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Multimicroparticulate pharmaceutical forms for oral administration

A pharmaceutical dosage form, microparticle technology, applied in the preparation of the above pharmaceutical dosage forms, dosage forms for oral administration, drug dosage forms with improved release, pharmaceutical dosage forms where alcohol intake is not recommended, can solve damage, dose dumping, unsatisfactory the solution of other issues

Active Publication Date: 2009-03-04
FLAMEL IRELAND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0031] For monolayer matrix dosage forms, accidental dose dumping can lead to very high concentrations of PA in the digestive system where the dosage form is located, which can cause damage
[0032] The issue of dose dumping in the presence of alcohol has not been satisfactorily addressed, especially for multiparticulate dosage forms

Method used

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  • Multimicroparticulate pharmaceutical forms for oral administration
  • Multimicroparticulate pharmaceutical forms for oral administration
  • Multimicroparticulate pharmaceutical forms for oral administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0283] Example 1: Acyclovir Capsules-Reagent D is contained in the inert carrier of microparticles

[0284] step 1 :

[0285] 288g acyclovir and 72g hydroxypropyl cellulose (Kluce1 / Aqualon) dispersed in 840g of water. The suspension was sprayed onto 240 g of guar gum (Danisco) in a fluidized bed (Glatt GPCG1).

[0286] step 2 :

[0287] Mix 1.4 g ethylcellulose (Ethocel 20 Premium / Dow), 9.24 g cellulose acetate butyrate (CAB 171-15 / Eastman), 1.68 g polysorbate 80 (Tween 80 / Uniqema) and 1.68 g tris-citrate Ethyl ester (Morflex) was dissolved in a mixed solution consisting of 94% acetone and 6% water. This solution was sprayed onto 56 g of acyclovir granules (prepared in step 1).

[0288] The prepared microparticles were then filled into size 0 gelatin capsules (the dose of aciclovir was 150 mg per capsule).

[0289] Under the paddle stirring speed of 75rpm, in the mixture (40 / 60v / v) of the 0.1N HCl of 900ml and the ethanol / 0.1N HCl of 500ml, the curve of the dissolu...

Embodiment 2

[0291] Example 2: Metformin Capsules-Reagent D is contained in the capsule coating film

[0292] step 1 :

[0293] 500 g of metformin were dispersed in 2586 g of water. This solution was sprayed onto 450 g of cellulose pellets (Asahi-Kasei) in a Glatt GPCG1.

[0294] step 2 :

[0295] 288g ethylcellulose (Ethocel 20 Premium / Dow), 30g povidone (Plasdone K29-32 / International Specialty Products Inc.), 12g polyoxyl-40 hydrogenated castor oil (polyoxyethylene glyceryl trihydroxystearate: CremophorRH 40 / ISP) and 30 g of castor oil were dissolved in a mixture of 60% acetone and 40% isopropanol. This solution was sprayed onto 700 g of the metformin granules prepared in step 1.

[0296] The prepared microparticles were then filled into No. 2 gelatin capsules (metformin dosage was 150 mg per capsule). The capsules were then film-coated with a sodium carboxymethylcellulose solution (Blanose 7LF / Aqualon) at a coating rate of 20 mg sodium carboxymethylcellulose per 60 mg gelatin. ...

Embodiment 3

[0299] Example 3: Acyclovir Capsules - Agent D contained in the inert carrier and capsule components of microparticles

[0300] step 1 :

[0301] 288g acyclovir and 72g hydroxypropyl cellulose (Klucel / Aqualon) dispersed in 840g of water. The suspension was sprayed onto 240 g of guar gum (Danisco) in a Glatt GPCG1.

[0302] step 2 :

[0303] Dissolve 9.84 g ethylcellulose (Ethocel 20 Premium / Dow), 0.24 g povidone (Plasdone K29-32 / ISP), 0.24 g Span 80 (Span 80 / Uniqema) and 1.68 g castor oil (Garbit Huilerie) in a mixture of 60% acetone and 40% isopropanol. This solution was sprayed onto 48 g of acyclovir granules (prepared in step 1).

[0304] The prepared microparticles were then loaded into size 0 vegetable capsules (based on hypromellose [or HPMC]) (acyclovir dose was 150 mg per capsule).

[0305] At a paddle stirring rate of 75rpm, the dissolution profile in 900ml 0.1N HCl and 500ml ethanol / 0.1N HCl mixture (40 / 60v / v) is as follows Figure 8 Shown:

[0306]It c...

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Abstract

The invention aims at minimizing the risks of release of the dose associated with the concurrent consumption of alcohol and certain pharmaceutical or dietary forms with modified release. The invention concerns an oral form comprising reservoir-type microparticles, with modified release of at least one active principle. The invention is characterized in that it is resistant to the immediate release of the dose of active principle in the presence of alcohol. In particular, the inventive oral form is characterized in that the releasing time of 50% of the active principle, in an alcohol-containing solution is not reduced by more than 3 times compared to the releasing time of 50% of the active principle in an alcohol-free aqueous medium. The form comprises an agent D which is a pharmaceutically acceptable compound of which the hydrating or solvating speed and capacity is higher in an alcohol-free aqueous medium than in an alcohol-containing solution.

Description

technical field [0001] The present invention relates to improved release pharmaceutical or nutraceutical dosage forms for oral administration of pharmaceutically active ingredients (PA). [0002] The present invention relates to a dosage form for oral administration comprising at least one PA and capable of maintaining an improved release of PA in alcoholic solution, ie the dosage form does not undergo dose dumping in the presence of alcohol. Preferably, the present invention relates to improved release pharmaceutical dosage forms, the release profile of which is not significantly affected in alcoholic solutions. [0003] The present invention relates more particularly to dosage forms of the type mentioned in the preceding paragraph, comprising a plurality of reservoir particles. [0004] The invention relates more particularly to pharmaceutical dosage forms for which the intake of alcohol is not recommended during administration. [0005] The present invention also relates ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/50A61K9/16A61K9/52A61K9/32A61K9/26
CPCA61K9/5078A61K9/4891A61K9/1652A61K9/2866A61K9/5047A61K9/1676A61K9/0095A61K9/5084A61K9/2077A61K9/5073A61K9/4816A61K9/48A61K9/20A61K9/16
Inventor 弗洛朗斯·纪穆伯蒂奥弗雷德里克·达尔勒拉斯
Owner FLAMEL IRELAND