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Stable extended release oral dosage composition

A composition and sustained-release technology, applied in the directions of drug combination, drug delivery, active ingredients of heterocyclic compounds, etc., can solve problems such as unpublished

Inactive Publication Date: 2007-12-05
MERCK & CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The prior art does not disclose the once-daily administration of the film-coated solid oral administration composition of the present invention

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0290] This example illustrates the preparation of a preferred orally administered composition of the invention. Its ingredients and specific amounts are listed below.

[0291] 1. Matrix core

[0292] A preparation method:

[0293] 1. Dissolve povidone in a mixture of 3 parts ethanol and 1 part purified water.

[0294] 2. Bring together pseudoephedrine sulfate, hydroxypropylmethylcellulose 2208, ethylcellulose and calcium hydrogen phosphate dihydrate in a suitable mixing bowl and blend under nitrogen atmosphere

[0295] 3. Granulate the blend from step 2 with the solution from step 1, pass the wet granules through a suitable milling equipment to crush larger granules

[0296] 4. Dry the wet agglomerate in a suitable fluidized bed treatment unit at about 70°C, with drying losses between 0.5% and 2.0% as measured by humidity balance or equivalent.

[0297] 5. Pass the dried granules through suitable grinding equipment.

[0298] 6. Add the required amount of silicon dioxide ...

Embodiment 2

[0326] The following more preferred compositions of the present invention were prepared according to the procedure of Example 1 above.

[0327] 1. Matrix core

[0328] Element mg / core

[0329] Pseudoephedrine Sulfate USP 240

[0330] Hydroxypropyl Methyl Cellulose 2208 USP 100000cps 320

[0331] Ethylcellulose NFType7 80

[0332] Dicalcium Phosphate Dihydrate USP 108

[0333] Povidone USP 40

[0334] Silica NF 8

[0335] Magnesium Stearate NF 4

[0336] Matrix Core Approximate Weight 800 mg

[0337] 2. Matrix core coating

[0338] 1. First film coating

[0339] Element mg / tablet

[0340]Simethicone 0.22

[0341] Polyethylene glycol 8000 0.27

[0342] Talc powder NF 2.72

[0343] Ethyl acrylate / methyl methacrylate neutral copolymer (30% aqueous dispersion) 2.72

[0344] The weight of the first coating 5.93 mg

[0345] 2. Second film (quick release) coating mg / tablet

[0346] Loratadine 5.0

[0347] Simethicone 0.28

[0348] Polyethylene glycol ...

Embodiment 3

[0364] The following more preferred compositions of the present invention were prepared according to the procedure of Example 1 above.

[0365] 1. Matrix core

[0366] Element mg / core

[0367] Pseudoephedrine Sulfate USP 240

[0368] Hydroxypropyl Methyl Cellulose 2208 USP 100000cps 320

[0369] Ethylcellulose NF Type 7 80

[0370] Dicalcium Phosphate Dihydrate USP 108

[0371] Povidone USP 40

[0372] Silica NF 8

[0373] Magnesium Stearate NF 4

[0374] Matrix Core Approximate Weight 800 mg

[0375] 2. Matrix core coating

[0376] 1. First film coating

[0377] Element mg / tablet

[0378] Simethicone 0.22

[0379] Polyethylene glycol 80000 0.27

[0380] Talc powder NF 2.72

[0381] Ethyl Acrylate / Methyl Methacrylate Neutral Copolymer (30% Aqueous Dispersion) 2.72

[0382] The weight of the first coating 5.93 mg

[0383] 2. Second film (quick release) coating mg / ml

[0384] Desloratadine 6.0

[0385] Simethicone 0.28

[0386] Polyethylene gly...

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PUM

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Abstract

A film-coated extended release solid oral dosage composition containing a nasal decongestant, pseudoephedrine or salt thereof, e.g., pseudoephedrine sulfate in a core effective to provide a geometric maximum plasma concentration of pseudoephedrine of about 345 ng / mL to about 365 ng / mL at a time of about 7.60 hrs to about 8.40 hrs and having two or three film-coatings on the core, the second one containing an amount of the non-sedating antihistamine, desloratadine, effective to provide a geometric maximum plasma concentration of desloratadine of about 2.10 ng / mL to about 2.45 ng / mL at a time of about 4.0 hours to about 4.5 hours, and use of the composition for treating patients showing the signs and symptoms associated with allergic and / or inflammatory conditions of the skin and airway passages are disclosed.

Description

[0001] This application is a divisional application of an invention patent application whose application date is December 20, 2000, and whose application number is 200510071301.4 and whose invention title is the same as this application. technical field [0002] The present invention relates to a film-coated sustained release solid oral administration composition comprising a nasal decongestant such as pseudoephedrine in a controlled release core and a non-sedating antihistamine desloratadine in an outer film coat (desloratadine). The solid oral administration composition of the present invention is used for the treatment of patients exhibiting signs and symptoms associated with allergic and / or inflammatory conditions such as the common cold, as well as allergic and / or inflammatory conditions associated with the skin or the upper and lower airways. Patients with signs and symptoms associated with conditions such as allergic rhinitis, seasonal allergic rhinitis and nasal conges...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4545A61K31/137A61K9/20A61P11/02A61K9/28A61K9/22A61K9/24A61K9/32A61K31/445A61K31/473A61K45/00A61K47/02A61K47/04A61K47/12A61K47/30A61K47/32A61K47/34A61K47/38A61P11/06A61P17/00A61P17/04
CPCA61K31/445A61K9/209A61P11/00A61P11/02A61P11/06A61P17/00A61P17/04A61P27/14A61P29/00A61P37/08A61P39/00A61P43/00A61K31/135A61K2300/00A61K9/20
Inventor J·H·顾
Owner MERCK & CO INC
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