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Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic

A dosage form and tablet technology, applied in the field of preparing the gastric retention type dosage form, can solve problems such as difficulties

Inactive Publication Date: 2011-06-22
蒂宝制药公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Finally, the production of acetaminophen in solid oral dosage forms is known to be difficult

Method used

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  • Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic
  • Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic
  • Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic

Examples

Experimental program
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preparation example Construction

[0114] Dosage forms disclosed herein prepared for oral administration will generally contain other inactive additives (excipients) such as binders, lubricants, disintegrants, fillers, stabilizers, surfactants, colorants and the like. Binders are used to impart cohesive properties to the tablet and thus ensure that the tablet remains intact after compression. Suitable binding substances include, but are not limited to, starches (including corn starch and pregelatinized starch), gelatin, sugars (including sucrose, glucose, dextrose, and lactose), polyethylene glycols, waxes, and natural and synthetic gums For example, gum arabic, sodium alginate, polyvinylpyrrolidone, cellulose polymers (including hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, microcrystalline cellulose, ethyl cellulose, hydroxyethyl cellulose Cellulose, etc.), and magnesium aluminum silicate (Veegum). The use of a lubricant facilitates tablet preparation, facilitates powder flow and...

Embodiment 1

[0196] Acetaminophen (APAP) and phenylephrine (PE) combination formulation.

[0197] Dosage forms were prepared using phenylephrine HCl ("PE") as a model. Phenylephrine has high water solubility (500mg / ml) and molecular weight (203.67 Dalton (Da)). This solubility is of the same order as the aforementioned opioids in a similar molecular weight range (approximately 350 to 450 Da), with similar milligram-based dose strengths and dose ranges.

[0198] Four formulations containing acetaminophen (APAP), phenylephrine (PE), and an extended release product 960 mg tablet of a swellable polymer were prepared using the dry blend method and processed on a Carver Auto C tablet press (Fred Carver, Inc. , Indiana). The formulation also includes polyvinylpyrrolidone (PVP) and magnesium stearate. In formulations (samples) 3 and 4, microcrystalline cellulose (MCC) was also added. The dry blend method involved mixing all ingredients in a glass jar and compressing into 960 mg tablets using 0...

Embodiment 2

[0229] Paracetamol and oxycodone hydrochloride extended-release gastroretentive formulation.

[0230] Contains acetaminophen, oxycodone hydrochloride, and two polyethylene oxide polymers (POLYOX ) of the sustained-release matrix is ​​prepared using a fluidized bed granulation process followed by sieving, mixing and compression. Each formulation was prepared in 1000 g batches and contained 42.3 to 42.4 wt% acetaminophen, 2.3 to 2.4 wt% oxycodone hydrochloride, and 1.4 wt% polyvinylpyrrolidone USP (K-29 / 32). After granulation, the API granules were sieved through a USP #20 mesh sieve and mixed with varying amounts of two different grades of POLYOX Microcrystalline cellulose (Avicel PH101NF) was blended with magnesium stearate NF. The mixture is then compressed into tablets, ready for analysis. The amount and type of polymer present varied from batch to batch. Table 11 below shows the POLYOX containing 1105 and POLYOX Batch formulations of N60K. Microcrystalline cellul...

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Abstract

Compositions and methods for the treatment of pain in a mammal are described. More specifically, a dosage form designed for release of acetaminophen and an opioid is described, wherein the dosage form provides delivery of the drugs to the upper gastrointestinal tract ('Gl') of a mammal for an extended period of time.

Description

[0001] This application claims the benefit of US Provisional Application No. 61 / 035,696, filed March 11, 2008, which is incorporated herein by reference. technical field [0002] Compositions and methods are described for alleviating or treating existing or anticipated pain. In some embodiments, a gastric-retentive ("GR") dosage form comprises acetaminophen (APAP) and a combined opioid analgesic and is administered to a person suffering from, diagnosed with, or at risk of experiencing pain. When the dosage form is administered to a mammal, generally about 3 hours to about 12 hours are provided for administration of one or both of the agents to the mammal's upper gastrointestinal tract ("GI"). The present disclosure also relates to methods of treating pain by providing such gastroretentive dosage forms, and methods of making such gastroretentive dosage forms. Background technique [0003] It is desirable to administer an opioid analgesic in combination with a non-opioid anal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/00
CPCA61K9/209A61K9/0065A61K31/167A61P25/04A61K2300/00
Inventor 韩建璇M·L·里德
Owner 蒂宝制药公司
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