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WO2006038217A1 - Systeme ameliore d’administration de medicaments a base de bromhydrate de citalopram et processus de production dudit systeme - Google Patents

Systeme ameliore d’administration de medicaments a base de bromhydrate de citalopram et processus de production dudit systeme Download PDF

Info

Publication number
WO2006038217A1
WO2006038217A1 PCT/IN2004/000308 IN2004000308W WO2006038217A1 WO 2006038217 A1 WO2006038217 A1 WO 2006038217A1 IN 2004000308 W IN2004000308 W IN 2004000308W WO 2006038217 A1 WO2006038217 A1 WO 2006038217A1
Authority
WO
WIPO (PCT)
Prior art keywords
delivery system
drug delivery
pellets
capsule
process according
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.)
Ceased
Application number
PCT/IN2004/000308
Other languages
English (en)
Inventor
V. S. Iyer
Satya Chetlapalli Srinivas
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.)
Strides Pharma Science Ltd
Original Assignee
Strides Arcolab 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 Strides Arcolab Ltd filed Critical Strides Arcolab Ltd
Priority to PCT/IN2004/000308 priority Critical patent/WO2006038217A1/fr
Publication of WO2006038217A1 publication Critical patent/WO2006038217A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose

Definitions

  • This invention in general relates to an improved drug delivery system of Citalopram hydrobromide and process for producing the same. More particularly the invention provides for devising pellets formulation of Citalopram hydrobromide and disposing the same into a capsule and a process for producing the same.
  • Citalopram hydrobromide belongs to a general class of antianxiety and antidepressant drugs. It is highly selective and potent serotonin reuptake inhibitor with minimal effects on the neuronal reuptake of norepinephrine and dopamine. The ability of citalopram to potentiate serotonergic activity in the central nervous system via inhibition of the neuronal reuptake of serotonin is thought to be responsible for its antidepressant action.
  • the prior art discloses many systems for the delivery of citalopram hydrobromide such as film-coated tablets, hard gelatin capsules, sustained release tablets etc.
  • WO 01/22941A1 discloses melt granulated composition and modified release dosage form prepared from said composition by one (or) more hydrophilic cellulose other polymers or a hydrophilic melt binder and (or) a therapeutically active ingredient.
  • NAD 299 a second component (b) which is citalopram, as the racemate or an enantiomer thereof in the form of its free base, or a pharmaceutically acceptable salt and/or solvate thereof, the preparation thereof, pharmaceutical formulations containing said composition, use of and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition as well as a kit containing said composition.
  • tablets or capsules are generally made either by granulation method or direct compression method. In both the methods, the dust generation during the process is very high. Being a potent drug, even in low dosage, exposure for longer period may cause unnecessary side effects for the people who are working in the manufacturing of the medicament.
  • an improved drug delivery system wherein the system comprises pellets of Citalopram hydrobromide disposed into a capsule whereby the system enables better bioavailability due to homogeneous distribution of the drug.
  • a process for producing pellets of citalopram hydrobromide comprises, solubilising Citalopram hydrobromide in a mixture of isopropyl alcohol and water to make a homogeneous solution and stirring the same for 10 to 15 minutes after adding fillers, binders, glidants, plastcizers and spraying uniformly on neutral pellets. This provides better content uniformity than conventional dosage forms and avoids dust generation.
  • Another embodiment of the present invention provides a process for producing pellets of citalopram hydrobromide, wherein the process comprises mixing Citalopram hydrobromide with suitable excipients like fillers, binders, glidants, plastcizers, and passing the same through spheronizer to form pellets.
  • a process for producing sustained release pellets of citalopram hydrobromide comprising mixing Citalopram hydrobromide with suitable excipients and passing the same through spheronizer to make pellets and coating the pellets with suitable polymer, selected from a group comprising, hydroxy propyl methyl cellulose, cellulose derivatives, methacrylic acid copolymer, ethyl cellulose, sodium alginate, guar gum, xanthan gum, carbopol, alginate derivative or a mixture thereof, to get desired drug release profile.
  • suitable polymer selected from a group comprising, hydroxy propyl methyl cellulose, cellulose derivatives, methacrylic acid copolymer, ethyl cellulose, sodium alginate, guar gum, xanthan gum, carbopol, alginate derivative or a mixture thereof, to get desired drug release profile.
  • an improved drug delivery system wherein the pellets formed by the above process are disposed in a capsule.
  • the present invention aims at providing an improved drug delivery system and process for producing the same.
  • the system is a capsule, which contains pellets form of citalopram hydrobromide.
  • the capsule disclosed in the invention can be any kind of capsule like hard gelatin or soft gelatin capsule.
  • the pellets used for filling in the capsules are immediate release pellets or sustained release pellets.
  • the pellets, which are to be sprayed with the active substance can be neutral pellets.
  • the quantity of the pellets is not essential for the present invention and may vary between approximately 20 to 88%.
  • the pellets coated with active substance are produced by dissolving the active in a solubiliser and mixing with other pharmaceutically acceptable excipients, which include fillers, binders, glidants, plastcizers etc. and spraying on non-pareil seeds. Pellet layering is done by spray coating/layering equipment.
  • the active substance Before the pellets are sprayed, the active substance may be mixed with further components.
  • Such components can be filler, binder, glidants, plastcizers, alone or in mixtures.
  • the solubiliser used in the present invention is selected from a group comprising, Isopropyl alcohol, ethanol, methylene chloride, purified water, acetone or mixture thereof.
  • the percentage range of solubiliser is varied from 10 to 90%.
  • the surface area of the drug is increased to a large extent in comparison to other oral dosage forms because fine particles of drug are coated on pellets due to which solubility of the drug increases.
  • the diluents / filler used in the invention can be selected from the group comprising, cellulose derivatives, lactose, maize starch, modified starch, pregelatinised starch, partially hydrolysed starch, calcium salts, magnesium salts, maltodextrin, sorbitol, mannitol, sucrose, mannose etc. Concentration of the diluents / fillers can vary from 1.0 to 75%.
  • Plasticizers used in the invention are selected from the group comprising, triacetin, polyetheylene glycol, propylene glycol, diethyl phthalate, castor oil alone or mixture thereof.
  • concentration of the plasticizers can vary from 0.1 to 38%.
  • the binder used in the invention is selected from starch derivatives, Povidone, gelatin.
  • the concentration of the binder can range from 0.5 % to 20%.
  • Another process to prepare a pellet of citalopram hydrobromide comprises, mixing citalopram hydrobromide with suitable pharmaceutical excipients disclosed above and passing through a spheronizer to form immediate release pellets which can be encapsulated in a capsule to provide improved drug delivery system.
  • pellets form containing citalopram hydrobromide are coated with suitable polymers to achieve desired release profile.
  • the polymer used is selected from a group comprising hydroxy propyl methyl cellulose, cellulose derivatives, Methacrylic acid copolymer, ethyl cellulose, sodium alginate, guar gum, xanthan gum, carbopol, alginate derivative, alone or in combination thereof.
  • the concentration of the polymers can vary from 2.0 to 65.0%.
  • the most preferred polymer is ethyl cellulose.
  • the viscosity of the ethyl cellulose can vary from 5 cps to 100 cps.

Landscapes

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

Abstract

La présente invention a pour objet un système amélioré d’administration de médicaments à base de bromhydrate de citalopram ainsi qu’un procédé destiné à produire ledit système. Le système d’administration de médicaments comprend une formulation sous forme de pellet dudit médicament inséré dans une gélule.
PCT/IN2004/000308 2004-10-05 2004-10-05 Systeme ameliore d’administration de medicaments a base de bromhydrate de citalopram et processus de production dudit systeme Ceased WO2006038217A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/IN2004/000308 WO2006038217A1 (fr) 2004-10-05 2004-10-05 Systeme ameliore d’administration de medicaments a base de bromhydrate de citalopram et processus de production dudit systeme

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2004/000308 WO2006038217A1 (fr) 2004-10-05 2004-10-05 Systeme ameliore d’administration de medicaments a base de bromhydrate de citalopram et processus de production dudit systeme

Publications (1)

Publication Number Publication Date
WO2006038217A1 true WO2006038217A1 (fr) 2006-04-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2004/000308 Ceased WO2006038217A1 (fr) 2004-10-05 2004-10-05 Systeme ameliore d’administration de medicaments a base de bromhydrate de citalopram et processus de production dudit systeme

Country Status (1)

Country Link
WO (1) WO2006038217A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019074464A3 (fr) * 2017-10-09 2019-05-31 Montero Gida Sanayi Ve Ticaret Anonim Sirketi Combinaison pharmaceutique comprenant de la dapoxétine et de la phosphodiestérase de type 5
CN120361104A (zh) * 2025-06-27 2025-07-25 杭州胡庆余堂药业有限公司 一种中药组合物在制备预防或治疗结肠炎药物中的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000015219A1 (fr) * 1998-09-16 2000-03-23 Astrazeneca Ab Nouvelle composition
WO2001080619A2 (fr) * 2000-08-10 2001-11-01 H. Lundbeck A/S Composition pharmaceutique contenant du citalopram

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000015219A1 (fr) * 1998-09-16 2000-03-23 Astrazeneca Ab Nouvelle composition
WO2001080619A2 (fr) * 2000-08-10 2001-11-01 H. Lundbeck A/S Composition pharmaceutique contenant du citalopram

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019074464A3 (fr) * 2017-10-09 2019-05-31 Montero Gida Sanayi Ve Ticaret Anonim Sirketi Combinaison pharmaceutique comprenant de la dapoxétine et de la phosphodiestérase de type 5
CN120361104A (zh) * 2025-06-27 2025-07-25 杭州胡庆余堂药业有限公司 一种中药组合物在制备预防或治疗结肠炎药物中的应用

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