ZA200207304B - Hydrophilic molecular disperse solutions of carvedilol. - Google Patents

Hydrophilic molecular disperse solutions of carvedilol. Download PDF

Info

Publication number: ZA200207304B
Authority: ZA; South Africa
Prior art keywords: carvedilol; composition according; composition; pharmaceutically acceptable; administration form
Prior art date: 2000-04-03

Application number

ZA200207304A

Other languages

English (en)

Inventor

Rolf-Dieter Gabel

Walter Preis

Alexander Wirl

Guenter Neugebauer

Original Assignee

Hoffmann La Roche

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.)

2000-04-03

Filing date

2002-09-11

Publication date

2003-12-11

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=8168348&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ZA200207304(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2002-09-11 Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche

2003-12-11 Publication of ZA200207304B publication Critical patent/ZA200207304B/en

Links

NPAKNKYSJIDKMW-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=NC3=CC=C[CH]C3=C12 NPAKNKYSJIDKMW-UHFFFAOYSA-N 0.000 title claims description 102
229960004195 carvedilol Drugs 0.000 title claims description 102
239000000203 mixture Substances 0.000 claims description 60
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 42
239000006104 solid solution Substances 0.000 claims description 42
239000002671 adjuvant Substances 0.000 claims description 31
229920001223 polyethylene glycol Polymers 0.000 claims description 28
239000002202 Polyethylene glycol Substances 0.000 claims description 25
239000013543 active substance Substances 0.000 claims description 23
238000000034 method Methods 0.000 claims description 21
239000000377 silicon dioxide Substances 0.000 claims description 21
235000012239 silicon dioxide Nutrition 0.000 claims description 21
-1 polyoxyethylene stearate Polymers 0.000 claims description 20
239000007787 solid Substances 0.000 claims description 18
239000000243 solution Substances 0.000 claims description 18
229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims description 16
238000007711 solidification Methods 0.000 claims description 15
238000004519 manufacturing process Methods 0.000 claims description 11
150000003839 salts Chemical class 0.000 claims description 11
239000003814 drug Substances 0.000 claims description 10
239000006185 dispersion Substances 0.000 claims description 9
238000011282 treatment Methods 0.000 claims description 8
230000008569 process Effects 0.000 claims description 7
SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims description 6
206010002383 Angina Pectoris Diseases 0.000 claims description 5
206010019280 Heart failures Diseases 0.000 claims description 5
206010020772 Hypertension Diseases 0.000 claims description 5
238000011321 prophylaxis Methods 0.000 claims description 5
239000000905 isomalt Substances 0.000 claims description 4
235000010439 isomalt Nutrition 0.000 claims description 4
HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims description 4
239000000126 substance Substances 0.000 claims description 4
235000021092 sugar substitutes Nutrition 0.000 claims description 3
239000004094 surface-active agent Substances 0.000 claims description 3
239000003765 sweetening agent Substances 0.000 claims description 3
235000000346 sugar Nutrition 0.000 claims description 2
239000000155 melt Substances 0.000 description 31
238000009472 formulation Methods 0.000 description 16
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 16
230000008023 solidification Effects 0.000 description 14
239000007921 spray Substances 0.000 description 13
239000003795 chemical substances by application Substances 0.000 description 10
238000009826 distribution Methods 0.000 description 10
229920000036 polyvinylpyrrolidone Polymers 0.000 description 9
239000001267 polyvinylpyrrolidone Substances 0.000 description 9
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 9
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 description 8
235000019359 magnesium stearate Nutrition 0.000 description 8
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 7
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 7
229920001993 poloxamer 188 Polymers 0.000 description 7
229920002678 cellulose Polymers 0.000 description 6
235000010980 cellulose Nutrition 0.000 description 6
229920001451 polypropylene glycol Polymers 0.000 description 6
239000000654 additive Substances 0.000 description 5
239000004606 Fillers/Extenders Substances 0.000 description 4
239000002775 capsule Substances 0.000 description 4
239000001913 cellulose Substances 0.000 description 4
239000003595 mist Substances 0.000 description 4
229910052708 sodium Inorganic materials 0.000 description 4
239000011734 sodium Substances 0.000 description 4
IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 3
YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
229920002153 Hydroxypropyl cellulose Polymers 0.000 description 3
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 3
239000002585 base Substances 0.000 description 3
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
239000000416 hydrocolloid Substances 0.000 description 3
235000010977 hydroxypropyl cellulose Nutrition 0.000 description 3
239000001866 hydroxypropyl methyl cellulose Substances 0.000 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 description 3
229940031702 hydroxypropyl methylcellulose 2208 Drugs 0.000 description 3
238000011835 investigation Methods 0.000 description 3
239000000314 lubricant Substances 0.000 description 3
239000000463 material Substances 0.000 description 3
239000011159 matrix material Substances 0.000 description 3
230000008018 melting Effects 0.000 description 3
238000002844 melting Methods 0.000 description 3
239000003960 organic solvent Substances 0.000 description 3
239000008385 outer phase Substances 0.000 description 3
239000008194 pharmaceutical composition Substances 0.000 description 3
239000000661 sodium alginate Substances 0.000 description 3
235000010413 sodium alginate Nutrition 0.000 description 3
229940005550 sodium alginate Drugs 0.000 description 3
239000007962 solid dispersion Substances 0.000 description 3
239000002904 solvent Substances 0.000 description 3
238000001694 spray drying Methods 0.000 description 3
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
229920003091 Methocel™ Polymers 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
238000002441 X-ray diffraction Methods 0.000 description 2
239000002253 acid Substances 0.000 description 2
239000012736 aqueous medium Substances 0.000 description 2
238000000889 atomisation Methods 0.000 description 2
150000001875 compounds Chemical class 0.000 description 2
239000013078 crystal Substances 0.000 description 2
230000001419 dependent effect Effects 0.000 description 2
238000004090 dissolution Methods 0.000 description 2
238000005516 engineering process Methods 0.000 description 2
210000000936 intestine Anatomy 0.000 description 2
BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 2
231100000252 nontoxic Toxicity 0.000 description 2
230000003000 nontoxic effect Effects 0.000 description 2
239000002245 particle Substances 0.000 description 2
239000000843 powder Substances 0.000 description 2
239000002244 precipitate Substances 0.000 description 2
230000007704 transition Effects 0.000 description 2
SERLAGPUMNYUCK-BLEZHGCXSA-N (2xi)-6-O-alpha-D-glucopyranosyl-D-arabino-hexitol Chemical compound OCC(O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-BLEZHGCXSA-N 0.000 description 1
LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 description 1
RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
KFZMGEQAYNKOFK-UHFFFAOYSA-N 2-propanol Substances CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 1
BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 1
PVXPPJIGRGXGCY-TZLCEDOOSA-N 6-O-alpha-D-glucopyranosyl-D-fructofuranose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)C(O)(CO)O1 PVXPPJIGRGXGCY-TZLCEDOOSA-N 0.000 description 1
229920002261 Corn starch Polymers 0.000 description 1
FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
239000001692 EU approved anti-caking agent Substances 0.000 description 1
229920003151 Eudragit® RL polymer Polymers 0.000 description 1
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 description 1
235000019759 Maize starch Nutrition 0.000 description 1
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
229920000168 Microcrystalline cellulose Polymers 0.000 description 1
GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
239000004698 Polyethylene Substances 0.000 description 1
OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
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 1
QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
230000001133 acceleration Effects 0.000 description 1
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 description 1
230000002378 acidificating effect Effects 0.000 description 1
150000007513 acids Chemical class 0.000 description 1
150000001298 alcohols Chemical class 0.000 description 1
229910052783 alkali metal Inorganic materials 0.000 description 1
229910052784 alkaline earth metal Inorganic materials 0.000 description 1
229910000147 aluminium phosphate Inorganic materials 0.000 description 1
230000008485 antagonism Effects 0.000 description 1
239000003963 antioxidant agent Substances 0.000 description 1
230000003078 antioxidant effect Effects 0.000 description 1
239000007864 aqueous solution Substances 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
229910052791 calcium Inorganic materials 0.000 description 1
239000001768 carboxy methyl cellulose Substances 0.000 description 1
230000000747 cardiac effect Effects 0.000 description 1
230000008859 change Effects 0.000 description 1
235000015165 citric acid Nutrition 0.000 description 1
210000001072 colon Anatomy 0.000 description 1
239000003246 corticosteroid Substances 0.000 description 1
229960001334 corticosteroids Drugs 0.000 description 1
238000002425 crystallisation Methods 0.000 description 1
230000008025 crystallization Effects 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
230000003111 delayed effect Effects 0.000 description 1
238000011161 development Methods 0.000 description 1
235000013681 dietary sucrose Nutrition 0.000 description 1
238000000113 differential scanning calorimetry Methods 0.000 description 1
230000004069 differentiation Effects 0.000 description 1
238000009792 diffusion process Methods 0.000 description 1
239000003085 diluting agent Substances 0.000 description 1
238000007907 direct compression Methods 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
239000002270 dispersing agent Substances 0.000 description 1
238000001035 drying Methods 0.000 description 1
239000003995 emulsifying agent Substances 0.000 description 1
230000003628 erosive effect Effects 0.000 description 1
239000000374 eutectic mixture Substances 0.000 description 1
238000002474 experimental method Methods 0.000 description 1
239000000945 filler Substances 0.000 description 1
239000007888 film coating Substances 0.000 description 1
238000009501 film coating Methods 0.000 description 1
235000019253 formic acid Nutrition 0.000 description 1
230000008014 freezing Effects 0.000 description 1
238000007710 freezing Methods 0.000 description 1
230000002496 gastric effect Effects 0.000 description 1
210000004051 gastric juice Anatomy 0.000 description 1
210000001035 gastrointestinal tract Anatomy 0.000 description 1
239000008187 granular material Substances 0.000 description 1
238000005469 granulation Methods 0.000 description 1
230000003179 granulation Effects 0.000 description 1
230000002209 hydrophobic effect Effects 0.000 description 1
239000001863 hydroxypropyl cellulose Substances 0.000 description 1
210000003405 ileum Anatomy 0.000 description 1
230000006872 improvement Effects 0.000 description 1
238000010348 incorporation Methods 0.000 description 1
239000011261 inert gas Substances 0.000 description 1
238000002347 injection Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
239000004922 lacquer Substances 0.000 description 1
239000008101 lactose Substances 0.000 description 1
229910052749 magnesium Inorganic materials 0.000 description 1
239000011777 magnesium Substances 0.000 description 1
238000012423 maintenance Methods 0.000 description 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
239000011976 maleic acid Substances 0.000 description 1
238000005259 measurement Methods 0.000 description 1
229920000609 methyl cellulose Polymers 0.000 description 1
239000001923 methylcellulose Substances 0.000 description 1
235000010981 methylcellulose Nutrition 0.000 description 1
235000019813 microcrystalline cellulose Nutrition 0.000 description 1
150000007522 mineralic acids Chemical class 0.000 description 1
DNKKLDKIFMDAPT-UHFFFAOYSA-N n,n-dimethylmethanamine;2-methylprop-2-enoic acid Chemical compound CN(C)C.CC(=C)C(O)=O.CC(=C)C(O)=O DNKKLDKIFMDAPT-UHFFFAOYSA-N 0.000 description 1
229910017604 nitric acid Inorganic materials 0.000 description 1
150000007524 organic acids Chemical class 0.000 description 1
229920000620 organic polymer Polymers 0.000 description 1
239000008188 pellet Substances 0.000 description 1
239000012071 phase Substances 0.000 description 1
235000011007 phosphoric acid Nutrition 0.000 description 1
239000004014 plasticizer Substances 0.000 description 1
229920000058 polyacrylate Polymers 0.000 description 1
229920000573 polyethylene Polymers 0.000 description 1
229940093429 polyethylene glycol 6000 Drugs 0.000 description 1
229920002451 polyvinyl alcohol Polymers 0.000 description 1
235000019422 polyvinyl alcohol Nutrition 0.000 description 1
229910052700 potassium Inorganic materials 0.000 description 1
238000012545 processing Methods 0.000 description 1
238000007712 rapid solidification Methods 0.000 description 1
230000009467 reduction Effects 0.000 description 1
239000012047 saturated solution Substances 0.000 description 1
238000000926 separation method Methods 0.000 description 1
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
229960002920 sorbitol Drugs 0.000 description 1
238000001179 sorption measurement Methods 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1
229960004793 sucrose Drugs 0.000 description 1
239000001117 sulphuric acid Substances 0.000 description 1
235000011149 sulphuric acid Nutrition 0.000 description 1
239000000725 suspension Substances 0.000 description 1
239000003826 tablet Substances 0.000 description 1
239000000454 talc Substances 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 1
238000002076 thermal analysis method Methods 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
230000000304 vasodilatating effect Effects 0.000 description 1
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—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
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives

Landscapes

Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
Cardiology (AREA)
Organic Chemistry (AREA)
Heart & Thoracic Surgery (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Hospice & Palliative Care (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)

ZA200207304A 2000-04-03 2002-09-11 Hydrophilic molecular disperse solutions of carvedilol. ZA200207304B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
EP00107093		2000-04-03

Publications (1)

Publication Number	Publication Date
ZA200207304B true ZA200207304B (en)	2003-12-11

Family

ID=8168348

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200207304A ZA200207304B (en)	2000-04-03	2002-09-11	Hydrophilic molecular disperse solutions of carvedilol.

Country Status (24)

Country	Link
US (3)	US20010036959A1 (de)
EP (1)	EP1272179B1 (de)
JP (1)	JP2003528915A (de)
KR (1)	KR100478793B1 (de)
CN (1)	CN1189171C (de)
AR (1)	AR029825A1 (de)
AT (1)	ATE450257T1 (de)
AU (2)	AU2001256227B2 (de)
BR (1)	BR0109779A (de)
CA (1)	CA2401910C (de)
CZ (1)	CZ20023625A3 (de)
DE (1)	DE60140662D1 (de)
HR (1)	HRP20020777A2 (de)
HU (1)	HUP0300342A3 (de)
IL (1)	IL151642A0 (de)
MA (1)	MA26888A1 (de)
MX (1)	MXPA02009725A (de)
NO (1)	NO20024733L (de)
NZ (1)	NZ521232A (de)
PL (1)	PL358103A1 (de)
RU (1)	RU2248204C2 (de)
WO (1)	WO2001074357A1 (de)
YU (1)	YU72602A (de)
ZA (1)	ZA200207304B (de)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP4533531B2 (ja) *	1998-04-03	2010-09-01	ビーエムリサーチエイ／エス	制御放出組成物
US20040234602A1 (en)	2001-09-21	2004-11-25	Gina Fischer	Polymer release system
EP1429744A1 (de) *	2001-09-21	2004-06-23	Egalet A/S	Polymeres freigabungssystem mit morphin
WO2003024426A1 (en) *	2001-09-21	2003-03-27	Egalet A/S	Controlled release solid dispersions
KR100752549B1 (ko) *	2001-09-28	2007-08-30	에프. 호프만-라 로슈 아게	카르베딜올의 유사다형태
US8101209B2 (en)	2001-10-09	2012-01-24	Flamel Technologies	Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles
AR038681A1 (es) *	2002-02-14	2005-01-26	Solvay Pharm Bv	Formulacion oral de solucion solida de una sustancia activa pobremente soluble en agua
EP1499310A4 (de) *	2002-04-30	2005-12-07	Sb Pharmco Inc	Carvedilolmonocitrat-monohydrat
WO2003092625A2 (en) *	2002-05-03	2003-11-13	Smithkline Beecham Pharmco Puerto Rico, Inc.	Carvedilol formulations
JP2005533822A (ja) *	2002-06-27	2005-11-10	エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド	臭化水素酸カルベジロール
MXPA04012923A (es) *	2002-06-27	2005-03-31	Sb Pharmco Inc	Sales de fosfato de carvedilol y/o solvatos de las mismas, composiciones correspondientes y/o metodos de tratamiento.
EP1562552A1 (de) *	2002-11-08	2005-08-17	Egalet A/S	Zusammensetzung zur kontrollierten wirkstoffabgabe von carvedilol
US7423004B2 (en)	2003-01-31	2008-09-09	Smithkline Beecham Corporation	Solid dispersion compositions
WO2004084868A1 (en) *	2003-03-26	2004-10-07	Egalet A/S	Morphine controlled release system
ATE454886T1 (de) *	2003-03-26	2010-01-15	Egalet As	Matrixzubereitungen für die kontrollierte darreichung von arzneistoffen
EP1641437A4 (de) *	2003-07-09	2009-06-03	Chong Kun Dang Pharm Corp	Feste dispersion von tacrolimus
WO2005020993A1 (en)	2003-08-29	2005-03-10	Lifecycle Pharma A/S	Modified release compositions comprising tacrolimus
US8591946B2 (en) *	2003-08-29	2013-11-26	Veloxis Pharmaceuticals A/S	Modified release compositions comprising tacrolimus
CA2547137A1 (en) *	2003-11-25	2005-06-09	Sb Pharmco Puerto Rico Inc.	Carvedilol free base, salts, anhydrous forms or solvates thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods
JP2007512372A (ja) *	2003-11-25	2007-05-17	エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド	カルベジロール塩、対応する組成物、送達および／または治療方法
EP1686967A4 (de) *	2003-11-25	2012-08-08	Smithkline Beecham Cork Ltd	Carvedilol-freie base, salze, wasserfreie formen oder solvate davon, entsprechende pharmazeutische zusammensetzungen, formulierungen mit kontrollierter freisetzung und behandlungs- oder abgabeverfahren
JP2007517016A (ja) *	2003-12-31	2007-06-28	ファイザー・プロダクツ・インク	低溶解性薬剤及びポロキサマーの固体組成物
ATE500819T1 (de) *	2003-12-31	2011-03-15	Bend Res Inc	Stabilisierte pharmazeutische feste zusammensetzungen von arzneimitteln mit geringer löslichkeit, poloxameren und stabilisierenden polymeren
CA2611081C (en) *	2005-06-03	2016-05-31	Egalet A/S	A drug delivery system for delivering active substances dispersed in a dispersion medium
US8367112B2 (en) *	2006-02-28	2013-02-05	Alkermes Pharma Ireland Limited	Nanoparticulate carverdilol formulations
US20090028935A1 (en) *	2006-12-01	2009-01-29	Kristin Arnold	Carvedilol forms, compositions, and methods of preparation thereof
US20080292695A1 (en) *	2006-12-01	2008-11-27	Kristin Arnold	Carvedilol forms, compositions, and methods of preparation thereof
US20080138404A1 (en) *	2006-12-06	2008-06-12	Biovail Laboratories International S.R.L.	Extended release formulations of carvedilol
NZ577560A (en) *	2007-01-16	2012-01-12	Egalet Ltd	Use of i) a polyglycol and ii) an active drug substance for the preparation of a pharmaceutical composition for i) mitigating the risk of alcohol induced dose dumping and/or ii) reducing the risk of drug abuse
BRPI0701904A2 (pt) *	2007-04-27	2008-12-09	Libbs Farmaceutica Ltda	forma farmacÊutica de liberaÇço controlada de princÍpios ativos com solubilidade dependente do baixo ph do meio e processo para preparar a forma farmacÊutica
EP2155167A2 (de)	2007-06-04	2010-02-24	Egalet A/S	Pharmazeutische zusammensetzungen mit gesteuerter freisetzung für verlängerte wirkung
ATE539769T1 (de) *	2008-03-04	2012-01-15	Lupin Ltd	Stabile pharmazeutische zusammensetzungen mit carvedilol
ES2330404B1 (es) *	2008-05-19	2010-09-22	Universidad De Barcelona	Solucion acuosa para la preservacion de tejidos y organos.
NZ594207A (en)	2009-02-06	2013-03-28	Egalet Ltd	Immediate release composition resistant to abuse by intake of alcohol
NZ597283A (en)	2009-06-24	2013-07-26	Egalet Ltd	Controlled release formulations
WO2011154009A1 (en) *	2010-06-10	2011-12-15	Lifecycle Pharma A/S	Composition comprising an active principle in an amorphous form and a porous adsorbent material
BR112015000150A2 (pt)	2012-07-06	2017-06-27	Egalet Ltd	composições farmacêuticas dissuasoras de abuso de liberação controlada
KR102158339B1 (ko)	2016-02-05	2020-09-21	삼진제약주식회사	인습성이 개선된 카르베딜롤 속방성 제제

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE2815926A1 (de) *	1978-04-13	1979-10-18	Boehringer Mannheim Gmbh	Neue carbazolyl-(4)-oxy-propanolamin-derivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
DE3319027A1 (de) *	1983-05-26	1984-11-29	Boehringer Mannheim Gmbh, 6800 Mannheim	Verfahren zur herstellung von optisch aktiven carbazol-derivaten, neue r- und s-carbazol-derivate, sowie arzneimittel, die diese verbindungen enthalten
US5258185A (en) *	1989-08-23	1993-11-02	Bauer Kurt H	Highly active, rapidly absorbable formulations of glibenclamide, processes for the production thereof and their use
US5281420A (en) *	1992-05-19	1994-01-25	The Procter & Gamble Company	Solid dispersion compositions of tebufelone
US5760069A (en) *	1995-02-08	1998-06-02	Boehringer Mannheim Pharmaceuticals Corporation-Smithkline Beecham Corporation Limited Partnership #1	Method of treatment for decreasing mortality resulting from congestive heart failure
GB9514473D0 (en) *	1995-07-14	1995-09-13	Glaxo Lab Sa	Chemical compounds
DE19637082A1 (de) *	1996-09-12	1998-03-19	Boehringer Mannheim Gmbh	Schnellzerfallende Pellets
IL131713A (en) *	1997-03-11	2004-08-31	Arakis Ltd	Dosage forms comprising separate portions of r- and s-enantiomers
DE19809242A1 (de) *	1998-03-05	1999-09-09	Basf Ag	Verfahren zur Herstellung von festen, sphärischen Formkörpern, enthaltend pharmazeutische Wirkstoffe in einer Bindemittelmatrix
US6852337B2 (en) *	1998-04-09	2005-02-08	Roche Diagnostics Gmbh	Carvedilol-galenics
DE19816036A1 (de) *	1998-04-09	1999-10-14	Roche Diagnostics Gmbh	Verfahren zur Herstellung schnellauflösender pharmazeutischer Zubereitungen von schwerlöslichen Wirkstoffen
US6664284B2 (en) *	1998-07-23	2003-12-16	Roche Diagnostics Gmbh	Stabilized carvedilol injection solution
US6395300B1 (en) *	1999-05-27	2002-05-28	Acusphere, Inc.	Porous drug matrices and methods of manufacture thereof
MXPA04006909A (es) *	2002-01-15	2005-04-19	Teva Pharma	Solidos cristalinos de carvedilol y procesos para su preparacion.

2001
- 2001-03-26 US US09/817,308 patent/US20010036959A1/en not_active Abandoned
- 2001-03-28 MX MXPA02009725A patent/MXPA02009725A/es active IP Right Grant
- 2001-03-28 DE DE60140662T patent/DE60140662D1/de not_active Expired - Fee Related
- 2001-03-28 PL PL01358103A patent/PL358103A1/xx not_active Application Discontinuation
- 2001-03-28 KR KR10-2002-7013230A patent/KR100478793B1/ko not_active Expired - Fee Related
- 2001-03-28 CN CNB018074278A patent/CN1189171C/zh not_active Expired - Fee Related
- 2001-03-28 AT AT01929462T patent/ATE450257T1/de not_active IP Right Cessation
- 2001-03-28 NZ NZ521232A patent/NZ521232A/en unknown
- 2001-03-28 HU HU0300342A patent/HUP0300342A3/hu unknown
- 2001-03-28 YU YU72602A patent/YU72602A/sh unknown
- 2001-03-28 CZ CZ20023625A patent/CZ20023625A3/cs unknown
- 2001-03-28 EP EP01929462A patent/EP1272179B1/de not_active Revoked
- 2001-03-28 CA CA002401910A patent/CA2401910C/en not_active Expired - Fee Related
- 2001-03-28 AU AU2001256227A patent/AU2001256227B2/en not_active Ceased
- 2001-03-28 HR HRP20020777 patent/HRP20020777A2/hr not_active Application Discontinuation
- 2001-03-28 IL IL15164201A patent/IL151642A0/xx unknown
- 2001-03-28 AU AU5622701A patent/AU5622701A/xx active Pending
- 2001-03-28 JP JP2001572101A patent/JP2003528915A/ja not_active Ceased
- 2001-03-28 RU RU2002129571/15A patent/RU2248204C2/ru not_active IP Right Cessation
- 2001-03-28 BR BR0109779-2A patent/BR0109779A/pt not_active Application Discontinuation
- 2001-03-28 WO PCT/EP2001/003502 patent/WO2001074357A1/en not_active Ceased
- 2001-03-30 AR ARP010101538A patent/AR029825A1/es not_active Application Discontinuation
2002
- 2002-08-08 US US10/214,697 patent/US20030004205A1/en not_active Abandoned
- 2002-09-11 ZA ZA200207304A patent/ZA200207304B/en unknown
- 2002-10-01 MA MA26845A patent/MA26888A1/fr unknown
- 2002-10-02 NO NO20024733A patent/NO20024733L/no unknown
2005
- 2005-08-16 US US11/204,614 patent/US20050271721A1/en not_active Abandoned

Also Published As

Publication number	Publication date
CN1189171C (zh)	2005-02-16
RU2248204C2 (ru)	2005-03-20
NO20024733D0 (no)	2002-10-02
CN1420771A (zh)	2003-05-28
PL358103A1 (pl)	2004-08-09
AU5622701A (en)	2001-10-15
NO20024733L (no)	2002-10-02
EP1272179B1 (de)	2009-12-02
YU72602A (sh)	2005-03-15
CA2401910C (en)	2008-04-15
RU2002129571A (ru)	2004-03-27
WO2001074357A1 (en)	2001-10-11
AR029825A1 (es)	2003-07-16
US20050271721A1 (en)	2005-12-08
JP2003528915A (ja)	2003-09-30
HUP0300342A2 (hu)	2003-06-28
HUP0300342A3 (en)	2005-07-28
MA26888A1 (fr)	2004-12-20
EP1272179A1 (de)	2003-01-08
US20030004205A1 (en)	2003-01-02
IL151642A0 (en)	2003-04-10
CZ20023625A3 (cs)	2003-04-16
KR100478793B1 (ko)	2005-03-24
NZ521232A (en)	2004-05-28
HRP20020777A2 (en)	2004-12-31
US20010036959A1 (en)	2001-11-01
CA2401910A1 (en)	2001-10-11
MXPA02009725A (es)	2003-03-27
BR0109779A (pt)	2003-01-21
ATE450257T1 (de)	2009-12-15
DE60140662D1 (de)	2010-01-14
KR20030019339A (ko)	2003-03-06
AU2001256227B2 (en)	2005-09-01

Publication	Publication Date	Title
CA2401910C (en)	2008-04-15	Hydrophilic molecular disperse solutions of carvedilol
AU2001256227A1 (en)	2002-01-03	Hydrophilic molecular disperse solutions of carvedilol
EP1272180B1 (de)	2004-09-29	Konzentrierte lösungen von carvedilol
JP2020513023A (ja)	2020-04-30	ルマテペロンｐ−トシラートの非晶質形態および固体分散体
TWI299994B (en)	2008-08-21	Anti-allergic agent pharmaceutical composition and production method therefor
EA027641B1 (ru)	2017-08-31	Продукт сомикронизации, включающий ацетат улипристала
DE60221683T2 (de)	2008-04-30	Pseudopolymorphe formen von carvedilol
WO2024096838A1 (en)	2024-05-10	A pharmaceutical composition comprising solid dispersion of empagliflozin
KR20230121867A (ko)	2023-08-21	무정형 고체 분산체
CN116963739A (zh)	2023-10-27	无定形固体分散体制剂
WO2024096839A1 (en)	2024-05-10	A pharmaceutical composition comprising solid dispersion of empagliflozin
KR20220095493A (ko)	2022-07-07	경구 생체이용률이 증가된 주석산을 포함하는 카베디롤 함유 고체분산체 및 이의 제조방법
JP2024016309A (ja)	2024-02-07	固体分散体
JP2019515029A (ja)	2019-06-06	アイバカフトールならびにアイバカフトールの塩及び誘導体の複合剤、その製造方法ならびにこれを含有する医薬組成物