AR017480A1 - PROLONGED RELEASE MICROSPHERES TO ENCAPSULATE ANALOGS OF THE LUTEINIZING HORMONE RELEASING HORMONE AND METHOD TO PREPARE THEM - Google Patents

PROLONGED RELEASE MICROSPHERES TO ENCAPSULATE ANALOGS OF THE LUTEINIZING HORMONE RELEASING HORMONE AND METHOD TO PREPARE THEM

Info

Publication number
AR017480A1
AR017480A1 ARP990101361A ARP990101361A AR017480A1 AR 017480 A1 AR017480 A1 AR 017480A1 AR P990101361 A ARP990101361 A AR P990101361A AR P990101361 A ARP990101361 A AR P990101361A AR 017480 A1 AR017480 A1 AR 017480A1
Authority
AR
Argentina
Prior art keywords
release
microsphere
hormone
luteinizing hormone
emulsion phase
Prior art date
Application number
ARP990101361A
Other languages
Spanish (es)
Original Assignee
Dong Kook Pharm Co 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 Dong Kook Pharm Co Ltd filed Critical Dong Kook Pharm Co Ltd
Publication of AR017480A1 publication Critical patent/AR017480A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens

Abstract

Se describe una microesfera de liberacion prolongada que puede liberar en forma constante drogas medicinales tales como análogos de la hormonaliberadora de la hormona luteinizante y las encapsula con altas tasas de contenido. Se prepara disolviendo un copolímero de láctido y glicolido en clorurode metileno, disolviendo un análogo de la hormona liberadora de la hormona luteinizante y un material controlador de la liberacion en un solventeauxiliar, combinando las dos soluciones obtenidas entre sípara producir una fase de emulsion, dispersando la fase de emulsion en una solucion de alcoholpolivinílico en agua destilada para dar un sistema de emulsion unica, eliminando el solvente combinado de la fase de emulsion para generar unamicroesfera polimérica; secando por congelacion la microesfera polimérica. La microesfera preparada tiene una estructura interna mucho más fina, en virtud delo cual la microesfera asegura un índice de liberacion constante. El sistema de emulsion unica que simplifica la preparacion, da lugar al mantenimiento de uncontenido de fármaco de 10% o más. Los grupos cargados de los materiales controladores de la liberacion asociados con los polímeros minimizan el excesode liberacion de las drogas con cargas opuestas en una etapa inicial, por lo que cumplen una funcion importante en el mantenimiento de la velocidad deliberacion constante.A prolonged-release microsphere is described that can constantly release medicinal drugs such as luteinizing hormone hormone-releasing analogues and encapsulates them with high content rates. It is prepared by dissolving a copolymer of lactide and glycolide in methylene chloride, dissolving an analogue of the luteinizing hormone releasing hormone and a release controlling material in an auxiliary solvent, combining the two solutions obtained from each other to produce an emulsion phase, dispersing the emulsion phase in a solution of polyvinyl alcohol in distilled water to give a unique emulsion system, removing the combined solvent from the emulsion phase to generate a polymeric microsphere; freezing the polymer microsphere. The prepared microsphere has a much finer internal structure, under which the microsphere ensures a constant release rate. The unique emulsion system that simplifies the preparation, results in the maintenance of a drug content of 10% or more. The groups loaded with the release control materials associated with the polymers minimize the excess release of drugs with opposite charges at an initial stage, thus fulfilling an important function in maintaining constant deliberation speed.

ARP990101361A 1998-12-30 1999-03-26 PROLONGED RELEASE MICROSPHERES TO ENCAPSULATE ANALOGS OF THE LUTEINIZING HORMONE RELEASING HORMONE AND METHOD TO PREPARE THEM AR017480A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1019980062142A KR100321854B1 (en) 1998-12-30 1998-12-30 Long-term sustained-release microspheres containing luteinizing hormone releasing hormone homologues and a method of producing the same

Publications (1)

Publication Number Publication Date
AR017480A1 true AR017480A1 (en) 2001-09-05

Family

ID=19568831

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990101361A AR017480A1 (en) 1998-12-30 1999-03-26 PROLONGED RELEASE MICROSPHERES TO ENCAPSULATE ANALOGS OF THE LUTEINIZING HORMONE RELEASING HORMONE AND METHOD TO PREPARE THEM

Country Status (10)

Country Link
JP (1) JP2002534392A (en)
KR (1) KR100321854B1 (en)
CN (1) CN1348383A (en)
AR (1) AR017480A1 (en)
BR (1) BR9916945A (en)
CA (1) CA2358495A1 (en)
MX (1) MXPA01005540A (en)
TR (1) TR200101913T2 (en)
WO (1) WO2000040259A1 (en)
ZA (1) ZA992059B (en)

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US6565874B1 (en) 1998-10-28 2003-05-20 Atrix Laboratories Polymeric delivery formulations of leuprolide with improved efficacy
US8470359B2 (en) 2000-11-13 2013-06-25 Qlt Usa, Inc. Sustained release polymer
WO2003075958A1 (en) 2002-03-11 2003-09-18 Takeda Chemical Industries, Ltd. Remedies for sex hormone-dependent disease
WO2003105917A2 (en) 2002-06-12 2003-12-24 Scimed Life Systems, Inc. Bulking agents
DK1532985T3 (en) 2002-06-25 2016-12-05 Takeda Pharmaceuticals Co PROCEDURE FOR PREPARING A COMPOSITION WITH LONG-TERM RELEASE
CA2533314C (en) * 2003-07-18 2013-07-09 Oakwood Laboratories, L.L.C. Prevention of molecular weight reduction of the polymer, impurity formation and gelling in polymer compositions
BR0305373A (en) * 2003-11-06 2005-06-28 Iseu Da Silva Nunes Nelson Edu Ammonium and magnesium phospholinoleate palmitoleate anhydride protein aggregate immunomodulator and process for obtaining and formulating it
TW200529890A (en) 2004-02-10 2005-09-16 Takeda Pharmaceutical Sustained-release preparations
KR100622996B1 (en) * 2005-03-03 2006-09-14 한국과학기술원 Nonporous microspheres including drug and manufacturing method thereof
US7963287B2 (en) 2005-04-28 2011-06-21 Boston Scientific Scimed, Inc. Tissue-treatment methods
US9463426B2 (en) 2005-06-24 2016-10-11 Boston Scientific Scimed, Inc. Methods and systems for coating particles
WO2009150136A1 (en) * 2008-06-09 2009-12-17 Boehringer Ingelheim International Gmbh Novel embedment particles for inhalation
CN104873979A (en) 2008-08-29 2015-09-02 健赞股份有限公司 Controlled-released Peptide Formulations
KR101663560B1 (en) * 2009-02-13 2016-10-10 동국제약 주식회사 Method for manufacturing uniform delayed-release microspheres
DE102011114864A1 (en) 2011-10-05 2013-04-11 Acino Ag Process for producing a homogeneous powder mixture and method for producing an implant and implant
HUE045661T2 (en) 2011-12-14 2020-01-28 Abraxis Bioscience Llc Use of polymeric excipients for lyophilization or freezing of particles
BR112016002342A8 (en) * 2013-08-06 2018-01-23 Dong Kook Pharm Co Ltd entecavir microsphere, method for preparation of an entecavir microsphere, and pharmaceutical composition
CN109394705B (en) * 2018-12-04 2021-11-19 沈阳药科大学 Goserelin sustained-release microsphere freeze-dried powder and preparation method thereof
US11617720B2 (en) 2020-05-08 2023-04-04 M. Technique Co., Ltd. Main agent uniformly dispersed microsphere and a sustained release formulation comprising the same
KR20220163418A (en) * 2020-05-08 2022-12-09 엠. 테크닉 가부시키가이샤 Microspheres in which physiologically active substances are uniformly dispersed and sustained-release preparations containing the microspheres
KR20220163416A (en) 2020-05-08 2022-12-09 엠. 테크닉 가부시키가이샤 Microspheres in which physiologically active substances are uniformly dispersed and sustained-release preparations containing the microspheres

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4675189A (en) * 1980-11-18 1987-06-23 Syntex (U.S.A.) Inc. Microencapsulation of water soluble active polypeptides
CH661206A5 (en) * 1983-09-23 1987-07-15 Debiopharm Sa PROCESS FOR THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF HORMONDEPENDENT DISEASES.
CH660302A5 (en) * 1984-10-17 1987-04-15 Debiopharm Sa HETEROGENEOUS PHASE MICRO-ENCAPSULATION PROCESS OF WATER-SOLUBLE DRUG SUBSTANCES.
GB2209937B (en) * 1987-09-21 1991-07-03 Depiopharm S A Water insoluble polypeptides
YU48420B (en) * 1991-03-25 1998-07-10 Hoechst Aktiengesellschaft PROCEDURE FOR OBTAINING BIOLOGICAL DEGRADABLE MICROPARTICLES WITH LONG TERM ACTION
FR2693905B1 (en) * 1992-07-27 1994-09-02 Rhone Merieux Process for the preparation of microspheres for the sustained release of the hormone LHRH and its analogs, microspheres and formulations obtained.

Also Published As

Publication number Publication date
JP2002534392A (en) 2002-10-15
KR100321854B1 (en) 2002-08-28
TR200101913T2 (en) 2001-11-21
CN1348383A (en) 2002-05-08
CA2358495A1 (en) 2000-07-13
BR9916945A (en) 2001-11-06
MXPA01005540A (en) 2004-06-22
ZA992059B (en) 1999-09-27
WO2000040259A1 (en) 2000-07-13
KR20000045577A (en) 2000-07-25

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