Pharmaceutical formulation, its use, and method for its manufacture

Abstract

A pharmaceutical formulation of a calcium salt and a dry plant extract in the form of a coated tablet, in which the formulation has a core of at least one dry plant extract, enveloped by at least one coating of at least one calcium salt. The plant extracts for the core may be selected from: Vitex agnus castus (chaste tree); Belamcanda chinensis (leopard lily); Cimicifuga racemosa (black cohosh); Trifolium pratense L. (purple trefoil); Oenothera biennis hom. (primrose); Glycine soja (soy bean); Serenoa repens (saw-palmetto); Urtica dioica (stinging nettle), in particular its root; Cucurbita pepo (pumpkin), in particular its seed; Pygeum africanum; as well as suitable mixtures of these. Methods for the use of the formulation in treating osteoporosis and for manufacturing the formulation are provided.

1 . A pharmaceutical formulation of a calcium salt and a dry plant extract, comprising an inner pressed body of at least one dry plant extract, which is enveloped by at least one calcium-containing coating. 
   
   
       2 . The pharmaceutical formulation in accordance with  claim 1 , wherein the dry plant extract is selected from the group consisting of extracts from:  Vitex agnus castus  (chaste tree);  Belamcanda chinensis  (leopard lily);  Cimicifuga racemosa  (black cohosh);  Trifolium pratense L.  (purple trefoil);  Oenothera biennis hom.  (primrose);  Glycine soja  (soy bean);  Serenoa repens  (saw-palmetto);  Urtica dioica  (stinging nettle);  Cucurbita pepo  (pumpkin);  Pygeum africanum;  and suitable mixtures thereof. 
   
   
       3 . The pharmaceutical formulation in accordance with  claim 2 , wherein the dry plant extract is selected from the group consisting of extracts from:  Urtica dioica  (stinging nettle) root;  Cucurbita pepo  (pumpkin) seed; and suitable mixtures thereof. 
   
   
       4 . The pharmaceutical formulation in accordance with  claim 1 , wherein the calcium salt is selected from the group consisting of: calcium carbonates; calcium hydrogen carbonates; calcium halides; calcium phosphates; calcium hydrogen phosphates; dicalcium hydrogen phosphates; calcium lactates; calcium lactonates; calcium succinates; calcium tartrates; calcium gluconates; and suitable mixtures thereof. 
   
   
       5 . The pharmaceutical formulation in accordance with  claim 4 , wherein the calcium salt is selected from the group consisting of: calcium chlorides; calcium iodides; calcium monohydrogen phosphate; and suitable mixtures thereof. 
   
   
       6 . The pharmaceutical formulation in accordance with  claim 1 , wherein said formulation is a coated tablet, said coating is a pressed body of at least one calcium salt, and said core is a pressed body of at least one dry plant extract. 
   
   
       7 . The pharmaceutical formulation in accordance with  claim 1 , wherein said formulation is a dot tablet (bull-eye tablet). 
   
   
       8 . The pharmaceutical formulation in accordance with  claim 1 , wherein the coating comprises a plurality of calcium layers. 
   
   
       9 . The pharmaceutical formulation in accordance with  claim 8 , wherein each said layer contains a different calcium salt. 
   
   
       10 . The pharmaceutical formulation in accordance with  claim 6 , wherein said formulation has a calcium content of about 50 to about 1000 mg per coated tablet and a dry plant extract content of about 0.5 to about 100 mg. 
   
   
       11 . The pharmaceutical formulation in accordance with  claim 1 , wherein said formulation further comprises a polymer film as an external envelope. 
   
   
       12 . The pharmaceutical formulation in accordance with  claim 6 , wherein said formulation has a calcium content of about 1250 mg of calcium carbonate (corresponding to about 500 mg of Ca2+) and about 200 I.U. vitamin D3 in the coating of the coated tablet, and about 20 mg dry extract preparation of Cimicifuga racemosa in the core of the coated tablet. 
   
   
       13 . The pharmaceutical formulation in accordance with  claim 1 , wherein said calcium-containing coating and/or said inner pressed body of dry plant extract formulation further comprises one or more cholecalciferols. 
   
   
       14 . The pharmaceutical formulation in accordance with  claim 13 , wherein said cholecalciferol is Colecalciferol (vitamin D3). 
   
   
       15 . The pharmaceutical formulation in accordance with  claim 19 , wherein said formulation further comprises at least one fluoride salt. 
   
   
       16 . The pharmaceutical formulation in accordance with  claim 15 , wherein said fluoride salt is sodium fluoride. 
   
   
       17 . The pharmaceutical formulation in accordance with  claim 15 , wherein said fluoride salt is present in the inner pressed body. 
   
   
       18 . The pharmaceutical formulation in accordance with  claim 11 , wherein said formulation further comprises one or more auxiliaries selected from the group consisting of disintegrants, binders, lubricants, and slip agents. 
   
   
       19 . The pharmaceutical formulation in accordance with  claim 18 , wherein said formulation is selected from the group consisting of a starch, a starch derivative, a microcrystalline cellulose, gum arabic, stearic acid, magnesium stearate, polyethylene glycol, and a mixture thereof. 
   
   
       20 . A method for the treatment or prevention of osteoporoses of various geneses, said method comprising administering to a subject in need thereof an effective amount of the formulation of  claim 1 . 
   
   
       21 . The method in accordance with  claim 20 , wherein said osteoporoses of various geneses are brought about by lack of sexual hormone, by a hormone-related geriatric complaint, by a menopausal complaint, by a prostate affliction, by an accompanying cardiovascular disorder, by a disturbances of lipid metabolism, by a disorder accompanying a calcium deficiency, or by a combination thereof. 
   
   
       22 . A method for manufacturing a pharmaceutical formulation in accordance with  claim 1 , said method comprising:
 preparing a pressed body core of a dry plant extract, wherein the dry plant extract is selected from the group consisting of extracts from:  Vitex agnus castus  (chaste tree);  Belamcanda chinensis  (leopard lily);  Cimicifuga racemosa  (black cohosh);  Trifolium pratense L.  (purple trefoil);  Oenothera biennis hom.  (primrose);  Glycine soja  (soy bean);  Serenoa repens  (saw-palmetto);  Urtica dioica  (stinging nettle);  Cucurbita pepo  (pumpkin);  Pygeum africanum;  and suitable mixtures thereof;   transferring said core to a first partial quantity of a coating mixture of at least one calcium salt, followed by filling with a second partial quantity of the coating mixture; and   pressing the entire formulation comprised of the core and the two partial quantities of the calcium salt-containing coating mixture to form the pharmaceutical formulation;   wherein the calcium salt is selected from the group consisting of:   calcium carbonates; calcium hydrogen carbonates; calcium halides; calcium phosphates; calcium hydrogen phosphates; dicalcium hydrogen phosphates, calcium lactates; calcium lactonates; calcium succinates; calcium tartrates; calcium gluconates; and suitable mixtures thereof.   
   
   
       23 . The method in accordance with  claim 22 , wherein the core is centered on the first partial quantity of the coating mixture. 
   
   
       24 . The method in accordance with  claim 23 , wherein the pharmaceutical formulation further comprises one or more auxiliaries selected from the group consisting of disintegrants, binders, lubricants, and slip agents. 
   
   
       25 . The method in accordance with  claim 24 , wherein said formulation is selected from the group consisting of a starch, a starch derivative, a microcrystalline cellulose, gum arabic, stearic acid, magnesium stearate, polyethylene glycol, and a mixture thereof.