Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1984-05-03
1987-04-07
Rose, Shep K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
A61K 924, A61K 928
Patent
active
046560246
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a new galenical preparation of METOCLOPRAMIDE, and the medicament comprising this preparation.
METOLCOPRAMIDE has been known for a number of years. In the dichlorhydrate or monochlorhydrate form it is widely used for treating gastro-intestinal functional troubles such as dyspepsies, gastro-duodenal and biliary dyskinesies, chronic gastritis, gastro-duodenal ulcers and nauseas and vomiting. From the pharmacological point of view, the action of METOCLOPRAMIDE is both central and peripheral.
However, the administration of METOCLOPRAMIDE in its present form presents considerable disadvantages by limiting convenience of use.
For example, it has been noted that the presentation in tablet form causes certain, more particularly gastric, intolerances, which prevents its use by a large category of patients, and which also limits its use for long term treatments.
Furthermore, after each administration, i.e. three of four per day if not more, a succession of rapid increases and decreases of the plasmatic rates has been noted, since the organism is subjected alternately to overdoses and underdoses.
Finally, the disadvantages of the conventional forms have not allowed up to now digestive troubles to be treated requiring extended administration, which on the contrary is possible with the new galenic form of administration of METOCLOPRAMIDE as will be demonstrated hereafter, this new form allowing steady release of the preparation in the organism for sufficiently long periods to allow simply a single unit to be taken daily.
BRIEF DESCRIPTION OF THE DRAWINGS
FIGS. 1, 2 and 3 are graphs illustrating the plasmatic concentration of metoclorpramide after oral doses according to the present invention and comparing these graphs with similar graphs showing plasmatic concentration of metoclopramide after conventional dosing.
The present invention has then as object a new galenic form with delayed programmed release of METOCLOPRAMIDE and is characterized in that it is formed by microgranules comprising a neutral core formed by a grain of an inert excipient comprising at least two components of the type belonging to the class formed by saccharose, starch, talc, desiccating silica, lactose and stearic acid, this neutral grain being provided with a first layer comprising METOCLOPRAMIDE, then a second outer layer formed by a microprous envelope comprising at least one natural and/or synthetic polymer belonging to the class formed by shellac, gum arabic, ethyl cellulose, cellulose acetophtalate, cellulose triacetate, polyoxyethyleneglycol, the methacrylates, styrene-acrylonitrile copolymer and polyvinylpyrrolidone in successive envelopes.
In particular, the microporous envelope may be formed from shellac in a proportion by weight varying between 1 and 10% and the inert excipient may be a mixture comprising 40 to 80% by weight of saccharose and 10 to 40% by weight of starch.
According to an advantageous embodiment of the invention, the first layer may comprise from 1 to 20% by weight of METOCLOPRAMIDE, from 0.01% to 0.5% by weight of stearic acid, from 5 to 15% by weight of talc and from 2 to 10% by weight of desiccating silica. Furthermore, the neutral core may comprise METOCLOPRAMIDE adsorbates.
The invention also has as object a process for obtaining the new galenic form remarkable in that neutral sifted and dried microgranules are prepared beforehand, in that a solution in absolute alcohol of METOCLOPRAMIDE is sprayed on these microgranules, in that said microgranules are then coated to form the first layer in one or more coatings, then the microporous envelope is formed by coating with said polymer in solution in a solvent.
Furthermore, the present invention has as object medicaments comprising the new form of administration of METOCLOPRAMIDE in the form of active micrographics mixed with non coated neutral microgranules so as to obtain a predetermined METOCLOPRAMIDE concentration, this assembly of microgranules being presented in the form of capsules, tablets, suppositories, syrup, granules or po
REFERENCES:
patent: 2963402 (1960-12-01), Nalin et al.
patent: 4264574 (1981-04-01), Cherqui et al.
Chem. Abs, vol. 83, No. 14, 10-6-75, p. 427, No. 12077m R. Shekerdzhiiski et al. "Antiemetic Preparation . . . .
Faraci C. Joseph
Rose Shep K.
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