Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Reexamination Certificate
1999-06-07
2002-01-22
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
C424S490000, C424S451000, C424S464000, C424S195110
Reexamination Certificate
active
06340478
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to formulations for the controlled or extended release of certain bioactive compounds, and to processes for the preparation of the same.
BACKGROUND OF THE INVENTION
Powdered and granulated herbal (botanical) extracts and dried, ground dry plants are good and well accepted sources of certain bioactive compounds.
Thus, for example, garlic is a good source for Allicin and &ggr;glutamyl peptides; St. John's Wort is a source for Hypericin and Hyperforine, and Echinacea is a source for certain Echinosides.
It has been established that many botanical and herbal extracts and plants can serve as an important nutritional supplement and therapeutic materials. However, it has been found that many of these materials are unstable and when stored for long periods, the active ingredients are often eliminated or otherwise rendered inactive.
SUMMARY OF THE INVENTION
The present invention seeks to provide improved herbal preparations which preparations offer a convenient oral dosage form of herbs for supplying optimum plasma concentrations of the biologically active compounds contained in the herbs (such as Ginsenoside R&ggr;1 and Ginsenoside R&bgr;1 from extracts of Panax Ginseng) and which facilitates user compliance with recommended procedures.
There is thus provided in accordance with a preferred embodiment of the invention an orally-administrable formulation for the controlled release of a ground herb, said formulation comprising ground herb and at least one carrier, adjuvant or excipient therefor.
There is also provided in accordance with a preferred embodiment of the invention an orally-administrable formulation for the stable storage of a ground herb, said formulation comprising a ground herb and at least one carrier, adjuvant or excipient therefor.
In the context of the present description and claims, the term “granulated herb” will be understood to refer to both powdered and granulated forms of both herbal extracts and herbal plants or portions of herbal plants, which extracts, plants or portions thereof have been ground to a particle size within the range of about 100 to about 2000 &mgr;m diameter, preferably in the range of about 300 to about 1000 &mgr;m diameter.
In one preferred embodiment of the invention, the orally-administrable formulation for the controlled release of granulated herb comprises granulated herb and at least one carrier, adjuvant or excipient therefor, and is characterized in that the total in vitro dissolution time of the formulation required for release of 75% of the active ingredient available from the formulation, is between about 4 and about 18 hours, as determined by the U.S.P. XXIII paddle method at a paddle speed of 150 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.8, and a temperature of 37° C.
In one preferred embodiment of the invention, the formulation is characterized in that it contains from 1 to 95 wt. % granulated herb.
In another preferred embodiment of the invention, the formulation is in a form selected from the group consisting of: a matrix tablet, a multicomponent formulation, a microcapsule of generally spherical shape, a microcapsule of generally non-spherical shape, a capsule containing microcapsules, and a tablet containing microcapsules.
In another preferred embodiment of the invention, the formulation comprises granulated herbs mixed or coated with an adjuvant or mixture of adjuvants selected from the group consisting of synthetic polyvinyl-type polymers, synthetic polyethylene-type polymers, cellulose-type polymers, synthetic polyacrylate-type polymers, fats, waxes, sugars and sugar alcohols.
In one preferred embodiment of the invention, the formulation is in the form of a tablet comprising granulated herbs embedded in a mixture of polyvinyl chloride an polyvinyl acetate, and magnesium stearate as a lubricant.
In another preferred embodiment of the invention, the formulation is in the form of a tablet comprising granulated herb embedded in a mixture of polyvinyl chloride and ethylcellulose, magnesium stearate as lubricant, and a material selected from hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose and paraffin.
In a preferred embodiment of the invention, the formulation is in the form of a hard gelatin two-piece capsule filled with microcapsules containing granulated herb.
In another preferred embodiment of the invention, the formulation is in the form of a tablet comprising microcapsules.
The invention also comprises a process for the preparation of an orally-administrable formulation for the controlled release of a granulated herb, said formulation comprising granulated herb and at least one carrier, adjuvant or excipient therefor, said process comprising the steps of;
providing a granulated herb; and
incorporating said granulated herb into said at least one carrier, adjuvant or excipient therefor;
wherein said formulation is characterized in that the total in vitro dissolution time of said formulation required for release of 75% of the active ingredients from said formulation is between about 4 and about 18 hours, as determined by to the U.S.P. XXIII paddle method, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.8, and temperature of 37° C.
In one preferred embodiment of the invention, the process is characterized in that the granulated herb is (i) mixed or coated with an adjuvant or mixture of adjuvants selected from the group consisting of synthetic polyvinyl-type polymers, synthetic polyethylene-type polymers, cellulose-type polymers, synthetic polyacrylate-type polymers, fats, waxes, sugars and sugar alcohols, and (ii) then compressed into tablets.
In another preferred embodiment of the invention, the process is characterized in that the granulated herb is (i) mixed or coated with an adjuvant or mixture of adjuvants selected from the group consisting of synthetic polyvinyl-type polymers, synthetic polyethylene-type polymers, cellulose-type polymers, synthetic polyacrylate-type polymers, fats, waxes and sugars , (ii) then processed into a form selected from the group of microcapsules and pellets, and (iii) the microcapsules or pellets are filled into hard gelatin capsules.
In a preferred embodiment of the invention, the process is characterized in that the granulated herb is (i) mixed or coated with an adjuvant or mixture of adjuvants selected from the group consisting of synthetic polyvinyl-type polymers, synthetic polyethylene-type polymers, cellulose-type polymers, synthetic polyacrylate-type polymers, fats, waxes and sugars, (ii) then processed into a form selected from the group of microcapsules and pellets, and (iii) said microcapsules or pellets are compressed into tablets.
There is also provided in accordance with a preferred embodiment of the invention an orally-administrable formulation for the controlled release of a granulated herb, comprising particles of granulated herb coated with a film comprising a mixture of at least one water soluble polymer and at least one water insoluble polymer, the at least one water soluble polymer and the at least one water insoluble polymer being present in a ratio that produces a substantially zero order linear release pattern of at least one active ingredient. In one preferred embodiment of the invention, the particles comprise particles which are non-spherically shaped. In another preferred embodiment of the invention, the particles comprise particles which are spherically shaped.
There is also provided in accordance with a preferred embodiment of the invention an orally-administrable formulation for the controlled release of a granulated herb, comprising particles of granulated herb coated with an enteric coating comprising a polymer film comprising a polymer which is insoluble at a pH below about 5.5. In a preferred embodiment of the invention, the particles comprise particles which are
Blatt Yoav
Cohen David
Kimmelman Eugene
Rotman Avner
Abelman ,Frayne & Schwab
Bio Dar Ltd.
Page Thurman K.
Pulliam Amy E
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