Title of Invention

"A PROCESS FOR PREPARATION OF A COMPOSITION FOR THE TREATMENT OF PERIODONTAL INFECTIONS"

Abstract

A process for preparation of a composition for the treatment of periodontal infections comprising the steps of: preparing polymeric dispersion by mixing 75-85% by weight of a polymer selected from hydroxypropyl methyl cellulose (HPMC E-15)., HPMC-E4M, HPMC-E5, Eudragit, Hydroxy Propyl Cllulose {HPC-L), L-Lactide and Poly (L-Lactide-Co-Gylycolide) in a solvent selected from methylene chloride, acetone and isopropanol, adding a plasticizer in said dispersion of step (a) wherein the amount of said palcticizer is 0,10 to 0.20% by weight of said poiymeric dispersion, adding drugs in the amount of 15-20% by weight of said polymeric dispersion in mixture of step (b) and preparaing dispersion in the manner such as herein described wherein said drug comprise for example a mixture of amoxycillin and metronidazoie in the ratio of 1:1 by weight, pouring the said dispersion of step (c) into glass rings placed over aluminium foil and drying said dispersion comprises a first step to dry the dispersion at the temperature of -5 to -10°C for a period of 8 to 10 hours followed by a second step of drying at room temperature for a period of 20 to 24 hours.

Full Text

This invention relates to a process for preparation of a composition for the treatment of periodontal infections. The systemic antibiotic therapy has been used for the management of human inflammatory periodontal diseases. In this, the drug, dosage form and duration of administration have been empirically selected merely based on clinical judgment. However there are disadvantages associated with this conventional therapy. One of the main disadvantages is that systemic, antibiotic therapy causes various side effects. Moreover the drug gets diluted several thousand times before it reaches to the site of action and therefore adequate concentrations needed produce the therapeutic response, are not attained. Another disadvantage is that the full potential of the drug may be unobtainable by systemic route of administration, since periodontal organisms require prolonged exposure to the drug. Yet another disadvantage is that drug is not applied directly to the site of infection and therefore high dosage of drug are required. Still another disadvantage is that the use of systemic antibiotics in periodontal therapy causes harmful effect on the periodontal tissues. The main object of this invention is to provide a process for preparation of a composition for the treatment of periodontal infections for low dose drug delivery that is capable of achieving and .. maintaining concentration above minimum inhibitory concentration of the drug against the microbal flora which is commonly implicated in these infections. Another objection of this invention is to provide a process for preparation of a composition for the treatment of periodontai infections which is applied at the site of infection in low doses. Yet another object of the present invention is to provide a drug delivery device which does not cause any side effects. According to this invention there is provided A process for preparation of a composition for the treatment of periodontai infections comprising the steps of: preparing polymeric dispersion by meting 75-85% by weight of a polymer selected from hydroxypropyl methyl cellulose (HPMC E-15), HPMC-E4M, HPMC-E5, Eudragit, Hydroxy Propyi Cellulose (HPC-L), L-Lactide and Poly (L-Lactide-Co-Gylycolide) in a solvent selected from methylene chloride, acetone and isopropanol, adding a plasticizer in said dispersion of step (a) wherein the amount of said palcticizer is 0.10 to 0.20% by weight of said polymeric dispersion, adding drugs in the amount of 15-20% by weight of said polymeric dispersion m mixture of step (b) and preparaing dispersion in the manner such as herein described wherein said drugs comprise for example a mixture of amoxyciltin and metronidazole in the ratio of 1:1 by weight, pouring the said dispersion of step (c) into glass rings placed over aluminium foil and drying said dispersion comprises a first step to dry the dispersion at the temperature of-5 to -10°C for a period of 8 to 10 hours followed by a second step of drying at room temperature for a period of 20 to 24 hours. In accordance with this invention 75-85% by weight of polymer is dispersed in methyien chloride solvent, 0.10 to 0.20% by weight of plasticizer for example diethyl phthalate is added into said dispersion 15-20% by weight of the drugs for example amoxycillin and metronidazole are added into the said dispersion. The drugs are mixed with each other in the ratio of 1:1. These drugs are in the powder form sieved through 80 to 120 mesh size. The drug are homogenousty into the polymer solution by vortexing for 2 to 10 minutes. The homogenous dispersion so obtained is poured into glass rings placed over aluminium foil and allowed to dry initially at -5 to 10° C for a period of 8 to 10 hours followed by drying at room temperature for a further period of 20 to 24 hours. The polymers used are hydroxypropyl methyl cellulose E-15 (HPMC E-15), HPMC-E4M, HPMC E5, Eudragit, Hydroxy Propyl Cellulose-L (HPC-L), L-Lactide, Poly-(L-Lactide-Co-Glycolide), biodegradable polymer (Poly (L-lactide-co-Glycolide) is preferred for use.The solvents used are methyiene chloride, Acetone and/or isopropanol The process for the preparation of a composition is herein described in detail in the following example. EXAMPLE 0.8 gm Poly (L-lactide-Co-Glycolide) was dispersed in a solvent like methyiene chloride. 0.2 ml diethyl phthalate was added into said solution 0.8 gm of amoxycillin and metronidazole mixed in the ratio of 1:11 and sieved through (80 to 120 mesh size) were added into the solution mixture. The mixture so obtained was dispersed homogenously by vortexing for 8 minutes. The dispersion so obtained was poured into glass rings placed over aluminium foil and allowed it to dry at a temperature of -10° C for 8 hours. The dispersion was further dried at room temperature for a period of 24 hours to prepare the drug delivery device. WE CLAIM: 1. A process for preparation of a composition for the treatment of periodontal infections comprising the steps of: (a) preparing polymeric dispersion by mixing 75-85% by weight of a polymer selected from hydroxypropyl methyl cellulose (HPMC E-15), HPMC-E4M, HPMC-E5, Eudragit, Hydroxy Propyl Cellulose (HPC-L), L-Lactide and Poly (fa) adding a plasticizer in said dispersion of step (a) wherein the amount of said palcticizer is 0.10 to 0.20% by weight of said polymeric dispersion, (c) adding drugs in the amount of 15-20% by weight of said polymeric dispersion in mixture of step (b) and preparaing dispersion in the manner such as herein described wherein said drugs comprise for example a mixture of amoxycillin and metronidazole in the ratio of 1:1 by weight, (d) pouring the said dispersion of step (c) into glass rings placed over aluminium foil and drying said dispersion comprises a first step to dry the dispersion at the temperature of-5 to -10°C for a period of 8 to 10 hours followed by a second step of drying at room temperature for a period of 20 to 24 hours. 2. A process as claimed in claim 1 wherein said polymer is preferably Poly (L-Lactide-Co-Gtycolide) and said solvent is preferably methylene chloride. 3. A process as claimed in claim 1 wherein the plasticizer is preferably phthalate. 4. A process as claimed in claim 1 wherein said drugs are used in the powder form sieved through a mesh of the size of 80 to 120. 5. A process as claimed in claim 1 wherein said dispersion of step (c) is homogenous, which is prepared by subjecting the mixture of step (c) to the step of vortexing for 2 to 10 minutes in a vortexing machine. 6. A process for preparation of a composition for the treatment of periodontai infections substantially as herein described and illustrated with reference to example.

Documents:

820-del-2002-abstract.pdf

820-del-2002-claims.pdf

820-del-2002-correspondence-others.pdf

820-del-2002-correspondence-po.pdf

820-del-2002-description (complete).pdf

820-del-2002-form-1.pdf

820-del-2002-form-2.pdf

820-del-2002-form-3.pdf

820-del-2002-form-4.pdf

820-del-2002-gpa.pdf