Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1997-01-21
1998-11-10
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
5147721, A61K 4734
Patent
active
058340041
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD OF THE INVENTION
This application is a continuation under 35 U.S.C. 371 of PCT/EP95/00973, filed Mar. 15, 1995.
The invention relates to dimethylpolysiloxane (dimethicone) to be used as a transport and carrier system and/or a drug delivery system for pharmaceutical drugs for instance for the treatment of gastro-intestinal diseases. Moreover, the invention relates to pharmaceutical compositions containing dimethylpolysiloxane as a transport and carrier system and/or as a drug delivery system in combination with an active ingredient and methods related thereto.
Commercial dimethicone-containing preparations are used to treat symptoms such as flatulence, sensation of repletion (bloating) and meteorism. Moreover, the use of dimeticone for treating inflammatory and ulcerous diseases of the esophagus, the stomach and the duodenum has been described.
BACKGROUND OF THE INVENTION
In order to avoid dose-related side effects, the galenics of a pharmaceutical composition should be such that only the dose of the active ingredient necessary to elicit the desired therapeutic effect needs to be administered.
Hence, it is desirable to apply the therapeutically active ingredient right at the site where it is to produce its effect or at the site where it is absorbed so as to increase the local bioavailability and/or general bioavailability of the active ingredient (for instance by averting a first pass effect in the liver) or so as to avoid systemic side effects as much as possible.
In view of the different physiological properties of the different sections of the gastro-intestinal tract (GI tract), local therapy is particularly difficult in this case.
The continuous peristalsis, the variation of the chemical conditions over the length of the digestive tract, and the morphology of the surface of the GI tract are obstacles to a prolonged residence time in the different sections of the tract (such as the esophagus, stomach, duodenum, and colon).
Especially in the case of chronic diseases, such as inflammatory, infectious, ulcerous or neoplastic changes of the GI tract, direct local therapy capable of being continued over a prolonged period of time is desirable.
Furthermore, local treatment is also desirable in the case of disorders in the cardiovascular system, the lungs, the brain, and all hollow organs.
Local treatment requires a suitable transport and carrier system and/or drug delivery system.
SUMMARY OF THE INVENTION
The present invention provides a carrier that lends itself for use in particular galenic pharmaceutical forms for oral, rectal and intraoperative applications which release and/or fix the active ingredient continuously at the very site where it is to produce its effect or is absorbed.
It was surprisingly found that dimethicone, because of its unique physico-chemical properties is ideally suited for such purposes. Dimethicone has a very wide range of viscosities, depending on the degree of polymerization. The viscosity of dimethicone to be used in accordance with the invention may vary, depending on the therapeutical purpose, the nature and location of the condition to be treated as well as the drug to be administered. Preferably, dimethicone having a kinematic viscosity in the range of 10 to 100,000 mm.sup.2. S.sup.-1 is used.
The use of dimethicone having a kinematic viscosity in the range of 300 to 1,500 mm2.5 S.sup.-1 is particularly preferred. Dimethicone may also be supplemented with silicone dioxide as it is for example contained in the product Simeticone.
Dimethicone was found to show a particular association with or affinity to the surface structure of the GI tract. Because of an increased adhesion resulting from the adhesive properties of dimethicone, the residence time of an active ingredient in a region of the GI tract can be substantially prolonged if dimethicone is used as a transport or carrier system.
However, because of the different chemical, morphological and physiological conditions along the GI tract, the affinity and association of dimethicone with the epithelial ce
REFERENCES:
patent: 4837029 (1989-06-01), Olsen
patent: 4960764 (1990-10-01), Figueroa, Jr. et al.
patent: 5229137 (1993-07-01), Wolfe
patent: 5422093 (1995-06-01), Kennedy et al.
Bioforum May 1993, p. 189.
Rote Liste 1993, pp. 289 and 299.
Marshall, B.J.: Unidentified Curved Bacilli on Gastric Epithelium in Active Chronic Gastritis; Lancet I (1983), pp. 1273-1275.
Dixon, M.F.: Helicobacter Pylori and Peptic Ulceration: Histopathological Aspects (1991), pp. 125-130.
Schmidt Alfred
Upmeyer Hans-Jurgen
LandOfFree
Enteral composition comprising dimethicone and a photosensitizer does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Enteral composition comprising dimethicone and a photosensitizer, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Enteral composition comprising dimethicone and a photosensitizer will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1514195