EP2101771A2 - Formulation stable de lercanidipine - Google Patents

Formulation stable de lercanidipine

Info

Publication number
EP2101771A2
EP2101771A2 EP07870544A EP07870544A EP2101771A2 EP 2101771 A2 EP2101771 A2 EP 2101771A2 EP 07870544 A EP07870544 A EP 07870544A EP 07870544 A EP07870544 A EP 07870544A EP 2101771 A2 EP2101771 A2 EP 2101771A2
Authority
EP
European Patent Office
Prior art keywords
lercanidipine
dosage form
solid oral
oral dosage
immediate release
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP07870544A
Other languages
German (de)
English (en)
Inventor
Jyothi Lakshmi Gunupati
Nagesh Nanda
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Torrent Pharmaceuticals Ltd
Original Assignee
Torrent Pharmaceuticals Ltd
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 Torrent Pharmaceuticals Ltd filed Critical Torrent Pharmaceuticals Ltd
Publication of EP2101771A2 publication Critical patent/EP2101771A2/fr
Withdrawn legal-status Critical Current

Links

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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • A61K9/1611—Inorganic 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
    • A61K9/16—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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; 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
    • A61K9/2009—Inorganic 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
    • A61K9/205—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
    • 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
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Definitions

  • the invention further relates to lercanidipine adsorbates that are obtainable by said process, as well as pharmaceutical formulations prepared while employing said lercanidipine adsorbates.
  • Lercanidipine is an example of a lipophilic and vasoselective dihydropyridine calcium channel blocker, owing to the lipophilic character of such compounds, considerable concentration occurs in lipid-containing membrane depots. The drug thus concentrated is slowly released from these depots and, subsequently, reach their targets, the L-type calcium channels. This phenomenon explains both the slow onset and the long duration of action of the drug. Owing to the slow onset of action reflex tachycardia is virtually absent. The long duration of action allows satisfactory control of blood pressure in hypertensive patients by means of a single daily dose.
  • the ratio of pharmaceutical active ingredient to adsorbing material according to the invention is in the range from 1 :0.1 to 1 :20, a range from 1 :1 to 1 :10 being particularly preferred.
  • the excipients present in the pharmaceutical composition according to the invention can be diluents such as microcrystalline cellulose, powdered cellulose, lactose, compressible sugar, fructose, dextrates, other sugars such as mannitol, sorbitol, lactitol, sacharose or a mixture thereof, silicified microcrystalline cellulose, calcium hydrogen phosphate, starches, calcium carbonate, calcium lactate or mixtures thereof and if required, other diluents known to person skilled in the art.
  • the excipients include at least one diluent, selected from microcrystalline cellulose and starch.
  • the pharmaceutical composition according to the invention can also comprise binders, such as polyvinyl pyrrolidone, microcrystalline cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, low- substituted hydroxypropyl cellulose, hydroxypropylmethyl cellulose or other cellulose ethers, starch, pregelatinised starch, or polymethacrylate or mixtures of binders and if required, other binders known to person skilled in the art . It is preferred that the excipients include at least one binder selected from povidone and starch.
  • the compressed tablet was film coated.
  • Dissolution Medium a) 0.01 N HCl 5 IOOO mL b) 3.O pH buffer, 100O mL,
  • the dissolution profiles of the tablets prepared as per B. No: 001, 002 and Carmen Tablet, market sample of Lercanidipine Tablets (Manufacturer: Berlin Chemie) are given in the table below:

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention porte sur une forme posologique orale solide stable de lercanidipine à l'aide d'un procédé de préparation d'adsorbats. L'invention porte en outre sur des adsorbats de lercanidipine qui peuvent être obtenus par ledit procédé, ainsi que sur des formulations pharmaceutiques préparées avec lesdits adsorbats de lercanidipine.
EP07870544A 2006-12-06 2007-12-05 Formulation stable de lercanidipine Withdrawn EP2101771A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2004MU2006 2006-12-06
PCT/IN2007/000585 WO2008068777A2 (fr) 2006-12-06 2007-12-05 Formulation stable de lercanidipine

Publications (1)

Publication Number Publication Date
EP2101771A2 true EP2101771A2 (fr) 2009-09-23

Family

ID=39363963

Family Applications (1)

Application Number Title Priority Date Filing Date
EP07870544A Withdrawn EP2101771A2 (fr) 2006-12-06 2007-12-05 Formulation stable de lercanidipine

Country Status (2)

Country Link
EP (1) EP2101771A2 (fr)
WO (1) WO2008068777A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010000856A (es) * 2007-07-23 2010-04-30 Pharmathen Sa Composicion farmaceutica que contiene un antagonista del canal de calcio de tipo dihidropiridina y metodo para la preparacion de la misma.
WO2011161223A2 (fr) 2010-06-23 2011-12-29 Krka, Tovarna Zdravil, D.D., Novo Mesto Formes pharmaceutiques à usage oral comprenant de la lercanidipine et de l'énalapril et leurs sels pharmaceutiquement acceptables
SI2654729T1 (sl) 2010-12-24 2016-08-31 Krka, D.D., Novo Mesto Homogene farmacevtske oralne dozirne oblike, ki obsegajo lerkanidipin in enalapril ali njune farmacevtsko sprejemljive soli skupaj z organsko kislino

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5266581A (en) * 1984-07-04 1993-11-30 Bayer Aktiengesellschaft Solid composition containing dihydropyridine, PVP and PVPP
US20060134212A1 (en) * 2004-09-02 2006-06-22 Forest Laboratories, Inc. Lercanidipine immediate release compositions
AR052918A1 (es) * 2005-02-25 2007-04-11 Recordati Ireland Ltd Clorhidrato de lercanidipina amorfo

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2008068777A3 *

Also Published As

Publication number Publication date
WO2008068777A2 (fr) 2008-06-12
WO2008068777A3 (fr) 2008-12-31

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