CA1239347A - Controlled release liquid dosage formulations for pharmaceuticals - Google Patents
Controlled release liquid dosage formulations for pharmaceuticalsInfo
- Publication number
- CA1239347A CA1239347A CA000471918A CA471918A CA1239347A CA 1239347 A CA1239347 A CA 1239347A CA 000471918 A CA000471918 A CA 000471918A CA 471918 A CA471918 A CA 471918A CA 1239347 A CA1239347 A CA 1239347A
- Authority
- CA
- Canada
- Prior art keywords
- coating
- dosage forms
- liquid
- controlled release
- liquid carrier
- 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.)
- Expired
Links
- 239000007788 liquid Substances 0.000 title claims abstract description 69
- 238000013270 controlled release Methods 0.000 title claims abstract description 59
- 239000000203 mixture Substances 0.000 title claims abstract description 40
- 239000003814 drug Substances 0.000 title claims abstract description 29
- 238000009472 formulation Methods 0.000 title claims abstract description 26
- 239000002552 dosage form Substances 0.000 claims abstract description 97
- 238000000576 coating method Methods 0.000 claims abstract description 75
- 239000011248 coating agent Substances 0.000 claims abstract description 67
- 230000009977 dual effect Effects 0.000 claims abstract description 34
- 238000002844 melting Methods 0.000 claims abstract description 17
- 230000008018 melting Effects 0.000 claims abstract description 17
- 230000037406 food intake Effects 0.000 claims abstract description 15
- 235000019534 high fructose corn syrup Nutrition 0.000 claims abstract description 11
- 229920002678 cellulose Polymers 0.000 claims abstract description 5
- 239000001913 cellulose Substances 0.000 claims abstract description 5
- 150000002632 lipids Chemical class 0.000 claims abstract description 4
- 108060006613 prolamin Proteins 0.000 claims abstract description 4
- XXRYFVCIMARHRS-UHFFFAOYSA-N propan-2-yl n-dimethoxyphosphorylcarbamate Chemical compound COP(=O)(OC)NC(=O)OC(C)C XXRYFVCIMARHRS-UHFFFAOYSA-N 0.000 claims abstract description 4
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims description 91
- 229960000278 theophylline Drugs 0.000 claims description 43
- 229940079593 drug Drugs 0.000 claims description 19
- 239000004005 microsphere Substances 0.000 claims description 16
- 239000003826 tablet Substances 0.000 claims description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 15
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 14
- 239000000194 fatty acid Substances 0.000 claims description 14
- 229930195729 fatty acid Natural products 0.000 claims description 14
- 150000004665 fatty acids Chemical class 0.000 claims description 14
- 125000005456 glyceride group Chemical group 0.000 claims description 14
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims description 13
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims description 13
- 239000004014 plasticizer Substances 0.000 claims description 13
- -1 carboxyl methyl ethyl Chemical group 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 11
- 235000019197 fats Nutrition 0.000 claims description 11
- 239000002775 capsule Substances 0.000 claims description 10
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 10
- 239000011324 bead Substances 0.000 claims description 9
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 8
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims description 8
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 8
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 8
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 8
- 239000012669 liquid formulation Substances 0.000 claims description 8
- 239000011159 matrix material Substances 0.000 claims description 8
- 239000003094 microcapsule Substances 0.000 claims description 8
- 239000000243 solution Substances 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 6
- 102000004190 Enzymes Human genes 0.000 claims description 6
- 108090000790 Enzymes Proteins 0.000 claims description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 6
- 229920002301 cellulose acetate Polymers 0.000 claims description 6
- ZQPPMHVWECSIRJ-MDZDMXLPSA-N elaidic acid Chemical compound CCCCCCCC\C=C\CCCCCCCC(O)=O ZQPPMHVWECSIRJ-MDZDMXLPSA-N 0.000 claims description 6
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 6
- 229920002472 Starch Polymers 0.000 claims description 5
- 150000002148 esters Chemical class 0.000 claims description 5
- 150000002191 fatty alcohols Chemical class 0.000 claims description 5
- 229930195733 hydrocarbon Natural products 0.000 claims description 5
- 150000002430 hydrocarbons Chemical class 0.000 claims description 5
- 235000020374 simple syrup Nutrition 0.000 claims description 5
- 235000019698 starch Nutrition 0.000 claims description 5
- 235000015112 vegetable and seed oil Nutrition 0.000 claims description 5
- 239000008158 vegetable oil Substances 0.000 claims description 5
- 239000001856 Ethyl cellulose Substances 0.000 claims description 4
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims description 4
- ZFOZVQLOBQUTQQ-UHFFFAOYSA-N Tributyl citrate Chemical compound CCCCOC(=O)CC(O)(C(=O)OCCCC)CC(=O)OCCCC ZFOZVQLOBQUTQQ-UHFFFAOYSA-N 0.000 claims description 4
- UYXTWWCETRIEDR-UHFFFAOYSA-N Tributyrin Chemical compound CCCC(=O)OCC(OC(=O)CCC)COC(=O)CCC UYXTWWCETRIEDR-UHFFFAOYSA-N 0.000 claims description 4
- 230000002776 aggregation Effects 0.000 claims description 4
- 229930013930 alkaloid Natural products 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 4
- 229960001948 caffeine Drugs 0.000 claims description 4
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims description 4
- 235000010980 cellulose Nutrition 0.000 claims description 4
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 claims description 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 3
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 3
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 3
- 244000215068 Acacia senegal Species 0.000 claims description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 3
- 108010010803 Gelatin Proteins 0.000 claims description 3
- 229920000084 Gum arabic Polymers 0.000 claims description 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 3
- 239000005642 Oleic acid Substances 0.000 claims description 3
- 102000035195 Peptidases Human genes 0.000 claims description 3
- 108091005804 Peptidases Proteins 0.000 claims description 3
- 239000004365 Protease Substances 0.000 claims description 3
- 239000004164 Wax ester Substances 0.000 claims description 3
- 239000000205 acacia gum Substances 0.000 claims description 3
- 235000010489 acacia gum Nutrition 0.000 claims description 3
- IYKJEILNJZQJPU-UHFFFAOYSA-N acetic acid;butanedioic acid Chemical compound CC(O)=O.OC(=O)CCC(O)=O IYKJEILNJZQJPU-UHFFFAOYSA-N 0.000 claims description 3
- 150000007513 acids Chemical class 0.000 claims description 3
- 238000005054 agglomeration Methods 0.000 claims description 3
- 150000001298 alcohols Chemical class 0.000 claims description 3
- 235000005550 amino acid supplement Nutrition 0.000 claims description 3
- 229940035676 analgesics Drugs 0.000 claims description 3
- 239000000730 antalgic agent Substances 0.000 claims description 3
- 239000000935 antidepressant agent Substances 0.000 claims description 3
- 229940005513 antidepressants Drugs 0.000 claims description 3
- 239000000739 antihistaminic agent Substances 0.000 claims description 3
- 235000014121 butter Nutrition 0.000 claims description 3
- 229940110456 cocoa butter Drugs 0.000 claims description 3
- 235000019868 cocoa butter Nutrition 0.000 claims description 3
- 229920001249 ethyl cellulose Polymers 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
- 235000011187 glycerol Nutrition 0.000 claims description 3
- 235000012907 honey Nutrition 0.000 claims description 3
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 3
- 235000013310 margarine Nutrition 0.000 claims description 3
- 239000003264 margarine Substances 0.000 claims description 3
- 159000000001 potassium salts Chemical class 0.000 claims description 3
- 238000004904 shortening Methods 0.000 claims description 3
- 239000003760 tallow Substances 0.000 claims description 3
- 150000003626 triacylglycerols Chemical class 0.000 claims description 3
- 235000019386 wax ester Nutrition 0.000 claims description 3
- 239000004359 castor oil Substances 0.000 claims description 2
- 235000019438 castor oil Nutrition 0.000 claims description 2
- 229920003086 cellulose ether Polymers 0.000 claims description 2
- 229960004126 codeine Drugs 0.000 claims description 2
- 229940099371 diacetylated monoglycerides Drugs 0.000 claims description 2
- 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 2
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 claims description 2
- 230000002209 hydrophobic effect Effects 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 235000000346 sugar Nutrition 0.000 claims description 2
- 239000002562 thickening agent Substances 0.000 claims description 2
- 229940105329 carboxymethylcellulose Drugs 0.000 claims 6
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 claims 4
- 229920002494 Zein Polymers 0.000 claims 3
- 239000005019 zein Substances 0.000 claims 3
- 229940093612 zein Drugs 0.000 claims 3
- 229920001817 Agar Polymers 0.000 claims 2
- 108010061711 Gliadin Proteins 0.000 claims 2
- 108010068370 Glutens Proteins 0.000 claims 2
- 235000021355 Stearic acid Nutrition 0.000 claims 2
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 2
- 108010055615 Zein Proteins 0.000 claims 2
- 229940022663 acetate Drugs 0.000 claims 2
- 239000008272 agar Substances 0.000 claims 2
- 235000010419 agar Nutrition 0.000 claims 2
- 230000001387 anti-histamine Effects 0.000 claims 2
- 230000036772 blood pressure Effects 0.000 claims 2
- 229960004667 ethyl cellulose Drugs 0.000 claims 2
- 235000010944 ethyl methyl cellulose Nutrition 0.000 claims 2
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims 2
- 230000001939 inductive effect Effects 0.000 claims 2
- 210000000936 intestine Anatomy 0.000 claims 2
- 229940073577 lithium chloride Drugs 0.000 claims 2
- 229920003087 methylethyl cellulose Polymers 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 2
- 239000008117 stearic acid Substances 0.000 claims 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 2
- 235000019871 vegetable fat Nutrition 0.000 claims 2
- GOJCZVPJCKEBQV-UHFFFAOYSA-N Butyl phthalyl butylglycolate Chemical compound CCCCOC(=O)COC(=O)C1=CC=CC=C1C(=O)OCCCC GOJCZVPJCKEBQV-UHFFFAOYSA-N 0.000 claims 1
- 239000004367 Lipase Substances 0.000 claims 1
- 102000004882 Lipase Human genes 0.000 claims 1
- 108090001060 Lipase Proteins 0.000 claims 1
- 238000007792 addition Methods 0.000 claims 1
- 235000014633 carbohydrates Nutrition 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical group CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 claims 1
- 125000005908 glyceryl ester group Chemical group 0.000 claims 1
- 239000001087 glyceryl triacetate Substances 0.000 claims 1
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 1
- 235000019421 lipase Nutrition 0.000 claims 1
- 229960002622 triacetin Drugs 0.000 claims 1
- 239000003925 fat Substances 0.000 abstract description 11
- 239000001993 wax Substances 0.000 abstract description 9
- 238000013268 sustained release Methods 0.000 abstract description 5
- 239000012730 sustained-release form Substances 0.000 abstract description 5
- 239000008297 liquid dosage form Substances 0.000 abstract 1
- 239000012085 test solution Substances 0.000 description 13
- 238000012360 testing method Methods 0.000 description 12
- 239000012530 fluid Substances 0.000 description 9
- 238000000338 in vitro Methods 0.000 description 9
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 230000002496 gastric effect Effects 0.000 description 5
- 239000006194 liquid suspension Substances 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 235000006679 Mentha X verticillata Nutrition 0.000 description 4
- 235000002899 Mentha suaveolens Nutrition 0.000 description 4
- 235000001636 Mentha x rotundifolia Nutrition 0.000 description 4
- 230000002378 acidificating effect Effects 0.000 description 4
- 230000000968 intestinal effect Effects 0.000 description 4
- 239000008363 phosphate buffer Substances 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 240000000662 Anethum graveolens Species 0.000 description 3
- 150000001261 hydroxy acids Chemical class 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- 244000068988 Glycine max Species 0.000 description 2
- 235000010469 Glycine max Nutrition 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 206010034016 Paronychia Diseases 0.000 description 2
- 241000208465 Proteaceae Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 150000001336 alkenes Chemical class 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 2
- 235000012343 cottonseed oil Nutrition 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 229940088598 enzyme Drugs 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 235000019198 oils Nutrition 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 235000019419 proteases Nutrition 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 238000003756 stirring Methods 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
- 235000009434 Actinidia chinensis Nutrition 0.000 description 1
- 244000298697 Actinidia deliciosa Species 0.000 description 1
- 235000009436 Actinidia deliciosa Nutrition 0.000 description 1
- NBGBEUITCPENLJ-UHFFFAOYSA-N Bunazosin hydrochloride Chemical compound Cl.C1CN(C(=O)CCC)CCCN1C1=NC(N)=C(C=C(OC)C(OC)=C2)C2=N1 NBGBEUITCPENLJ-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 101001075022 Dictyostelium discoideum Ras guanine nucleotide exchange factor A Proteins 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 description 1
- 241001441571 Hiodontidae Species 0.000 description 1
- 241001069921 Libido Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 102000057297 Pepsin A Human genes 0.000 description 1
- 108090000284 Pepsin A Proteins 0.000 description 1
- 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 description 1
- 239000011149 active material Substances 0.000 description 1
- 238000004220 aggregation Methods 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 230000001088 anti-asthma Effects 0.000 description 1
- 239000000924 antiasthmatic agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000005243 fluidization Methods 0.000 description 1
- 235000021588 free fatty acids Nutrition 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 150000002314 glycerols Chemical class 0.000 description 1
- 150000002327 glycerophospholipids Chemical class 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 239000002085 irritant Substances 0.000 description 1
- 231100000021 irritant Toxicity 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 235000013372 meat Nutrition 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 229940111688 monobasic potassium phosphate Drugs 0.000 description 1
- 235000019796 monopotassium phosphate Nutrition 0.000 description 1
- 210000003254 palate Anatomy 0.000 description 1
- 229940111202 pepsin Drugs 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 125000001557 phthalyl group Chemical group C(=O)(O)C1=C(C(=O)*)C=CC=C1 0.000 description 1
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 150000003333 secondary alcohols Chemical class 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 150000003505 terpenes Chemical class 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 210000002438 upper gastrointestinal tract Anatomy 0.000 description 1
- 239000011800 void material 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
- A61K9/0087—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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57046984A | 1984-01-13 | 1984-01-13 | |
| US570,469 | 1984-01-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1239347A true CA1239347A (en) | 1988-07-19 |
Family
ID=24279767
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000471918A Expired CA1239347A (en) | 1984-01-13 | 1985-01-11 | Controlled release liquid dosage formulations for pharmaceuticals |
Country Status (11)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0302065B1 (en) * | 1986-03-21 | 1994-08-10 | Eurasiam Laboratories, Inc. | Pharmaceutical compositions |
| SE8605515D0 (sv) * | 1986-12-22 | 1986-12-22 | Astra Laekemedel Ab | A liquid dosage form for oral administration of a pharmaceutically active substance |
| FI77573C (fi) * | 1987-05-08 | 1989-04-10 | Orion Yhtymae Oy | Ny konsistens. |
| US5030454A (en) * | 1987-10-26 | 1991-07-09 | Alza Corporation | Method for delivering drug in tiny pills in liquid carrier |
| US4853229A (en) * | 1987-10-26 | 1989-08-01 | Alza Corporation | Method for adminstering tiny pills |
| IT1226940B (it) * | 1988-09-16 | 1991-02-22 | Recordati Chem Pharm | Sistema terapeutico a rilascio controllato per formulazioni farmaceutiche liquide |
| US5296236A (en) * | 1988-09-16 | 1994-03-22 | Recordati S.A., Chemical And Pharmaceutical Company | Controlled release therapeutic system for a liquid pharmaceutical formulations |
| US5202128A (en) * | 1989-01-06 | 1993-04-13 | F. H. Faulding & Co. Limited | Sustained release pharmaceutical composition |
| EP0535937B2 (en) * | 1991-10-01 | 2008-05-21 | Takeda Chemical Industries, Ltd. | Prolonged release microparticle preparation and production of the same |
| US5160742A (en) * | 1991-12-31 | 1992-11-03 | Abbott Laboratories | System for delivering an active substance for sustained release |
| IL104093A (en) * | 1991-12-31 | 1999-06-20 | Abbott Lab | Prolamine is expected to mask the taste of drugs given orally |
| AU4198793A (en) † | 1992-07-24 | 1994-01-27 | Takeda Chemical Industries Ltd. | Microparticle preparation and production thereof |
| US5744164A (en) * | 1994-12-16 | 1998-04-28 | Nestec S.A. | Sustained release microparticulate caffeine formulation |
| FR2791888B1 (fr) * | 1999-04-06 | 2004-10-08 | Ethypharm Lab Prod Ethiques | Suspension pharmaceutique buvable |
| PT1165042E (pt) | 1999-04-06 | 2005-06-30 | Ethypharm Sa | Suspensao farmaceutica bebivel de ibuprofeno |
| FR2821745B1 (fr) * | 2001-03-09 | 2004-07-02 | Ethypharm Lab Prod Ethiques | Granules et granules enrobes au gout masque |
| WO2004096175A2 (en) * | 2003-04-30 | 2004-11-11 | Ranbaxy Laboratories Limited | Taste masked microcapsules and processes for their preparation |
| CA2959414C (en) | 2014-09-05 | 2023-03-14 | Symbiomix Therapeutics, Llc | Secnidazole for use in the treatment of bacterial vaginosis |
| US12280037B2 (en) | 2020-09-22 | 2025-04-22 | Evofem Biosciences, Inc. | Method and pharmaceutical composition for treating or preventing trichomoniasis and uses thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2805977A (en) * | 1955-01-04 | 1957-09-10 | Smith Kline French Lab | Sustained release pharmaceutical preparation |
| US3265629A (en) * | 1958-12-22 | 1966-08-09 | Ncr Co | Coating by phase separation |
| US3432593A (en) * | 1963-09-18 | 1969-03-11 | Key Pharm Inc | Delayed and sustained release type pharmaceutical preparation |
-
1985
- 1985-01-08 NZ NZ210785A patent/NZ210785A/en unknown
- 1985-01-09 JP JP60500315A patent/JPS61500910A/ja active Pending
- 1985-01-09 WO PCT/US1985/000042 patent/WO1985003000A1/en not_active Application Discontinuation
- 1985-01-09 AU AU38358/85A patent/AU3835885A/en not_active Abandoned
- 1985-01-09 EP EP85900864A patent/EP0169236A1/en not_active Withdrawn
- 1985-01-10 ZA ZA85239A patent/ZA85239B/xx unknown
- 1985-01-10 GR GR850069A patent/GR850069B/el unknown
- 1985-01-11 IT IT19086/85A patent/IT1184309B/it active
- 1985-01-11 CA CA000471918A patent/CA1239347A/en not_active Expired
- 1985-01-11 ES ES539500A patent/ES8605975A1/es not_active Expired
- 1985-01-13 IL IL74049A patent/IL74049A0/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL74049A0 (en) | 1985-04-30 |
| ZA85239B (en) | 1985-08-28 |
| AU3835885A (en) | 1985-07-30 |
| IT8519086A0 (it) | 1985-01-11 |
| EP0169236A1 (en) | 1986-01-29 |
| GR850069B (enrdf_load_stackoverflow) | 1985-05-03 |
| ES8605975A1 (es) | 1986-04-01 |
| JPS61500910A (ja) | 1986-05-08 |
| ES539500A0 (es) | 1986-04-01 |
| IT1184309B (it) | 1987-10-28 |
| NZ210785A (en) | 1987-11-27 |
| WO1985003000A1 (en) | 1985-07-18 |
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