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Gastric retentive pharmaceutical compositions for immediate and extended release of acetaminophen

A paracetamol, extended-release technology, applied in the direction of drug combination, drug delivery, antipyretics, etc., can solve the problems of increasing gastric delivery of acetaminophen and insufficient compression of acetaminophen powder into tablets

Inactive Publication Date: 2012-07-18
蒂宝制药公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Adding to the difficulty of formulating such tablets for gastric delivery of acetaminophen is the fact that acetaminophen powder cannot be compressed adequately into tablets

Method used

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  • Gastric retentive pharmaceutical compositions for immediate and extended release of acetaminophen
  • Gastric retentive pharmaceutical compositions for immediate and extended release of acetaminophen
  • Gastric retentive pharmaceutical compositions for immediate and extended release of acetaminophen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0171] Example 1: Formulation of a gastric-retentive tablet with 650 mg of acetaminophen

[0172] A prototype gastric retentive (GR) tablet containing 650 mg of acetaminophen in the gastric retentive layer was developed as follows.

[0173] Granulation of acetaminophen (Acetaminophen USP; Spectrum Chemical Mfg. Corp.) and binder (Plasdone K29 / 32; ISP Technologies) in glass jars along with other excipients listed in the table below Dry blend. Tablets were then manually prepared on a Carver Auto C Press (Fred Carver, Inc., Indiana) by compressing the granulation mixture into tablets using a 0.3937" x 0.7086" modified oval die (Natoli Engineering, St. Charles, MO). The parameters used to operate the Carver Auto C Press were as follows: 3000 lbs force, 0 second dwell time (settings on the Carver Press), and 100% compression speed. The formulations for the 2 tablet prototypes (Samples 1 and 2) are set forth in Table 1 below. The numbers in Table 1 reflect the amount of acetamin...

Embodiment 2

[0178] A prototype tablet containing 90% by weight of acetaminophen and 10% excipients by weight in various blends containing hydrophilic polymers. This granular powder of acetaminophen and related excipients was dry blended with the other excipients in the amounts detailed in Table 3, and tablets were prepared manually at the Carver Press as described in Example 1. Samples 3-5 were compressed into single GR layer tablets, while samples 6 and 7 were bilayer tablets where the GR layer was compressed together with the immediate release layer with the formulation presented in Table 4. As with the GR layer, the IR layer was generated by dry blending direct compression grade acetaminophen with other excipients prior to compression into bilayer tablets. The weight percent composition of the GR layer in samples 6 and 7 was the same as that of sample 4.

[0179]

[0180] The release rate profile of samples 4 and 5 was investigated using the USP disintegration apparatus and dissol...

Embodiment 3

[0185] Example 3: Erosion study on 650 mg gastroretentive tablet

[0186] This is a study in 5 healthy female beagles weighing between 12-16 kg to determine the erosion time of gastric-retained extended-release tablets of acetaminophen. After an overnight fast of at least 14 hours, dogs were fed 100 g of canned dog food (Pedigree® Traditional ground Dinner with Chunky Chicken). Within 15 minutes of the dogs consuming the meal, they administered acetaminophen gastric-retentive extended-release tablets.

[0187] Erosion of gastric-retained extended-release acetaminophen tablets assessed using fluoroscopy. Each tablet contains 2 radiopaque lines in the shape of an "X". Separation of the lines is considered to indicate complete erosion of the tablet. Images were acquired every 30 minutes until the lines separated. The results showed that the erosion time for the 650 mg GR tablet was 4.6 ± 0.5 hours. This predicts an erosion time of about 8 hours in humans.

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Abstract

Gastric retentive dosage forms for extended release of acetaminophen or for both immediate and extended release of acetaminophen are described. The dosage forms allow effective pain relief upon once- or twice-daily dosing Methods of treatment using the dosage forms and methods of making the dosage forms are also described.

Description

[0001] This application claims the benefit of US Provisional Application No. 61 / 238,374, filed August 31, 2009, which is incorporated herein by reference in its entirety. technical field [0002] The presented subject matter generally relates to dosage forms for immediate and extended release of acetaminophen into the stomach of patients in fed mode, and to methods of treatment using such dosage forms. Background technique [0003] Acetaminophen is widely accepted as an over-the-counter pain reliever and is available under many brand names and generic products. Acetaminophen is used for therapeutic indications, including pain and arthritis, and is also effective in reducing fever. Currently available dosage forms include tablets, caplets and oral suspensions. These dosage forms provide acetaminophen release over a period of 3, 4, 6 or 8 hours. [0004] Tylenol ER (extended release) formulations became available in 1995. The tablets are available as 650 mg caplets with an ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K47/30A61K9/22A61K9/20A61K31/16A61P1/04A61P1/00
CPCA61K31/167A61K9/2031A61K9/0065A61K9/2027A61K9/209A61P1/00A61P1/04A61P29/00A61P29/02A61K9/20A61K31/16A61K47/30
Inventor S.Y.E.候T.瓦加斯
Owner 蒂宝制药公司