WO2010029575A2 - Formulation de docétaxel lyophilisé à usage parentéral pour système de libération de médicament sécurisé et son procédé de préparation - Google Patents

Formulation de docétaxel lyophilisé à usage parentéral pour système de libération de médicament sécurisé et son procédé de préparation Download PDF

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Publication number
WO2010029575A2
WO2010029575A2 PCT/IN2009/000453 IN2009000453W WO2010029575A2 WO 2010029575 A2 WO2010029575 A2 WO 2010029575A2 IN 2009000453 W IN2009000453 W IN 2009000453W WO 2010029575 A2 WO2010029575 A2 WO 2010029575A2
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WO
WIPO (PCT)
Prior art keywords
docetaxel
formulation
lyophilized
solution
making
Prior art date
Application number
PCT/IN2009/000453
Other languages
English (en)
Other versions
WO2010029575A3 (fr
Inventor
Vishwanath Kannan
Vishwanathan Kash
Original Assignee
Vishwanath Kannan
Vishwanathan Kash
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 Vishwanath Kannan, Vishwanathan Kash filed Critical Vishwanath Kannan
Publication of WO2010029575A2 publication Critical patent/WO2010029575A2/fr
Publication of WO2010029575A3 publication Critical patent/WO2010029575A3/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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof

Definitions

  • the present invention relates to novel docetaxel formulation for parentaral administration for safe drug delivery system and process of making the same, containing docetaxel is an anti-neoplasic drug that has shown a proven efficacy in the treatment of the following carcinomas, such as breast, ovary, non small cells lung cancer, prostate, gastric, the formulation is able to be used as single dose or multi-dose formulations, and to their uses in medicaments.
  • WO 01/72299 which teaches about the composition for oral administration containing docetraxel, carrier such as saturated polyglycolysed glyceroids, modified castor oil, stearate esters, sorbitan esters, fatty acids, glycerides etc,
  • the pre-medication scheme consists of the administration of 8 mg dose of dexametasone during three days.
  • dexamethasone produces adverse reactions on the gastric or gastrointestinal tract.
  • this pre-medication regimen requires a gastro-protective regimen including (cimetidine, ranitidine, omeprazole or lanzoprazole) in order to avoid said gastric injuries produced by the dexametasone administration. Severe fluid retention occurred in 6.5% (6/92) of patients despite use of a 3-day dexamethasone premedication regimen.
  • An important object of the present invention which produce a visible increase in the in the Health System expenses due to high cost and complexity involved by the administration of chemotherapy regimen, to which the pre-medication regimen increase the final total treatment cost.
  • the present invention relates to novel formulations of Docetaxel and process of making thereof, without using Polysorbate or Chremophor to avoid their known toxicological problems. More particularly Modified natural cyclodextrins has been used for our novel formulation, such as glucosyl-alpha-Cyclodextrin & maltosyl-alpha- Cyclodextrin
  • modified cyclodextrins were selected owing to their basket-like structures which have a stronger capacity to encapsulate bulky molecules like docetaxel. Since very less concentrations of the cyclodextrins are required is being achieved, an advantage of minimizing the concentration of the solubilizer so as to make available the API in a considerably large amount with respect to the modified cyclodextrin. This has resulted in the absence of any adverse reactions in the patients who were administered with these novel preparations.
  • the formulation storage will be at room temperature (possibility of include climatic zone 4) and avoiding the special cares requires by cold storage (temperature store between 2°C - 8 0 C). the process of making the formulation comrpsing the following stages,
  • the first formulation is obtained by the lyophilization of Docetaxel in an organic solvent to obtain a cake of pure Docetaxel. This cake can be easily dissolved with an aqueous solution of tensoactives with much less toxicity than Polysorbate.
  • the second formulation is obtained by a two lyophilization steps process in which the first one is the lyophilization of pure Docetaxel to obtain a lyophilized bulk. It is easily soluble in aqueous solutions of tensoactives to provide, under a second lyophilization step, a cake in a vial containing practically no residual solvent, and capable of being dissolved even in only water.
  • Formulations obtained applying these technologies are based on the facility to dissolve Docetaxel API, anhydrous or hydrates, in some solvents that are able of being processed by a lyophilization process to obtain a cake of Docetaxel lyophilized in the first case, or Docetaxel lyophilized together with nonionic tensoactive plus additives in the second case.
  • Docetaxel is obtained as pure active ingredient lyophilized in vials containing only some residual solvent
  • the formulation is accompanied by a diluent that should be combined with the lyophilized Docetaxel in order to obtain a reconstituted solution that upon dilution in normal saline solution or 5% dextrose solution, provide a solution ready for perfusion.
  • a lyophilizate of Docetaxel accompanied by a tensoactive, a pH regulator (citric acid) and an additive to provide structural rigidity to the cake is obtained.
  • the formulation is completed with a solution to reconstitute the cake that could be only Water, normal saline solution, 5% dextrose, or any of them accompanied by some tensoactive.
  • Polysorbate 80 are:
  • Modified natural cyclodextrins is taken in vesel, along with nonionic tensoactive added additives, and a diluents, combined with the lyophilized Docetaxel in order to obtain a reconstituted solution that upon diluted in normal saline solution or 5% dextrose solution,the formulation wherein the modified natural cylcodextrine used is selected from the group of glucosyl-alpha- Cyclodextrin & maltosyl-alpha-Cyclodextrin,

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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne une nouvelle formulation de Docétaxel et son procédé de préparation, sans utiliser de Polysorbate® ou Chremophor® pour éviter leurs effets toxicologiques connus. Le procédé comprend, en particulier, des cyclodextrines naturelles modifiées, avec des tensioactifs non ioniques plus additifs, et un diluant, combinés au Docétaxel lyophilisé pour obtenir une solution reconstituée après dilution dans une solution saline normale ou une solution de dextrose à 5 %.
PCT/IN2009/000453 2008-08-18 2009-08-13 Formulation de docétaxel lyophilisé à usage parentéral pour système de libération de médicament sécurisé et son procédé de préparation WO2010029575A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1744/MUM/2008 2008-08-18
IN1744MU2008 2008-08-18

Publications (2)

Publication Number Publication Date
WO2010029575A2 true WO2010029575A2 (fr) 2010-03-18
WO2010029575A3 WO2010029575A3 (fr) 2010-06-17

Family

ID=42005585

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2009/000453 WO2010029575A2 (fr) 2008-08-18 2009-08-13 Formulation de docétaxel lyophilisé à usage parentéral pour système de libération de médicament sécurisé et son procédé de préparation

Country Status (1)

Country Link
WO (1) WO2010029575A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110755371A (zh) * 2018-07-25 2020-02-07 比卡生物科技（广州）有限公司 一种注射用多西他赛组合物及其制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0605753A1 (fr) * 1992-11-27 1994-07-13 Ensuiko Sugar Refining Company, Limited Complexe d'inclusion du taxol, procédé pour sa préparation et utilisation
EP0639380A1 (fr) * 1993-08-19 1995-02-22 Ensuiko Sugar Refining Company, Limited Produits d'inclusion du taxol dans la cyclodextrine, leur préparation et application

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0605753A1 (fr) * 1992-11-27 1994-07-13 Ensuiko Sugar Refining Company, Limited Complexe d'inclusion du taxol, procédé pour sa préparation et utilisation
EP0639380A1 (fr) * 1993-08-19 1995-02-22 Ensuiko Sugar Refining Company, Limited Produits d'inclusion du taxol dans la cyclodextrine, leur préparation et application

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110755371A (zh) * 2018-07-25 2020-02-07 比卡生物科技（广州）有限公司 一种注射用多西他赛组合物及其制备方法
CN110755371B (zh) * 2018-07-25 2021-08-31 比卡生物科技（广州）有限公司 一种注射用多西他赛组合物及其制备方法

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Publication number Publication date
WO2010029575A3 (fr) 2010-06-17

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