CA2543223A1 - Comprimes de methylcellulose a desintegration rapide - Google Patents

Info

Publication number

CA2543223A1

CA2543223A1 CA002543223A CA2543223A CA2543223A1 CA 2543223 A1 CA2543223 A1 CA 2543223A1 CA 002543223 A CA002543223 A CA 002543223A CA 2543223 A CA2543223 A CA 2543223A CA 2543223 A1 CA2543223 A1 CA 2543223A1

Authority

CA

Canada

Prior art keywords

tablet according

sodium

methylcellulose

tablet

extragranular

Prior art date

1997-08-22

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.)

Abandoned

Links

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• 229920000609 methyl cellulose Polymers 0.000 title claims abstract description 68
• 239000001923 methylcellulose Substances 0.000 title claims abstract description 66
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 68
• 235000010981 methylcellulose Nutrition 0.000 claims description 64
• 239000000203 mixture Substances 0.000 claims description 55
• 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 49
• DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 48
• WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 44
• 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 42
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 42
• 235000019359 magnesium stearate Nutrition 0.000 claims description 34
• 229940069328 povidone Drugs 0.000 claims description 29
• 239000003085 diluting agent Substances 0.000 claims description 21
• 229920002261 Corn starch Polymers 0.000 claims description 20
• 239000003795 chemical substances by application Substances 0.000 claims description 20
• 239000008120 corn starch Substances 0.000 claims description 20
• 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 19
• 229940016286 microcrystalline cellulose Drugs 0.000 claims description 19
• 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 19
• 239000008108 microcrystalline cellulose Substances 0.000 claims description 19
• 229920003109 sodium starch glycolate Polymers 0.000 claims description 18
• 239000008109 sodium starch glycolate Substances 0.000 claims description 18
• 229940079832 sodium starch glycolate Drugs 0.000 claims description 18
• 229940032147 starch Drugs 0.000 claims description 18
• 235000019698 starch Nutrition 0.000 claims description 18
• 229920002472 Starch Polymers 0.000 claims description 17
• 239000008107 starch Substances 0.000 claims description 17
• 239000007884 disintegrant Substances 0.000 claims description 15
• 239000008187 granular material Substances 0.000 claims description 13
• 239000000314 lubricant Substances 0.000 claims description 12
• 239000000080 wetting agent Substances 0.000 claims description 12
• 239000001768 carboxy methyl cellulose Substances 0.000 claims description 11
• 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
• 241000416162 Astragalus gummifer Species 0.000 claims description 8
• 229920000881 Modified starch Polymers 0.000 claims description 8
• 229920001615 Tragacanth Polymers 0.000 claims description 8
• 239000011230 binding agent Substances 0.000 claims description 8
• 235000010487 tragacanth Nutrition 0.000 claims description 8
• 239000000196 tragacanth Substances 0.000 claims description 8
• 229940116362 tragacanth Drugs 0.000 claims description 8
• 229940099112 cornstarch Drugs 0.000 claims description 7
• 239000002245 particle Substances 0.000 claims description 7
• -1 veegum Polymers 0.000 claims description 7
• 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 6
• 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 6
• 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 6
• 229940105329 carboxymethylcellulose Drugs 0.000 claims description 6
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
• 229920001817 Agar Polymers 0.000 claims description 5
• 235000013912 Ceratonia siliqua Nutrition 0.000 claims description 5
• 240000008886 Ceratonia siliqua Species 0.000 claims description 5
• 244000303965 Cyamopsis psoralioides Species 0.000 claims description 5
• 235000015125 Sterculia urens Nutrition 0.000 claims description 5
• 240000001058 Sterculia urens Species 0.000 claims description 5
• 239000008272 agar Substances 0.000 claims description 5
• 235000010443 alginic acid Nutrition 0.000 claims description 5
• 229920000615 alginic acid Polymers 0.000 claims description 5
• 229960000913 crospovidone Drugs 0.000 claims description 5
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 5
• 239000001814 pectin Substances 0.000 claims description 5
• 235000010987 pectin Nutrition 0.000 claims description 5
• 229920001277 pectin Polymers 0.000 claims description 5
• 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 5
• 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 5
• 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 5
• 206010010774 Constipation Diseases 0.000 claims description 4
• 241000124008 Mammalia Species 0.000 claims description 4
• 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
• 108010010803 Gelatin Proteins 0.000 claims description 3
• 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 3
• 235000010643 Leucaena leucocephala Nutrition 0.000 claims description 3
• 240000007472 Leucaena leucocephala Species 0.000 claims description 3
• 239000004480 active ingredient Substances 0.000 claims description 3
• 239000008273 gelatin Substances 0.000 claims description 3
• 229920000159 gelatin Polymers 0.000 claims description 3
• 235000019322 gelatine Nutrition 0.000 claims description 3
• 235000011852 gelatine desserts Nutrition 0.000 claims description 3
• 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 3
• 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 3
• 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 description 3
• 230000001050 lubricating effect Effects 0.000 claims description 3
• VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
• 235000021355 Stearic acid Nutrition 0.000 claims description 2
• CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 2
• 239000008116 calcium stearate Substances 0.000 claims description 2
• 235000013539 calcium stearate Nutrition 0.000 claims description 2
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
• RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims description 2
• 239000008117 stearic acid Substances 0.000 claims description 2
• 239000000454 talc Substances 0.000 claims description 2
• 229910052623 talc Inorganic materials 0.000 claims description 2
• 229920002785 Croscarmellose sodium Polymers 0.000 claims 4
• 229960001681 croscarmellose sodium Drugs 0.000 claims 4
• 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 4
• 239000001267 polyvinylpyrrolidone Substances 0.000 claims 3
• 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 3
• FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims 1
• AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 claims 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 claims 1
• 229940072056 alginate Drugs 0.000 claims 1
• 229940075614 colloidal silicon dioxide Drugs 0.000 claims 1
• 239000011734 sodium Substances 0.000 claims 1
• 229910052708 sodium Inorganic materials 0.000 claims 1
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 42
• VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract description 21
• 238000004519 manufacturing process Methods 0.000 abstract description 5
• 239000008194 pharmaceutical composition Substances 0.000 abstract 1
• 239000003826 tablet Substances 0.000 description 69
• 238000009472 formulation Methods 0.000 description 25
• 235000000346 sugar Nutrition 0.000 description 20
• 229920003108 Methocel™ A4M Polymers 0.000 description 18
• 239000004615 ingredient Substances 0.000 description 18
• 229920003084 Avicel® PH-102 Polymers 0.000 description 15
• 229920003086 cellulose ether Polymers 0.000 description 12
• 238000000034 method Methods 0.000 description 12
• 239000000975 dye Substances 0.000 description 11
• 238000004040 coloring Methods 0.000 description 10
• 239000000843 powder Substances 0.000 description 9
• 239000002253 acid Substances 0.000 description 8
• 230000008569 process Effects 0.000 description 7
• 238000002156 mixing Methods 0.000 description 6
• 238000002360 preparation method Methods 0.000 description 6
• 239000000725 suspension Substances 0.000 description 6
• 239000008280 blood Substances 0.000 description 5
• 210000004369 blood Anatomy 0.000 description 5
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
• 239000000243 solution Substances 0.000 description 5
• CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
• 229930006000 Sucrose Natural products 0.000 description 4
• 239000011248 coating agent Substances 0.000 description 4
• 239000002552 dosage form Substances 0.000 description 4
• 239000000945 filler Substances 0.000 description 4
• 210000001035 gastrointestinal tract Anatomy 0.000 description 4
• 239000008141 laxative Substances 0.000 description 4
• 230000002475 laxative effect Effects 0.000 description 4
• 239000005720 sucrose Substances 0.000 description 4
• 239000008142 bulk forming laxative Substances 0.000 description 3
• MYWUZJCMWCOHBA-VIFPVBQESA-N methamphetamine Chemical compound CN[C@@H](C)CC1=CC=CC=C1 MYWUZJCMWCOHBA-VIFPVBQESA-N 0.000 description 3
• 239000007916 tablet composition Substances 0.000 description 3
• 238000012360 testing method Methods 0.000 description 3
• 239000007864 aqueous solution Substances 0.000 description 2
• 239000007894 caplet Substances 0.000 description 2
• 229940081970 citrucel Drugs 0.000 description 2
• 239000003086 colorant Substances 0.000 description 2
• 238000007906 compression Methods 0.000 description 2
• 230000006835 compression Effects 0.000 description 2
• 239000002270 dispersing agent Substances 0.000 description 2
• 238000009826 distribution Methods 0.000 description 2
• 238000001035 drying Methods 0.000 description 2
• 239000012530 fluid Substances 0.000 description 2
• 239000000499 gel Substances 0.000 description 2
• 230000036571 hydration Effects 0.000 description 2
• 238000006703 hydration reaction Methods 0.000 description 2
• XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 description 2
• 239000007788 liquid Substances 0.000 description 2
• 229940057948 magnesium stearate Drugs 0.000 description 2
• 239000007968 orange flavor Substances 0.000 description 2
• 150000008163 sugars Chemical class 0.000 description 2
• 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 description 1
• PNEYBMLMFCGWSK-UHFFFAOYSA-N Alumina Chemical compound [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
• 241001550224 Apha Species 0.000 description 1
• 239000004150 EU approved colour Substances 0.000 description 1
• 229930091371 Fructose Natural products 0.000 description 1
• 239000005715 Fructose Substances 0.000 description 1
• RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
• WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
• 206010028813 Nausea Diseases 0.000 description 1
• 206010047700 Vomiting Diseases 0.000 description 1
• 240000008042 Zea mays Species 0.000 description 1
• 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 description 1
• 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
• WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
• 235000010980 cellulose Nutrition 0.000 description 1
• 229920002678 cellulose Polymers 0.000 description 1
• 239000001913 cellulose Substances 0.000 description 1
• 238000000576 coating method Methods 0.000 description 1
• 239000007891 compressed tablet Substances 0.000 description 1
• 235000005822 corn Nutrition 0.000 description 1
• MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 description 1
• 229940043264 dodecyl sulfate Drugs 0.000 description 1
• 230000000694 effects Effects 0.000 description 1
• 238000005516 engineering process Methods 0.000 description 1
• 239000000835 fiber Substances 0.000 description 1
• 239000000796 flavoring agent Substances 0.000 description 1
• 235000019634 flavors Nutrition 0.000 description 1
• 235000003599 food sweetener Nutrition 0.000 description 1
• 210000004051 gastric juice Anatomy 0.000 description 1
• 238000001879 gelation Methods 0.000 description 1
• 239000008103 glucose Substances 0.000 description 1
• 238000009478 high shear granulation Methods 0.000 description 1
• 230000000887 hydrating effect Effects 0.000 description 1
• 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
• 238000000338 in vitro Methods 0.000 description 1
• 229940125722 laxative agent Drugs 0.000 description 1
• 229940037627 magnesium lauryl sulfate Drugs 0.000 description 1
• HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 description 1
• 230000010534 mechanism of action Effects 0.000 description 1
• 238000003801 milling Methods 0.000 description 1
• 238000012986 modification Methods 0.000 description 1
• 230000004048 modification Effects 0.000 description 1
• 230000008693 nausea Effects 0.000 description 1
• 230000000050 nutritive effect Effects 0.000 description 1
• 229940006093 opthalmologic coloring agent diagnostic Drugs 0.000 description 1
• 229940124531 pharmaceutical excipient Drugs 0.000 description 1
• 239000008279 sol Substances 0.000 description 1
• 239000007787 solid Substances 0.000 description 1
• 239000007909 solid dosage form Substances 0.000 description 1
• 238000005507 spraying Methods 0.000 description 1
• 239000000126 substance Substances 0.000 description 1
• 239000003765 sweetening agent Substances 0.000 description 1
• 239000006188 syrup Substances 0.000 description 1
• 235000020357 syrup Nutrition 0.000 description 1
• 230000008673 vomiting Effects 0.000 description 1
• 238000005550 wet granulation Methods 0.000 description 1