Time limit pulse discharge system 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(JP2017019858) 時限​パルス​放出​システム
公开号/公开日
JP2017019858 A 2017-01-26 [JP2017019858] / 2017-01-26
申请号/申请日
2016JP-0201704 / 2016-10-13
发明人
;
申请人
ADAIR PHARMACEUTICALS;
主分类号
IPC分类号
A61K-009/20A61K-009/50A61K-047/10A61K-047/14A61K-047/32A61K-047/36A61K-047/38A61K-047/44A61K-047/46
摘要
(JP2017019858) A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described.  The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating.  Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics.  The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications.  (From EP2638899 A1)
机翻摘要
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地址
代理人
代理机构
;
优先权号
2005US-11120139 2005-05-02
主权利要求
(JP2017019858)  1. Immediately discharge (IR) the beads and time limit pulse discharge (TPR) include the blend of the beads being the medical supply multi particle medicine shapes which, the aforementioned TPR beads, a) The basic active medicine component of 1 kinds or plural kinds or that the core particle which includes the salt which is allowed pharmacy and, b) Inside surrounding the aforementioned core particle, being barrier coating, inside including i) intestinal soluble macromolecule or II) water insoluble macromolecule independently, or combining with the water soluble structure hole macromolecule barrier coating and, c) The water insoluble macromolecule the intestinal soluble macromolecule and outside including together, being delay coating, outside at least bringing the delay time of approximately 5 hours to start of medicine discharge, the membrane It includes, medical supply multi particle medicine shapes. 2. The aforementioned active medicine component, the anesthetic medicine and the anti- spasm medicine, the anti- diabetes medicine and the anti- infection medicine, the anti- malignant tumor medicine and the anti- parkinson's disease medicine, the anti- [riumachi] medicine, the heart blood vessel medicine, CNS (central nervous system) the stimulus medicine, the dopamine receptor operation medicine, the system *** medicine, the stomach medicine, the psychotherapy medicine, the [opioido] operation medicine and the [opioido] competition medicine, the anti- epilepsy medicine, is selected from the histamine H2 competition medicine, the anti- asthmatic medicine and the group which consists of the skeletal muscle relaxation medicine, in claim 1 medical supply multi particle medicine shapes of statement. 3. The beads group of two or more which give the target medicine movement profile which is suited for the dosage plan of one day 1 time or 2 times is included, when released metal content test doing USP device 1 or 2, and two gradual liquation solvent (first 2 hours, after that 900mL (pH6.8) in) of making use in HCl of 0.1N of 700mL, each group specified (goal) shows medicine discharge profile, in claim 1 medical supply multi particle medicine shapes of statement. 4. At least, the IR beads group of 1 kinds, the 1TPR beads group and the 2TPR beads group are included, of the IR beads and ratio of the aforementioned 1TPR beads group and the aforementioned 2TPR beads group, changes from each one approximately 10/20/70 up to approximately 30/60/10 degree of alkalinity of the aforementioned active ingredient, pH dependant solubility and/or according to discharge half-life, in claim 1 medical supply multi particle medicine shapes of statement. 5. The aforementioned core particle, i) The inactive particle which with the active ingredient and the high-molecular binder was covered, or II) [rotoguraniyureshiyon] and granulation - it pushed out and it was produced - spheroidization or granulation - by tablet conversion, the aforementioned active ingredient, the pellet which contains the high-molecular binder and diluent/the bulking agent or the mini- or micro tablet is included, in claim 1 medical supply multi particle medicine shapes of statement. 6. The aforementioned high-molecular binder, poly- vinyl pyrolidone, the methyl cellulose, the hydroxypropyl cellulose and the hydroxypropyl methyl cellulose, is selected from the cornstarch, the alpha conversion starch and the group which consists of those blends, in claim 5 medical supply multi particle medicine shapes of statement. 7. The aforementioned particle barrier coating, the acetic acid phthalic acid cellulose, the phthalic acid hydroxypropyl methyl cellulose and the succinic acid hydroxypropyl methyl cellulose, poly- vinyl acetate phthalate and pH sensitivity methacrylic acid - methyl methacrylate copolymer, includes the intestinal soluble macromolecule which is selected from the shellac, those derivatives, and the group which consists of those blends, in claim 1 medical supply multi particle medicine shapes of statement. 8. The aforementioned barrier coating constitutes approximately 5-20 of the aforementioned barrier coating beads weight %, in claim 7 medical supply multi particle medicine shapes of statement. 9. The particle core, the water insoluble macromolecule independently, or combining with the water solubility macromolecule approximately 9:1-5: The barrier coating which is included at ratio of 5 is had, the aforementioned barrier coating is administered in order approximately 1.5-15 weight % just weight to increase with the weight of the aforementioned coating beads as a standard, in claim 1 medical supply multi particle medicine shapes of statement. 10. The aforementioned water solubility the macromolecule, the methyl cellulose, the hydroxypropyl methyl cellulose and the hydroxypropyl cellulose, are selected from the group which consists of poly- vinyl pyrolidone and polyethylene glycol and those blends etc, in claim 9 medical supply medicine shape of statement. 11. Way delay coating outside the description above, approximately 30-60 weight % just weight it increases with the weight of the aforementioned TPR beads as a standard, the water insoluble macromolecule and the intestinal soluble macromolecule the respective approximately 10:1-1: It includes at ratio of 2, in claim 1 medical supply medicine shape of statement. 12. The aforementioned water insoluble macromolecule, the ethyl cellulose and cellulose acetate, is selected from the polymer of poly- vinyl acetate and methyl methacrylate ester and the group which consists of those blends, in claim 11 medical supply medicine shape of statement. 13. At least one side of barrier coating inside the description above and delay coating outside the description above, the triacetin, citric acid tributyl, citric acid triethyl, acetyl citric acid tributyl, the phthalic acid diethyl, dibutyl sebacate, polyethylene glycol and polypropylene glycol, the castor oil, the plasticizer which is selected from acetylation mono glyceride and the group which consists of [jiguriserido], and those blends is included, in claim 1 medical supply medicine shape of statement. 14. The aforementioned delay coating, to the respective approximately 3:1- approximately 1:1 includes the water insoluble macromolecule and the intestinal soluble macromolecule at various ratios, in claim 1 medical supply medicine shape of statement. 15. The aforementioned medicine shape, the immediately discharge which gives the load dosage quantity by discharging approximately 90% or more of the aforementioned active ingredient which is included in the aforementioned IR beads within 1 hours of beginning after the oral administration of the aforementioned medicine shape (IR) furthermore includes the beads, in claim 1 medical supply medicine shape of statement. 16. The aforementioned medicine shape time limit pulse discharge of 2 types (TPR) includes the beads group at least, the emission characteristic where each TPR beads group follows to specified delay time the oral administration time of the aforementioned medicine shape and differs is shown, in claim 1 medical supply medicine shape of statement. 17. The aforementioned delay coating, includes the ethyl cellulose and the phthalic acid hydroxypropyl methyl cellulose, in claim 1 medical supply medicine shape of statement. 18. A) The basic active medicine component of 1 kinds or plural kinds or that IR which includes the salt which is allowed pharmacy (immediately discharge) the step which produces the beads and, b) Being the step which administers barrier coating to the aforementioned IR beads, in order the aforementioned barrier coating just approximately 1.5%-20% weight to increase with the dry weight of the aforementioned coating beads as a standard, the step which includes the intestinal soluble macromolecule or the water insoluble macromolecule and, c) In order just approximately 30%-60% weight to increase with the dry weight of the aforementioned coating beads as standard, the water insoluble macromolecule combining with the intestinal soluble macromolecule the respective approximately 10:1-1: Outside including at ratio of 2, by administering delay coating time limit pulse discharge (TPR) the step which forms the beads and, d) It fills up the TPR beads group of 1 kinds or plural kinds of proper quantity in the gelatin capsule, or former tablet or ODT (the collapse lock inside the buccal cavity) compressed, (one day it was suited for the dosage plan of 1 time or 2 times in the patient who needs that kind of active medicine component) goal PK (medicine movement) the step which achieves profile It includes, production method of multi particle medicine shapes. 19. Delay coating outside the description above is administered from the solution or the water dispersed liquid of the solvent type which is allowed pharmacy, in claim 18 method of statement. 20. When the aforementioned medical supply medicine shape, the gelatin capsule, enters into the stomach hard, collapsing quickly, the former tablet which becomes the coating beads, or (cheek side) collapsing quickly in the buccal cavity, it is form of the oral collapsible tablet which forms the suspensoid which it is easy to swallow, in claim 18 method of statement. 21. The aforementioned medical supply medicine shape, the IR beads which give the target PK discharge profile in the patient who needs that kind of remedy furthermore are included, in claim 18 method of statement. 22. In the claim 1 which contains the active medicine component of 1 kinds or plural kinds of quantity which remedy is effective medicine shape of statement the method of including the fact that it prescribes to the patient orally. 23. Medicine shape of statement being the method of including the fact that it prescribes to the patient orally in claim 1, the IR beads group and it includes 1 kinds or plural kinds of the active medicine component of 1 kinds or plural kinds of quantity where the aforementioned medicine shape remedy is effective the multilayer coating TPR beads group, the method of showing the emission characteristic where each multilayer coating TPR beads group follows to the delay time of 5 hours at least and differs.
法律状态
(JP2017019858) LEGAL DETAILS FOR JP2017019858  Actual or expected expiration date=2026-05-01    Legal state=ALIVE    Status=PENDING     Event publication date=2016-10-13  Event code=JP/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=JP JP2016201704  Application date=2016-10-13  Standardized application number=2016JP-0201704     Event publication date=2016-10-31  Event code=JP/A621  Event indicator=Pos  Event type=Examination events  Written request for application examination  Effective date of the event=2016-10-31  JAPANESE INTERMEDIATE CODE: A621     Event publication date=2017-01-26  Event code=JP/A  Event indicator=Pos  Event type=Examination events  Published application  Publication country=JP  Publication number=JP2017019858  Publication stage Code=A  Publication date=2017-01-26  Standardized publication number=JP2017019858
专利类型码
A
国别省市代码
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