Budesonide pellets with a controlled released pattern and proces

Details Budesonide pellets with a controlled released pattern and proces Budesonide pellets with a controlled released pattern and proces

1996-07-15

1999-08-03

Levy, Neil S.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424490, 424485, 424462, 424473, A61K 914

Patent

active

059322497

DESCRIPTION:

BRIEF SUMMARY
The invention relates to budesonide pellets with controlled release profile and to a process for producing them. In particular, it relates to budesonide pellets with a release-controlling membrane comprising two separate lacquer layers.
Budesonide (16a, 17-butylidenedioxy-1b,21-dihydroxy-1,4-pregnadiene-3,20-dione) is a highly active corticosteroid which has been shown to be extremely effective for the treatment of inflammatory processes of the middle and lower intestinal tract. Thus, budesonide in oral slow-release form has brought about remission of active Crohn's disease and has few side effects on adrenocortical function (cf. the pilot study in "Der Kassenarzt, 13, pages 34 to 37, 1993"). A review of the pharmacological properties and the therapeutic efficacy of budesonide for asthma and rhinitis is given in "Drugs 44 (3), 375-407, 1992". The absorption of budesonide is low and it is subject to extensive first-pass metabolism. Since inflammatory processes often affect relatively large sections of the intestinal tract, there is a demand for a pharmaceutical form which spreads reproducibly over wide areas of the intestine and, moreover, releases the active substance only there.
An object of the invention is therefore to provide a pharmaceutical composition which ensures optimal distribution of the small amount of active substance (1 to 3 mg/dose) at the site of inflammation. Furthermore, the active substance is to be released neither in the stomach nor in the duodenum or the proximal jejunum but only from the middle jejunum onwards. From this section onwards there should be relatively rapid release (about 80 to 90% in 2 hours), differing distinctly from a slow-release form (for example 90% release in 6 to 8 hours).
Furthermore, a reproducible onset of action is to be ensured through rapid passage of the pharmaceutical composition through the stomach.
After a release-controlling shell has been detached, the sparingly soluble, very finely micronized active substance is to become rapidly resuspended in the intestinal fluid and display its effect on the inflamed mucosa. It is furthermore intended to provide a process for producing the pellets.
The invention is also in a process for producing budesonide pellets with a controlled release profile.
The various features of novelty which characterizes the invention are pointed out with particularity in the claims annexed to and forming a part of this specification. For a better understanding of the invention, its operating advantages and specific objects obtained by its use, reference should be had to the accompanying drawings and descriptive matter in which there is illustrated and described a preferred embodiment of the invention .


BRIEF DESCRIPTION OF THE DRAWINGS

The FIGURE schematically depicts a flow diagram for a process for producing the pellets of the invention.
This object is best achieved by pellets packed, for example, in hard gelatin capsules. After disintegration of the capsule in the stomach they are expelled into the intestine in accordance with the motility phase prevailing in the stomach at the time. This results in a distribution effect, and the active substance is able to display its effect on larger areas of the intestinal mucosa than a single-dose form.
It has been found, surprisingly, that budesonide pellets with controlled release profile can be obtained when the active substance is enveloped by a release-controlling membrane comprising two separate lacquer layers, one lacquer layer I consisting of 80 to 97% of lacquers which are insoluble in gastric fluid and soluble in intestinal fluid and 3 to 20% of lacquers which are insoluble in gastric and intestinal fluids, and a lacquer layer II consisting of 100% lacquers which are insoluble in gastric and intestinal fluids.
The invention thus relates to budesonide pellets with controlled release profile, which are characterized in that they comprise, from the inside to the outside, more water-soluble auxiliaries, in gastric fluid and soluble in intestinal fluid and 3 to 20% of lacquers which a

REFERENCES:
patent: 5188836 (1993-02-01), Muhammad et al.
patent: 5213808 (1993-05-01), Bar-Shalom et al.
patent: 5643602 (1997-07-01), Ulmius
patent: 5681584 (1997-10-01), Savastano et al.

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