US20120101030A1 - Caspofungin Composition - Google Patents

Caspofungin Composition Download PDF

Info

Publication number
US20120101030A1
US20120101030A1 US13/237,193 US201113237193A US2012101030A1 US 20120101030 A1 US20120101030 A1 US 20120101030A1 US 201113237193 A US201113237193 A US 201113237193A US 2012101030 A1 US2012101030 A1 US 2012101030A1
Authority
US
United States
Prior art keywords
pharmaceutically acceptable
caspofungin
composition
composition according
buffering agent
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.)
Abandoned
Application number
US13/237,193
Other languages
English (en)
Inventor
Swapnil Shirode
Piyush Patel
Suresh Gidwani
Neil Parikh
Atul Patil
Anita Bevetek Mocnik
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.)
Xellia Pharmaceuticals ApS
Original Assignee
Xellia Pharmaceuticals ApS
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 Xellia Pharmaceuticals ApS filed Critical Xellia Pharmaceuticals ApS
Priority to US13/237,193 priority Critical patent/US20120101030A1/en
Assigned to XELLIA PHARMACEUTICALS APS reassignment XELLIA PHARMACEUTICALS APS ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: PARIKH, NEIL, GIDWANI, SURESH, MOCNIK, ANITA BEVETEK, PATEL, PIYUSH, PATIL, ATUL, SHIRODE, SWAPNIL P.
Publication of US20120101030A1 publication Critical patent/US20120101030A1/en
Priority to US14/547,742 priority patent/US9393307B2/en
Abandoned legal-status Critical Current

Links

Images

Classifications

    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/08—Solutions
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics

Definitions

  • the present invention relates to a composition
  • a composition comprising caspofungin or a pharmaceutical acceptable salt thereof and succinate or lactate as a buffering agent.
  • Caspofungin (CAS 162808-62-0) is the first of a new class of semi-synthetic antifungal agents belonging to the class of echinocandins. It may be represented by the formula I
  • Caspofungin is commonly prepared by synthetic derivatisation of pneumocandin B 0 which is obtained by fermentation of the fungus Glarea lozoyensis .
  • the antifungal activity of caspofungin is due to its inhibition of the biosynthesis of ⁇ -(1,3)-D-glucan, an integral component of the fungal cell wall. It is used for the treatment of invasive aspergillosis in patients who are refractory to or intolerant of other therapies, as well as empirical therapy for presumed fungal infections in febrile, neutropenic patients.
  • Caspofungin as a compound is claimed in the U.S. Pat. No. 5,378,804 issued to Merck & Co.
  • U.S. Pat. No. 5,952,300 discloses a composition for treating and/or preventing fungal infections comprising caspofungin and the pharmaceutically active salt thereof, a pharmaceutically active amount of an acetate buffer and a pharmaceutically acceptable amount of excipients such as a sucrose/mannitol mixture to form a lyophilized cake.
  • a lyophilized caspofungin product is available on the marketed as its diacetate salt by Merck & Co., under the trade name Cancidas® (RLD product).
  • Cancidas® contains in addition to the active ingredient caspofungin diacetate, acetic acid, sodium hydroxide, sucrose and mannitol.
  • the lyophilized product is reconstituted by adding a diluent and the desired amount of the diluted mixture is transferred to infusion bag to be administered to the patient in need thereof.
  • caspofungin compositions prepared for reconstitution prior to administration to the patient are highly unstable resulting in the formation of various degradation products such as e.g. hydrolysis products (impurity B) and dimerization products (impurity C).
  • impurity B hydrolysis products
  • impurity C dimerization products
  • impurity C impurity C
  • a lyophilized caspofungin composition comprising in addition to caspofungin diacetate and an acetate buffer, one or more non-reducing sugars such as trehalose, sucrose, raffinose, or sorbitol or combinations thereof is disclosed.
  • a caspofungin composition comprising, in addition to a pharmaceutically acceptable salt of caspofungin and excipients, only very low levels of a buffering agent, or which is free of a buffering agent.
  • an antifungal composition according to the present invention comprising caspofungin or a pharmaceutically acceptable salt thereof, one or more pharmaceutically acceptable excipients and including succinat or lactate as a buffering agent, is stable resulting in reduced formation of degradation products during storage.
  • the present invention therefore provides a composition
  • a composition comprising a) a pharmaceutically effective amount of caspofungin or a pharmaceutically acceptable salt thereof; b) a pharmaceutically acceptable amount of one or more pharmaceutically acceptable excipients effective to form a lyophilized cake; and c) a pharmaceutically effective amount of a buffering agent selected from the group consisting of lactate and succinate.
  • the pharmaceutically acceptable salt of caspofungin is an acetate salt.
  • the composition according to the invention comprises a diacetate salt of caspofungin.
  • the buffering agent of the composition is succinate. According to yet another aspect of the invention, the buffering agent of the composition is lactate.
  • composition wherein the excipients is selected from the group consisting of stabilisers, diluents, antioxidants, or preservatives.
  • the stabilisators are selected from the group consisting of sucrose and mannitol; or a combination thereof.
  • a compositing comprising a) pharmaceutically acceptable amount of caspofungin or a pharmaceutically acceptable salt thereof; b) about 10-200 mg/ml of one or more pharmaceutically acceptable excipients effective to form a lyophilized cake; and c) a pharmaceutically effective amount of lactate or succinate providing a pharmaceutically acceptable pH.
  • the composition of the invention comprises an amount of caspofungin or a salt thereof corresponding to about 42 mg/ml caspofungin.
  • the composition of the invention comprises about 46 mg/ml diacetate salt of caspofungin; about 30 mg/ml sucrose and about 20 mg/ml mannitol; and about 1.5 mg/ml succinate or about 1.15 mg/ml lactate.
  • the present invention furthermore provides a process for making a caspofungin composition according the invention comprising the steps of a) mixing an aqueous solution comprising a pharmaceutically acceptable amount of one or more excipients with a pharmaceutically effective amount of a buffering agent selected from the group consisting of lactate and succinate; b) optionally adjusting the pH by adding a base to obtain a pharmaceutically acceptable pH; c) adding to the mixture of a) a pharmaceutically acceptable amount of caspofungin or a pharmaceutically acceptable salt thereof; d) optionally adjusting the pH by adding a base to obtain a pharmaceutically acceptable pH; and e) filtering the solution obtained in d).
  • step a) is performed by firstly preparing an aqueous solution comprising a pharmaceutically effective amount of a buffering agent selected from the group consisting of lactate and succinate; then adding to the said solution of buffering agent a pharmaceutically acceptable amount of one or more excipients dissolved in water.
  • step a) is performed by firstly dissolving a pharmaceutically acceptable amount of one or more excipients in water; then adding to said solution of excipient(s) a pharmaceutically effective amount of a buffering agent selected from the group consisting of lactate and succinate.
  • the pH of step b) of the present invention is adjusted to 5.0-5.7. According to another embodiment, the pH of step d) of the present invention is adjusted to about 6.
  • a caspofungin salt preferably caspofungin diacetate, is added in step c) of the process.
  • the present invention also provides a lyophilized formulation which consists of a composition which prior to lyophilization corresponds to a composition according to present invention.
  • the present invention furthermore provides a formulation for parenteral administration consisting of a lyophilized formulation according to the invention, wherein said lyophilized formulation is dissolved in a pharmaceutically acceptable reconstitution solution suitable for parenteral administration to a patient in need thereof.
  • the pharmaceutically acceptable reconstitution solution may e.g. be selected from the group consisting of distilled or sterile water commonly used for injections, physiologic saline, and bacteriostatic water.
  • a kit comprising a first container comprising the lyophilized formulation according to the invention and a second container comprising a parenterally acceptable solvent for reconstitution thereof, and optionally a container comprising means for administrating the reconstituted solution to a patient in need thereof.
  • the reconstituted formulation according to the present invention may preferably be used in a method for treating or preventing a fungal infection comprising parenterally administering to a patient in need thereof, e.g. wherein the administration is performed by infusion or injection.
  • the present invention finally provides a use of a composition according to the invention for the preparation of a formulation for parenteral administration for the treatment or prevention of fungal infection, such as infections caused by a fungus belonging to the species Candida or Aspergillus , such as e.g. infections is caused by a fungus belonging to the species infection is caused by C. albicans, C. tropicalis, C. krusei, C. glabrata, A. fumigatus, A. flavus and A. nigerc .
  • a method according to any of the claims 15 - 16 for the treatment or prevention of fungal infection, wherein the infections is caused by a fungus belonging to the species Candida or Aspergillus.
  • FIG. 1 shows the change in the amount of the total impurities in the lyophilized formulations prepared according to example 1 after storage in 1 month (1M) and 2 months (2M), respectively, i.e., caspofungin composition comprising caspofungin diacetate, sucrose, mannitol and as buffering agent either lactate, succinate, tartrate or acetate, and as control, a composition as above not comprising a buffering agent.
  • caspofungin composition comprising caspofungin diacetate, sucrose, mannitol and as buffering agent either lactate, succinate, tartrate or acetate, and as control, a composition as above not comprising a buffering agent.
  • FIG. 2 shows the changes in impurity B (hydrolysis degradation product), Impurity C (dimerization product) and the total amounts of impurities in the lyophilized formulation prepared according to example 2 after storage in 1 month (1M), 2 months (2M) and 3 months (3M).
  • FIG. 3 shows the changes in impurity B (hydrolysis degradation product), Impurity C (dimerization product) and the total amounts of impurities in the lyophilized formulation prepared according to example 3 after storage in 1 month (1M), 2 months (2M) and 3 months (3M).
  • caspofungin as used herein means caspofungin free base known under the CAS number 162808-62-0.
  • the composition of the present invention may comprise caspofungin or a pharmaceutical acceptable salt thereof.
  • pharmaceutically acceptable salts of caspofungin as used herein means any non-toxic salts of caspofungin.
  • suitable organic or inorganic acids that may be used to form salts of caspofungin, including mono-, di- and tri acid forms.
  • pharmaceutically acceptable acid addition salts may be formed using acids such as hydrochloric, hydrobromic, sulphonic, phosphoric, maleic, malic, lactic, citric, acetic, tartaric, propionic, succinic, oxalic, glutamic, pamoic acid etc.
  • acids such as hydrochloric, hydrobromic, sulphonic, phosphoric, maleic, malic, lactic, citric, acetic, tartaric, propionic, succinic, oxalic, glutamic, pamoic acid etc.
  • acids well known to the skilled person in respect of forming pharmaceutically active salts may be used.
  • Several pharmaceutical acceptable salts of caspofungin are furthermore known from e.g. U.S. Pat. No. 5,952,300, and WO 2008/12310.
  • a lyophilized formulation comprising the acetate salt of caspofungin.
  • a lyophilized formulation comprising the diacetate salt of caspofungin.
  • An acetate salt of caspofungin, such as a diacetate salt of caspofungin may be prepared as disclosed in U.S. Pat. No. 5,952,300.
  • lyophilized formulation means a formulation being prepared by lyophilization/freeze drying of a mixture comprising a pharmaceutically effective amount of caspofungin or a pharmaceutically acceptable salt thereof; a pharmaceutically acceptable amount of one or more pharmaceutically acceptable excipients; and a pharmaceutically acceptable amount of a buffering agent selected from the group consisting of lactate and succinate.
  • the lyophilized formulation may be comprised in lyophilization vials suitable for transport and handling, and for the providing of a reconstituted formulation ready to be administered to a patient in need thereof.
  • the one or more pharmaceutically acceptable excipients of the composition of the invention may be any pharmaceutically acceptable excipients suitable for formation of a lyophilized cake.
  • the one or more pharmaceutically acceptable excipients may further be well known diluent(s) or carrier(s) suitable for parenteral administration and which are well known to the skilled person.
  • Suitable excipients that may be comprised in a composition according to the present invention may be selected from the non-limiting list of the group consisting of stabilizers, diluents, antioxidants, preservatives and the like.
  • a non-limiting list of stabilizers useful in the composition of the present invention comprises sucrose, trehalose, raffinose, sorbitol and/or mannitol.
  • the composition of the present invention comprises sucrose or mannitol, or a combination thereof. Based on the teaching of the present invention, the skilled person will be able to select the appropriate excipients and amounts thereof for the manufacturing of a composition according to the present invention.
  • the composition of the invention comprises as a buffering agent lactate or succinate.
  • the buffering agent can be obtained by either dissolving the salt or the acid form of the buffering agent into water e.g. lactate-salt or lactic acid or succinate-salt or succinic acid.
  • the buffer agent may also be used in solid form, such as by adding succinic acid or lactic acid into a solution of excipients.
  • Said buffering agent is used in a pharmaceutically effective amount ensuring the providing and maintenance of a pharmaceutically acceptable pH value. More specifically, a pharmaceutically acceptable pH value within the meaning of the present invention is in the range of about 5 to about 8, such as e.g. about 5.5-7.5, such as about 5.5-7.0, such as about 5.5-6.5, such as e.g. about 6.0.
  • the composition of the present invention results in reduced formation of total impurities during storage of a lyophilized formulation prepared therefrom compared with lyophilized formulations based on an acetate buffer system or lyophilized formulations known in the art prepared from a composition not comprising a buffering agent.
  • total impurities as used herein means the total amount of impurities commonly present in a pharmaceutically acceptable caspofungin product or a pharmaceutically active caspofungin salt prepared according to method for preparing caspofungin or a salt thereof well known to the skilled person in the art. The total amount of impurities present may be measured by HPLC-analysis.
  • the change in the total amount of impurities during storage may be presented as the sum of the area percentage of the total amount of impurities in a formulation to be analysed.
  • the persons skilled in the art are familiar with various applicable HPLC devices and methods for measuring the formation of impurities during storage.
  • the composition according to the present invention is prepared by dissolving and mixing the ingredients, filtering the obtained mixture, and after transferring the solution to suitable vials.
  • the so obtained solution is lyophilized to obtain a lyophilized cake.
  • Lyophilization or freeze-drying, is a dehydration process typically used to preserve unstable materials or make a material more convenient for transport. It is commonly used within the pharmaceutical industry and involves freezing of the material in question and reduction of the surrounding pressure, adding enough heat to allow the frozen water in the material to sublime and thus be removed from the resulting lyophilized product.
  • the skilled person is well known with the various means and devices available for lyophilization within the pharmaceutical area.
  • the composition according to the present invention is preferably lyophilized in pharmaceutically acceptable vials according to the method of the present invention to obtain a lyophilized cake of the composition of the present invention.
  • formulation for parenteral administration means liquid formulation comprising a pharmaceutically effective amount of the caspofungin composition according to the present invention, and wherein said composition have been dissolved in or mixed with one or more pharmaceutically acceptable reconstitution solutions.
  • the reconstitution may be performed by dissolving the lyophilized product in a pharmaceutically acceptable reconstitution solution.
  • a pharmaceutically acceptable reconstitution solution is e.g. distilled or sterile water commonly used for injections, physiologic saline, or bacteriostatic water for injection.
  • Bacteriostatic water commonly comprises bacteriostatic compounds as preservatives, such as e.g. benzyl alcohol.
  • a pharmaceutically acceptable amount of the reconstituted formulation may then be transferred to means suitable for parenteral administration, such as e.g. intramuscular, subcutaneous, intravenous, intra-peritoneal administration.
  • the reconstituted formulation according to the present invention may be used to treat or prevent infections in a patient.
  • the formulation may inter alia be used to prevent or fight an infections caused by fungus belonging to the Candida species and Aspergillus species. More specifically, said formulation may be used to treat or prevent infections caused by e.g. C. albicans, C. tropicalis, C. krusei, C. glabrata, A. fumigatus, A. flavus and A. niger .
  • the present invention therefore also provides a method for the treatment or prevention of fungal infection, such as the infections cause by the above mentioned species.
  • a caspofungin composition was prepared by firstly dissolving mannitol in water, then adding sucrose and succinic acid. After the addition of succinic acid, pH was determined and 0.1 M NaOH was then added to adjust the pH to 4.0. To the so-obtained solution, caspofungin diacetate corresponding to 42 mg/ml caspofungin was added. The pH of the so obtained solution was then again adjusted to pH 6.1 with 0.1 M NaOH, and the solution was mixed by stirring.
  • the volume of the solution was adjusted to 400 ml by adding water acceptable for injection, and filtered through a 0.22 ⁇ m filter. The solution was thereafter transferred to 10 ml lyophilization vials and stopped with sterile rubber stoppers. The solution was then subjected to lyophilization. The preparation of the composition, except during freeze drying, was performed at a temperature of 2-8° C.
  • a caspofungin composition was prepared by firstly dissolving succinic acid in water, then the pH of the solution was adjusted to about 5.5-5.7 by adding NaOH solution. Then secondly sucrose and mannitol were added to the above solution. If needed the pH was again adjusted to about 5.5-5.7 by addition of NaOH. To the so obtained solution, caspofungin diacetate was added. After complete dissolution the pH was again adjusted with NaOH to reach about 5.9-6.1. The solution volume was then adjusted to final value to reach the concentrations given in Table 1.
  • composition was filtered through a 0.22 ⁇ m filter and thereafter transferred to 10 ml lyophilization vials and stopped with sterile rubber stoppers. The solution was then subjected to lyophilization.
  • a caspofungin composition was prepared by firstly dissolving lactic acid in water, then the pH of the solution was adjusted to about 5.0 by adding NaOH solution. Then secondly sucrose and mannitol were added to the above solution. If needed the pH was again adjusted to about 5.0 by addition of NaOH. To the so obtained solution, caspofungin diacetate was added. After complete dissolution the pH was, if needed, adjusted with NaOH to reach about 6.3. The solution volume was then adjusted to final value to reach the concentrations given in Table 2 below.
  • composition was filtered through a 0.22 ⁇ m filter and thereafter transferred to 10 ml lyophilization vials and stopped with sterile rubber stoppers. The solution was then subjected to lyophilization.
  • the stability testing according to FIG. 1 revealed that a lyophilized formulation based on a composition prepared using succinate or lactate as a buffering agent showed lower formation of total impurities compared with the compositions comprising acetate or tartrate.
  • acetate seems not to be superior in respect of formation of the impurities determined is surprising taking into account the teaching of the prior art.
  • U.S. Pat. No. 5,952,300 teach that the use of tartrate buffer results in the formation of undesired degradation product in contrast to acetate buffer. It is furthermore surprisingly observed that the amount of impurities increase during storage when no buffering agent is added, contrary to the teaching of WO2008/12310.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
US13/237,193 2010-09-20 2011-09-20 Caspofungin Composition Abandoned US20120101030A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US13/237,193 US20120101030A1 (en) 2010-09-20 2011-09-20 Caspofungin Composition
US14/547,742 US9393307B2 (en) 2010-09-20 2014-11-19 Caspofungin composition

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38433310P 2010-09-20 2010-09-20
US13/237,193 US20120101030A1 (en) 2010-09-20 2011-09-20 Caspofungin Composition

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US14/547,742 Continuation US9393307B2 (en) 2010-09-20 2014-11-19 Caspofungin composition

Publications (1)

Publication Number Publication Date
US20120101030A1 true US20120101030A1 (en) 2012-04-26

Family

ID=44677877

Family Applications (2)

Application Number Title Priority Date Filing Date
US13/237,193 Abandoned US20120101030A1 (en) 2010-09-20 2011-09-20 Caspofungin Composition
US14/547,742 Active 2031-11-05 US9393307B2 (en) 2010-09-20 2014-11-19 Caspofungin composition

Family Applications After (1)

Application Number Title Priority Date Filing Date
US14/547,742 Active 2031-11-05 US9393307B2 (en) 2010-09-20 2014-11-19 Caspofungin composition

Country Status (20)

Country Link
US (2) US20120101030A1 (de)
EP (1) EP2618814B1 (de)
JP (1) JP5914486B2 (de)
KR (1) KR20130136466A (de)
CN (1) CN103118663A (de)
AU (1) AU2011304408B2 (de)
CA (1) CA2810112A1 (de)
DK (1) DK2618814T3 (de)
ES (1) ES2593727T3 (de)
HR (1) HRP20161236T1 (de)
HU (1) HUE030464T2 (de)
IL (1) IL225339A0 (de)
MX (1) MX2013003045A (de)
PL (1) PL2618814T3 (de)
PT (1) PT2618814T (de)
RS (1) RS55216B1 (de)
RU (1) RU2013114993A (de)
UA (1) UA111599C2 (de)
WO (1) WO2012038371A1 (de)
ZA (1) ZA201302113B (de)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103212058A (zh) * 2012-01-18 2013-07-24 江苏恒瑞医药股份有限公司 含有抗真菌药物和乳酸盐缓冲剂的组合物
CN103212059A (zh) * 2012-01-18 2013-07-24 江苏恒瑞医药股份有限公司 含有抗真菌药物和乳酸盐缓冲液的组合物
WO2014081443A1 (en) 2012-11-20 2014-05-30 Fresenius Kabi Usa, Llc Caspofungin acetate formulations
CN103142997A (zh) * 2013-03-13 2013-06-12 浙江海正药业股份有限公司 含有抗真菌剂和琥珀酸盐缓冲液的药物组合物
KR20140123782A (ko) * 2013-04-15 2014-10-23 에스케이케미칼주식회사 카스포펀진 및 완충제를 포함하는 안정성이 개선된 약학적 조성물
CN104116716A (zh) * 2013-04-25 2014-10-29 四川海思科制药有限公司 一种含卡泊芬净的冻干粉针剂药物组合物
EP3054924B1 (de) * 2013-10-07 2020-11-25 Galenicum Health S.L.U. Stabile pharmazeutische formulierungen von caspofungin
GR1008818B (el) * 2015-05-22 2016-08-01 Φαρματεν Ανωνυμος Βιομηχανικη Και Εμπορικη Εταιρεια Φαρμακευτικων Ιατρικων Και Καλλυντικων Προϊοντων Φαρμακευτικο σκευασμα περιεχον εναν αντιμυκητιασικο παραγοντα εχινοκανδινης και μεθοδος παρασκευης αυτου
CN108760937B (zh) * 2018-07-27 2020-12-29 杭州华东医药集团新药研究院有限公司 醋酸卡泊芬净中残留乙二胺的测定及其应用
CN109758426B (zh) * 2019-01-24 2021-04-27 四川制药制剂有限公司 一种注射用醋酸卡泊芬净药物组合物及其制备方法
CN110859950B (zh) * 2019-11-25 2021-08-10 武汉大学 一种用于白念珠菌棘白菌素类药物耐药菌的药物组合物及其应用
EP4364566A1 (de) * 2022-11-04 2024-05-08 B. Braun Melsungen AG Antimykotische zusammensetzung

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991015121A1 (en) * 1990-03-30 1991-10-17 Smithkline Beecham Corporation Method for treating fungal infection
US5952300A (en) * 1996-04-19 1999-09-14 Merck & Co., Inc. Antifungal compositions
WO2009002481A1 (en) * 2007-06-26 2008-12-31 Merck & Co., Inc. Lyophilized anti-fungal composition
US20090170753A1 (en) * 2006-07-26 2009-07-02 Christian Welz Capsofungin formulations

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2930823B2 (ja) 1991-12-11 1999-08-09 株式会社東芝 Ｘ線ｃｔスキャナ用検出器及びｘ線検出装置用シンチレータチャネルセパレータ
US5378804A (en) 1993-03-16 1995-01-03 Merck & Co., Inc. Aza cyclohexapeptide compounds
US20080046580A1 (en) 2006-06-29 2008-02-21 Nokia Corporation Account creation system and call processing system
CN101516387B (zh) * 2006-07-26 2014-06-04 桑多斯股份公司 卡泊芬净制剂
EP2285236A1 (de) * 2008-05-30 2011-02-23 DSM IP Assets B.V. Verwendung von bernsteinsäure
US20090324635A1 (en) 2008-06-25 2009-12-31 Ferenc Korodi Caspofungin free of caspofungin impurity A

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991015121A1 (en) * 1990-03-30 1991-10-17 Smithkline Beecham Corporation Method for treating fungal infection
US5952300A (en) * 1996-04-19 1999-09-14 Merck & Co., Inc. Antifungal compositions
US20090170753A1 (en) * 2006-07-26 2009-07-02 Christian Welz Capsofungin formulations
WO2009002481A1 (en) * 2007-06-26 2008-12-31 Merck & Co., Inc. Lyophilized anti-fungal composition

Also Published As

Publication number Publication date
ES2593727T3 (es) 2016-12-12
HRP20161236T1 (hr) 2016-11-18
CN103118663A (zh) 2013-05-22
WO2012038371A1 (en) 2012-03-29
DK2618814T3 (en) 2016-10-10
ZA201302113B (en) 2014-05-28
JP2013537212A (ja) 2013-09-30
JP5914486B2 (ja) 2016-05-11
PL2618814T3 (pl) 2017-01-31
PT2618814T (pt) 2016-10-06
UA111599C2 (uk) 2016-05-25
US9393307B2 (en) 2016-07-19
IL225339A0 (en) 2013-06-27
RS55216B1 (sr) 2017-02-28
HUE030464T2 (en) 2017-05-29
KR20130136466A (ko) 2013-12-12
US20150072923A1 (en) 2015-03-12
AU2011304408A1 (en) 2013-03-28
EP2618814A1 (de) 2013-07-31
CA2810112A1 (en) 2012-03-29
EP2618814B1 (de) 2016-07-27
MX2013003045A (es) 2013-06-24
AU2011304408B2 (en) 2015-01-15
RU2013114993A (ru) 2014-10-27

Similar Documents

Publication Publication Date Title
US9393307B2 (en) Caspofungin composition
US7198796B2 (en) Antifungal parenteral products
US8980827B2 (en) Medicinal composition containing echinocandin antifungal agent micafungin and preparation method and use thereof
US8431539B2 (en) Formulations of daptomycin
JP7229999B2 (ja) ダプトマイシン製剤
JP6832281B2 (ja) バンコマイシンの水溶液製剤
US9149502B2 (en) Low impurity content caspofungin preparation, method for preparing same, and use thereof
AU9723198A (en) Human growth hormone-containing aqueous pharmaceutical composition
US20130338060A1 (en) Liquid medicinal composition containing echinocandin antifungal agent micafungin
US10376559B2 (en) Formulations of vancomycin
US20180071393A1 (en) Stable intravenous formulation
US20150216928A1 (en) Daptomycin injectable formulation
EP3054924B1 (de) Stabile pharmazeutische formulierungen von caspofungin
US20230068866A1 (en) Daptomycin formulation
US11058745B1 (en) Stable liquid pharmaceutical compositions of daptomycin
WO2022034545A1 (en) Etelcalcetide formulations for parenteral use
WO2024088301A1 (zh) 一种棘白素类似物的药物组合物及其制备方法

Legal Events

Date Code Title Description
AS Assignment

Owner name: XELLIA PHARMACEUTICALS APS, DENMARK

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:SHIRODE, SWAPNIL P.;PATEL, PIYUSH;MOCNIK, ANITA BEVETEK;AND OTHERS;SIGNING DATES FROM 20111018 TO 20111209;REEL/FRAME:027489/0897

STCB Information on status: application discontinuation

Free format text: ABANDONED -- FAILURE TO RESPOND TO AN OFFICE ACTION