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Controlled release pharmaceutical formulations of nitazoxanide

A controlled release agent, nitazoxanide technology, applied to solid dosage forms of nitazoxanide and nitazoxanide analogues, for the treatment of patients with hepatitis C, a field of patients, capable of addressing nitazoxanide The absorption of tezoxanide and tizoxanide is variable, side effects, and the mechanism of action of nitazoxanide is not clear, etc.

Inactive Publication Date: 2012-03-28
ROMARK LAB L C
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Problems that must be overcome in the development of new optimized dosage forms for the treatment of chronic hepatitis C are: variable absorption of nitazoxanide and tizoxanide in different dosage forms, very short half-life of tizoxanide in plasma and side effects associated with high doses of nitazoxanide and tizoxanide in the gut
In addition, since the mechanism of action of nitazoxanide against HCV is unknown, it is impossible to know whether fluctuations in the highest and lowest concentrations at the site of infection are beneficial or detrimental to improved efficacy

Method used

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  • Controlled release pharmaceutical formulations of nitazoxanide
  • Controlled release pharmaceutical formulations of nitazoxanide
  • Controlled release pharmaceutical formulations of nitazoxanide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Factors affecting the bioavailability of nitazoxanide

[0065] In order to investigate the impact of the following factors on the bioavailability of nitazoxanide, the present invention has been studied: (1) the absorption of tizoxanide is compared with the absorption of nitazoxanide, (2) changes in the absorption of nitazoxanide in the gastrointestinal tract Site of release, (3) effect of different polymers, and (4) effect of granulation in alcohol versus water.

[0066] To study each factor, six different nitazoxanide and / or tizoxanide formulations were orally administered with food to four healthy adult male volunteers. Each volunteer received each of the six dosage forms in six different treatment periods with at least one week between each treatment period. The dosage form is administered orally with food. Blood samples were collected at the following eleven time points: just before dosing and 1, 2, 3, 4, 5, 6, 7, 8, 10, and 12 hours after dosing. Administer th...

Embodiment 2

[0088] bilayer tablet dosage form

[0089] Bilayer tablets containing a total of 650 mg of nitazoxanide were manufactured using standard dosage form techniques as previously described. The composition of the bilayer tablet is listed in Table 2.

[0090] Table 2: Composition of 675 mg Nitazoxanide Controlled Release Tablets.

[0091]

[0092]

[0093] * Refer to the current version.

Embodiment 3

[0095] Batch formulation of bilayer tablets

[0096] As indicated in Table 3, a batch of 100,000 bilayer tablets of nitazoxanide of Example 2 (650 mg) was prepared.

[0097] Table 3. Batch production formulation of 675mg nitazoxanide controlled release tablet

[0098]

[0099]

[0100] Tablets were manufactured following the manufacturing protocol outlined below.

[0101] a. equipment

[0102] Frewitt Sieve

[0103] Collette Planetary Blender

[0104] oven

[0105] Tablet Press - Manesty BB Press

[0106] tablet duster

[0107] Coating Equipment-Accelacota

[0108] Clean all production equipment before use.

[0109] b. Preparation of Immediate Release Granules (Granule A)

[0110] 1. Weigh the raw material and put it into a sealed plastic bag.

[0111] 2. Check the integrity of the machine before and after use.

[0112] 3. If necessary, nitazoxanide and cornstarch were sifted through a sieve with a mesh size of 1.25 mm using a Frewitt machine.

[0113] 4....

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Abstract

Solid dosage formulations of nitazoxanide or a nitazoxanide analogue are provided that comprise a controlled release portion and an immediate release portion. The pharmaceutical composition is typically in the form of a bilayer solid oral dosage form comprising (a) a first layer comprising a first quantity of nitazoxanide or analogue thereof in a controlled release formulation; and (b) a second layer comprising a second quantity of nitazoxanide or analogue thereof in an immediate release formulation. Method of using the formulations in the treatment of hepatitis C are also provided.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application No. 61 / 202,285, filed February 13, 2009. Background technique [0003] Nitazoxanide (2-(acetoxy)-N-(5-nitro-2-thiazolyl)benzamide) is a compound having the following structure: [0004] [0005] The preparation and use of this compound is disclosed, for example, in US Patent No. 3,950,351 to Rossignol. [0006] A pharmaceutical composition containing nitazoxanide and its metabolite (tizoxanide) was initially developed and marketed for the treatment of intestinal parasitic infections. [0007] Following oral administration of nitazoxanide or a mixture of nitazoxanide and tizoxanide, in humans, these compounds are partially absorbed from the intestinal tract, and nitazoxanide is rapidly hydrolyzed in plasma to yield tizoxanide. Tizoxanide is a conjugated glucuronic acid, and the drug is excreted in urine and bile as tizoxanide or tizoxanide glucuronide. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/60A61K31/495
CPCA61K38/21A61K31/7056A61K9/284A61K9/2853A61K9/209A61K31/426A61K9/2086A61K2300/00A61P1/16A61P29/00A61P31/14A61P43/00A61K9/0053A61K9/28A61K9/48A61K2121/00A61K9/4808
Inventor 珍-弗朗索瓦·罗西诺尔马克·艾尔斯
Owner ROMARK LAB L C
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