Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1997-04-22
1999-03-02
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
A61F 1300
Patent
active
058767444
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to aqueous compositions containing mixtures of synthetic polymers and biopolymers, useful in the treatment of skin and mucosal tissues dryness, and suitable as vehicles of active ingredients.
PRIOR ART DISCLOSURE
Skin and mucosal tissues dryness and dehydration are very frequent conditions and may be caused by environmental factors, viruses, bacteria, or associated with etiologically different primary diseases. When affecting mucous membranes, said conditions are usually described as dryness of the buccal cavity (e.g. dry stomatopharyngitis in Sjogren's syndrome), of the vaginal, nasal and intestinal mucous membranes, and dryness of the eye (e.g. keratitis sicca).
Skin dryness and/or dehydration are not only important from an aesthetic point of view, but above all said conditions represent alterations of the cutis physiological function as a protective and defensive barrier. Furthermore, said dryness, which is per se a tissual damage causing lesions in the most serious cases, is also a hindrance to the absorption of possible products and/or drugs that can be administered in the treatment of the diseases affecting said tissues.
The methods most commonly used in the restoration of adequate moisture levels and in the prevention of further dehydration of the tissues consist in the application of creams, lotions or gels, which are capable of supplementing the water content of the tissues with highly hydrophilic agents or capable of forming a hydrophobic impermeable barrier on the tissue to be treated.
In the former case, it is well known in the state of the art the use of small synthetic hydrophilic molecules having humectant properties, such as glycerol, optionally mixed with water; it is also well known the use of macromolecules physiologically present in the tissues such as mucropolysaccharides, i.e. hyaluronic acid, dermatan sulfate and chondroitin sulfate, proteins such as collagen, elastin and placental proteins, having good properties as moisturizers and humectants.
As regards percutaneous absorption of active principles, it is to be stressed that the biological response to an active ingredient is often influenced by factors unrelated to the administered amount of the same principle. In particular, this is typical of topical administrations designed for local effect "in situ" as well as of oral administrations designed for absorption by general routes, which is often incomplete or in any case variable. In fact it is known that the bioavailability of active principles may be limited by the residence and contact times with the surface where absorption has to occur, e.g. the gastrointestinal tract in the case of oral preparations.
Therefore, several research works have lately been oriented to the development of bio- and/or mucoadhesive matrixes capable of binding themselves both to the stratum corneum of the cutis and to the film covering the mucous membranes, in particular the nasal one of the upper respiratory tract, the buccal, rectal, vaginal and ophthalmic ones.
The term "bioadhesion" has traditionally been used to describe the aggregation of biological and non-biological materials, rather than the interaction between materials having both biological origin. When the mucous membrane is covered by mucus, it is necessary to introduce the concept of mucoadhesion, which means that it is the same layer of mucus that comes into close contact with the adhesive substance through a typical "interface" phenomenon involving the interpenetration of the two phases.
Therefore, the "efficiency" of a bioadhesive matrix is influenced by specific physical and thermodynamic parameters, which determine the adhesion strength, and in particular by:
i) the "adhesive" molecular weight (e.g. the polyethylene glycol adhesiveness seems to increase with increasing the molecular weight, up to an optimal value of 4,000,000);
ii) the molecular mobility, which favors diffusion, and a sufficiently high viscosity;
iii) the ability to swell and form gels by osmosis with the substr
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Cerini Roberto
della Valle Francesco
Lorenzi Silvana
Marcolongo Gabriele
Howard Sharon
Lifegroup S.P.A.
Page Thurman K.
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