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Diclofenac Formulations and Methods of Use

a technology of diclofenac and formulation, which is applied in the field ofdiclofenac formulations and methods of use, can solve the problems of inability to treat all symptoms of diclofenac, difficulty in dissolving sachets, and inability to meet the needs of patients, and achieves the effects of rapid bioavailability of formulations, improved consistency of bioavailability, and improved drug safety

Inactive Publication Date: 2009-08-06
APR APPLIED PHARMA RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a new method for treating migraines and other acute pain with a fast-acting form of diclofenac. These formulations provide sustained relief for up to a full day, and can prevent rebound headaches. The method involves administering a liquid formulation of diclofenac that is dissolved or suspended in water and has a rapid onset of action. These formulations are more effective than traditional NSAIDs and can provide better relief of symptoms associated with migraines, such as photophobia and phonophobia. The method can be used to treat migraines that are accompanied by photophobia and phonophobia. The invention also provides a method for preparing powder diclofenac sachets with consistent bioavailability and a controlled particle size. Overall, the invention provides a more effective and consistent treatment for migraines and other acute pain.

Problems solved by technology

None of the studies reported to date suggests that a 50 mg. diclofenac product could treat all of these symptoms within two hours of treatment.
One of the primary obstacles in the manufacture of powder sachets is the distribution of the drug in the powder, and the uniformity of content in the finished product.
These hurdles are magnified in the production of diclofenac sachets due to the poor aftertaste of diclofenac, and the need to incorporate additional ingredients to compensate for this poor taste.
The method described by Reiner et al. produces an excellent pharmaceutical dosage form but suffers from a number of disadvantages including the size of the sachet (2 g) which makes the sachet more difficult to dissolve, and the presence of sugar in the formulation, which should be avoided in the diabetic population.

Method used

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  • Diclofenac Formulations and Methods of Use

Examples

Experimental program
Comparison scheme
Effect test

example 1

Comparative Study of Diclofenac-K Sachet, Diclofenac-K Tablets and Placebo in Treatment of Migraine

[0100]A randomized, double-blind, double-dummy multi-center, single dose, placebo- and active-controlled crossover study, with an eight hour evaluation was undertaken in adult migraine patients. 328 patients were randomized among treatments and a comparison made among treatments with a 50 mg. diclofenac potassium sachet formulation, the 50 mg. diclofenac potassium sugar coated tablet marketed commercially as Cataflam®, and placebo. Results are reported in Table 1.

TABLE 1Pain on Verbal ScaleDiclofenac-KParameterSachetDiclofenac-K TabletPlaceboPain free at 2 hours% of patients% of patients% of patientsITT pop24.7%18.5%11.7%PP pop23.6%17.8%12.9%Mod-sev24.2%17.0%12.5%baseline painHeadache response46.0%41.6%24.1%2 hoursSustained response36.8%30.9%18.4%Sustained pain free22.3%15.1%9.4%

example 2

Comparative Study of Diclofenac-K Sachet, Diclofenac-K Tablets, and Placebo in Treatment of Acute Dental Pain

[0101]A double-blind, randomized, parallel-group trial compared the analgesic efficacy of single 50 mg doses of diclofenac potassium sachets and tablets with placebo in 184 patients with moderate / severe pain after extraction of impacted third molar(s). The primary efficacy variable was the average pain reduction from baseline during the first 2 hours after intake of study medication, assessed using a visual analog scale (VAS). During the first 2 hours post-dose sachets and tablets demonstrated significantly less pain (P<0.05) versus placebo and sachets were more effective than tablets (P<0.05). Onset of analgesic effect (VAS) was maintained for 8 hours for sachets and tablets (P<0.05). Fewer patients remedicated versus placebo and the results for pain relief and intensity assessed on a verbal scale confirmed the findings for VAS pain intensity. No safety issues were identifie...

example 3

Representative 900 mg. Powder Sachet Formulation

[0102]Table 3 describes the composition of a representative 900 mg. powder sachet formulation containing 50 g. of diclofenac potassium that is suitable for practicing the present invention.

TABLE 3Name of theUnitcomponent(mg.)FunctionReference standardDiclofenac50.0Active substancePh. Eur.potassium1Glycerol dibehenate2.0LubricantPh. Eur.Saccharin sodium5.0Sweetening agent,Ph. Eur.Flavoring enhancerAnise flavor15.0Flavoring agentIn-house specificationsPotassium hydrogen22.0Buffering agentPh. Eur.CarbonateMint flavor35.0Flavoring agentIn-house specificationsAspartame50.0Sweetening agent,Ph. Eur.Flavoring enhancerMannitol2721.0DiluentPh. Eur. +additional specificationTotal weight900.01Particle size distribution:Not less than 90% ≦500 μmNot less than 40% and not more than 70% ≦200 μmNot less than 35% and not more than 65% ≦150 μmNot less than 30% ≦100 μm2As Mannitol “coarse quality” (648.0 mg) and Mannitol “fine quality” (73.0 mg).

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Abstract

Methods and formulations are provided for treating migraine and other acute pain episodes using diclofenac, and formulations of diclofenac that provide both rapid and sustained relief from acute pain. Methods and formulations are also provided for treating symptoms that often accompany migraine and acute pain such as photophobia, phonophobia, nausea and vomiting.

Description

RELATED APPLICATIONS[0001]This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Patent Application Nos. 60 / 692,024 (filed Jun. 17, 2005), and 60 / 691,757 (filed Jun. 17, 2005).FIELD OF THE INVENTION[0002]This invention concerns methods and formulations for treating migraine and other acute pain episodes using diclofenac, and formulations of diclofenac that provide both rapid and sustained relief from acute pain. The invention further concerns methods and formulations for treating symptoms that often accompany migraine and acute pain such as rebound headache, photophobia, phonophobia, nausea and vomiting.BACKGROUND OF THE INVENTION[0003]Diclofenac is a non-steroidal anti-inflammatory drug (“NSAID”) known chemically as [(2,6-dichloro-anilino)-2-phenyl]-2-acetic acid. The drug was developed in the 1960s by scientists at Ciba-Geigy and is sold around the world by Novartis under various trade names, including Cataflam® and Voltaren® in the United States. A wet gran...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/196C07C63/00A61P25/06
CPCA61K9/0095A61K9/08A61K47/14A61K31/196A61K9/14A61K47/10A61K9/145A61K9/1623A61K9/2013A61P25/06A61P29/00A61K9/16A61K47/02A61K9/0053
Inventor REINER, GIORGIOREINER, ALBERTOMEYER
Owner APR APPLIED PHARMA RES
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