New pharmaceutical forms for administration of medicaments by oral route, with programmed release
AssigneeElan Corporation, plc
InventorsDonald E. Panoz, Gilbert Corneille
Life of this patent
Estimating the term…
Abstract
The present invention relates to a new pharmaceutical form for oral use, in the nature of delayed action and controlled absorption medicaments. The form of the present invention comprises an association of miniaturized granules obtained by high to very high compression: (a) with Ph control agents, (b) coated with excipients determining the slow penetration of digestive liquids, and/or (c) coated with a very thin layer of lipids. These miniaturized granules may contain glucose, may have pH control agents with different solubilities, and may be in the form of miniaturized granules with a pH gradient.
Claims20
A pharmaceutical form of medicaments for oral administration with selectively adjustable programmed release and controlled absorption, comprising at least one of:
- (a) granulated highly compressed pulverized particles obtained by high to very high compression at a pressure equal to or greater than 10 tons and thereafter grinding to produce said particles having a diameter between 0.2 and 2 mm, of at least one active ingredient with an active excipient containing a physiologically active neutralization agent for controlling the pH;
- (b) granulated highly compressed pulverized particles obtained by high to very high compression at a pressure equal to or greater than 10 tons and thereafter grinding to produce said particles having a diameter between 0.2 and 2 mm, containing at least one active ingredient, coated with excipients determining the slow penetration of the digestive and alimentary liquids;
- and
- (c) granulated highly compressed pulverized particles containing at least one active ingredient obtained by high to very high compression at a pressure equal to or greater than 10 tons and thereafter grinding to produce said particles having a diameter between 0.2 and 2 mm, coated with a very thin layer of lipids present at a rate of 5 to 30% in relation to the active ingredient(s), the relative proportion of each of these types of particles (a), (b) and (c) varying from 0 to 100% according to the desired absorption curve of the medicament associated with said pharmaceutical form;
- wherein said active ingredients is selected from the group consisting of diazepam, cephalexin, cimetidin, cephalotin, methyldopa, cephazolin, propranolol, indomethacin, ibuprofen, doxycyclin, amoxycillin, furosemide, dipyridamole, spironolactone, erythromycin, gentamicin, diclofenac, glibenclamide, althiaside, naproxen, propoxyphene, allopurinol, sulfamethoxazole, ampicillin, prosultiame, lincomycin, betamethasone, troleandomycin, vincamine, clonidine, glafenine, clometacine, disopyramide, sulpiride, oxyphenbutazone, clorazepate, cephalosporin, rifamycin, sulindac and vincamine hydrochlorate.
A pharmaceutical form according to claim 16, wherein the excipient separating the layers which contain the medicament, for particles of type (a), or coating the particles of type (b), or mixed with the active ingredient(s) for the particles of type (c), is also composed of one or two substances chosen from the group consisting of polyvinylpyrrolidone, cellulose, ethylcellulose, methacrylates, acetophthalates and shellac.
In a pharmaceutical form of medicaments for oral administration with selectively adjustable programmed release and controlled absorption, the improvement comprising at least one of:
- (a) granulated highly compressed pulverized particles obtained by high to very high compression at a pressure equal to or greater than 10 tons and thereafter grinding to produce said particles having a diameter between 0.2 and 2 mm, of at least one active ingredient with an active excipient containing a physiologically active neutralization agent for controlling the pH;
- (b) granulated highly compressed pulverized particles obtained by high to very high compression at a pressure equal to or greater than 10 tons and thereafter grinding to produce said particles having a diameter between 0.2 and 1 mm, containing at least one active ingredient coated with excipients determining the slow penetration of the digestive and alimentary liquids;
- and
- (c) granulated highly compressed pulverized particles containing at least one active ingredient, obtained by high to very high compression at a pressure equal to or greater than 10 tons and thereafter grinding to produce said particles having a diameter between 0.2 and 2 mm, coated with a very thin layer of lipids present at a rate of 5 to 30% in relation to the active ingredient(s),
- the relative proportion of each of these types of particles (a), (b) and (c) varying from 0 to 100% according to the desired absorption curve of the medicament associated with said pharmaceutical form;
- wherein said active ingredient is selected from the group consisting of diazepam, cephalexin, cimetidin, cephalotin, methyldopa, cephazolin, propranolol, indomethacin, ibuprofen, doxycyclin, amoxycillin, furosemide, dipyridamole, spironolactone, erythromycin, gentamicin, diclofenac, glibenclamide, althiaside, naproxen, propoxyphene, allopurinol, sulfamethoxazole, ampicillin, prosultiame, lincomycin, betamethasone, troleandomycin, vincamine, clonidine, glafenine, clometacine, disopyramide, sulpiride, oxyphenbutazone, clorazepate, cephalosporin, rifamycin, sulindac and vincamine hydrochlorate.
Dependencies are inferred from the claim text.