous citric acid Drugs 0.000 claims description 6
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 6
- 229960004106 citric acid Drugs 0.000 claims description 6
- 239000001530 fumaric acid Substances 0.000 claims description 6
- 239000001509 sodium citrate Substances 0.000 claims description 6
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims description 6
- 239000011975 tartaric acid Substances 0.000 claims description 6
- 235000002906 tartaric acid Nutrition 0.000 claims description 6
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 6
- 229960003511 macrogol Drugs 0.000 claims description 5
- 238000002156 mixing Methods 0.000 claims description 5
- 208000000003 Breakthrough pain Diseases 0.000 claims description 4
- 239000004359 castor oil Substances 0.000 claims description 4
- 235000019438 castor oil Nutrition 0.000 claims description 4
- 239000003240 coconut oil Substances 0.000 claims description 4
- 235000019864 coconut oil Nutrition 0.000 claims description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 4
- 239000004006 olive oil Substances 0.000 claims description 4
- 235000008390 olive oil Nutrition 0.000 claims description 4
- BYKRNSHANADUFY-UHFFFAOYSA-M sodium octanoate Chemical compound [Na+].CCCCCCCC([O-])=O BYKRNSHANADUFY-UHFFFAOYSA-M 0.000 claims description 4
- 208000003251 Pruritus Diseases 0.000 claims description 3
- 238000001035 drying Methods 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 238000010298 pulverizing process Methods 0.000 claims description 3
- 229960005480 sodium caprylate Drugs 0.000 claims description 3
- 206010011224 Cough Diseases 0.000 claims description 2
- 208000005171 Dysmenorrhea Diseases 0.000 claims description 2
- 206010013935 Dysmenorrhoea Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 206010015958 Eye pain Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 208000019025 Hypokalemia Diseases 0.000 claims description 2
- 206010021036 Hyponatraemia Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 208000000913 Kidney Calculi Diseases 0.000 claims description 2
- 206010029148 Nephrolithiasis Diseases 0.000 claims description 2
- 208000001294 Nociceptive Pain Diseases 0.000 claims description 2
- 206010030113 Oedema Diseases 0.000 claims description 2
- 208000005141 Otitis Diseases 0.000 claims description 2
- 208000004550 Postoperative Pain Diseases 0.000 claims description 2
- 206010046823 Uterine spasm Diseases 0.000 claims description 2
- 230000002917 arthritic effect Effects 0.000 claims description 2
- 159000000007 calcium salts Chemical class 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 201000006549 dyspepsia Diseases 0.000 claims description 2
- 208000019258 ear infection Diseases 0.000 claims description 2
- 208000008384 ileus Diseases 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 208000004296 neuralgia Diseases 0.000 claims description 2
- 208000021722 neuropathic pain Diseases 0.000 claims description 2
- 208000024896 potassium deficiency disease Diseases 0.000 claims description 2
- 208000009935 visceral pain Diseases 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 5
- 239000003002 pH adjusting agent Substances 0.000 claims 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 1
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract description 23
- 238000000034 method Methods 0.000 abstract description 10
- -1 amide compound Chemical class 0.000 abstract description 9
- 238000002360 preparation method Methods 0.000 abstract description 8
- 239000000203 mixture Substances 0.000 description 40
- 238000009472 formulation Methods 0.000 description 38
- UQFYDAAKCZKDHS-UHFFFAOYSA-M sodium;4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate Chemical compound [Na+].OC1=CC(Cl)=CC=C1C(=O)NCCCC([O-])=O UQFYDAAKCZKDHS-UHFFFAOYSA-M 0.000 description 20
- 229920001184 polypeptide Polymers 0.000 description 18
- 102000004196 processed proteins & peptides Human genes 0.000 description 18
- PDBBUDRTWRVCFN-UNTBIKODSA-N [(2R)-3-carboxy-2-dodecanoyloxypropyl]-trimethylazanium chloride Chemical compound [Cl-].CCCCCCCCCCCC(=O)O[C@H](CC(O)=O)C[N+](C)(C)C PDBBUDRTWRVCFN-UNTBIKODSA-N 0.000 description 16
- 239000008280 blood Substances 0.000 description 15
- 210000004369 blood Anatomy 0.000 description 15
- 241000282472 Canis lupus familiaris Species 0.000 description 14
- 230000000694 effects Effects 0.000 description 13
- 230000036470 plasma concentration Effects 0.000 description 13
- 239000000243 solution Substances 0.000 description 13
- 229940079593 drug Drugs 0.000 description 11
- 238000001990 intravenous administration Methods 0.000 description 9
- UOENJXXSKABLJL-UHFFFAOYSA-M sodium;8-[(2-hydroxybenzoyl)amino]octanoate Chemical compound [Na+].OC1=CC=CC=C1C(=O)NCCCCCCCC([O-])=O UOENJXXSKABLJL-UHFFFAOYSA-M 0.000 description 9
- 230000002496 gastric effect Effects 0.000 description 7
- 239000003826 tablet Substances 0.000 description 7
- 229920000151 polyglycol Polymers 0.000 description 6
- 239000010695 polyglycol Substances 0.000 description 6
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 description 5
- OBETXYAYXDNJHR-UHFFFAOYSA-N alpha-ethylcaproic acid Natural products CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 description 4
- 235000014113 dietary fatty acids Nutrition 0.000 description 4
- 229930195729 fatty acid Natural products 0.000 description 4
- 239000000194 fatty acid Substances 0.000 description 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group 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 3
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 3
- 229920003078 Povidone K 12 Polymers 0.000 description 3
- 238000011049 filling Methods 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- WWZKQHOCKIZLMA-UHFFFAOYSA-M octanoate Chemical compound CCCCCCCC([O-])=O WWZKQHOCKIZLMA-UHFFFAOYSA-M 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 239000002504 physiological saline solution Substances 0.000 description 3
- 229940068886 polyethylene glycol 300 Drugs 0.000 description 3
- 239000011591 potassium Substances 0.000 description 3
- 229910052700 potassium Inorganic materials 0.000 description 3
- 238000002604 ultrasonography Methods 0.000 description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical group [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- 108091005804 Peptidases Proteins 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 238000001704 evaporation Methods 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 238000000227 grinding Methods 0.000 description 2
- 239000007902 hard capsule Substances 0.000 description 2
- BKIMMITUMNQMOS-UHFFFAOYSA-N nonane Chemical compound CCCCCCCCC BKIMMITUMNQMOS-UHFFFAOYSA-N 0.000 description 2
- 239000006186 oral dosage form Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 238000007873 sieving Methods 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 241000283690 Bos taurus Species 0.000 description 1
- 241000282465 Canis Species 0.000 description 1
- 208000000094 Chronic Pain Diseases 0.000 description 1
- 241000283073 Equus caballus Species 0.000 description 1
- 241000282324 Felis Species 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 208000005298 acute pain Diseases 0.000 description 1
- 230000001270 agonistic effect Effects 0.000 description 1
- 125000001931 aliphatic group Chemical group 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000007931 coated granule Substances 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229920000223 polyglycerol Polymers 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 229940024999 proteolytic enzymes for treatment of wounds and ulcers Drugs 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- BTURAGWYSMTVOW-UHFFFAOYSA-M sodium dodecanoate Chemical compound [Na+].CCCCCCCCCCCC([O-])=O BTURAGWYSMTVOW-UHFFFAOYSA-M 0.000 description 1
- UDWXLZLRRVQONG-UHFFFAOYSA-M sodium hexanoate Chemical compound [Na+].CCCCCC([O-])=O UDWXLZLRRVQONG-UHFFFAOYSA-M 0.000 description 1
- 229940082004 sodium laurate Drugs 0.000 description 1
- 229940045845 sodium myristate Drugs 0.000 description 1
- 229940045870 sodium palmitate Drugs 0.000 description 1
- GGXKEBACDBNFAF-UHFFFAOYSA-M sodium;hexadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCC([O-])=O GGXKEBACDBNFAF-UHFFFAOYSA-M 0.000 description 1
- JUQGWKYSEXPRGL-UHFFFAOYSA-M sodium;tetradecanoate Chemical compound [Na+].CCCCCCCCCCCCCC([O-])=O JUQGWKYSEXPRGL-UHFFFAOYSA-M 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007944 soluble tablet Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/08—Solutions
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biomedical Technology (AREA)
- Physiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Nutrition Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
Claims (34)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN202010179149 | 2020-03-18 | ||
CN2020101791496 | 2020-03-18 | ||
CN202110268405 | 2021-03-12 | ||
CN2021102684053 | 2021-03-12 | ||
PCT/CN2021/081224 WO2021185265A1 (zh) | 2020-03-18 | 2021-03-17 | 口服药物组合物 |
Publications (1)
Publication Number | Publication Date |
---|---|
CN115209910A true CN115209910A (zh) | 2022-10-18 |
Family
ID=77770153
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN202180017925.5A Pending CN115209910A (zh) | 2020-03-18 | 2021-03-17 | 口服药物组合物 |
Country Status (5)
Country | Link |
---|---|
US (1) | US20230172866A1 (zh) |
EP (1) | EP4122483A4 (zh) |
CN (1) | CN115209910A (zh) |
TW (1) | TW202143997A (zh) |
WO (1) | WO2021185265A1 (zh) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2024517396A (ja) * | 2021-04-12 | 2024-04-22 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | ペプチドアミド系化合物の、掻痒を治療するための薬物の製造における用途 |
TW202337460A (zh) * | 2022-03-23 | 2023-10-01 | 大陸商江蘇恩華藥業股份有限公司 | 多醯胺類化合物、其製備方法及其醫藥用途 |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20020094346A1 (en) * | 1995-05-17 | 2002-07-18 | M. D. Henry C. Lin | Method and compositions for improving digestion and absorption in the small intestine |
CN101627049A (zh) * | 2006-11-10 | 2010-01-13 | 卡拉治疗学股份有限公司 | 合成酞酰胺 |
CN108135962A (zh) * | 2015-10-07 | 2018-06-08 | 塞浦路迈德有限责任公司 | 用于口服递送肽类药物的药物制剂 |
WO2019015644A1 (zh) * | 2017-07-21 | 2019-01-24 | 四川海思科制药有限公司 | 肽酰胺类化合物及其制备方法和在医药上的用途 |
WO2019042247A1 (zh) * | 2017-08-28 | 2019-03-07 | 江苏恒瑞医药股份有限公司 | 一种cyp17抑制剂的药物组合物及其制备方法 |
CN109862906A (zh) * | 2016-08-17 | 2019-06-07 | 安提拉生物有限公司 | 用于口服的活性剂的制剂 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AR071375A1 (es) * | 2008-04-22 | 2010-06-16 | Solvay Pharm Gmbh | Formulaciones para ingredientes farmaceuticos activos de permeabilidad deficiente, proceso de preparacion y producto |
CN101574343B (zh) * | 2008-05-07 | 2011-06-01 | 吉林大学 | 一种治疗糖尿病的药物组合物 |
AU2009283821B2 (en) * | 2008-08-18 | 2014-05-29 | Entera Bio Ltd. | Methods and compositions for oral administration of proteins |
-
2021
- 2021-03-17 CN CN202180017925.5A patent/CN115209910A/zh active Pending
- 2021-03-17 EP EP21772438.4A patent/EP4122483A4/en active Pending
- 2021-03-17 TW TW110109517A patent/TW202143997A/zh unknown
- 2021-03-17 WO PCT/CN2021/081224 patent/WO2021185265A1/zh unknown
- 2021-03-17 US US17/906,555 patent/US20230172866A1/en active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20020094346A1 (en) * | 1995-05-17 | 2002-07-18 | M. D. Henry C. Lin | Method and compositions for improving digestion and absorption in the small intestine |
CN101627049A (zh) * | 2006-11-10 | 2010-01-13 | 卡拉治疗学股份有限公司 | 合成酞酰胺 |
CN108135962A (zh) * | 2015-10-07 | 2018-06-08 | 塞浦路迈德有限责任公司 | 用于口服递送肽类药物的药物制剂 |
CN109862906A (zh) * | 2016-08-17 | 2019-06-07 | 安提拉生物有限公司 | 用于口服的活性剂的制剂 |
WO2019015644A1 (zh) * | 2017-07-21 | 2019-01-24 | 四川海思科制药有限公司 | 肽酰胺类化合物及其制备方法和在医药上的用途 |
WO2019042247A1 (zh) * | 2017-08-28 | 2019-03-07 | 江苏恒瑞医药股份有限公司 | 一种cyp17抑制剂的药物组合物及其制备方法 |
Also Published As
Publication number | Publication date |
---|---|
WO2021185265A1 (zh) | 2021-09-23 |
US20230172866A1 (en) | 2023-06-08 |
EP4122483A4 (en) | 2024-03-27 |
EP4122483A1 (en) | 2023-01-25 |
TW202143997A (zh) | 2021-12-01 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP6647368B2 (ja) | メチルナルトレキソンの経口製剤および親油性塩 | |
EP1750677B1 (en) | Oral therapeutic compound delivery system | |
CN102946869A (zh) | γ-羟基丁酸的速释制剂及剂型 | |
KR20130093015A (ko) | 트라마돌 및 콕시브의 공결정의 약학적 조성물 | |
JPH07558B2 (ja) | モピダモール製剤 | |
PT2316473E (pt) | Utilização de calcitonina na osteoartrite | |
JP2013544230A (ja) | 口腔内分散性製剤 | |
EP2846780B1 (en) | Solubilized capsule formulation of 1,1-dimethylethyl [(1s)-1-{[(2s,4r)-4-(7-chloro-4methoxyisoquinolin-1-yloxy)-2-({(1r,2s)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl}carbamoyl)pyrrolidin-1-yl]carbonyl}-2,2-dimethylpropyl]carbamate | |
CN115209910A (zh) | 口服药物组合物 | |
KR20070008720A (ko) | 습윤 헤파린의 고체 투여형 | |
EP3930685A1 (en) | Dipivefrin orally disintegrating tablet formulations | |
KR101050076B1 (ko) | 제어 방출성 아세클로페낙을 함유하는 경구 제제의 조성물 및 그의 제조방법 | |
US20230381265A1 (en) | Oligosaccharide formulations of kappa opioid receptor agonists | |
KR101093781B1 (ko) | pH조절제를 함유하는 목시플록사신 고형 조성물 | |
CN1173698C (zh) | 包含包衣的雷尼替丁、碱式柠檬酸铋和硫糖铝的对胃肠障碍具有治疗作用的可口服给药的药物制剂 | |
KR101076648B1 (ko) | 제어 방출성 아세클로페낙을 함유하는 경구 제제의 조성물 및 그의 제조방법 | |
WO2014125085A1 (en) | Oral pharmaceutical formulations comprising nimesulide and thiocolchicoside | |
KR101779513B1 (ko) | 애엽의 이소프로판올 추출물을 포함하는 약제학적 조성물 | |
CN109381466A (zh) | 促进糖尿病病人伤口愈合的治疗剂 | |
US20130143912A1 (en) | Sublingual zolpidem formulations | |
KR20170001668A (ko) | 애엽의 이소프로판올 추출물을 포함하는 약제학적 조성물 | |
CN1966072A (zh) | 一种降钙素口服肠溶组合物及其制备方法 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
PB01 | Publication | ||
PB01 | Publication | ||
REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 40073810 Country of ref document: HK |
|
SE01 | Entry into force of request for substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
TA01 | Transfer of patent application right |
Effective date of registration: 20231225 Address after: 856099 Xingfu Jiayuan Economic Development Zone, Gyerba, Nedong District, Shannan City, Tibet Autonomous Region Applicant after: Tibet Haisike Pharmaceutical Co.,Ltd. Address before: 611130 Sichuan Chengdu Wenjiang District Science and Technology Park cross strait Bailey Road 136 Applicant before: SICHUAN HAISCO PHARMACEUTICAL Co.,Ltd. |
|
TA01 | Transfer of patent application right |