Nova Patents
IS2182B

Ziprasidone formulations

Abstract

Compositions comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size less than 85 mu m, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to treat psychoses such as schizophrenia.

Term

Term ended

Expired 11 June 2019, 7.3 years ago.

  1. Priority
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  3. Granted
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  5. Today

14 claims: 14 independent, 0 dependent

  1. 1
    Demands Kröfur 1. A composition comprising a crystalline free base of ziprasidone or crystalline siprasidone hydrochloride particles having a median magnesium ester equal to or less than about 85 μm and a pharmaceutically acceptable diluent such as a carrier. 1. Samsetning sem samanstendur af kristölluðum frjálsum basa síprasídóns eda kristölluðum siprasidón hýdróklóríd ögnum sem hafa medalagnastaerd sem er jöfn eða minni en um það bil 85 pm og lyfjafrsedilega hæfu pynningarefni eda burdarefni.
  2. 2
    Composition of Compound # 1 in Compound 1, a pair of said composition comprising ziprasidone hydrochloride monohydrate. 2. Samsetning i samraemi vid krofu 1, par sem fyrmefnd samsetning inniheldur síprasidón hýdróklóríð einhýdrat.
  3. 3
    Samsetning ί samraemi vid krdfu 1, par sem fyrmefnd medalagnastaerd er join eda minni en 50 pm. 3. The composition of the group 1, pair of the aforementioned medalagnasterderd is less than 50 pm.
  4. 4
    Composition of the combination at krdfu 3, pair with the aforementioned medal scale score from 5 to 50 pm. 4. Samsetning f samraemi vid krdfu 3, par sem fyrmefnd medalagnastærd er frá 5 til 50 pm.
  5. 5
    Composition in combination 4, pair of the aforementioned medalagnastaerd is from 5 to 40 pm. 5. Samsetning Í samraemi vid krdfu 4, par sem fyrmefnd medalagnastaerd er frá 5 til 40 pm.
  6. 6
    Composition of samraemi at krdfu 5, pair of aforementioned medalagnasterderd is from 5 to 30 pm. 6. Samsetning i samraemi vid krdfu 5, par sem fyrmefnd medalagnastaerd er frd 5 til 30 pm.
  7. 7
    A composition of the foregoing, which shows the AUC and / or Cma, which is at least 80% of the AUC and / or Cma, which is equivalent to an equilibrium combination (by the mediagnasticated siprasidden) 20 pm. 7. Samsetning f samraemi vid hveija sem er af krdfunum hér á undan sem sýnir AUC og/eda Cmu sem er ad minnsta kosti 80% af medaltals AUC og/eda Cmu sem sóst fyrir jafngilda samsetningu sem er einungis fidbrugdin (pvi ad medalagnastaerd siprasfddns er 20 pm.
  8. 8
    Composition of cohabitation at 7th of which the bait pasta is a meal with Malvern Ijdsbroti. 8. Samsetning ί samraemi vid krdfu 7 par sem agnastaerdin er maeld med Malvern Ijdsbroti.
  9. 9
    A composition according to any one of the preceding claims, a pair of which the amount of said composition containing 100 mg less of the free base of siphrasis or 113.2 mg less of ziprasidone hydrochloride is found in USP-2 instrumentation containing 900 ml of 9. Samsetning f samraemi vid hverja sem er af krdfunum hér á undan, par sem, pegar magn af fyrmefndri samsetningu sem inniheldur 100 mg eda minna af frjdlsum basa siprasfddns eda 113,2 mg eda minna af síprasídón hýdrókldrfði er komid fyrir í USP-2 tækjabúnaði sem inniheldur 900 ml af NaH2PO4 aqueous solution pad pH 7.5 containing 2% w / v sodium dddecyl sulfate and equipped with splines at 75 cycles per minute, at least 70% of the sulfide buffer dissolved in the 45 minutes. NaH2PO4 vatnslausnarstudpúða, pH 7,5, sem inniheldur 2% (w/v) natrium dddekýl súliat, og er útbúínn med spddum sem hraera vid 75 hringi á mínútu, að minnsta kosti 70% af sfpraslddninu sem ar þar Í leysist upp innan 45 minútna.
  10. 10
    Notkun á samsetningu eins og skilgreind er ί hverri sem er af krdfunum hér á undan i framleiðslunni á lyfi til medhdndlunar eda fyrirbyggingar á gednofi. 10. Use of a composition as defined in any of the foregoing claims in the manufacture of a medicament for the prevention of dementia.
  11. 11
    A process for the production of large crystals of siphrasidone hydrochloride monohydrate, which consists of the steps of:11. Adferd til framleidslu á stórum kristöllum af siprasídón hýdrókldríð einhýdrati, sem felst f skrefunum ad: 1) dissolve a free base of ziprasidone solvent consisting of THF and water, (v / v ratio of about 22-35 volumes of THF at about 1.5-8 volumes of water;1) leysa upp frjálsan basa síprasídóns ί leysi sem samanstendur af THF og vatni, (rúmmálshlutfalli uppá um pad bil 22-35 einingarúmmál af THF á mdti um pad bil 1,5-8 rúmmálum af vatni;2) heat the solution resulting from step (1);2) hita lausnina sem kemur úr skrefi (1);3) Baeta HCI into the solution resulting from step (2);and 3) baeta HCI út f lausnina sem kemur úr skrefi (2);og 4) Kaela solution coming out of step (3). 4) kaela lausnina sem kemur úr skrefi (3).
  12. 12
    Adferd I samraemi vid krdfu 11, par sem rúmmálshlutfallið af THF á mdti vatni {fyrmefndum leysi er 24-30 á mdti 2-6. 12. Behavior In the case of rhodium 11, a pair of volumes of THF in water (the said solvent is 24-30 at 2-6.
  13. 13
    Adferd I samræmi vid annad hvort kidfu 11 eda krdfu 12, par sem, I fyrmefndu skrefi (3), er hitastigi fyrmefndrar lausnar haldid fyrir nedan bakflaedi. 13. Behavior In accordance with each other, if the kidneys are 12, the number of which, in the aforementioned step (3), the temperature of the aforementioned solution is maintained below the backing.
  14. 14
    Adferd Í samraemi vid krdfu 13, par sem fyrmefnt hitastig er 60-64°C. 14. Behavior In samraemi at krdfu 13, couples whose former temperature is 60-64 ° C.
Independent claims14