Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Reexamination Certificate
2001-03-19
2003-11-25
Rose, Shep K. (Department: 1614)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
C424S048000, C424S435000, C424S682000, C424S602000, C426S003000, C426S074000, C426S648000, C426S660000
Reexamination Certificate
active
06652875
ABSTRACT:
TECHNICAL FIELD
The invention relates to formulations designed to deliver bioactive constituents to biological surfaces, in particular, but not limited to, dental surfaces.
BACKGROUND ART
The casein formulations of the prior art have not described an isolated and purified casein protein, together with at least one bioactive constituent, wherein the formulation provides a delivery system for the bioactive constituent, whilst at the same time maintaining the activity of the casein protein and associated bioactive constituent. Further, the formulations of the prior art suffer from a number of significant disadvantages. For example, the prior art formulations have a limited shelf life at room temperature, before the occurrence of odorous bacterial breakdown or the appearance of a precipitate of protein resulting from the addition of incompatible components.
The present invention provides a formulation for the delivery of bioactive constituents to biological surfaces, wherein said formulation comprises at least one isolated and purified casein protein or salt thereof, together with at least one bioactive constituent. Further, such a formulation displays an extended shelf life, whilst maintaining the activity of the casein protein and associated bioactive constituent, and a formulation which with added dispersing agents provides an increased dissolution rate for pre-dried formulations in aqueous solutions.
OBJECT OF THE INVENTION
An object of the invention is to provide a casein protein based formulation which acts as a delivery system for bioactive substances.
DISCLOSURE OF THE INVENTION
According to a first embodiment of the invention, there is provided a formulation for the delivery of bioactive constituents to biological surfaces, wherein said formulation comprises a suspension or solution of at least one isolated and purified casein protein or salt thereof, in water, together with at least one bioactive constituent.
Typically, the formulation delivers the bioactive constituents to biological surfaces in mammals. More typically, the biological surfaces include dental surfaces, such as teeth and gums. Even more typically, the biological surfaces include all tissues of the oral cavity, but can also include skin, and the alimentary tract, including the linings of the stomach and intestinal walls.
Typically, the biological activity of the casein protein within the formulation is maintained regardless of the bioactive constituent associated therewith.
Typically, the casein protein present in the formulation may be present as a mixture of any two or more of the casein proteins outlined below.
Typically, the isolated and purified casein protein may comprise a casein protein as disclosed in Whitney, R. Proteins of Milk. In: Fundamentals of diary chemistry 3rd Edn. (1988) (ed. N. P. Wong), Van Nostrand Reinhold, N.Y. USA, pages; 82-91, the disclosure of which is incorporated herein by reference. More typically, the casein protein is selected from the group consisting of: &agr;-casein, &bgr;-casein, &kgr;-casein, and mixtures thereof. Yet even more typically, the casein protein is selected from the group consisting of:
A. &agr;
S1
-Caseins
1. &agr;
S1
-Casein X
n
—8P (genetic variants—A, B, C, D-9P, and E)
2. &agr;
S1
-Casein X
a
—9P (genetic variants—A, B, C, D-10P, and E)
3. &agr;
S1
-Casein fragments
B. &agr;
S1
-Caseins
1. &agr;
S1
-Casein X
a
—10P (genetic variants—A, B, C-9P, and D-7P)
2. &agr;
S1
-casein X
a
—11P (genetic variants—A, B, C,-10, and D-8P)
3. &agr;
S1
-Casein X
a
—12P (genetic variants—A, B, C-11P, and D-9P)
4. &agr;
S1
-Casein X
a
—13P (genetic variants—A, B, C-12P, and D-10P)
C. &bgr;-Caseins
1. &bgr;-Casein X
a
—5P (genetic variants—A
1
, A
2
, A
3
B, C-4P, D-4P, and E)
2. &bgr;-Casein X
a
—1P (f29-209) (genetic variants—A
1
, A
2
, A
3
, and B)
3. &bgr;-Casein X
a
—(f106-209) (genetic variants—A
2
, A
3
, and B)
4. &bgr;-Casein X
a
—(f108-209) (genetic variants—A and B)
5. &bgr;-Casein X
a
—4P (f1-28)
b
6. &bgr;-Casein X
a
—5P (f1-105)
b
7. &bgr;-Casein X
a
—5P (f1~107)
b
8. &bgr;-Casein X
a
—1P (f29~105)
b
9. &bgr;-Casein X
a
—1P (f29~107)
b
D. &kgr;-Caseins
1. &kgr;-Casein X
a
—1P (genetic variants—A and B)
2. Minor &kgr;-caseins X
a
—1, —2, —3, etc. (genetic variants—A and B)
Generally, the casein protein is a phosphoprotein, and may be present in the form of a salt. Typically, the salts are selected from the group consisting of: alkaline metals or alkaline earth metals. More typically, the alkaline earth metals are selected from the group consisting of: sodium, calcium, zinc, copper, aluminium, potassium, strontium, magnesium and nickel salts.
Typically, the casein phosphoprotein is in the form of a divalent or trivalent metal ion complex or aggregate. More typically, the casein phosphoprotein is in the form of caseinate calcium phosphate or caseinate calcium fluorophosphate. Even more typically, the casein phosphoprotein is in the form of casein calcium phosphate complex or caseinate calcium fluorophosphate complex.
Typically, the formulation of the present invention also includes a phosphatase inhibitor. More typically, the phosphatase inhibitor is selected from the group consisting of: fluoride ions, vinyl ether maleic acid polymers, and divalent and trivalent metal ions.
Typically, the casein protein may be isolated and purified from bovine, ovine or caprine milk. More typically, the casein protein for use in the invention is any commercially available casein protein.
Note that unless otherwise stated, all percentages of components of the formulation are by weight, based on the total weight of the formulation.
Typically, the amount of casein protein, typically, present as casein phosphoprotein, in the formulation is between about 0.05 and about 50%. More typically, the amount of casein phosphoprotein present in the formulation is between about 0.5 and about 25%. Even more typically, the amount of casein phosphoprotein present in the formulation is between about 1 and about 20%. Still more typically, the amount of casein phosphoprotein present in the formulation is between about 1 and about 15%. Yet still more typically, the amount of casein phosphoprotein present in the formulation is between about 1 and about 10%.
Typically, the isolated and purified casein protein, and at least one bioactive constituent are present in association within the formulation in accordance with the present invention. More typically, the association between the isolated and purified casein protein and the bioactive constituent is by virtue of the presence of both negative and positive groups associated along the length of the casein polypeptide chain, wherein these groups can ionically interact with a range of bioactive constituents to form a complex with the isolated and purified casein protein to be soluble in water. Even more typically, wherein the bioactive constituents include constituents insoluble in water, the constituents may be stabilised in an emulsion or suspension within the casein protein formulation of the present invention. Thus, the formulation of the present invention comprising a suspension or solution of at least one isolated and purified casein protein, together with at least one bioactive constituent, provides a delivery system for a range of bioactive constituents.
In particular, casein protein, typically, casein phosphoprotein has an affinity for biological surfaces, and as a consequence, when the formulation in accordance with the present invention is applied to a biological surface, by virtue of this affinity of the casein protein resident in the formulation, the concentration of the associated bioactive constituent at the biological surface is increased, thereby providing a delivery system wherein the bioactive constituent is presented to the biological surface.
Typically, inorganic bioactive constituents are selected from the group consisting of: calcium, phosphate, fluorophosphate, fluoride, zirconia, magnesium, barium, zinc, iron, copper, aluminium, tin, silver, and salts of said bioactive constituents, selected from the group consisting of: t
McDonnell & Boehnen Hulbert & Berghoff
Pacific Biolink Pty. Limited
Rose Shep K.
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