Preparation of a slow-release drug

Details Preparation of a slow-release drug Preparation of a slow-release drug

1987-07-09

1989-02-28

Lusignan, Michael

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424494, A61K 916

Patent

active

048084166

DESCRIPTION:

BRIEF SUMMARY
This invention concerns a slow-release preparation of a drug, characterized by the coating of a core comprising an active principle, such as Metoclopramide, first with a substance which retards its release, such as a copolymer of methyl methacrylate and ethyl acrylate (known as EUDRAGIT E30D), cellulose ethyl, etc., and then with an enteric coating such as cellulose hydroxypropylmethyl phthalate (known as HP-55), carboxymethylcellulose, etc.
The diagram of FIG. 1 indicates the structure of the preparation.
The active principle can be used in granule form, as well as deposited around a neutral core, such as a sucrose granule. Coating is then undertaken with one of the substances listed above, capable of retarding the release of the active principle under acid or basic dissolution conditions, so as to assure a constant dissolution of the active principle in the gastrointestinal tract.
The copolymer sold under the name of EUDRAGIT E30D (Rohm Pharma Co.) is the one most suitable for application of the invention.
Finally, external coating of the preparation is undertaken by means of an enteric substace, preferably the cellulose byproduct sold under the name of HP-55 (SHIN-ETSU CHEMICAL CO.).
A working example of the invention is given in order to illustrate the preparation.
Four hundred parts of 32-42 mesh size sucrose granules are coated in a centrifugal granulator with a solution of SHELLAC resin (44 parts) in ethanol (290 parts) containing talc (60 parts). Then the granules are coated with Metoclopramide in a 5 percent aqueous solution of TC-5R brand hydroxypropyl methyl cellulose ether.
The resulting granules (comprising 30 percent by weight of Metoclopramide) are then coated with Eudragit-E30D in a fluidized bed granulator and a solution of HP-55, cellulose hydroxy propylmethyl phthalate, (15 g) in a 50/50 mixture of ethanol and dichloroethane (400 g) is sprayed thereon in order to obtain the Metoclopramide slow-release preparation.


DISSOLUTION TEST



______________________________________ Method A TIME (HOURS) 0.5 1 2 3 4 6 7 8 ______________________________________ Rate of dissolution (%) -- 15 30 40 50 60 65 70 of sample (I) Rate of dissolution (%) 65 80 85 90 92 95 97 98 of sample (II) ______________________________________


______________________________________ Method B TIME (HOURS) 1 2 3 4 6 8 ______________________________________ Rate of dissolution (%) 32 55 63 72 82 86 of sample (I) Rate of dissolution (%) 30 53 64 70 80 85 of sample (II) ______________________________________
1. Slow-release preparation comprising, in sequence, a core of a granule having deposited thereon metoclopramide; a first shell of a copolymer of ethyl acrylate and methyl methacrylate in an effective amount of ensure uniform dissolution of said metoclopramide upon oral ingestion; and a second shell of an enteric coating of cellulose hydroxypropylmethylphthalate.

DESCRIPTION
The active principle can be used in granule form, as well as deposited around a neutral core, such as a sucrose granule. Coating is then undertaken with one of the substances listed above, capable of retarding the release of the active principle under acid or basic dissolution conditions, so as to assure a constant dissolution of the active principle in the gastrointestinal tract.
The copolymer sold under the name of EUDRAGIT E30D (Rohm Pharma Co.) is the one most suitable for application of the invention.
Finally, external coating of the preparation is undertaken by means of an enteric substace, preferably the cellulose byproduct sold under the name of HP-55 (SHIN-ETSU CHEMICAL CO.).
A working example of the invention is given in order to illustrate the preparation.
Four hundred parts of 32-42 mesh size sucrose granules are coated in a centrifugal granulator with a solution of SHELLAC resin (44 parts) in ethanol (290 parts) containing talc (60 parts). Then the granules are coated with Metoclopramide in a 5 percent aqueous solution of TC-5R brand hydroxypropyl methyl cellulose ether

REFERENCES:
patent: 4656024 (1987-04-01), Leruelle

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