Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Reexamination Certificate
1998-10-07
2001-08-07
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
C424S476000, C424S468000, C424S494000
Reexamination Certificate
active
06270803
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 garlic are good sources of allicin, &ggr;-glutamyl peptides and certain other bioactive compounds. Allicin and &ggr;-glutamyl peptides have broad and significant biological and therapeutic activities, including prevention of arteriosclerosis; lowering elevated levels of serum cholesterol and triglycerides; hypotensive effects; anticarcinogenic effects; antidiabetic effects; inhibition of platelet aggregation; and activation of fibrinolysis (Reuter & Sendl, “
Allium sativum
and
Allium ursinum
: Chemistry, Pharmacology, and Medicinal Applications”, in: Economic and Medicinal Plant Research, Academic Press, New York, 1994, pp. 54-113; Koch & Hahn, “Knoblauch: Grundlagen der therapeutischen Anwendung von
Allium sativum L.
”, Urban & Schwarzenberg, Munich 1988; Kochh & Lawson, “Garlic, The Science and Therapeutic Application of
Allium sativum L.
and Related Species”, Williams & Wilkins 1996).
It has thus been established that Garlic powder and granules can serve as a important nutritional supplement, and that garlic, in the proper form, is a good source of those biologically active compounds which are believed to be responsible for the above-mentioned therapeutic effects. However, it has also been found that in garlic powder or granules which is stored for long periods, the active ingredients present in freshly ground garlic are often eliminated or otherwise rendered inactive.
SUMMARY OF THE INVENTION
The present invention seeks to provide an improved garlic preparation, which preparation offers a convenient oral dosage form of garlic for supplying optimum plasma concentrations of biologically active allicin and related compounds, 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 granulated garlic, comprising granulated garlic and at least one carrier, adjuvant or excipient therefor.
In one preferred embodiment of the invention, the orally-administrable formulation for the controlled release of granulated garlic comprises granulated garlic 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 Allicin available from the formulation, based upon the total amount of alliin initially present in 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 garlic.
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 garlic 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 garlic embedded in a mixture of polyvinyl chloride and 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 garlic embedded in a mixture of polyvinyl chloride and ethyl cellulose, 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 garlic.
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 granulated garlic, said preparation comprising granulated garlic and at least one carrier, adjuvant or excipient therefor, said process comprising the steps of:
providing granulated garlic; and
incorporating said granulated garlic into said at least one carrier, adjuvant or excipient therefor;
wherein said at least one carrier, adjuvant or excipient therefor is characterized in that the total in vitro dissolution time of said formulation required for release of 75% of the Allicin from said formulation based upon the total amount of alliin initially present in said formulation is between about 4 and about 18 hours, as determined by to 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 process is characterized in that the granulated garlic 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 garlic 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 garlic 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 granulated garlic, comprising particles of granulated garlic 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.
In a preferred embodiment of the invention, the at least one active ingredient is allicin. In another preferred embodiment of the invention, the at least one active ingredient is alliin.
There is also provided in accordan
Blatt Yoav
Cohen David
Friedman Oded
Kimmelman Eugene
Rotman Avner
Abelman ,Frayne & Schwab
Bio Dar Ltd.
Fubara Blessing
Page Thurman K.
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