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Methods, dosage forms, and kits for administering ziprasidone without food

A technology of ziprasidone and dosage forms, which is applied in the direction of pharmaceutical formulas, drug combinations, medical preparations containing active ingredients, etc., and can solve problems such as poor compliance

Inactive Publication Date: 2011-04-13
PFIZER INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Adherence among patients was similarly poor: about 40% of patients interviewed took at least half of their weekly ziprasidone doses without any source of calories

Method used

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  • Methods, dosage forms, and kits for administering ziprasidone without food
  • Methods, dosage forms, and kits for administering ziprasidone without food
  • Methods, dosage forms, and kits for administering ziprasidone without food

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0172] Ziprasidone dissolved in SBECD

[0173] Preparation of Ziprasidone Test Formulation: The ziprasidone test formulation comprises ziprasidone mesylate-SBECD lyophilized powder combined with HPMCAS in a mass ratio of about 1:6:2. The formulation was prepared according to the procedure given below: SBECD was charged into a flask containing water for injection (WFI) and heated until a solution was obtained. Subsequently, ziprasidone mesylate was added to the flask and heated until a solution was obtained. The solution was cooled and kept between 35 and 40C, then filtered through a 0.45 micron Kleenpak Ultipro N66 filter into a holding vessel. Subsequently, the solution was transferred to a dish. The solution was frozen at at least -40°C before the lyophilization cycle was initiated. Take a few weeks to warm up. The final drying cycle reduces the moisture content to less than 2%. The lyophilized powder is subsequently milled. 176.2 mg of milled lyophilized powder (equiv...

Embodiment 2

[0186] Ziprasidone nanoparticles

[0187] Preparation of Candidate Formulations: The test formulation, referred to herein as Formulation B, contained ziprasidone free base in nanoparticulate form. The formulation was prepared according to the procedure given below: A coarse suspension was prepared by placing 8.85 gm of ziprasidone free base into a 100 ml milling chamber containing 48.89 gm of milling media (500 micron polystyrene beads) liquid. To this was added 4.2ml of each of the following solutions 10% of F108 solution, 80 and 5% lecithin solutions. Additionally, 23.8 ml of water for injection was added to the milling chamber. The above mixture was stirred until a homogeneous suspension was obtained. Subsequently, the suspension was milled in a Nanomill-1 (Manufacturer ElanDrug Delivery, Inc.) at 2100 RPM for 30 minutes, with the temperature maintained at 4°C during milling. The resulting suspension was vacuum filtered to remove the milling media. An appropriate v...

Embodiment 3

[0198] Ziprasidone HCl

[0199] Ziprasidone coated crystals containing 35% active ziprasidone hydrochloride monohydrate coated with the precipitation inhibiting polymer HPMCAS were prepared as described in the aforementioned US Patent Application Publication 2007 / 0190129.

[0200] The test ziprasidone formulation of Example 3 (referred to as "Formulation C") was administered in the form of a powder-in-capsule (1 x 40 mg). The test drug information is shown in Table 5.

[0201] Table 5 Information on Study Drugs

[0202]

[0203] Results: The PK parameters after a single dose of the test formulations in the fed and fasted state, as well as after a single dose of the commercially available capsules in the fed state are summarized in Table 6. These data show the fasted AUC of the test formulation inf is the fed AUC of the test formulation inf 57% of and the fasting AUC of the test formulation inf It is 62% of the commercially available capsules fed state.

[0204] Table ...

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Abstract

The present invention provides methods, dosage forms and kits for treating with an effective amount of ziprasidone a CNS disorder in a human when the human is in a fasted state. In one embodiment, the invention relates to a method for treating a CNS disorder in a human, which method comprises administering to the human in a fasted state, a solid oral dosage form comprising an amount of ziprasidone effective to treat said CNS disorder, wherein the area under the serum concentration versus time curve (AUC0-inf) of the ziprasidone in the human subsequent to said administering is from 70% to 140% of the mean area under the ziprasidone serum concentration versus time curve (AUC0-inf) resulting from administration of a control ziprasidone immediate release oral capsule containing the same amount of ziprasidone to a cohort of humans in a fed state.

Description

Background technique [0001] Food has a significant effect on the absorption of many orally administered drugs (Welling PG. Effects of food on drug absorption. Annu Rev Nutr. 1996; 16:383-415). For some drugs, absorption is impaired when ingested with food. For other drugs, food facilitates absorption. Changes in drug absorption can have a major impact on potency and toxicity. Unexpectedly low absorption rates can manifest as reduced potency, while higher drug absorption rates can lead to greater odds of adverse events (AEs). Either consequence can affect treatment success and treatment compliance. [0002] Ziprasidone (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro- 2H-indol-2-one) is used for schizophrenia (Harvey PD, Bowie CR. ziprasidone: efficacy, tolerance, and emerging data on wide-ranging effectiveness. Expert Opin Pharmacother.2005; 6(2): 337-346 ) and bipolar disorder (Patel NC, Keck PE, Jr. ziprasidone: efficacy and safety in patient...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P25/18
CPCA61K31/496A61P25/00A61P25/18
Inventor 威廉·J·库拉托洛斯科特·M·赫比格阿维纳什·G·托姆布雷杰明·C·尚谢里·L·香布林蒂莫西·卢卡斯威廉·B·考德威尔德韦恩·T·弗里森戴维·K·莱昂克里斯托弗·D·克雷格
Owner PFIZER INC
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