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WO2016001843A1 - Comprimés de voglibose à rétention gastrique et à libération prolongée - Google Patents

Comprimés de voglibose à rétention gastrique et à libération prolongée Download PDF

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Publication number
WO2016001843A1
WO2016001843A1 PCT/IB2015/054916 IB2015054916W WO2016001843A1 WO 2016001843 A1 WO2016001843 A1 WO 2016001843A1 IB 2015054916 W IB2015054916 W IB 2015054916W WO 2016001843 A1 WO2016001843 A1 WO 2016001843A1
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WO
WIPO (PCT)
Prior art keywords
voglibose
release
extended
tablet
polymers
Prior art date
Application number
PCT/IB2015/054916
Other languages
English (en)
Inventor
Ravish Sharma
Anuj Kumar Fanda
Kumaravel Vivek
Romi Barat Singh
Original Assignee
Sun Pharmaceutical Industries Limited
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.)
Filing date
Publication date
Application filed by Sun Pharmaceutical Industries Limited filed Critical Sun Pharmaceutical Industries Limited
Publication of WO2016001843A1 publication Critical patent/WO2016001843A1/fr

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Classifications

    • 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
    • A61K31/13—Amines
    • A61K31/133—Amines having hydroxy groups, e.g. sphingosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Definitions

  • the present invention relates to extended-release gastroretentive tablets of voglibose and processes for their preparation.
  • EP Patent No. 1 561 458 discloses an orally rapidly disintegrable solid preparation comprising voglibose, a sugar or sugar alcohol, and a low-substituted hydroxypropyl cellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group.
  • PCT Publication No. WO 2013/115742 discloses a composition comprising voglibose, characterized in that said formulation comprises talc, magnesium stearate, polyethylene glycol, silicon dioxide, sodium benzoate, potassium benzoate, stearic acid, sodium stearyl fumarate and/or a combination thereof as lubricant.
  • PCT Publication No. WO 2013/115741 discloses a composition comprising voglibose, acarbose, or miglitol characterized in that the ratio of bulk density to compressed density of the composition is minimum 0.75, and particle size distribution value of voglibose, acarbose, or miglitol is in the range of 10 to 600 ⁇ .
  • Voglibose Due to the digestion of carbohydrates occurring mostly in the upper jejunum, a post-prandial rise in blood glucose is generally seen within one hour after the start of a meal. Therefore, there is a need to administer voglibose prior to a mealtime to achieve the maximal effect.
  • Voglibose is commercially available as immediate release tablets with a dosage administration of thrice daily just before the start of every meal. Further, the half- life of voglibose is short, thereby necessitating frequent administration, leading to a high level of patient non-compliance.
  • extended-release tablets of voglibose remain highly desirable over immediate-release tablets. Further, prolongation of gastric residence time can be used as one of the ways to design extended-release tablets of voglibose. This helps reduce the inter-subject variability leading to a more predictable bioavailability. It further reduces the number of doses required, leading to enhanced patient compliance.
  • EP Patent No. 1 022 028 discloses a prolonged gastrointestinal residence type preparation of -glucosidase inhibitor, such as voglibose, as a gastrointestinal mucosa- adherent preparation, an intragastric floating preparation, or an intragastric residence preparation utilizing a shape-memory type polymer.
  • the sustained-release oral preparation comprises a matrix of polyglycerol fatty acid ester and/or a lipid.
  • the present invention provides extended-release gastroretentive tablets of voglibose, wherein voglibose is released over a prolonged period of time for enhanced therapeutic efficacy. Further, the tablets of the present invention have a once daily dosage regimen, resulting in improved patient compliance.
  • the present invention relates to extended-release gastroretentive tablets of voglibose and processes for their preparation.
  • compositions of the present invention are a significant advance over conventional immediate-release tablets of voglibose as these compositions provide improved patient compliance to the dosage regimen with optimum clinical benefits.
  • a first aspect of the present invention provides an extended-release gastroretentive tablet of voglibose for once-a-day therapy comprising voglibose and one or more release- controlling polymers.
  • the extended-release gastroretentive tablet of voglibose further comprises one or more water-swellable polymers.
  • the extended-release gastroretentive tablet of voglibose includes an immediate-release layer of the voglibose.
  • a second aspect of the present invention provides a process for the preparation of an extended-release gastroretentive tablet of voglibose, wherein the process comprises:
  • step (i) blending or granulating voglibose with one or more release-controlling polymers, one or more water-swellable polymers, and one or more pharmaceutically acceptable excipients; (ii) compressing the blend or granules of step (i) to form a tablet core; and
  • step (iii) optionally applying a coating composition comprising voglibose, one or more film-forming polymers, and one or more pharmaceutically acceptable coating additives over the tablet core of step (ii).
  • a third aspect of the present invention provides a process for the preparation of an extended-release gastroretentive tablet of voglibose, wherein the process comprises:
  • step (ii) compressing the blend or granules of step (i) to form a tablet core
  • step (iv) applying the coating composition of step (iii) over the tablet core of step (ii);
  • step (v) optionally applying a coating composition comprising voglibose, one or more film-forming polymers, and one or more pharmaceutically acceptable coating additives over the coated tablet core of step (iv).
  • a fourth aspect of the present invention provides a process for the preparation of an extended-release gastroretentive tablet of voglibose, wherein the process comprises:
  • step (ii) compressing the blend or granules of step (i) to form a tablet core
  • step (iv) applying the coating composition of step (iii) over the tablet core of step (ii);
  • step (vi) applying the coating composition of step (v) over the coated tablet core of step (iv);
  • a fifth aspect of the present invention provides a process for the preparation of an extended-release gastroretentive tablet of voglibose, wherein the process comprises:
  • step (iii) compressing the blend or granules of step (i) and the blend or granules of step (ii) to form a bi-layered tablet core;
  • step (v) applying the coating composition of step (iv) over the bi-layered tablet core of step (iii);
  • step (vi) optionally applying a coating composition comprising voglibose, one or more film-forming polymers, and one or more pharmaceutically acceptable coating additives over the coated bi-layered tablet core of step (v).
  • a sixth aspect of the present invention provides a method of treating diabetes by administering once-a-day extended-release gastroretentive tablet of voglibose comprising voglibose and one or more release-controlling polymers.
  • the extended-release gastroretentive tablet of voglibose further comprises one or more water-swellable polymers.
  • the extended-release gastroretentive tablet of voglibose includes an immediate -release layer of the voglibose.
  • voglibose refers to ( ⁇ S,2S,3R,4S,5S)-5-( ⁇ ,3- dihydroxypropan-2-ylamino)- 1 -(hydroxymethyl)cyclohexane- 1 ,2,3 ,4-tetraol . It further includes salts, polymorphs, hydrates, solvates, prodrugs, chelates, and complexes thereof.
  • stomach means that upon oral administration at least a portion of the tablet remains in the stomach for a period that is longer than the normal emptying time from the stomach, i.e., longer than about 2 hours, particularly longer than about 3 hours, and more particularly longer than about 4, 6, 8, or 10 hours.
  • extended-release refers to voglibose release over a prolonged period of time, e.g., more than about 4, 6, 8, 16, or 24 hours following ingestion.
  • immediate-release refers to voglibose release over a short period of time, e.g., within about 1 hour, preferably within about 30 minutes following ingestion.
  • the tablet core of the present invention may be a single layer or a multi-layered tablet core.
  • the layers can be compressed in any order.
  • the extended-release gastroretentive tablets of the present invention may comprise an outer immediate-release layer of voglibose.
  • This outer layer provides the initial burst release of voglibose, and after a predetermined time interval another release of voglibose occurs resulting in a pulsatile delivery.
  • the time interval between the two releases can be controlled by the amount of release-controlling polymer in the extended-release layer and the thickness of the extended-release layer.
  • the extended-release tablets of the present invention utilize a gastroretentive floating system which remains buoyant in the stomach and releases voglibose over a prolonged period of time.
  • the gastroretentive floating systems of the present invention have a floatation time up to 24 hours.
  • water-swellable polymer refers to a polymer which expands upon contact with water. Suitable examples of water-swellable polymers are selected from the group comprising carboxyvinyl polymers (such as those available under the trade name Carbopol ® ); cellulose derivatives e.g., hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, methyl cellulose, sodium carboxymethyl cellulose, hydroxyethylmethyl cellulose, and microcrystalline cellulose; polyethylene derivatives e.g., polyethylene glycol and polyethylene oxide; gums e.g., guar gum, locust bean gum, tragacanth, carrageenan, alginic acid, gum acacia, gum arabic, gellan gum, and xanthan gum; proteins e.g., gelatin, casein, and zein; saccharides e.g., dextrin, dextran,
  • release-controlling polymer refers to a polymer that helps to control the release of voglibose.
  • Suitable examples of release-controlling polymers are selected from the group comprising cellulose derivatives e.g., ethylcellulose, hydroxypropylmethyl cellulose (such as Methocel ® K100), cellulose acetate, cellulose acetate phthalate, cellulose acetate mellitate, cellulose acetate succinate,
  • carboxy vinyl polymers such as those available under the trade name Carbopol ® );
  • polyethylene derivatives e.g., polyethylene oxide
  • gums e.g., guar gum, locust bean gum, tragacanth, carrageenan, alginic acid, gum acacia, gum arabic, gellan gum, and xanthan gum
  • waxes e.g., Compritol ® , Lubritab ® , and Gelucires ®
  • lipids fatty acids or their salts/derivatives
  • a mixture of polyvinyl acetate and polyvinyl pyrrolidone e.g., Kollidon ® SR; and combinations thereof.
  • the percentage of extended-release polymer in the extended-release layer and thickness of the extended-release layer is critical for controlling the release of voglibose.
  • the amount of the extended-release polymer used in the present invention may vary from about 40% to about 90% w/w based on the total weight of the extended release layer.
  • pharmaceutically acceptable excipients refers to excipients that are routinely used in pharmaceutical compositions.
  • suitable examples of pharmaceutically acceptable excipients are selected from the group consisting of binders, diluents, disintegrating agents, lubricants, glidants, osmotic agents, effervescent agents, and combinations thereof.
  • Suitable binders are selected from the group comprising celluloses e.g., methyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, ethyl cellulose, and sodium carboxy methyl cellulose; polymethacrylates;
  • carboxyvinyl polymers e.g., acacia, alginic acid, sodium alginate, tragacanth, and guar gum; sugars e.g., lactose, liquid glucose, sucrose, and dextrin; polydextroses; starch or its derivatives; kaolin; povidone; copovidone; polyethylene oxide; polyvinyl pyrrolidone; polyvinyl alcohol; poly-N-vinyl amide; polyethylene glycol; gelatin;
  • polypropylene glycol polypropylene glycol
  • glyceryl behenate oils e.g., hydrogenated vegetable oil, castor oil, and sunflower oil; zein; paraffin; higher aliphatic alcohols; higher aliphatic acids; fatty acid esters; fatty acid glycerides; agar; chitosan; maltodextrin; magnesium aluminum silicate; inulin; waxes; and mixtures thereof.
  • Suitable diluents are selected from the group comprising microcrystalline cellulose, silicified microcrystalline methyl cellulose, ethyl cellulose, lactose, dibasic or tribasic calcium phosphate, cellulose acetate, confectioner's sugar, compressible sugar, sugar spheres, dextrates, dextrin, dextrose, fructose, maltose, sodium chloride, lactitol, maltitol, xylitol, erythritol, isomalt, sorbitol, maltodextrin, mannitol, sucrose, fructose, glyceryl palmitostearate, semithicone, magnesium aluminum silicate, starch,
  • pregelatinized starch pregelatinized starch, sulfobutylether ?-cyclodextrin, polymethacrylates, talc, trehalose, ammonium alginate, calcium carbonate, calcium silicate, calcium carbonate, magnesium carbonate, magnesium oxide, calcium sulphate, and mixtures thereof.
  • Suitable disintegrating agents are selected from the group comprising cellulose or its derivatives e.g., low-substituted hydroxypropyl cellulose, cross-linked sodium carboxymethyl cellulose, carboxymethyl calcium cellulose, and microcrystalline cellulose; starches e.g., starch, pregelatinized starch, hydroxypropyl starch, sodium carboxymethyl starch, and sodium starch glycolate; ion-exchange resins e.g., polacrillin potassium; gums e.g., guar gum, sodium alginate, calcium alginate, and alginic acid; clays e.g., bentonite and veegum; povidone; cross-linked polyvinyl pyrrolidone; formalin-casein; chitosan; magnesium aluminum silicate; colloidal silicon dioxide; and mixtures thereof.
  • cellulose or its derivatives e.g., low-substituted hydroxypropyl cellulose, cross-linked sodium carboxymethyl
  • Suitable lubricants are selected from the group comprising magnesium stearate, aluminum stearate, calcium stearate, zinc stearate, sodium stearyl fumarate, talc, colloidal silica, polyethylene glycol, polyvinyl alcohol, glyceryl behenate, glyceryl monostearate, glyceryl palmitostearate, potassium benzoate, sodium benzoate, mineral oil, palmitic acid, myristic acid, stearic acid, hydrogenated vegetable oil, hydrogenated soybean oil, stearyl alcohol, leucine, sodium lauryl sulfate, ethylene oxide polymers, poloxamer,
  • octyldodecanol and mixtures thereof.
  • Suitable glidants are selected from the group comprising powdered cellulose, starch, talc, tribasic calcium phosphate, calcium silicate, magnesium silicate, magnesium trisilicate, colloidal silicon dioxide, silicon hydrogels, and mixtures thereof.
  • Suitable osmotic agents are selected from the group comprising water soluble salts of inorganic acids e.g., magnesium chloride, magnesium sulfate, lithium chloride, sodium chloride, potassium chloride, lithium hydrogen phosphate, sodium hydrogen phosphate, potassium hydrogen phosphate, lithium dihydrogen phosphate, sodium dihydrogen phosphate, and potassium dihydrogen phosphate; water soluble salts of organic acids e.g., sodium acetate, potassium acetate, magnesium succinate, sodium benzoate, sodium citrate, and sodium ascorbate; non-ionic organic compounds with high water solubility e.g., carbohydrates such as mannitol, sorbitol, arabinose, ribose, xylose, glucose, fructose, mannose, galactose, sucrose, maltose, lactose, and raffinose; water-soluble amino acids e.g., glycine, leucine, alanine, or methi
  • Effervescent agents comprise an acid source and a base source.
  • a suitable acid source is selected from the group comprising citric acid, fumaric acid, tartaric acid, ascorbic acid, malic acid, acetylsalicylic acid, sodium dihydrogen citrate, disodium hydrogen citrate, nicotinic acid, adipic acid, or mixtures thereof.
  • a suitable base source is selected from the group comprising sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, amino acid-alkali metal carbonate derivatives, and mixtures thereof.
  • the tablet core of the present invention can be prepared by any method known in the art such as by direct compression, dry granulation, wet granulation, or melt granulation.
  • the immediate -release layer of the present invention comprises voglibose, one or more film-forming polymers, and one or more coating additives.
  • Pharmaceutically acceptable coating additives may be selected from the group consisting of binders, diluents, plasticizers, opacifiers, coloring agents, lubricants, and pore -formers.
  • Suitable film-forming polymers are selected from the group comprising cellulose or its derivatives e.g., hydroxypropylmethyl cellulose, hydroxypropyl cellulose, ethyl cellulose, methyl cellulose, carboxymethyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, cellulose acetate, hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, and cellulose acetate trimellitate; waxes e.g., polyethylene glycol; methacrylic acid polymers e.g., Eudragit ® ; and polyvinyl pyrrolidone.
  • coating compositions comprising film-forming polymers marketed under various trade names, such as Opadry ® may also be used.
  • Suitable plasticizers are selected from the group comprising triethyl citrate, dibutyl sebacate, acetylated triacetin, tributyl citrate, glycerol tributyrate, acetyl tributyl citrate, diacetylated monoglyceride, rapeseed oil, olive oil, sesame oil, glycerin, sorbitol, diethyl oxalate, diethyl phthalate, diethyl malate, diethyl fumarate, dibutyl succinate, diethyl malonate, dioctyl phthalate, and combinations thereof.
  • Suitable opacifiers are selected from the group comprising titanium dioxide, manganese dioxide, iron oxide, silicon dioxide, and combinations thereof.
  • Suitable pore-formers are selected from the group comprising polyethylene glycols e.g., polyethylene glycol 6000 and polyethylene glycol 400; celluloses e.g.,
  • polysaccharides e.g., alginates, xanthan gum, chitosan, carrageenan, and dextran;
  • polyalkylene oxides e.g., polyethylene oxide; vinyl acetate copolymers; methacrylic acid copolymers; maleic anhydride/methyl vinyl ether copolymers; carboxyvinyl polymers; and combinations thereof.
  • the present invention also encompasses a seal -coating layer present in between the core and extended-release layer and/or between the extended-release layer and immediate- release layer.
  • the seal-coating layer may also be present as the outermost layer.
  • the seal-coating layer may comprise one or more film-forming polymers, and one or more coating additives.
  • Layering may be performed by applying the coating composition as a solution or suspension using any conventional coating technique known in the art, such as spray coating in a coating pan or fluidized bed processor, or dip coating.
  • Solvents used for wet granulation and for preparing the coating solution or dispersion are selected from the group comprising methylene chloride, isopropyl alcohol, acetone, methanol, ethanol, purified water, ethyl acetate, acetic acid, glycols,
  • dichloromethane dimethylformamide, dimethyl sulfoxide, chloroform, toluene, ethoxyethyl acetate, ethylene glycol monoacetate, ethyl lactate, monoethyl acetate, methyl ethyl ketone, or mixtures thereof.
  • the extended-release gastroretentive tablet of the present invention may further include one or more anti -diabetic drugs such as acarbose, miglitol, metformin, repaglinide, nateglinide, glibenclamide, glimepride, glipizide, gliclazide, chloropropamide, tolbutamide, phenformin, aloglitin, sitagliptin, linagliptin, saxagliptin, rosiglitazone, pioglitazone, troglitazone, faraglitazar, englitazone, darglitazone, isaglitazone, zorglitazone, liraglutide, muraglitazar, peliglitazar, tesaglitazar, canagliflozin, dapagliflozin, remogliflozin, sergliflozin, or any other known anti-diabetic drug
  • Voglibose and polyvinylpyrrolidone were dissolved in purified water to form a solution.
  • step 3 The granules of step 2 were blended with a mixture of crospovidone, carboxyvinyl polymer, and colloidal silica.
  • step 3 The blend of step 3 was lubricated with magnesium stearate.
  • step 4 The lubricated blend of step 4 was compressed into a tablet core.
  • Ethyl cellulose and hydroxypropylmethyl cellulose were dispersed into a solution of purified water and isopropyl alcohol.
  • step 7 The tablet core of step 5 was coated with the dispersion of step 6 to form an
  • Voglibose and hydroxypropylmethyl cellulose were dispersed into a solution of purified water and isopropyl alcohol.
  • step 7 The coated tablet core of step 7 was coated with the dispersion of step 8.
  • hydroxypropylmethyl cellulose, polyvinylpyrrolidone, and colloidal silica were sifted together and mixed.
  • step 2 The mixture of step 1 was blended with magnesium stearate.
  • step 3 The blend of step 2 was compressed into a tablet core.
  • Voglibose and hydroxypropymethyl cellulose were dispersed into a solution of purified water and isopropyl alcohol.
  • step 3 The tablet core of step 3 was coated with the dispersion of step 4. Extended-release layer
  • Polyethylene glycol 6000 and polyethylene glycol 400 were dissolved in purified water to form a solution.
  • step 6 The solution of step 6 was mixed with acetone.
  • step 5 The coated tablet core of step 5 was coated with the dispersion of step 8.
  • Voglibose and hydroxypropylmethyl cellulose were dispersed into a solution of purified water and isopropyl alcohol.
  • step 9 The coated tablet core of step 9 was coated with the dispersion of step 10.
  • Microcrystalline cellulose, carboxyvinyl polymer, hydroxypropymethyl cellulose, polyvinylpyrrolidone, crospovidone, and colloidal silica were sifted together and mixed.
  • step 2 The mixture of step 1 was blended with magnesium stearate.
  • Voglibose and polyvinylpyrrolidone were dissolved in purified water.
  • step 4 The granules of step 4 were blended with colloidal silica and magnesium stearate.
  • step 2 The blends of step 2 and step 5 were compressed into a bi-layered tablet core.
  • Ethyl cellulose and hydroxypropylmethyl cellulose were dispersed into a solution of purified water and isopropyl alcohol.
  • Voglibose and hydroxypropylmethyl cellulose were dispersed into a solution of purified water and isopropyl alcohol.
  • step 8 The coated bi-layered tablet core of step 8 was coated with the dispersion of step 9.
  • Voglibose was mixed with colloidal silicon dioxide and a portion of lactose. 2. Hydroxypropylmethyl cellulose, carboxyvinyl polymer, remaining portion of lactose, crosslinked polyvinylpyrolidone, and magnesium stearate were mixed together.
  • step 1 was blended with the mix of step 2.
  • step 3 The blend of step 3 was compressed into a tablet.
  • Voglibose was mixed with colloidal silicon dioxide and a portion of
  • microcrystalline cellulose microcrystalline cellulose
  • Hydroxypropylmethyl cellulose, carboxyvinyl polymer, remaining portion of microcrystalline cellulose, crosslinked polyvinylpyrolidone, and magnesium stearate were mixed together.
  • step 1 was blended with the mix of step 2.
  • step 3 The blend of step 3 was compressed into a tablet.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
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  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne des comprimés de voglibose à rétention gastrique et à libération prolongée, et des procédés pour leur préparation.
PCT/IB2015/054916 2014-06-30 2015-06-30 Comprimés de voglibose à rétention gastrique et à libération prolongée WO2016001843A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1739/DEL/2014 2014-06-30
IN1739DE2014 2014-06-30

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WO2016001843A1 true WO2016001843A1 (fr) 2016-01-07

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113116846A (zh) * 2019-12-31 2021-07-16 广州玻思韬控释药业有限公司 胃滞留片
CN114081944A (zh) * 2021-10-26 2022-02-25 吉林市国科医工科技发展有限公司 一种用于治疗幽门螺旋杆菌感染的胃漂浮剂

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999026606A2 (fr) * 1997-11-25 1999-06-03 Bayer Aktiengesellschaft FORMULATIONS A LIBERATION LENTE COMPRENANT DES INHIBITEURS DE L'α-GLUCOSIDASE
WO2003045356A1 (fr) * 2000-11-20 2003-06-05 The Procter & Gamble Company Forme de dose pharmaceutique a films multiples
US7776345B2 (en) * 2001-07-04 2010-08-17 Sun Pharma Advanced Research Company Ltd Gastric retention controlled drug delivery system
WO2013115744A1 (fr) * 2012-01-31 2013-08-08 Mahmut Bilgic Procédé de préparation de compositions pharmaceutiques (effervescentes) contenant un inhibiteur de l'apha-glucosidase (p. ex. voglibose et metformine)

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999026606A2 (fr) * 1997-11-25 1999-06-03 Bayer Aktiengesellschaft FORMULATIONS A LIBERATION LENTE COMPRENANT DES INHIBITEURS DE L'α-GLUCOSIDASE
WO2003045356A1 (fr) * 2000-11-20 2003-06-05 The Procter & Gamble Company Forme de dose pharmaceutique a films multiples
US7776345B2 (en) * 2001-07-04 2010-08-17 Sun Pharma Advanced Research Company Ltd Gastric retention controlled drug delivery system
WO2013115744A1 (fr) * 2012-01-31 2013-08-08 Mahmut Bilgic Procédé de préparation de compositions pharmaceutiques (effervescentes) contenant un inhibiteur de l'apha-glucosidase (p. ex. voglibose et metformine)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113116846A (zh) * 2019-12-31 2021-07-16 广州玻思韬控释药业有限公司 胃滞留片
CN113116850A (zh) * 2019-12-31 2021-07-16 广州玻思韬控释药业有限公司 胃滞留片
CN113116845A (zh) * 2019-12-31 2021-07-16 广州玻思韬控释药业有限公司 胃滞留片
CN113116850B (zh) * 2019-12-31 2024-03-19 广州玻思韬控释药业有限公司 胃滞留片
CN113116846B (zh) * 2019-12-31 2024-03-19 广州玻思韬控释药业有限公司 胃滞留片
CN113116845B (zh) * 2019-12-31 2024-03-19 广州玻思韬控释药业有限公司 胃滞留片
CN114081944A (zh) * 2021-10-26 2022-02-25 吉林市国科医工科技发展有限公司 一种用于治疗幽门螺旋杆菌感染的胃漂浮剂

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