Absorbable solid compositions for topical treatment of oral mucosal disorders

Abstract

The invention provides a solid, self-bioadhesive composition for topical application that adheres to the oral mucosal tissue comprising a therapeutically effective amount of at least one herbal or homeopathic active agent; and a pharmaceutically acceptable solid bioadhesive carrier in an amount from about 40 to 99 percent based on the weight of the whole composition.

1 . A solid, self-bioadhesive composition for topical application that adheres to the oral mucosal tissue comprising:
 (a) a therapeutically effective amount of at least one herbal active agent selected from the group consisting of bioactive herb extracts, tinctures, essential oils, and mixtures thereof; and   (b) 15 to 99 percent based on the weight of the whole composition of a bioadhesive polyacrylic acid;   and wherein the composition is in the form of a compressed tablet.   
     
     
         2 . A solid composition according to  claim 1  wherein said composition is in the form of a disc of 2-15 mm diameter and 0.4 to 2.3 mm thick that adheres to oral mucosal tissue for at least 30 minutes 
     
     
         3 . A solid composition according to  claim 1  wherein said composition is in the form of a disc of 5-11 mm diameter and 1 to 2 mm thick with tissue adherence of at least 1 hour. 
     
     
         4 . A composition according to  claim 1 , wherein the herbal active agent is selected from the group consisting of an either anti-inflammatory, analgesic, antiaching, anesthetic, antimicrobial, antifungal, antiseptic, antiviral, antibiotic, and an antiparasite agent and combinations thereof. 
     
     
         5 . (canceled) 
     
     
         6 . A composition according to  claim 3 , wherein the herb tincture active agents are selected from the group consisting of:  Gotu Kola, Echinacea, Salvia offinc, Hypericum, Myrrah, Camphoria, Uncaria , Elder,  Plantago, Baptisia, Calendula, Phytolaca , Catechu black, Coneflower,  Krameria, Tsuga , grape fruit seed extract,  Rosmarinus, Styrax, Crataegus, Glycerrhiza, Angelica, Krameria, Matricaria , Mallow, Propolis, Sage, Barberine from  hydrastis canadensis  L. and other berberidaccae plant family, gentian from the gentianaceae family of plants for the treatment of fungal infections, monoterpenes of three unsaturations,  Taraxacum  extract,  Lonicera  flower extract,  Scutellaria  root extract,  Gardenia  fruit extract,  Pulsatilla  root extract,  Pueraria  root extract, Radix gentianae Longdancao antifungal agent and combinations thereof. 
     
     
         7 . The composition of  claim 1 , wherein the herb essential oils active agents are selected from the group consisting of: citronella oil, lemon oil, citron oil, pomela peel oil, cedrwood oil, juniper berries oil, lemon basil oil,  rosmarinus offencinalis  oil, cinnamon oil, cajeput oil, eucalyptus oil, fennel oil, geranium oil, girofle oil, lavender oil, clove oil, spearmint oil, myrte oil, origano oil, pine oil, rosemary oil, sarriette oil, thyme oil, and tea-tree oil. 
     
     
         8 . The composition of  claim 1  wherein the essential oil is selected from the group consisting of cinnamon oil, tea-tree oil and citronella oil and mixtures thereof. 
     
     
         9 . A composition according to  claim 7 , wherein said essential oil comprises at least one monoterpene with three unsaturations. 
     
     
         10 . A composition according to  claim 9 , wherein said essential oil is a natural or synthetic mixture consisting of limonene, myrcene, a-pinene, b-pinene, sabinene characterized in that at least 60% by weight is limonene. 
     
     
         11 . A composition according to  claim 9 , wherein said monoterpenes with three unsaturations is of citrus oil selected from the group consisting of lemon, pomella and citron. 
     
     
         12 . A composition according to  claim 6 , further comprising a salt selected from the group consisting of MgBr 2 , NaCl, KCl and mixtures thereof. 
     
     
         13 . A composition according to  claim 6 , further comprising Carnallite in a synergistic and effective amount. 
     
     
         14 . A composition according to  claim 13 , wherein said Carnallite is present in an amount of about 5-50% wt/wt of the active composition. 
     
     
         15 . The composition of  claim 1 , further comprising a non-herbal active agent selected from the group consisting of analgesics, steroidal and non-stroidal anti-inflammatory agents, antihistaminic or antiallergics, steroids, antimicrobial drugs, vitamins, enzymes, anti-allergic drugs, antipyretics, antimalarial, antiulcer drugs, peptides, DNA plasmid and antisense based therapeutic agents, 
     
     
         16 . The composition of  claim 15 , wherein the anesthetic agent is selected from the group consisting of procaine, lidocaine, prilocaine, mepivacaine, dyclonine, dibucaine, benzocaine, chloroprocaine, tetracaine, bupivacaine, and etidocaine and is in the form of the base or an acid-addition salt or both forms. 
     
     
         17 . The composition of  claim 15 , wherein the non-herbal agent consists of dexamethasone, triamcinolone, hydrocortisone, and the like, amphotericine B, nystatin, itraconazole, and the like, chlorhexidine, quaternary ammonium salts, parabens, dextranase enzymes, is in the form of the base or an acid-addition salt or both forms. 
     
     
         18 . The composition of  claim 4 , wherein salts comprising of Carnallite and its individual salts are used to improve the activity of the herbal active agents. 
     
     
         19 . The composition of  claim 4 , wherein the active agent consists of a mixture of natural or synthetic monoterpenes with three unsaturations comprising of: limonene, myrcene, pinenes, sabinene, terpinene, and the like. 
     
     
         20 . The active agent of  claim 15  comprising a cirton oil and Carnallite salt at a weight ratio between 1:10 to 1:1. 
     
     
         21 . The active agent of  claim 15  comprising a cirton oil and Carnallite salt at a weight ratio between 1:10 to 1:1 and a local anesthetic such as lidocaine, benzocaine, or bupivecaine. 
     
     
         22 . The composition of  claim 1 , further comprising a natural, semisynthetic or synthetic polyhydric polymer. 
     
     
         23 . The composition of  claim 22  wherein said polyhydric polymer comprises at least one member selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethylcellulose, carboxymethyl cellulose, dextran, arabinogalactan, pullulan, gaur-gum, hyaluronic acid, pectins, starch derivatives, polymers of vinyl alcohols, alkoxy polymers, polyethylene oxide polymers, polyethers, and mixtures thereof. 
     
     
         24 . A composition according to  claim 22  in the form of a tablet wherein said adhesive additionally contains one or more members selected from the group consisting of fillers, tableting excipients, lubricants, enhancers, flavors, taste-masking agents, pH controlling compounds, dyes, stabilizers, enyzme inhibitors, and lubricants. 
     
     
         25 . A composition according to  claim 22  wherein said enhancers are salts of bile acids, limonene and limonene derivatives. 
     
     
         26 . A composition according to  claim 1  wherein the polyacrylic acids are polyacrylic acid polymers lightly crosslinked with a polyalkenyl polyether and cellulose derivatives and mixtures thereof 
     
     
         27 - 31 . (canceled) 
     
     
         32 . A method for treating oral mucosal disorders, comprising administering to a patient a composition comprising a terpenoid oil consisting of at least 65% limonene oil in combination with a suitable solid self-bioadhesive carrier. 
     
     
         33 . A method for treating or preventing oral mucositis (stomatitis), aphthous lesions, or gingivitis in a patient, comprising administering a composition of  claim 1 . 
     
     
         34 . A method for reducing the depth of periodontal pockets in a patient, comprising administering a composition of  claim 1 . 
     
     
         35 . The composition according to  claim 26 , wherein the polyacrylic acids are polyacrylic acid polymers lightly crosslinked with a polyalkenyl polyether.