CN102552109A - External in-situ forming gel for treating dentin anaphylaxy - Google Patents
External in-situ forming gel for treating dentin anaphylaxy Download PDFInfo
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- CN102552109A CN102552109A CN2012100686271A CN201210068627A CN102552109A CN 102552109 A CN102552109 A CN 102552109A CN 2012100686271 A CN2012100686271 A CN 2012100686271A CN 201210068627 A CN201210068627 A CN 201210068627A CN 102552109 A CN102552109 A CN 102552109A
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Abstract
The invention discloses an external in-situ forming gel for treating dentin anaphylaxy. The external in-situ forming gel comprises an in-situ forming matrix and an antiallergic medicine, wherein the matrix comprises an in-situ forming gel and a forming agent; the in-situ forming gel consists of the following components in percentage by weight: 0.5 to 5 percent of sodium alginate, 0.5 to 3 percent of carbomer, 10 to 25 percent of glycerol, 2 to 15 percent of triethanolamine, 0.2 percent of preservative and the balance of water; the forming agent is an aqueous solution of a calcium salt, wherein the mass concentration of calcium ions is 1 to 20 percent, and a solute is one or a combination of more of calcium chloride, calcium gluconate, tricalcium citrate, calcium lactate and calcium lactate gluconate; and the antiallergic medicine comprises sodium fluoride glycerol and potassium oxalate. The external in-situ forming gel has a special effect on diastema which desensitizers in ordinary formulations cannot reach, can prolong the action time of the desensitizers on the surface of dentin effectively and is convenient to use, and a curative effect of treating the dentin anaphylaxy is improved greatly.
Description
Technical field
The present invention relates to a kind of external formed in situ gel that is used to desensitize, belong to medical technical field.
Background technology
Sodium alginate is a kind of natural polysaccharide compounds from extracting algae such as Thallus Laminariae (Thallus Eckloniae), Macrocystis pyrifera (L.) Ag.s, links the linear block copolymers that form with 3 kinds of modes (MM section, GG section and MG section) through α (1-4) glycosidic bond by guluronic acid (G section) and 2 kinds of construction units of its stereoisomer mannuronic acid (M section).Alginate can be when pH value be low (under the acid medium environment) and water or multivalent ion (like calcium ion etc.) produce gel; Utilize the agglomerative characteristic of this swelling of alginate, in commercial production, often be used as gel-type vehicle, thickening agent, stabilizing agent, film material, aqueous blocker etc.In recent years, the pharmaceutical grade sodium alginate also was widely used at home, as was used to prepare sulphur ointment, the pharmaceutical preparation of blood pressure lowering class, sulfa drugs preparation etc.Safety experiment and big quantity research show that sodium alginate is extremely safe (FDA, 1985) as food additive, and it allows intake is 0～25mgkg
-D
-1(U.S. FDA/WHO) has been recorded by American Pharmacopeia at present and has been used for pharmaceuticals industry, and is main as adhesive, disintegrating agent and slow-release material in pharmaceuticals industry.
Dental hypersensitiveness is the commonly encountered diseases and the frequently-occurring disease of the department of stomatology, and its pathogenesis, Most scholars are tended to the hydrodynamics theory, thinks that the dentin hypersensitiveness and the whole process of dentinal tubule flow open and that the little intraluminal fluid unit interval is interior is relevant.Theoretical according to hydrodynamics, be sealing dentinal tubule to effective treatment of dentin hypersensitiveness, to reduce or to avoid the liquid flow in the dentin.
Sodium fluoride glycerol solvent is through infiltrating fluorion, stops up dentinal tubule and combines to generate the strong fluor-apatite of acid-resisting with hydroxyapatite, change dentin permeability and bring into play therapeutic effect.The potassium oxalate solvent can form insoluble inorganic crystal complex; Dentin surface exposing forms a continuous precipitation layer, and degree of depth machinery stops up dentinal tubule, in addition; Owing to from the solution crystal precipitation, discharge potassium ion; Suppress the neural unpolarizing of dental pulp, thereby reduced neural irritability, stoped the propagation that stimulates.
Mainly be dentin desensitizer and daily antiallergic toothpaste through clinically for the treatment of dentin hypersensitiveness at present, drug desensitization is of short duration action time, and desensitization effect is not obvious.This research mainly is through inventing a kind of novel formed in situ desensitization sustained-release gel, increase the action time of drug desensitization, letting the patient treat voluntarily, and is easy to use.
Summary of the invention
The objective of the invention is for overcoming the deficiency of above-mentioned prior art; A kind of external formed in situ gel that is used to treat dental hypersensitiveness is provided; It can prolong drug in the action time of dentin surface, easy to use, improved the curative effect of treatment dental hypersensitiveness widely.
For realizing above-mentioned purpose, the present invention adopts following technical proposals:
A kind of external formed in situ gel that is used to treat dental hypersensitiveness; Comprise in-situ forming matrix and Claritin, substrate is divided into formed in situ gel and forming agent again, wherein; The formed in situ gel is made up of following components in weight percentage: sodium alginate 0.5～5%; Carbomer 0.5～3%, glycerol 10～25%, triethanolamine 2～15%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 1～20%, solute be in calcium chloride, calcium gluconate, citric acid tricalcium, calcium lactate, the lactic acid calcium gluconate any or appoint several kinds combination in any; Said Claritin is sodium fluoride glycerol or potassium oxalate.
Said Claritin is sodium fluoride glycerol (sodium fluoride 75g, glycerol 25g), and the percentage by weight that sodium fluoride glycerol accounts for the formed in situ gel is 5%-10%.
Said Claritin is a potassium oxalate, and the percentage by weight that potassium oxalate accounts for the formed in situ gel is 10%-15%.
Said antiseptic is an additive commonly used in the prior art, and the present invention does not have specific (special) requirements to its composition, repeats no more at this.
When said formed in situ gel prepares, each component is mixed, be stirred to solute and dissolve fully, form gel and get final product.When forming agent prepares, calcium salt is dissolved in distilled water gets final product.
Use: with the dental surface of formed in situ gel inlet intracavity sensitivity, reuse forming agent flushing formed in situ gel makes its forming and hardening on the throne.Diastema for the general formulation drug desensitization is difficult to arrive is especially effective.
Inventor of the present invention has carried out the interior and in vitro tests of body of formed in situ gel; Pharmacological evaluation and result show: formed in situ gel of the present invention is in position after the molding; Can effectively be covered on the responsive facing; Effectively prolonged the action time of medicine in the oral cavity, the treatment of dental hypersensitiveness has been had actively significantly effect.
The specific embodiment
Through instantiation the present invention is further set forth below, should be noted that following explanation only is in order to explain the present invention, its content not to be limited.
Embodiment 1: the preparation of sodium fluoride glycerol formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 0.5%; Carbomer 3%; Glycerol 15%, triethanolamine 5%, sodium fluoride glycerol 10%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 10%, and solute is a calcium chloride.Wherein sodium fluoride glycerol 10% is Claritin.
Process for preparation:
(1) preparation of pastille formed in situ gel: get sodium alginate 0.5%, carbomer 3%, glycerol 15%, triethanolamine 5%, sodium fluoride glycerol 10%; Antiseptic 0.2%; Add distilled water to 100%, be stirred to it and dissolve fully, be pastille formed in situ gel.
(2) preparation of forming agent: it is 10% to get final product that calcium chloride is dissolved in the mass concentration that makes its calcium ion in the distilled water.
Embodiment 2: the preparation of sodium fluoride glycerol formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 1%; Carbomer 0.5%; Glycerol 20%, triethanolamine 10%, sodium fluoride glycerol 5%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 15%, and solute is a calcium gluconate.Process for preparation is with embodiment 1.
Embodiment 3: the preparation of sodium fluoride glycerol formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 2%; Carbomer 1%; Glycerol 10%, triethanolamine 15%, sodium fluoride glycerol 6%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 20%, and solute is a calcium lactate.Process for preparation is with embodiment 1.
Embodiment 4: the preparation of sodium fluoride glycerol formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 3%; Carbomer 2%; Glycerol 25%, triethanolamine 2%, sodium fluoride glycerol 7%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 1%, and solute is the lactic acid calcium gluconate.Process for preparation is with embodiment 1.
Embodiment 5: the preparation of sodium fluoride glycerol formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 4%; Carbomer 2.5%; Glycerol 15%, triethanolamine 7%, sodium fluoride glycerol 8%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 3%, and solute is a citric acid tricalcium.Process for preparation is with embodiment 1.
Embodiment 6: the preparation of sodium fluoride glycerol formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 5%; Carbomer 1.5%; Glycerol 10%, triethanolamine 5%, sodium fluoride glycerol 9%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 5%, and solute is calcium chloride and citric acid tricalcium, does not have the restriction of consumption ratio between the two, as long as calcium ion concentration meets the demands.Process for preparation is with embodiment 1.
Embodiment 7: the preparation of potassium oxalate formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 5%; Carbomer 2%; Glycerol 10%, triethanolamine 15%, potassium oxalate 10%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 1%, and solute is calcium chloride and lactic acid calcium gluconate, does not have the restriction of consumption ratio between the two, as long as calcium ion concentration meets the demands.Process for preparation just is changed to potassium oxalate with sodium fluoride glycerol with embodiment 1, and adjusts its content and get final product.
Embodiment 8: the preparation of potassium oxalate formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 0.5%; Carbomer 3%; Glycerol 20%, triethanolamine 2%, potassium oxalate 15%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 10%, and solute is calcium lactate and calcium gluconate, does not have the restriction of consumption ratio between the two, as long as calcium ion concentration meets the demands.Process for preparation is with embodiment 7.
Embodiment 9: the preparation of potassium oxalate formed in situ gel
A kind of external in-situ forming matrix that is used to treat dentin hypersensitiveness; Comprise the formed in situ gel, the forming agent that contain Claritin, wherein, pastille formed in situ gel is made up of following components in weight percentage: sodium alginate 3%; Carbomer 0.5%; Glycerol 25%, triethanolamine 10%, potassium oxalate 12%, antiseptic 0.2%, surplus is a water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 20%, and solute is a citric acid tricalcium.Process for preparation is with embodiment 7.Experiment: antiallergic experiment in the antiallergic original position molding gelinite
Select dental hypersensitiveness patient 20 people totally 120 teeth; Separating tests group and matched group, test group are divided into sodium fluoride glycerol group and calcium oxalate group with the medicine of in-situ forming matrix dosage form; Matched group uses the medicine of regular dosage form, is divided into sodium fluoride glycerol group and calcium oxalate group.Measure the preceding dentine hypersensitivity degree that reaches 2 week of medication back patients of treatment respectively with VAS scale (visual analogue scale).The clinical examination of dentine hypersensitivity: to the cheek side test pain reaction of above-mentioned case at each tooth.In when test, the pointed probe head is vertical with the root face, and each slides to swipe and positions with the zone to sensitivity for 3 times along the vertical and horizontal directions.After the stimulation, the patient gives a mark to discomfort according to the VAS scale.Rest 20min implements air-blowing experiment again, is tried tooth and wipes away driedly with cotton cloth, at a distance from wet, is imposing on facing with exsiccant compressed air apart from root face 2～3mm place, and the persistent period is 5s.Require the patient to give a mark again.The VAS of 10cm is expressed as " no pain " at 0 end, be designated as 0 fen, is " intolerable pain " at 10cm end, is designated as 10 fens, confirms that through being determined on the 10cm line distance from 0 to patient's gauge point pain keeps the score.The clinical indices of all patient's dentine hypersensitivity degree is measured by a clinician through calibration and is accomplished.Data are seen table one, table two, table three, table four, table five, table six, table seven.
Compare
before and after the table Zymafluor glycerol formed in situ gel for treating
Annotate: P＜0.05
Compare
before and after the common drug treatment of table sodium bifluoride glycerol
Annotate: P＜0.05
Compare
before and after the table three potassium oxalate formed in situ gel for treating
Annotate: P＜0.05
Compare
before and after the common drug treatment of table potassium tetroxalate
Annotate: P＜0.05
Two kinds of administering modes of table five sodium fluoride glycerol are
relatively
Annotate: P＜0.05
Two kinds of administering modes of table six potassium oxalate are
relatively
Annotate: P＜0.05
Table seven sodium fluoride glycerol and potassium oxalate formed in situ gel for treating be
relatively
Annotate: P＞0.05
The result: the patient's dentine hypersensitivity reaction score of the common administration group treatment of sodium fluoride glycerol formed in situ gel group, the common administration group of sodium fluoride glycerol, potassium oxalate formed in situ gel group and potassium oxalate back is all than reducing before the treatment, and difference has statistical significance.Treatment back sodium fluoride glycerol formed in situ gel group is low than the common administration group of sodium fluoride glycerol dentine hypersensitivity reaction score, and difference has statistical significance; Treatment back potassium oxalate formed in situ gel group is low than the common administration group of potassium oxalate dentine hypersensitivity reaction score, and difference has statistical significance.Treatment back sodium fluoride glycerol formed in situ gel group and potassium oxalate formed in situ gel group dentine hypersensitivity reaction score difference not statistically significant.
Conclusion: these two kinds of ingredients of sodium fluoride glycerol and potassium oxalate are all effective in cure to the treatment dentine hypersensitivity.And through after changing pharmaceutical dosage form and being made into the formed in situ gel, the more common administration of its therapeutic effect is better.
Claims (3)
1. an external formed in situ gel that is used to treat dental hypersensitiveness is characterized in that, comprises in-situ forming matrix and Claritin; Substrate is divided into formed in situ gel and forming agent again; Wherein, the formed in situ gel is made up of following components in weight percentage: sodium alginate 0.5～5%, carbomer 0.5～3%; Glycerol 10～25%, triethanolamine 2～15%, antiseptic 0.2%, surplus are water; Forming agent is the aqueous solution of calcium salt, and wherein the mass concentration of calcium ion is 1～20%, solute be in calcium chloride, calcium gluconate, citric acid tricalcium, calcium lactate, the lactic acid calcium gluconate any or appoint several kinds combination in any; Said Claritin is sodium fluoride glycerol or potassium oxalate.
2. the external formed in situ gel that is used to treat dental hypersensitiveness as claimed in claim 1 is characterized in that said Claritin is a sodium fluoride glycerol, and the percentage by weight that sodium fluoride glycerol accounts for the formed in situ gel is 5%-10%.
3. the external formed in situ gel that is used to treat dental hypersensitiveness as claimed in claim 1 is characterized in that said Claritin is a potassium oxalate, and the percentage by weight that potassium oxalate accounts for the formed in situ gel is 10%-15%.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012100686271A CN102552109A (en) | 2012-03-15 | 2012-03-15 | External in-situ forming gel for treating dentin anaphylaxy |
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| CN2012100686271A CN102552109A (en) | 2012-03-15 | 2012-03-15 | External in-situ forming gel for treating dentin anaphylaxy |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105072927A (en) * | 2013-03-21 | 2015-11-18 | 罗蒂株式会社 | Oral composition for alleviating hyperesthesia |
| CN106974834A (en) * | 2017-04-01 | 2017-07-25 | 首都医科大学附属北京口腔医院 | A kind of utilization deferred reaction forms material and its application of mineral matter in dentinal tubule |
| US20190175469A1 (en) * | 2013-10-28 | 2019-06-13 | The Procter & Gamble Company | Tooth Desensitizing Oral Care Compositions, Devices, And Methods |
| CN111163841A (en) * | 2017-09-29 | 2020-05-15 | 3M创新有限公司 | Oral care fluoride aqueous treatment compositions and methods |
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| WO2007091856A1 (en) * | 2006-02-10 | 2007-08-16 | Lg Household & Health Care Ltd. | In-situ melting and gelling tablet composition for oral care |
| CN101584889A (en) * | 2009-07-10 | 2009-11-25 | 山东大学威海分校 | External in-situ forming matrix used for treating periodontal diseases |
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2012
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| WO2007091856A1 (en) * | 2006-02-10 | 2007-08-16 | Lg Household & Health Care Ltd. | In-situ melting and gelling tablet composition for oral care |
| CN101584889A (en) * | 2009-07-10 | 2009-11-25 | 山东大学威海分校 | External in-situ forming matrix used for treating periodontal diseases |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105072927A (en) * | 2013-03-21 | 2015-11-18 | 罗蒂株式会社 | Oral composition for alleviating hyperesthesia |
| US20190175469A1 (en) * | 2013-10-28 | 2019-06-13 | The Procter & Gamble Company | Tooth Desensitizing Oral Care Compositions, Devices, And Methods |
| CN106974834A (en) * | 2017-04-01 | 2017-07-25 | 首都医科大学附属北京口腔医院 | A kind of utilization deferred reaction forms material and its application of mineral matter in dentinal tubule |
| CN106974834B (en) * | 2017-04-01 | 2020-10-27 | 首都医科大学附属北京口腔医院 | Material for forming mineral substance in dentin tubule by delayed reaction and its application |
| CN111163841A (en) * | 2017-09-29 | 2020-05-15 | 3M创新有限公司 | Oral care fluoride aqueous treatment compositions and methods |
| CN111163841B (en) * | 2017-09-29 | 2024-03-12 | 3M创新有限公司 | Oral care fluoride aqueous therapeutic compositions and methods |
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Application publication date: 20120711 |