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WO2018109731A1 - Compositions pharmaceutiques de taxane et de ses dérivés - Google Patents

Compositions pharmaceutiques de taxane et de ses dérivés Download PDF

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Publication number
WO2018109731A1
WO2018109731A1 PCT/IB2017/057981 IB2017057981W WO2018109731A1 WO 2018109731 A1 WO2018109731 A1 WO 2018109731A1 IB 2017057981 W IB2017057981 W IB 2017057981W WO 2018109731 A1 WO2018109731 A1 WO 2018109731A1
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Prior art keywords
composition
ready
cyclodextrin
pharmaceutical composition
beta
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Ceased
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PCT/IB2017/057981
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English (en)
Inventor
Mohan MAILATUR SIVARAMAN
Hiren Patel
Bhaveshkumar VALLABHBHAI PATEL
Raghu KANNEKANTI
Mohammad RAHEESH
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Orbicular Pharmaceutical Technologies Private Ltd
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Orbicular Pharmaceutical Technologies Private Ltd
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Publication date
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Publication of WO2018109731A1 publication Critical patent/WO2018109731A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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

Definitions

  • the present invention relates to pharmaceutical compositions of taxane and its derivatives, cyclodextrins derivative, wherein the composition is free of surfactants and glycols.
  • a taxane is a type of mitotic inhibitor and a type of antimicrotubule agent. They are used to treat cancer. Taxanes interfere with microtubules (cellular structures that help move chromosomes during mitosis). Taxanes include a class of chemotherapy compounds that includes paclitaxel, docetaxel and cabazitaxel. As antimicrotubule agents, taxanes inhibit the normal process of reorganisation of the microtubule network essential for cellular function, which leads to of mitosis (cell division).
  • Taxane derivatives such as paclitaxel, docetaxel and cabazitaxel are well known and established drugs in the treatment of malignant tumors.
  • paclitaxel is marketed by Bristol-Myers-Squibb under the trade name Taxol®
  • docetaxel is marketed by Sanofi-Aventis under the trade name Taxotere ®
  • cabazitaxel is marketed under the trade name Jevtana ® Kit.
  • the low solubility of paclitaxel, docetaxel and cabazitaxel are well documented and is the major cause for preparation of the formulation for injection containing surfactant.
  • polyethoxylated castor oils as suitable surfactants respectively.
  • Taxotere ® The currently marketed formulation of Taxotere ® is fairly complicated in manufacturing as it involves preparation of a solution of docetaxel in polysorbate 80 and ethanol with subsequent evaporation of ethanol and filling of the viscous solution. This process requires special equipment in term of evaporation, filtration and filling.
  • the marketing composition of docetaxel is complicated to
  • Jevtana is supplied as a kit comprising of drug with surfactant polysorbate 80 and other diluent vial comprising ethanol in water for injection.
  • the drug vials prior to use has to be reconstituted with the diluent vial making sure that the polysorbate 80 is properly reconstituted but without significant foaming.
  • This solution then has to be further diluted by injection of the appropriate amount of solution into an infusion bag.
  • the currently marketed formulation contains an overfill for both the drug vial and the solvent vial. Thus apart from the handling this implies a risk for the proper dosing to the patient.
  • compositions comprising taxanes with cyclodextrins have been disclosed.
  • WO2014122498 A1 publication discloses lyophilized and liquid composition comprising cabazitaxel and sulfobutyl ether beta cyclodextrins, wherein the composition exhibited desirable stability in aqueous media, without need of ethanol and surfactants.
  • composition comprising, a taxane complexed with a beta-cyclodextrin or beta- cyclodextrin derivative, a low molecular weight polyethylene glycol, an alcohol suitable for parenteral administration, and water.
  • composition comprising cabazitaxel, at least one solubilizer such as
  • polyethylene glycol and a solvent such as ethanol.
  • the present invention relates to a pharmaceutical composition
  • a pharmaceutical composition comprising taxane or its derivatives, cyclodextrins derivative, and optionally with other pharmaceutically acceptable excipients, wherein the composition is free of surfactants and glycols.
  • Taxane or its derivatives include paclitaxel, docetaxel, cabazitaxel, its derivatives or any mixtures thereof.
  • cyclodextrins derivative include but not limited to beta-cyclodextrin, gama - cyclodextrin, hydxoxyalkyl-beta-cyclodextrin, hydxoxypropyl-beta-cyclodextrin, hydroxypropyl-gama-cyclodextrin, dimethyl-beta-cyclodextrin, methylated-beta- cyclodextrin, carboxymethyl-beta-cyclodextrin, sulfoalkyl-beta-cyclodextrin, sulfobutylether-beta-cyclodextrin, modified cyclodextrins and its derivatives or any mixtures thereof; optionally other excipients include but not limited to acidifying agent/ pH modifier, chelating agent, solvent/ co-solvent, tonicity modifier, antioxidant/preservative or any mixtures thereof.
  • compositions wherein, the composition is free of surfactants such as polyethoxylated sorbitan fatty ester such as polysorbate 80, polyethoxylated castor oils its derivatives or mixtures thereof, glycols such as polyethylene glycol, propylene glycol and the like or any mixtures thereof.
  • surfactants such as polyethoxylated sorbitan fatty ester such as polysorbate 80, polyethoxylated castor oils its derivatives or mixtures thereof, glycols such as polyethylene glycol, propylene glycol and the like or any mixtures thereof.
  • composition according to the present invention is lyophilized composition, liquid composition, ready to dilute, ready to use, ready to infuse compositions and the like.
  • compositions comprising paclitaxel, docetaxel, cabazitaxel or its derivatives, cyclodextrins derivative, and optionally with other pharmaceutically acceptable excipients, the composition is free of surfactants.
  • composition wherein it increases rate of administration and reduced administration duration to the patient, wherein the composition comprises of taxane or its derivatives, cyclodextrins derivative, and optionally pharmaceutically acceptable excipients, the composition is free of surfactants and glycols; the pharmaceutical
  • composition is lyophilized composition, liquid composition, ready to dilute, ready to use, ready to infuse compositions, wherein composition is in the concentration of about 0.1 mg/ml_ to about 7.0 mg/ml_.
  • Another aspect relates to a pharmaceutical composition with increased rate of administration and reduced administration duration to the patient, wherein
  • composition comprises of cabazitaxel or its pharmaceutically
  • composition is free of surfactants and glycols
  • the pharmaceutical composition is lyophilized composition, liquid
  • composition ready to dilute, ready to use, ready to infuse compositions; d. the composition is in the concentration of about 0.1 mg/ml_ to about 7.0 mg/ml_.
  • Another aspect relates to the pharmaceutical composition according to the above embodiments is used to treat cancer, carcinoma or malignant disease such as carcinoma of the ovary, prostate cancer, breast cancer, and related conditions thereof.
  • the present invention relates to a pharmaceutical composition
  • a pharmaceutical composition comprising taxane or its derivatives, cyclodextrins derivative, and
  • Taxane or its derivatives include paclitaxel, docetaxel, cabazitaxel, its derivatives or any mixtures thereof.
  • the present invention relates to pharmaceutical composition comprising paclitaxel, or pharmaceutically acceptable salts thereof with at least one cyclodextrins derivative, optionally with other pharmaceutically acceptable excipients, and wherein the composition is free of surfactants and glycols.
  • the present invention relates to pharmaceutical composition
  • pharmaceutical composition comprising docetaxel, or pharmaceutically acceptable salts thereof with at least one cyclodextrins derivative, optionally with other pharmaceutically acceptable excipients, and wherein the composition is free of surfactants and glycols.
  • the present invention relates to pharmaceutical composition
  • pharmaceutical composition comprising cabazitaxel, or pharmaceutically acceptable salts thereof with at least one cyclodextrins derivative, optionally with other pharmaceutically acceptable excipients, and wherein the composition is free of surfactants and glycols.
  • active ingredient refers to a substance that has a physiological effect when ingested or otherwise introduced into the body, in particular or a chemical substance used in the treatment, cure, prevention, or diagnosis of disease or used to otherwise enhance physical or mental well- being.
  • excipient or “pharmaceutically acceptable excipient” or “adjuvant” means a component of a pharmaceutical product that is not a pharmacologically active ingredient, such as diluent, bulking agent, carrier, acidifying agent, pH modifier, chelating agent, solvent, co-solvent, tonicity modifier, antioxidant, preservative and the like added to a drug to increase or aid its effect.
  • a pharmacologically active ingredient such as diluent, bulking agent, carrier, acidifying agent, pH modifier, chelating agent, solvent, co-solvent, tonicity modifier, antioxidant, preservative and the like added to a drug to increase or aid its effect.
  • compositions are generally safe, non- toxic, and neither biologically nor otherwise undesirable, and are acceptable for veterinary use as well as human pharmaceutical use.
  • the term includes one or more excipients or adjuvants.
  • composition is intended to encompass a combination including active ingredients and pharmaceutically acceptable excipients, as well as any product which results, directly or indirectly, from combination, complexation, or aggregation of any two or more of the ingredients, or from dissociation of one or more of the ingredients, or from other types of reactions or interactions involving one or more of the ingredients.
  • composition refers to finished pharmaceutical products that are suitable for administration, including, but not limited to, injections, etc.
  • composition relates to aqueous compositions and or its related compositions as known in the art.
  • Stability or “stable” as used herein includes both physical and chemical stability. Stability parameters include but not limited to potency, stable pH value and other physico-chemical parameters.
  • Carrier or “vehicle” or “solvent” as used herein refers to
  • pharmacologically inert materials that provide a more or less fluid matrix, suitable for topical drug administration.
  • Carriers and vehicles useful herein include any such materials known in the art, which are nontoxic and do not interact with other components of a pharmaceutical formulation or drug delivery system in a deleterious manner.
  • the formulations of the present invention are particularly suitable for parenteral administration.
  • Formulations suitable for parenteral dosage forms such as injectable like intravenous, intramuscular or subcutaneous, implants and the like.
  • Other parenteral ingredients used in the formulation are generally those commonly used and recognized by persons skilled in the art of parenteral formulations.
  • “Pharmaceutically-acceptable salts” refer to derivatives of the disclosed compounds wherein the parent compound is modified by making acid or base salts, solvate, hydrate, esters and the like thereof.
  • Pharmaceutically-acceptable salt forms of compounds provided herein are synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods.
  • Pharmaceutically acceptable salts are those forms of compounds, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit/risk ratio.
  • the pharmaceutical composition comprises of cyclodextrins derivative as one of the component which will form an inclusion complex with the taxane or its derivative.
  • cyclodextrins derivative as one of the component which will form an inclusion complex with the taxane or its derivative.
  • This theory has been disclosed in Ren et al., US848151 1 B2 and US8765716 B2 that current study showed that application of cyclodextrin inclusion technology can not only enhance docetaxel stability, enhance its solubility, but also can significantly enhance the drug activity and reduce toxic and side effects, which publications are incorporated herein in their entirety.
  • compositions of the present invention would form inclusion complexes of paclitaxel, docetaxel, and cabazitaxel with cyclodextrins derivatives.
  • Cyclodextrins derivatives include but not limited to beta-cyclodextrin, gama -cyclodextrin, hydxoxyalkyl-beta-cyclodextrin, hydxoxypropyl-beta- cyclodextrin, hydroxypropyl-gama-cyclodextrin, dimethyl-beta-cyclodextrin, methylated-beta-cyclodextrin, carboxymethyl-beta-cyclodextrin, sulfoalkyl-beta- cyclodextrin, sulfobutyl-ether-beta-cyclodextrin (SBECD), modified cyclodextrins or its derivatives or any mixtures thereof.
  • Pharmaceutically acceptable excipient includes acidifying agent, pH modifier, chelating agent, solvent, co-solvent, tonicity modifier, antioxidant, preservative and the like or any mixtures thereof.
  • Acidifying agents or pH modifier include but not limited to ascorbic acid, boric acid, citric acid, tartaric acid, lactic acid, oxalic acid, formic acid, benzene sulphonic acid, benzoic acid, maleic acid, malonic acid, glutamic acid, succinic acid, aspartic acid, diatrizoic acid, acetic acid and the like or mixtures thereof.
  • Chelating agent include but not limited to ethylene diamine tetraacetic acid (EDTA) and acceptable salts thereof, ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA) and acceptable salts thereof, and 8- Amino-2-[(2-amino-5-methylphenoxy) methyl]-6-methoxyquinoline-N,N,N',N'- tetraacetic acid, tetrapotassium salt (QUIN-2) and acceptable salts thereof.
  • EDTA ethylene diamine tetraacetic acid
  • EGTA ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid
  • QUIN-2 8- Amino-2-[(2-amino-5-methylphenoxy) methyl]-6-methoxyquinoline-N,N,N',N'- te
  • Solvent or co-solvent include but not limited to alkanols, water; lower alkanols like C1 - C4 alkanols; it includes ethanol, dehydrated alcohol, absolute alcohol and the like or any mixtures thereof.
  • Tonicity modifier include those commonly used in the parenteral preparations but not limited to sodium chloride, dextrose, mannitol, glycerol and the like or any mixtures thereof.
  • Antioxidant or preservative include but not limited to ascorbic acid, acetylcysteine, sulfurous acid salts (bisulfite, metabisulfite), monothioglyercol, phenol, metacresol, benzyl alcohol, parabens (methyl, propyl, butyl), benzalkonium chloride, chlorobutanol, thimerosal and the like or any mixtures thereof.
  • composition is free of surfactants such as polyethoxylated sorbitan fatty ester such as polysorbate 80 its derivatives or mixtures thereof, polyethoxylated castor oils its derivatives or mixtures thereof, glycols such as polyethylene glycol, propylene glycol and the like or any mixtures thereof.
  • surfactants such as polyethoxylated sorbitan fatty ester such as polysorbate 80 its derivatives or mixtures thereof, polyethoxylated castor oils its derivatives or mixtures thereof, glycols such as polyethylene glycol, propylene glycol and the like or any mixtures thereof.
  • the pharmaceutical composition is lyophilized composition, liquid composition, ready to dilute, ready to use, ready to infuse compositions and the like.
  • the pharmaceutical composition comprising taxane include liquid composition, ready to dilute, ready to use, ready to infuse compositions can be diluted with a suitable diluent before administration.
  • the pharmaceutical composition is a ready to use and/or ready to infuse formulation.
  • a ready to use composition is a formulation that is suitable for administration with or without further dilution.
  • the pharmaceutical composition is a ready to dilute formulation.
  • a ready to dilute composition is a formulation that is suitable for administration after dilution with a suitable diluent.
  • Suitable diluents include, but are not limited to, water, saline, dextrose, water for injection and the like or mixtures thereof.
  • the lyophilized powder comprising of the taxane can also be reconstituted directly with a suitable diluent before administration.
  • Suitable diluents include, but are not limited to, water, saline, dextrose, and water for injection.
  • pharmaceutical composition comprises of taxane and cyclodextrins derivative.
  • composition comprises of paclitaxel and cyclodextrins derivative.
  • composition comprises of docetaxel and cyclodextrins derivative.
  • composition comprises of cabazitaxel and cyclodextrins derivative.
  • pharmaceutical composition comprises of taxane, a cyclodextrins derivative, and optionally acidifying or buffering agent.
  • composition comprises of paclitaxel, cyclodextrins derivative and optionally acidifying or buffering agent.
  • composition comprises of docetaxel, cyclodextrins derivative and optionally acidifying or buffering agent.
  • pharmaceutical composition comprises of cabazitaxel, cyclodextrins derivative and optionally acidifying or buffering agent.
  • pharmaceutical composition comprises of taxane, cyclodextrins derivative, optionally acidifying or buffering agent and chelating agent.
  • composition comprises of paclitaxel, cyclodextrins derivative, optionally acidifying or buffering agent and chelating agent.
  • composition comprises of docetaxel, cyclodextrins derivative, optionally acidifying or buffering agent and chelating agent.
  • composition comprises of cabazitaxel, cyclodextrins derivative, optionally acidifying or buffering agent and chelating agent.
  • composition comprises of paclitaxel, sulfobutylether ⁇ -cyclodextrin, optionally acidifying or buffering agent and chelating agent.
  • composition comprises of docetaxel, sulfobutylether ⁇ -cyclodextrin, optionally acidifying or buffering agent and chelating agent.
  • composition comprises of
  • cabazitaxel sulfobutylether ⁇ -cyclodextrin, optionally acidifying or buffering agent and chelating agent.
  • compositions have a pH between about 2 to about 8, example between about 2.5 to about 7.5.
  • compositions the process includes:
  • taxane or its derivatives is taken and mixed with suitable solvent; c) the above drug solution is added to the cyclodextrins solution and mixed, optionally acidifying agent or pH modifier or chelating agent may be added;
  • compositions the process includes:
  • step b) cabazitaxel or its derivatives is taken and mixed with suitable solvent; c) the above drug solution of step b) is added to the cyclodextrins
  • the concentration of taxanes used in the composition is between about 0.1 mg/ml_ to about 7.0mg/ml_.
  • the concentration of paclitaxel used in the composition is between about 0.1 mg/ml_ to about 7.0mg/ml_.
  • the concentration of docetaxel used in the composition is between about 0.1 mg/mL to about 7.0mg/ml_.
  • the concentration of cabazitaxel used in the composition is between about 0.1 mg/mL to about 7.0mg/ml_.
  • composition which includes increased rate of administration and reduced administration duration to the patient, wherein the composition comprises of taxane or its derivatives, cyclodextrins derivative, and optionally pharmaceutically acceptable excipients, the composition is free of surfactants and glycols.
  • the taxane is administered
  • intravenously as part of an intravenous infusion.
  • Contemplated infusion volumes are preferably less, with each volume varying about +/-10% or +/-15% being preferred in some aspects.
  • the intravenous administration volume is suitable for IV bolus administration and may also include an amount of pharmaceutically acceptable diluent. As such, smaller volumes are required to deliver therapeutic doses to patients and the patients are spared exposure to excess fluid and sodium during therapy.
  • Another aspect relates to a pharmaceutical composition with increased rate of administration and reduced administration duration to the patient, wherein
  • composition comprises of cabazitaxel or its pharmaceutically
  • composition is free of surfactants and glycols
  • the pharmaceutical composition is lyophilized composition, liquid
  • composition ready to dilute, ready to use, ready to infuse compositions; d. the composition is in the concentration of about 0.1 mg/ml_ to about 7.0 mg/ml_.
  • composition would allow to increase rate of administration and reduced administration duration to the patient when compared to the existing formulations, hence thereby providing ease of administration to the patients depending on these type of compositions.
  • composition would reduce the handling difficulties and reconstitution challenges. Ready to use and/or ready to dilute compositions will minimize dosing errors resulting from reconstitution steps. Hence, ready to use and/or ready to dilute compositions reduce the time required for administration.
  • the present innovative composition being aqueous would reduce administration of high toxic excipients, thereby providing higher concentration of the drug in lower volumes, increase rate of administration and reduced administration duration to the patient when compared to the existing formulations.
  • ready to use and/or ready to dilute compositions may be in the concentration range from about 0.1 mg/mL to about 7 mg/mL and preferred volume of not more than about 700 mL.
  • ready to use and/or ready to dilute compositions may be in the concentration range from about 0.1 mg/mL to about 0.26mg/mL and preferred volume of not more than about 250 mL.
  • compositions may be in the concentration range from about 1 mg/mL to about 5 mg/mL and preferred volume of not more than about 250 mL.
  • the pharmaceutical composition according to above embodiments include lyophilized composition, liquid composition, ready to dilute, ready to use, ready to infuse compositions and the like.
  • the pharmaceutical composition according to above embodiments include lyophilized composition, liquid composition, ready to dilute, ready to use composition, ready to infuse composition, wherein composition is in the concentration of about 0.1 mg/mL to about 7.0 mg/mL.
  • the pharmaceutical composition according to the above embodiments is used to treat cancer, carcinoma or malignant disease such as carcinoma of the ovary, prostate cancer, breast cancer, and related conditions thereof.
  • Taxanes with or without other therapeutically active agents may also be used in combination or prior to administering taxane comprising composition without departing from the present invention or to prevent side effects (e.g., hypersensitivity reactions, gastrointestinal symptoms) associated with the administration of the inventive compositions. These agents may optionally be added to the compositions. Preferably the therapeutically active agents synergistically enhance the effect of Taxanes.
  • therapeutic agents examples include, but are not limited to alkylating agents, antihistamines, hormonal agents, H 2 antagonists, steroids, plant-derived agents, biologic agents, platinum containing anticancer agents, interleukins, interferons, cytokines, immuno-modulating agents, monoclonal antibodies, other anticancer agents and combinations thereof.
  • the present invention is presented in an ampoule, a vial, IV bag, or a suitable parenteral container that provides the composition comprising taxane or its derivatives, cyclodextrins derivative, and optionally with other pharmaceutically acceptable excipients, the composition is free of surfactants or glycols.
  • the present invention is presented in an ampoule, vial, IV bag, or a suitable parenteral container that provides the solution composition or alternately lyophilized composition comprising, taxane or its derivatives, cyclodextrins derivative, and optionally with other pharmaceutically acceptable excipients, the composition is free of surfactants or glycols.
  • the present invention provides a ready to use solution in bag or IV bag comprising a separate single dose container containing solution comprising taxane or its derivatives, cyclodextrins derivative, and optionally with other pharmaceutically acceptable excipients, the composition is free of surfactants or glycols with suitable diluents such as dextrose, sodium chloride, mannitol and the like.
  • the present invention provides a ready to infuse solution in bag or IV bag comprising a separate single dose container containing solution comprising taxane or its derivatives, cyclodextrins derivative, and optionally with other pharmaceutically acceptable excipients, the composition is free of surfactants or glycols, with suitable diluents such as dextrose, sodium chloride, mannitol and the like.
  • the composition comprises a kit comprising the pharmaceutical composition with increased rate of administration and reduced administration duration to the patient, wherein,
  • composition comprises of cabazitaxel or its pharmaceutically
  • composition is free of surfactants and glycols;
  • the pharmaceutical composition is lyophilized composition, liquid
  • composition ready to dilute, ready to use, ready to infuse compositions; d. the composition is in the concentration of about 0.1 mg/ml_ to about 7.0 mg/ml_;
  • composition is presented in a suitable parenteral container, wrapped over or covered with a suitable secondary packaging system.
  • Example 1 Compositions with 1 mg/ml_ [Ready to dilute and/or ready to infuse compositions]
  • Example 2 Compositions with 0.26mg/ml_ [Ready to infuse composition]
  • Example 3 Compositions with 3 mg/ml_ [Ready to dilute composition]
  • compositions CA1 , CA2, CA3 and CA4 are stable, easy to use and administer for the patients unlike that of the available compositions. Further it was concluded that there is no impact of citric acid on the formulation stability.

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

Abstract

La présente invention concerne une composition pharmaceutique comprenant du cabazitaxel ou ses dérivés, un dérivé de cyclodextrines et éventuellement d'autres excipients pharmaceutiquement acceptables, a) la composition étant exempte de tensioactifs et de glycols, b) la composition étant prête à être diluée, prête à être utilisée, prête à être perfusée, c) la composition étant à la concentration d'environ 0,1 mg/ml à environ 7,0 mg/ml; les compositions sont administrées au patient à de faibles volumes, à une vitesse d'administration accrue et pendant une durée d'administration réduite.
PCT/IB2017/057981 2016-12-16 2017-12-15 Compositions pharmaceutiques de taxane et de ses dérivés Ceased WO2018109731A1 (fr)

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Application Number Priority Date Filing Date Title
IN201641043004 2016-12-16
IN201641043004 2016-12-16

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WO2018109731A1 true WO2018109731A1 (fr) 2018-06-21

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013022960A1 (fr) * 2011-08-10 2013-02-14 Scidose Llc Formulations de cabazitaxel et leurs procédés de préparation
US8765716B2 (en) * 2006-09-12 2014-07-01 Meridian Laboratories, Inc. Pharmaceutical composition containing docetaxel-cyclodextrin inclusion complex and its preparing process
WO2014122498A2 (fr) * 2012-12-24 2014-08-14 Supratek Pharma Inc. Composition de cabazitaxel

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8765716B2 (en) * 2006-09-12 2014-07-01 Meridian Laboratories, Inc. Pharmaceutical composition containing docetaxel-cyclodextrin inclusion complex and its preparing process
WO2013022960A1 (fr) * 2011-08-10 2013-02-14 Scidose Llc Formulations de cabazitaxel et leurs procédés de préparation
WO2014122498A2 (fr) * 2012-12-24 2014-08-14 Supratek Pharma Inc. Composition de cabazitaxel

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