TH12970Y - This document describes the composition of an oral ointment containing a complex mixture of quaternized beta-cyclodextrin derivatives, chitosan, and alpha-mangostin, as well as the preparation method for such ointment. - Google Patents

Abstract

Revised Abstract of Invention 26/08/2016. This invention relates to the development of a formulation of an oral ointment containing a complex of quaternized beta-cyclodextrin chitosan derivatives and alpha-mangostin. The composition of the oral ointment according to this invention consists of: a) a gelling agent composed of hydroxypropyl methylcellulose (HPMC), quaternized chitosan derivatives (QCS), carrageenan, and konjac powder; and b) a complex of quaternized beta-cyclodextrin chitosan derivatives and alpha-mangostin. (alpha-mangostin inclusion complexes between quaternized chitosan grafted beta-cyclodextrin) and c) additives consisting of glycerine and water. The oral ointment formulated in this invention has the ability to relieve inflammation of oral tissues and inhibit the growth of pathogenic microorganisms in the oral cavity and is not toxic to buccal mucosal cells. Furthermore, the carrier derivative that encapsulates the active ingredient, mangosteen peel extract, can increase the adhesion to buccal tissue, thereby increasing the efficacy and duration of action of the oral ointment formulation. ----------------------------------------------------- New Request for Improvement: This invention relates to the development of an oral ointment formulation containing a complex of quaternized beta-cyclodextrin derivatives, chitosan, and alpha-mangostin. The composition of the oral ointment formulated in this invention consists of a) a gelling agent consisting of hydroxypropylmethylcellulose. The oral ointment formulated in this invention consists of: a) quaternized chitosan derivatives (QCS), carrageenan, and konjac powder; b) alpha-mangostin inclusion complexes between quaternized chitosan grafted beta-cyclodextrin; and c) an additive consisting of glycerine and water. The oral ointment exhibits anti-inflammatory properties for oral tissues and inhibits the growth of oral pathogenic microorganisms without being toxic to buccal mucosal cells. Furthermore, the carrier substance encapsulating the active ingredient, mangosteen peel extract, enhances its adhesion to buccal tissue, thereby improving the efficacy and duration of action of the oral ointment formulation.

Claims (8)

Revised 26/08/2016 1. Composition of the oral ointment, consisting of: - Gelling agents composed of hydroxypropyl methylcellulose (HPMC), quaternized chitosan derivatives (QCS), carrageenan, and konjac powder. - Complexes between quaternized beta-cyclodextrin chitosan derivatives and alpha-mangostin. - Additives consisting of glycerine. - Water. 2. Composition of the oral ointment... According to the appropriate Patent 1, the oral ointment composition shall consist of: - Hydroxypropyl methylcellulose, 1.5-3% by weight; - Quaternized chitosan derivative, 1-5% by weight; - Carrageenan, 0.5-3% by weight; - Konjac powder, 0.5-7% by weight; - Complex of quaternized beta-cyclodextrin chitosan derivative and alpha-mangostin, 1-5% by weight; - Glycerin, 1-5% by weight; - Water, in an amount totaling 100% by weight. 3. The composition of the oral ointment according to Patent 1 or 2, where the said additives may also consist of selected substances from the group comprising flavoring agents, cooling agents, preservatives, sweeteners, and mixtures of such substances. 4. The composition of the oral ointment according to Patent 1 or 2, where the appropriate complex of quaternized beta-cyclodextrin chitosan derivative and alpha-mangostin shall consist of: It is a complex compound between quaternized beta-cyclodextrin chitosan derivatives and alpha-mangostin prepared from quaternized beta-cyclodextrin chitosan derivatives with the following chemical structure (chemical formula) where a+b+c = 1, where a = 0.09, b ranges from 0.75-0.80, and the degree of beta-cyclodextrin attachment to the chitosan chain, i.e., the value of c ranges from 0.10-0.12. 5. Composition of oral ointment according to claim 3, where the suitable quaternized chitosan derivative is a quaternized chitosan derivative with the following chemical structure (chemical formula) where a+b+c = 1, where a = 0.1 and b+c = 0.9, and has a substitution degree of the group. Glycidyltrimethylammonium chloride (GTMAC) (degree of quaternization, DQ) is defined as a c value in the range of 0.7-0.9. 6. Preparation process of the oral ointment, consisting of the following steps: - Preparation of the first solution consisting of hydroxypropyl methylcellulose in water. - Preparation of the second solution consisting of carrageenan, konjac powder, and glycerin in water. - Preparation of the third solution consisting of a complex of quaternized chitosan derivatives, beta-cyclodextrin chitosan, and alpha-mangostin, quaternized chitosan derivatives (QCS) in water. - Mixing the first and second solutions until homogeneous. - Mixing the third solution with the mixture of the first and second solutions using a homogenizer to obtain the oral ointment formulation. 7. The preparation method for the oral ointment under claim 6 may be further enhanced by adding a solution of the sweetener in water to the mixture of solutions part one, part two, and part three, and then mixing until homogeneous. 8. The preparation method for the oral ointment under claim 6 or 7 may be further enhanced by adding a solution of the flavoring agent, cooling agent, preservative, and a mixture of these agents in water to the mixture of solutions part one, part two, and part three, and then mixing until homogeneous. ------------------------------------------------------------------- New Application (Revised) 1. Composition of the oral ointment, consisting of: - Gelling agents composed of hydroxypropyl methylcellulose (HPMC), quaternized chitosan derivatives (QCS), carrageenan, and konjac powder. - Alpha-mangostin inclusion complexes between quaternized chitosan grafted beta-cyclodextrin. - Additives consisting of glycerine. - Water. 2. Composition of the oral ointment, consisting of: - Hydroxypropyl methylcellulose, 1.5-3% by weight - Quaternized chitosan derivative, 1-5% by weight - Carrageenan, 0.5-3% by weight - Konjac powder, 0.5-7% by weight - Complex of quaternized beta-cyclodextrin chitosan derivative and alpha-mangostin, 1-5% by weight - Glycerin, 1-5% by weight - Water, to make 100% by weight. 3. The composition of the oral ointment as per claim 1 or 2, where such additive may also contain additional substances of a choice from a group of flavoring agents, cooling agents, preservatives, sweeteners and mixtures thereof. 4. Composition of the oral ointment according to claim 1 or 2, where the appropriate complex between quaternized beta-cyclodextrin chitosan derivatives and alpha-mangostin is the complex between quaternized beta-cyclodextrin chitosan derivatives and alpha-mangostin prepared from quaternized beta-cyclodextrin chitosan derivatives with the following chemical structure (chemical formula): Quaternized chitosan grafted beta-cyclodextrin (QCD-g-CS) where a+b+c = 1, where a = 0.09, b ranges from 0.75-0.80, and the degree of beta-cyclodextrin attachment to the chitosan chain, i.e., the value of c ranges from 0.10-0.12. 5. Composition of the oral ointment according to claim 3, where the appropriate quaternized chitosan derivative is a quaternized chitosan derivative with the following chemical structure (chemical formula): Quaternized chitosan (QCS) where a+b+c = 1, where a = 0.1 and b+c = 0.9, and with a degree of quaternization (DQ) of glycidyltrimethylammonium chloride (GTMAC), i.e., the value of c is in the range of 0.7-0.9. 6. Preparation process of the oral ointment, consisting of the following steps: - Preparation of the first solution consisting of hydroxypropyl methylcellulose in water. - Preparation of the second solution consisting of carrageenan, konjac powder, and glycerin in water. - Preparation of the third solution consisting of a complex of quaternized beta-cyclodextrin chitosan and alpha-mangostin, quaternized chitosan derivatives (QCS) in water. - Mixing the first and second solutions until homogeneous. - Mixing the third solution with the mixture of the first and second solutions using a homogenizer. This will obtain the oral ointment formulation containing the complex of quaternized beta-cyclodextrin chitosan and alpha-mangostin. 7. The procedure for preparing the oral ointment as per claim 6 may be further enhanced by adding a solution of the sweetener in water to the mixture of the first, second, and third solutions and mixing until they are homogeneous. 8. The procedure for preparing the lip ointment as per claim 6 or 7 may include the addition of a solution of flavoring agents, cooling agents, preservatives, and a mixture of these agents in water to the first, second, and third solutions mentioned above, and then mixing until they are dissolved into a homogeneous mixture.