WO2016042563A1 - Formulation à libération prolongée de carbamazépine - Google Patents
Formulation à libération prolongée de carbamazépine Download PDFInfo
- Publication number
- WO2016042563A1 WO2016042563A1 PCT/IN2014/000598 IN2014000598W WO2016042563A1 WO 2016042563 A1 WO2016042563 A1 WO 2016042563A1 IN 2014000598 W IN2014000598 W IN 2014000598W WO 2016042563 A1 WO2016042563 A1 WO 2016042563A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- carbamazepine
- pharmaceutical composition
- release
- lubricant
- instamodel
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 52
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 title claims abstract description 47
- 229960000623 carbamazepine Drugs 0.000 title claims abstract description 46
- 238000009472 formulation Methods 0.000 title abstract description 27
- 238000013265 extended release Methods 0.000 title abstract description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 13
- 238000004519 manufacturing process Methods 0.000 claims abstract description 6
- 150000003839 salts Chemical class 0.000 claims abstract description 5
- 238000002156 mixing Methods 0.000 claims description 13
- 239000007787 solid Substances 0.000 claims description 13
- 239000000314 lubricant Substances 0.000 claims description 12
- 229920000642 polymer Polymers 0.000 claims description 12
- 239000011230 binding agent Substances 0.000 claims description 11
- 238000005550 wet granulation Methods 0.000 claims description 7
- 238000001035 drying Methods 0.000 claims description 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 5
- 238000007906 compression Methods 0.000 claims description 5
- 230000006835 compression Effects 0.000 claims description 5
- 239000007888 film coating Substances 0.000 claims description 4
- 238000009501 film coating Methods 0.000 claims description 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 3
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 3
- 235000019359 magnesium stearate Nutrition 0.000 claims description 3
- 238000007873 sieving Methods 0.000 claims description 3
- 229920003081 Povidone K 30 Polymers 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims description 2
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 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
- 229920006316 polyvinylpyrrolidine Polymers 0.000 claims description 2
- 229940045902 sodium stearyl fumarate Drugs 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
- 235000012222 talc Nutrition 0.000 claims description 2
- 229920002554 vinyl polymer Polymers 0.000 claims description 2
- 239000003086 colorant Substances 0.000 claims 1
- 239000003605 opacifier Substances 0.000 claims 1
- 239000002552 dosage form Substances 0.000 abstract description 18
- 238000000034 method Methods 0.000 abstract description 9
- 235000015872 dietary supplement Nutrition 0.000 abstract description 4
- 230000008569 process Effects 0.000 abstract description 3
- 241001465754 Metazoa Species 0.000 abstract description 2
- 239000000654 additive Substances 0.000 abstract description 2
- 230000000996 additive effect Effects 0.000 abstract description 2
- 239000002537 cosmetic Substances 0.000 abstract description 2
- 230000001105 regulatory effect Effects 0.000 abstract description 2
- 229940079593 drug Drugs 0.000 description 19
- 239000003814 drug Substances 0.000 description 19
- 239000003826 tablet Substances 0.000 description 17
- 239000006186 oral dosage form Substances 0.000 description 10
- 206010010904 Convulsion Diseases 0.000 description 9
- 239000008187 granular material Substances 0.000 description 7
- 239000004615 ingredient Substances 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- 239000001961 anticonvulsive agent Substances 0.000 description 6
- 239000002775 capsule Substances 0.000 description 6
- 238000004090 dissolution Methods 0.000 description 5
- 239000011248 coating agent Substances 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- -1 disc Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 206010061334 Partial seizures Diseases 0.000 description 3
- 230000001773 anti-convulsant effect Effects 0.000 description 3
- 229960003965 antiepileptics Drugs 0.000 description 3
- 239000003125 aqueous solvent Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000011159 matrix material Substances 0.000 description 3
- 239000008185 minitablet Substances 0.000 description 3
- 239000008188 pellet Substances 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000007894 caplet Substances 0.000 description 2
- 238000013270 controlled release Methods 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 239000000543 intermediate Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000007912 modified release tablet Substances 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 238000004080 punching Methods 0.000 description 2
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 description 1
- 229910002012 Aerosil® Inorganic materials 0.000 description 1
- 239000004956 Amodel Substances 0.000 description 1
- 102000015427 Angiotensins Human genes 0.000 description 1
- 108010064733 Angiotensins Proteins 0.000 description 1
- 108090000312 Calcium Channels Proteins 0.000 description 1
- 102000003922 Calcium Channels Human genes 0.000 description 1
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 1
- 238000005773 Enders reaction Methods 0.000 description 1
- 208000010228 Erectile Dysfunction Diseases 0.000 description 1
- 229940122957 Histamine H2 receptor antagonist Drugs 0.000 description 1
- 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 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000003741 agents affecting lipid metabolism Substances 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 229940124339 anthelmintic agent Drugs 0.000 description 1
- 239000000921 anthelmintic agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 230000000078 anti-malarial effect Effects 0.000 description 1
- 230000001754 anti-pyretic effect Effects 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 229940127219 anticoagulant drug Drugs 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000003430 antimalarial agent Substances 0.000 description 1
- 239000004599 antimicrobial Substances 0.000 description 1
- 239000000164 antipsychotic agent Substances 0.000 description 1
- 239000002221 antipyretic Substances 0.000 description 1
- 229940125716 antipyretic agent Drugs 0.000 description 1
- 239000003443 antiviral agent Substances 0.000 description 1
- 239000002249 anxiolytic agent Substances 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 229960000074 biopharmaceutical Drugs 0.000 description 1
- 239000002981 blocking agent Substances 0.000 description 1
- 239000000544 cholinesterase inhibitor Substances 0.000 description 1
- 239000008199 coating composition Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 230000001882 diuretic effect Effects 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000009506 drug dissolution testing Methods 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000027119 gastric acid secretion Effects 0.000 description 1
- 229940127208 glucose-lowering drug Drugs 0.000 description 1
- 231100001261 hazardous Toxicity 0.000 description 1
- 239000003485 histamine H2 receptor antagonist Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000004941 influx Effects 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000002572 peristaltic effect Effects 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 239000013557 residual solvent Substances 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 210000003478 temporal lobe Anatomy 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 230000003442 weekly effect Effects 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
- A61K9/20—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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
Definitions
- the present invention relates to a dry ready to use modified release dosage formulation for Carbamazepine dosage forms and its salts and derivati ves thereof, a process for preparing extended release tablet using IN STAMODEL (A43 D00047) manufactured by Ideal Cures Private. Limited Mumbai India thereof also use thereof as additive to animal feeds, foods and food supplements and also cosmetic and pharmaceutical compositions.
- Invention also relates to ready-to-use modi fied release compositions capable of regulating release of Carbamazepine at various dosage strength, a process for production thereof and also use thereof as formulated pharmaceutica l compositions.
- Carbamazepine are indicated for use as an anticonvulsant drug or commonly known as antiepileptic drugs.
- state of art evidence supporting efficacy of carbamazepine as an anticonvulsant was derived from acti ve drug-controlled studies that enrolled, patients, with the many seizure types namely Partial seizures, Generalized tonic-clonic seizures mixed seizures etc.
- Partial seizures w ith complex syrnp- tomatology (psychomotor, temporal lobe) , patients with these seizures appear to show greater improvement than those with other types.
- M i xed seizure patterns which incl ude the above, or other partial or generalized seizures.
- Carbamazepine is administered through so lid dosage form 200 mg twice a day. Increase at weekly intervals by adding up to 200 mg/day using a thrice a day. or quarter a day. regimen until the optima l response is obta ined.
- Dosage genera l ly shou ld not exceed 1000 mg daily in children 1 2 to 1 5 years of age, and 1 200 mg dai ly in patients above 1 5 years of age.
- Carbamazepine is poorly soluble in water leading io erratic dissolution, oral absorption and therefore poor bioavailabil ity (less char 70% ) is olso observed.
- Carbamazepine is a BCS Class-Il drug (Biopharmaceutical Classification System) i.e. Low solubility and H igh permeabi l ity and it is the most widely used as anticonvulsant, anti-epileptic and anti-neuralgic drag. Further as Carbamazepine. has poor solubility in water it leads to erratic d issol ution, on:!
- modified release compositions are developed to provide relatively constant drug plasma levels and sustained efficacy for longer period of time.
- extended and modified release composition is to get required therapeutic concentration of the active in the blood stream and maintain its therapeutic concentration without deviation from strength during specified period.
- Cellulosic matrix based system work by the swelling and gelling function i.e. these polymer swell through influx of liquids and a gel like physical structure is formed which provides extended release effect facilitated by diffusion of the Carbamazepine.
- the object of the present invention is to provide a ready-to-use matrix system and method of preparation for Carbamazepine extended release or modified release for- mulation.
- the present invention provides hydrophilic matrix system based ready to use technology for Modified or Extended Release Formulation of Carbamazepine Hydrochloride using INSTAMODEL (A43 D00047) manufactured and supplied by Ideal Cures Private Limited.
- the present invention also provides method for making ready to use Carbamazepine modified or extended release formulation, involving steps of aqueous granulation,, drying, lubrication and punching of tablets.
- present invention also provides once a day Carbamazepine table dosage form.
- Extended release or modified release tablet formulation cars be in the form of single or multilayer tablets, capsule shaped oral dosage form, caplet, granules, disc, pellets, granules in capsule, mini-tablets in oral dosage form and other possible oral dosage form mean thereof.
- the solid oral dosage form can optionally include one or more pharmaceutically acceptable excipients.
- composition according to the invention in the context of the present invention, is taken to mean the property that the composition according to the invention can be used directly for its purposes by the user by simply dispersi ng it in required quantity of water.
- 'modified release' is in context, of the invention as a way -of active drug delivery where the rate of release of the active drug from the composition i s not ex clusively dependent on the concentration of active drug remaining in the dosage form and / or the solubility of the active drug in the liquid surrounding thexomposiiion, and where the time course with or without respective location of release of active drug from an oral dosage form are chosen to accomplish therapeutic or convenience objectives not offered by conventional dosage forms.
- active drug is selected from Carbamazepine, its intermediates and deri vati ves thereo f
- 'Carbamazepine' is in context of the invention includes its polymorphic forms, the pharmaceutically acceptable salts, inc luding salts esters and pother chemical derivatives or intermediates etc.
- the solid pharmaceutical composition comprises Carbamazepine from 1 to 80 w/w % of dosage form.
- the term 'dosage', 'solid pharmaceutical composition' may include one -or more of tablet, capsule, powder, disc, caplet, granules, pellets, granules in capsule, minitablets, minitablets in capsule, pellets in capsule, sachet and the like.
- the solid pharmaceutica l composition also includes multilayer tablets. The solid pharmaceutical compositions are meant for oral administration.
- tablette includes pharmaceutical compositions of all shapes and sizes, whether coated or uncoated.
- Lubricant of present invention includes but not limited to talc, magnesium stearate, stearic acid, sodium stearyl fumarate and there derivatives thereof.
- Glidant in the context of the present invention, is taken to mean that an ingredient which enhance product flow by reducing inter-particulate friction.
- Glidant can be used in present invention includes but not limited to silicon di-oxide, colloidal silicon dioxide and there derivatives thereof. It is available under several brand names like AEROSIL® and CAB-O-SIL®.
- Solvent in the context of the present invention, is taken to mean ingredient that facilitate mixing of components in wet granulation process.
- Solvent can be used in present invention includes but not limited to Acetone, efhanol, methylene di chloride, isopropyl alcohol, water or their mixture thereof.
- Solvent can be used in present invention includes but not l imited to polyvinyl polymers, Polyvinyl pyrrolidone K30 (PVP K30) and there derivatives thereof.
- the ready to use composition in accordance, with present invention comprise INSTAMODEL (A43 D00047).
- Carbamazepine is formulated with ready to use composition to prepare modified release dosage form.
- di fferent salts, derivatives, polymorphs of Carbamazepine could be combined to achieve ready-to-use composition to achieve extended or modified release dosage form.
- Carbamazepine is blended with the ready to use polymer and aqueous granulated further the granu lated mix ture is compressed to produce a solid formulation.
- the ingredients are blended to form a uniform powder and then compressed with means generally known to skilled in the art.
- Carbamazepine. and INS TAMODEL are blended together with binding agent and thereafter wet granulated and dried. These dried granules are then processed in presence of lubricant and glidant, and thereafter compressed to form appropriate dosage form and finally coated.
- Carbamazepine and INSTAMODEL are blended together with binding agent and thereafter wet granulated and dried. These dried granules are then processed in presence of lubricant and glidant, and . thereafter compressed to form appropriate dosage form and optionally coated.
- This system of formulation uses simple and economic polymers hence, cost effective to the customer.
- Another advantage of the present formulation is its robust and reproducible results for extended release dose form without batch to batch variations. Further by using aqueous solvent system for granulation dosage form does not have any residual solvent or hazardous effect found in many organic solvent based formulations.
- Inventive dosage form may be prepared by blending Carbamazepine, their derivatives or combination thereof along with ready to use composition. Therefore inventive formulation preparation comprise steps as
- inventive dosage form is prepared by blending ready to use composition (Instamodel A43D00047), process blending is performed by , conventional dry blender or a food processor or 'V-blender' or a similar function device. Further Carbamazepine are processed using aqueous sol vent with binder through wet granulation or a similar wet mixing method to generate dosage formulation . Dosage formulation is further dried, sieved and compressed optional ly with addition of lubricant, binder, glidant to form modified release oral dosage form.
- inventive dosage formulations are prepared by blending Carbamazepine along with Instamodel (A43 D00047). I nitial ly all components are blended by conventional dry blending in a food processor or 'V- b!ender' or a similar function device. Other solid oral dosage formulation components like binders, lubricants, glidants, detackifier, excipients can be added to create inventive formulation. Further mixture is then processed with appropriate quantity of aqueous solvent with binder and wet granulated. Obtained sieved granulated is then uniformly mixed with premeasured amount of the lubricant to improve industrial acceptability and oral dosage compression quality. Subsequently uniform mixed inventive formulation is compressed in standard pharmacopoeial equipment to get a controlled release oral dosage formulation of the correct desi red weight and strength.
- hardness of tablets produced is in range of 7 Kg/cm 2 to 15 Kg/cm 2 .
- oral dosage forms produced by inventive composition having human administrate active ingredient is suitable for human use.
- drug suitable for veterinary purpose formulated in accordance with present composition will be suitable for veterinary use.
- Carbamazepine is formulated in oral dosage form for modified or extended release delivery.
- Inventive composition comprises 50, 100, 200, 300 mg or 500 mg of Carbamazepine in plural ity of dosage formulations.
- Controlled release formulation can have combination of one or more additional drugs.
- Suitable APIs that can be used with the present invention include, but are not limited to: andrenergic blocking agent; acetyl-cholin-esterase inhibitor; analgesic or antipyretics; angiotensin modulator; anthelmintic agents; anti anxiety agent; antibacterial; antibiotic; anticoagulant; anticonvulsant; antidepressant; antifungal ; antihistamine; antimalarial; antimicrobial agent; antipsychotic agent; Antiviral agents; blood glucose lowering drug; calcium channel modulator; diuretic; erectile dysfunction; gastric acid secretion inhibitor; histamine H2-receptor antagonist; inhibitor of steroid Type II 5[alpha]- reductase including; lipid regulating agents; selecti ve H l - receptor antagonist; vasodilator; vitamins.
- the dosage formulation for 100,000 (30.00 kg) Tablets of Carbamazepine is prepared using composition as stated in table:- 1 wherein Carbamazepine is 20.0 kg and weighed accordingly, subsequently sieved to get uniformly granu lated powder through 40 mesh scree,. It is noted that other size screen could be used to get simi lar results.
- Sieved Carbamazepine is blended with 7.90 kg of ready to use I nstainodel (A43D00047) in blender for 20 minutes (e.g. RMG granulator).
- Solvent system for wet granulation is prepared by taking 1.2 kg PVP K -30 in 5 kg of water , in RMG granulator in low to medium speed in the duration of 10 minutes followed by 5 minutes of high speed with chopper.
- tray drier or Fluidized bed dryer
- coating suspenstion is prepared in water with sti rrer and mixed for about 45 minutes
- Coated tablets are then dried and packed as per pharmacopoieal guidelines.
- the active ingredient content for present invention is standardized for m sustained release profile is as per table 2
- the drug dissolved profile o f the Reference products and Carbamazepine hav ing dose strength of 200 mg using Instarnodel (A43D00047) formulations are compared:
- the release exponents for the Reference and formulated Carbamazepine is found to be having similar modified release profile indicating a predoin inan tiy di ffusion based drug release mechanism.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention concerne une formulation galénique à libération modifiée sèche prête à l'emploi pour les formes galéniques de carbamazépine et ses sels et dérivés, un procédé de préparation de comprimé à libération prolongée en utilisant de l'INSTAMODEL (A43D00045) fabriqué par Ideal Cures Private Limited Bombay Inde ainsi que son utilisation comme additif à des aliments pour animaux, des aliments et des compléments alimentaires, ainsi que des compositions cosmétiques et pharmaceutiques. L'invention concerne également des compositions à libération modifiée prêtes à l'emploi capables de réguler la libération de carbamazépine à diverses concentrations de dose, un procédé pour les produire et leur utilisation en tant que compositions pharmaceutiques formulées.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IN2014/000598 WO2016042563A1 (fr) | 2014-09-16 | 2014-09-16 | Formulation à libération prolongée de carbamazépine |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IN2014/000598 WO2016042563A1 (fr) | 2014-09-16 | 2014-09-16 | Formulation à libération prolongée de carbamazépine |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2016042563A1 true WO2016042563A1 (fr) | 2016-03-24 |
Family
ID=55532648
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IN2014/000598 WO2016042563A1 (fr) | 2014-09-16 | 2014-09-16 | Formulation à libération prolongée de carbamazépine |
Country Status (1)
Country | Link |
---|---|
WO (1) | WO2016042563A1 (fr) |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20030175353A1 (en) * | 2002-03-14 | 2003-09-18 | Sun Pharmaceutical Industries Limited | Oral controlled drug delivery system |
US20070071819A1 (en) * | 2005-05-30 | 2007-03-29 | Kesarwani Amit K | Multiple unit modified release compositions of carbamazepine and process for their preparation |
-
2014
- 2014-09-16 WO PCT/IN2014/000598 patent/WO2016042563A1/fr active Application Filing
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20030175353A1 (en) * | 2002-03-14 | 2003-09-18 | Sun Pharmaceutical Industries Limited | Oral controlled drug delivery system |
US20070071819A1 (en) * | 2005-05-30 | 2007-03-29 | Kesarwani Amit K | Multiple unit modified release compositions of carbamazepine and process for their preparation |
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