Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2001-02-23
2002-10-01
Lankford, Jr., Leon B. (Department: 1651)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S725000, C424S730000, C424S733000, C424S736000, C424S746000, C424S757000, C424S768000
Reexamination Certificate
active
06458384
ABSTRACT:
SUMMARY OF THE INVENTION
The invention relates to a pharmaceutical in which a first pharmacologically active substance, or a pharmaceutically acceptable salt thereof, which acts on a specific biological function, is integrated such therein that it is released according to a predetermined first release profile (D.1), which generates a first activity profile (I.1) with at least one flank of increasing and at least one flank of decreasing activity intensity, especially a set forth below, processes for the manufacture thereof and to methods of treatment comprising administering such a pharmaceutical.
BACKGROUND OF THE INVENTION
Pharmaceuticals contain at least one pharmacologically active substance which, after administration of the pharmaceutical to a human or an animal, is to act via biological-chemical pathways in regard to at least one biological function of the human or animal, wherein the activity may be of a therapeutic or prophylactic nature or desired for other reasons. In many cases, the requirements placed on the pharmaceutical not only relate to a specific type of action but also a specific temporal course of the activity intensity, i.e., a specific activity profile.
The activity profile of an administered pharmacologically active substance is not directly measurable in many cases. However, based on medical experience and optionally with the aid of the temporal course of the corresponding blood level, the activity profile can be deduced for large groups of pharmacologically active substances and for different administration methods with sufficient reliability.
The type of action as well as the activity profile of a pharmaceutical, respectively, of a pharmacologically active substance contained in the pharmaceutical depend on pharmacodynamic parameters which determine the effect of the active substance on the organism (in particular, dosage and responsiveness) and on the pharmacokinetic parameters which determine the effect of the organism on the active substance (in particular, resorption, distribution, and storage in the organism as well as elimination by excretion or metabolism). It is attempted in many different ways to produce pharmaceuticals by which not only a pharmacologically active substance is administered to the organism but by which also additionally at least some of the above-mentioned parameters can be affected such that an activity profile that is as optimal as possible for the application is achieved with a dosage that is as minimal as possible.
For generating an activity profile as advantageous as possible, the pharmacologically active substance is administered according to a selected administration profile (administration dosage as a function of time), in a selected form (for example, lipid-soluble or water-soluble), and in a selected way (orally, intravenously, intramuscularly, etc.), the pharmaceutical is designed such that the substance according to a selected release profile (the amount of the active substance released in the organism as a function of time), and/or additional active substances are administered as “regulating substances” which regulating substances act on the organism in the sense of an advantageous control of the pharmacokinetics of the pharmacologically active substance.
Particularly for pharmaceuticals which are orally administered, a plurality of methods are known in order to generate for the pharmacologically active substances contained in the pharmaceutical freely selectable release profiles within wide limits. Such release profiles comprise, for example, a delayed release (for example, according to U.S. Pat. No. 5,788,987), a release as uniformly as possible over a time period as long as possible or a pulsatile release over an extended period of time (for example, according to U.S. Pat. No. 5,229,131). Moreover, administration forms are known in which two or more release types are combined to a release profile such that, for example, of a pharmacologically active substance a first portion is immediately released (burst) and the residual amount is distributed over a longer period of time (for example, according to U.S. Pat. Nos. 5,879,710, 5,738,874, or 5,407,686) or that, after a uniform release over a certain period of time, a release burst takes place (according to U.S. Pat. No. 5,213,808). It has also been proposed to administer the pharmacologically active substance in the form of a plurality of particles, wherein particles, which are designed for different release times, can be combined to a mixture with a substantially freely selectable release profile (for example, according to U.S. Pat. No. 5,840,329).
It is also known to employ administration forms in which different release types are combined with one another for the combined administration of more than one pharmacologically active substance wherein, for example, a first one of the substances is designed to provide a desired pharmacological activity and wherein a further one of the substances is administered for regulating the pharmacokinetics of the first substance. The administration of a substance (for example, benserazide or carbidopa), which is administered in combination with L-dopa against Parkinson's disease and which is released before L-dopa, as described, for example, in U.S. Pat. No. 5,738,874, is to be understood in this way. The regulating substance delays the metabolism of L-dopa to dopamine and ensures that a quantity as large as possible of the administered amount reaches in the form of unchanged L-dopa the blood-brain interface which it can pass only in this unchanged form. In a similar way, substances for inhibiting or ameliorating the undesirable side effects of a first active substance are released as, for example, the release of a substance, described in the same publication, for inhibiting irritation of the mucous membranes of the gastro-intestinal tract before the release of a pharmacologically active substance which irritates these mucous membranes as an undesirable side effect.
With the above addressed pharmaceuticals it is thus attempted, in particular, via the release profile and via the pharmacokinetics, to adapt the activity profile of a pharmacologically active substance to specific requirements, wherein, however, a plurality of parameters which determine such an activity profile, in particular, such parameters which are coupled with one another, may remain unaffected.
DE 43 25 465 describes a pharmaceutical allowing release of an opioid antagonist before an opioid agonist. The former shall overcome the paralytic effects of the opioid on peristaltic motion of the gut leading to constipation, while the therapeutic effect of the opioid agonist is not negatively affected. GB 791 644 describes the timely staggered use of glutarimide in a pharmaceutical in combination with barbiturates in order to overcome toxic effects of barbiturate overdosing. In both cases, the drugs to be released at different time points are combined such that the negative and undesirable effects of an active compound (paralysis of peristaltic motion, toxicity) are diminished while the desired activity remains intact.. On the other hand, U.S. Pat. No. 3,287,220 describes the increase in activity of a drug cocktail against asthma by a protease that is encapsulated in the core of a solid pharmaceutical also comprising the members of the drug cocktail. FR 25 84 604 describes the use of combinations of two pharmaceuticals, especially analgetics, A and B where one of these components is integrated such into a pharmaceutical that it is released fast, the other in a retarded way, so that the (analgetic) activity starts fast due to the fast release of the first component and lasts longer due to slower release of the second. Finally, FR 23 46 087 describes the combination of a soporific drug and a blood pressure stabilizing/circulation enhancing drug that is released some time after the soporific drug in order to maintain sleep in elder people by avoiding their awakening due to a critical lowering of blood pressure that occurs late in the night. In all these cases, the
Grünwald Jörg
Hänggi Benedikt
Jaenicke Christof
Burns Doane Swecker & Mathis L.L.P.
Davis Ruth A.
Impetus AG
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