KR890009975A - Novel cyclosporin crystal form, preparation method thereof, pharmaceutical composition containing the same and use thereof - Google Patents

Novel cyclosporin crystal form, preparation method thereof, pharmaceutical composition containing the same and use thereof Download PDF

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Publication number
KR890009975A
KR890009975A KR1019880017194A KR880017194A KR890009975A KR 890009975 A KR890009975 A KR 890009975A KR 1019880017194 A KR1019880017194 A KR 1019880017194A KR 880017194 A KR880017194 A KR 880017194A KR 890009975 A KR890009975 A KR 890009975A
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South Korea
Prior art keywords
cyclosporin
pharmaceutical composition
cyclosporine
crystal form
tetragonal
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KR1019880017194A
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Korean (ko)
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KR100188305B1 (en
Inventor
지롱 다니엘르
리스트 마틴
리흐터 프리드리흐
우이케 야수이우키
페터 베버 한스
Original Assignee
예안 크라메르, 한스 루돌프 하우스
산도즈 리미티드
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Publication of KR890009975A publication Critical patent/KR890009975A/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C07K7/645—Cyclosporins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

내용 없음No content

Description

신규의 시클로스포린 결정 형태, 이것의 제조방법 및 이것을 함유한 약학 조성물 및 그 용도Novel cyclosporin crystal form, preparation method thereof, pharmaceutical composition containing the same and use thereof

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

제1도 내지 제3도는 CY/A/X-Ⅲ으로서 시클로스포린 0.1중량%을 함유하는 본 발명 조성물을 사용하는 결과와 위약 및 통상의 경구 용액 형태로 0.1% 시클로스토린을 적용한 것의 결과를 비교하여 나타낸다.1 to 3 compare the results of using the compositions of the present invention containing 0.1% by weight of cyclosporin as CY / A / X-III and the results of applying 0.1% cyclostorine in placebo and conventional oral solution forms. It is shown.

Claims (23)

비-용해화합물 같은 형태의 시클로스포린.Cyclosporine in the form of a non-soluble compound. 제1항에 있어서, 결정 격자 a=12.7 A, b=15.7 A, c=36.3 A 비대칭 단위당 부피-1804 A를 가지는 시클로스포린.The cyclosporine of claim 1 having a crystal lattice a = 12.7 A, b = 15.7 A, c = 36.3 A volume-1804 A per asymmetric unit. 제1항에 있어서, 하기 X-선회절 특성을 보이는 시클로스포린.The cyclosporin of claim 1, wherein the cyclosporin exhibits the following X-ray diffraction properties. VS=매우강함VS = very strong S=강함S = strong M=중간M = middle 제1항에 있어서, 다른 형태의 시클로스포린이 없거나 또는 거의 없는 시클로스포린.The cyclosporin of claim 1, wherein the cyclosporin is free or almost free of other forms of cyclosporin. 제1항에 있어서, 수수하거나, 또는 거의 순수한 형태의 시클로스포린.The cyclosporin of claim 1, in a simple or nearly pure form. 제1항에 있어서, 미세 미립자 형태의 시클로스포린.The cyclosporine of claim 1 in the form of fine particulates. 제6항에 있어서, 그 성분 입자가M의 평균입자가 크기를 갖는 시클로스포린.The method of claim 6 wherein the component particles Cyclosporin having an average particle size of M. 제7항에 있어서, 그 성분 입자가 0.5 내지M의 평균입자 크기를 갖는 시클로스포린.The method according to claim 7, wherein the component particles are from 0.5 to Cyclosporine with an average particle size of M. 제6항에 있어서, 그 성분 입자가 〈25μM의 평균입자 크기를 갖는 시클로스포린.The cyclosporin of claim 6, wherein the component particles have an average particle size of <25 μM. 제1항에 있어서, 주로, 또는 전적으로 또는 거의 전적으로 비-분쇄된 결정 물질로 구성된 시클로스포린.The cyclosporin of claim 1, which consists predominantly or wholly or almost entirely of non-milled crystalline material. 제6항에 있어서, 그 성분 입자가 주로 또는 전적으로 또는 거의 전적으로 비-분쇄된 미소-결정성 물질로 구성된 시클로스포린.7. The cyclosporine of claim 6, wherein the component particles consist mainly of wholly or almost entirely non-milled microcrystalline material. 제1항에 있어서, 멸균 또는 거의 멸균상태의 시클로스포린.The cyclosporine of claim 1 which is sterile or near sterile. a) 활성 성분으로서 사방정계 결정성 형태의 시클로스포린과 함계 b) 그것을 위한 약학적 허용 희석제 또는 담체를 함유하는 약학적 조성물.A) A pharmaceutical composition comprising as an active ingredient cyclosporine in tetragonal crystalline form and b) a pharmaceutically acceptable diluent or carrier therefor. 제13항에 있어서, 그 조성물에 존재하는 시클로스포린이 주로, 또는 전적으로 또는 거의 전적으로 사방정계 결정 형태로 존재하는 약학 조성물.The pharmaceutical composition of claim 13, wherein the cyclosporin present in the composition is present in predominantly or wholly or almost entirely tetragonal crystal form. 제13항에 있어서, 사방정계 결정 형태로 시클로스포린을 함유하는 적어도 하난의 컴파트먼트 또는 페이스(상)을 가지며, 그 결정 형태는 그 컴파트먼트 또는 페이스 전체에 분포되어 있는 약학 조성물.The pharmaceutical composition according to claim 13, having at least one compartment or phase (phase) containing cyclosporin in a tetragonal crystal form, the crystal form being distributed throughout the compartment or face. 제13항에 있어서, 비-용매 화합물 사방정계 결정 형태를 함유하는 약학 조성물.The pharmaceutical composition of claim 13, wherein the pharmaceutical composition contains a non-solvent compound tetragonal crystal form. 제13항에 있어서, 주사 또는 주입에 의해 유동성 형태로 국소 적용되거나 또는 적용되는 약학 조성물.The pharmaceutical composition of claim 13, wherein the pharmaceutical composition is topically applied or applied in a flowable form by injection or infusion. 제13항에 있어서, 그 조성물의 총 중량에 대하여 0.05 내지 30중량%의 시클로스포린을 함유하는비 약학 조성물.A non-pharmaceutical composition according to claim 13, which contains from 0.05 to 30% by weight of cyclosporin relative to the total weight of the composition. 치료를 요하는 환자에게 사방정계 결정 형태로 유효량의 시클로스포린을 투여하여, 환자에 시클로스포린 치료를 실시하는 방법.A method for administering cyclosporine to a patient in need thereof by administering an effective amount of cyclosporin in a tetragonal crystal form. 제19항에 있어서, 치료가 필요한 환자에게 사방정계 결정 형태로 유효량의 시클로스포린을 투여하여 면역 억제치료 또는 항-염증 치료를 실시하는 방법.The method of claim 19, wherein the patient in need thereof is administered an immunosuppressive or anti-inflammatory treatment by administering an effective amount of cyclosporin in the form of tetragonal crystals. 제19항에 있어서, 그 시클로스포린이 비-용매 화합물 사방정계 결정 형태인 것인 방법.20. The method of claim 19, wherein the cyclosporin is in a non-solvent compound tetragonal crystal form. 제19항에 있어서, 그 투여가 국소적이거나 또는 주사에 의한 것인 방법.The method of claim 19, wherein the administration is topical or by injection. 제19항에 있어서, 그 투여가 국소적 안(眼) 적용 또는 피부적용이거나 또는 병소내 또는 관절내 주사에 의한 것인 방법.The method of claim 19, wherein the administration is topical ophthalmic application or skin application or by intra- or intra-articular injection. ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: It is to be disclosed based on the initial application.
KR1019880017194A 1987-12-21 1988-12-20 Orthorhombic ciclosporin crystal form, process for its production and pharmaceutical compositions containing it KR100188305B1 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US13623087A 1987-12-21 1987-12-21
US17261388A 1988-03-24 1988-03-24
US21254888A 1988-06-28 1988-06-28
US212548 1988-06-28
US172613 1998-10-15
US136230 2002-05-01

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KR890009975A true KR890009975A (en) 1989-08-05
KR100188305B1 KR100188305B1 (en) 1999-06-01

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KR1019880017194A KR100188305B1 (en) 1987-12-21 1988-12-20 Orthorhombic ciclosporin crystal form, process for its production and pharmaceutical compositions containing it

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JP (1) JPH0791316B2 (en)
KR (1) KR100188305B1 (en)
AT (1) AT403163B (en)
AU (1) AU626274B2 (en)
BE (1) BE1002665A4 (en)
CA (1) CA1341396C (en)
CH (1) CH677926A5 (en)
CY (1) CY1799A (en)
DE (1) DE3843054C2 (en)
DK (1) DK175220B1 (en)
ES (1) ES2012580A6 (en)
FI (1) FI89065C (en)
FR (1) FR2624863B1 (en)
GB (1) GB2211848B (en)
GR (1) GR1002486B (en)
HK (1) HK102894A (en)
HU (1) HU203564B (en)
IE (1) IE62006B1 (en)
IL (1) IL88719A0 (en)
IT (1) IT1235356B (en)
LU (1) LU87409A1 (en)
MY (1) MY103943A (en)
NL (1) NL195096C (en)
NO (1) NO177228C (en)
NZ (1) NZ227384A (en)
SE (1) SE503174C2 (en)
SG (1) SG99494G (en)

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GB9105705D0 (en) * 1991-03-18 1991-05-01 Sandoz Ltd Improvements in or relating to organic compounds
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US7732404B2 (en) 1999-12-30 2010-06-08 Dexcel Ltd Pro-nanodispersion for the delivery of cyclosporin
AU2005209201B2 (en) 2004-01-20 2010-06-03 Allergan, Inc. Compositions for localized therapy of the eye, comprising preferably triamcinolone acetonide and hyaluronic acid
CN1763084B (en) * 2005-10-11 2010-04-21 山东新时代药业有限公司 High purity cyclosporin A preparation method
UA113627C2 (en) * 2011-05-27 2017-02-27 CRYSTAL FORM OF CYCLOSPORIN A, PHARMACEUTICAL COMPOSITION AND METHOD OF TREATMENT
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EP2780358B1 (en) * 2011-11-15 2016-03-23 Allergan, Inc. Cyclosporine a form 2 and method of making same
EP2779993B1 (en) * 2011-11-15 2018-04-04 Allergan, Inc. Autoclavable suspensions of cyclosporin a form 2
CA2856057C (en) 2011-11-15 2017-01-03 Allergan, Inc. Suspensions of cyclosporin a form 2

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Also Published As

Publication number Publication date
LU87409A1 (en) 1989-07-07
DE3843054C2 (en) 2003-08-21
GR880100850A (en) 1994-03-31
NO885625L (en) 1989-06-22
AU2705588A (en) 1989-06-22
JPH01211598A (en) 1989-08-24
ES2012580A6 (en) 1990-04-01
CA1341396C (en) 2002-11-05
NZ227384A (en) 1991-09-25
FR2624863A1 (en) 1989-06-23
NO885625D0 (en) 1988-12-19
IE62006B1 (en) 1994-12-14
IT8848690A0 (en) 1988-12-20
CY1799A (en) 1995-02-17
SE8804570L (en) 1989-06-22
FI89065C (en) 1993-09-30
AU626274B2 (en) 1992-07-30
NL195096C (en) 2004-02-09
SE8804570D0 (en) 1988-12-19
IE883779L (en) 1989-06-21
KR100188305B1 (en) 1999-06-01
GB8829556D0 (en) 1989-02-08
NO177228B (en) 1995-05-02
NO177228C (en) 1995-08-09
HU203564B (en) 1991-08-28
GB2211848A (en) 1989-07-12
BE1002665A4 (en) 1991-04-30
FI885869A0 (en) 1988-12-19
JPH0791316B2 (en) 1995-10-04
CH677926A5 (en) 1991-07-15
SE503174C2 (en) 1996-04-15
FI89065B (en) 1993-04-30
DK175220B1 (en) 2004-07-12
MY103943A (en) 1993-10-30
DE3843054A1 (en) 1989-07-27
SG99494G (en) 1994-10-28
GR1002486B (en) 1996-12-09
IL88719A0 (en) 1989-07-31
FI885869A (en) 1989-06-22
GB2211848B (en) 1991-11-06
DK705488A (en) 1989-06-22
FR2624863B1 (en) 1991-04-26
ATA309588A (en) 1997-04-15
IT1235356B (en) 1992-06-30
HK102894A (en) 1994-09-30
DK705488D0 (en) 1988-12-19
NL8803125A (en) 1989-07-17
AT403163B (en) 1997-11-25
HUT49893A (en) 1989-11-28

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