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Modafinil oral lyophilizate

a technology of oral lyophilizate and modafinil, which is applied in the direction of pill delivery, digestive system, metabolism disorder, etc., can solve the problems of inconvenient use of additives and preserving agents, inability to meet patients' diet restrictions, and inability to tolerate liquid dosage forms containing saccharose or sodium, etc., to achieve the effect of convenient swallowing

Inactive Publication Date: 2006-02-02
CEPHALON FRANCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nevertheless, although these modafinil tablets offer potential advantages regarding dose schedule by reducing the total number of doses of modafinil required per day by a patient, and a decreased size / volume, patients may remain noncompliant to their treatment, particularly when high dosage units are indicated for the treatment of disease or disorders.
However, dosing of active ingredients in liquid form is a random process even when using a dose spoon.
Also, liquid dosage forms generally contain saccharose or sodium which are not suitable for patients subjected to a restrictive diet.
The use of additives and preserving agents is thus generally unnecessary.
In addition, due to the small size of the microbeads, their modafinil dosage strength is very limited.
This dosage form is thus not suitable for a convenient administration of high strength modafinil dosages.

Method used

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  • Modafinil oral lyophilizate
  • Modafinil oral lyophilizate
  • Modafinil oral lyophilizate

Examples

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examples

Material and Methods

[0187] The modafinil particles of size 20-40 μm are commercially available (Cephalon, Inc., West Chester, Pa.). The modafinil particles of size 1-10 μm were prepared by micronizing modafinil particles of commercial grade 20-40 μm using a micronizer type Jet mill (Microjet Mill, Switzerland). The modafinil particles of size 200-315 μm were obtained by screening an API modafinil batch (Active Pharmaceutical Ingredient) through a 200 μm screen and a 315 μm screen. Modafinil lot with bounded particles size may be prepared by methods discloses in WO 2004 / 006905.

[0188] The glycerol palmitostearate was purchased as Precirol ATO 5® from Gattefossé (France).

Measurement of the Dissolution Kinetics of Oral Lyophilizates (Dissolution Assay)

[0189] The modafinil dissolution rate of oral lyophilizates was measured according to the following protocol.

[0190] The solutions to be analyzed were prepared by introducing an oral lyophilizate into 1L of HCl 0.1 M kept at a temper...

examples 1 to 4

[0205]

TABLE IExamples1234Modafinil particle size1-10μm20-40μm200-315μm300-500μmModafinil280mg280mg300mg300mgCopovidone0.7mg0.7mg0.7mg0.7mgDextran 7015mg15mg15mg15mgAspartam7mg7mg7mg7mgAcesulfam K10mg10mg10mg10mgFlavor (pineapple)15mg15mg15mg15mgCitric acid5mg5mg5mg5mgMannitol367.3mg367.3mg347.3mg347.3mgWater380mg380mg380mg380mgUnit weight700mg700mg700mg700mgTasteBitterBitterMaskedMaskedDissolution at 30 mn100%96%85%53%

[0206] As apparent from Table I, oral lyophilizates of modafinil with small particle size (1-10 μm or 20-40 μm) exhibited a bitter taste while an equivalent formulation prepared with large particle size (superior to 200 μm) is have a masked taste. However, the dissolution of oral lyophilizates with large particles is notably slower (FIG. 1).

examples 5 and 6

[0207] Oral lyophilizates were prepared as Example 1 according to the formulations set out in Table II and using modafinil particles of 20-40 μm coated with 4% and 50% by weight of glycerylpalmitostearate with respect to modafinil weight, respectively.

[0208] These coated modafinil particles were prepared by melting a specified quantity of glycerylpalmitostearate (Precirol® ATO5 from Gattefossé) in an appropriate vessel (a planetary or a turbosphere mixer) at about 60° C.-65° C. Modafinil of the specified particle size was then introduced and mixed until homogeneization. The obtained granules were screened through a 1 mm screen and stored at room temperature. They are used according to the same procedure as uncoated particles.

TABLE IIExamples56Modafinil (96%)Modafinil (50%)Precirol ®Precirol ®ATO 5 (4%)ATO 5 (50%)Modafinil (20-40 μm)300mg 140mgPrecirol ® ATO 512.5mg140mgCopovidone0.7mg0.7mgDextran 7015mg15mgAspartam7mg7mgAcesulfam K10mg10mgFlavor (pineapple)15mg15mgCitric acid5mg5...

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Abstract

The invention concerns an oral lyophilizate comprising modafinil particles having a median diameter of about 10 to about 1000 μm in association with an appropriate amount of at least one excipient selected from the group consisting of fatty acid esters of glycerol, cyclic oligosaccharides, sweeteners or mixtures thereof.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority of U.S. Provisional Application Ser. No. 60 / 598,553 filed Aug. 4, 2004. A right to priority is also claimed under 35 U.S.C. § 119 of European Patent Application No. 04291946.4, filed Jul. 29, 2004. The disclosures of these priority applications are incorporated herein by reference in their entireties for all purposes.FIELD OF THE INVENTION [0002] The present invention is related to oral lyophilizates of modafinil and a process of preparation thereof. The present invention relates to palatable lyophylizate that include modafinil and at least one or more diluents, binders and taste-masking, sweeteners and flavors. The present invention further relates to processes for preparing a solid form of modafinil by mixing and lyophilizing modafinil and excipients. BACKGROUND OF THE INVENTION [0003] Modafinil, C15H15NO2S of formula (I), is also known as 2-(benzhydrylsulfinyl)acetamide, or 2-[(diphenylmethyl)sulfinyl...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K31/165
CPCA61K9/0056A61K9/2081A61K31/165A61K9/5015A61K9/2095A61P1/00A61P11/00A61P25/00A61P25/16A61P25/20A61P25/24A61P25/28A61P3/04A61P9/00A61P9/10
Inventor NGUYEN, THANH-TAMLEYDER, JOELLE
Owner CEPHALON FRANCE
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