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Encapsulation of oral care active agents

A technology for oral care and active agents, which is applied in the field of encapsulating water-soluble oral care active agents, and can solve problems such as uncomfortable oral care active agents

Inactive Publication Date: 2017-05-10
KONINKLJIJKE PHILIPS NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these solvents are not suitable for creating general-purpose encapsulation systems for oral care actives because several important such agents, such as carbamide peroxide and chlorhexidine, are soluble in these solvents

Method used

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  • Encapsulation of oral care active agents
  • Encapsulation of oral care active agents
  • Encapsulation of oral care active agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] A polymer solution was prepared by dissolving 6 g of cellulose acetate in 40 ml of ethyl formate overnight (14 hours) at room temperature in a glass sealed container. Chlorhexidine diacetate (1.5 g) was then dispersed into the pre-cooled polymer solution, placed on ice while stirring with a magnetic stirrer at 300 rpm for 10 minutes, and then the suspension was poured into a circulating water bath connected to in a jacketed reactor to control the temperature at 5 °C. On a weight basis, the active / polymer ratio is 1 / 4. A mixture containing magnesium stearate (anti-aggregation and release rate controlling agent (MS, 1 g) prepared by blending at 8000 rpm for 2 minutes with a high shear rotor stator mixer (Silverson L4RT) while cooling the system with an ice bath. ) and polyglycerol polyricinoleate emulsifier (PGPR, 0.5g) anti-solvent liquid paraffin (200mL) was pumped (6mL / min) into the previously prepared active-polymer suspension while using The pitched blade impeller ...

Embodiment 2

[0060] Dissolve 4 g of cellulose acetate in 20 ml of ethyl formate. The continuous phase was prepared by adding 0.85 g MS to 70 ml liquid paraffin containing 0.35 g PGPR emulsifier and mixing with a high shear rotor stator mixer (Silverson L4RT) at 8000 rpm for 2 minutes while cooling the system with an ice bath. A given amount of chlorhexidine was then added to the polymer solution, placed on ice, to achieve a specific active / polymer ratio (1 / 2; 1 / 3) with stirring. The mixture was further stirred at 300 rpm for 10 min with a magnetic stirrer, then it was added to the reactor containing the previously prepared continuous phase, saturated with 30% (v / v) ethyl formate (i.e., 21 mL) and cooled to 5°C. The mixture was magnetically stirred at 400 rpm for 2 hours using a six pitched blade Rushton impeller to create an emulsion. The oil-in-oil emulsion was gradually heated to 20°C and stirred at this temperature for 16 hours to allow the diffusion of ethyl formate into the liquid p...

Embodiment 3

[0063] NaF-loaded microparticles were prepared by emulsion solvent evaporation according to a two-level factorial design (Table 4) with three factors: polymer concentration (10% and 20%, weight / volume), solvent evaporation temperature (10°C and 20°C) and solvent concentration in the continuous phase (ie, the amount of ethyl formate in liquid paraffin at the start of emulsification, 15% (10.5 mL) and 30% (21 mL), v / v). Samples were prepared according to the procedure described in Example 2 with MS in the dispersed phase. To the CAB solution containing 1 g or 0.5 g NaF was added 0.85 g magnesium stearate dispersed in 5 mL ethyl formate with an ice-containing ultrasonic bath for 30 minutes to achieve an active polymer ratio of 1:4. Polymer solutions containing 10% and 20% polymer in total ethyl formate were prepared by dissolving 2 g and 4 g of polymer, respectively, in 15 mL of ethyl formate. NaF was dispersed into the polymer solution for 7 minutes before MS was added and the ...

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Abstract

Disclosed is a process for encapsulating a water-soluble oral care active agent by a shell comprising a hydrophobic polymer. Two routes are described, both of which involve providing a system comprising a hydrophobic polymer, a solvent selected from the group consisting of ethyl formate, ethyl acetate, methyl acetate, propyl acetate, butyl acetate, isobutyl acetate, isopropyl acetate, isoamyl acetate, and mixtures thereof, an oral care active agent, and an oily liquid such as liquid paraffin. In the first route one first has separate phases (viz. the O / O emulsion) from which one allows precipitation by solvent removal. In the other route, the separate phases are created so as to trigger precipitation. In both routes a temperature rise takes place so as to force solvent removal, resulting in solidification.

Description

technical field [0001] The present invention relates to a method of encapsulating water-soluble oral care actives. In particular, the present invention relates to formulations for the controlled release of water-soluble oral care actives in the mouth. Background technique [0002] The human oral cavity, especially the teeth and gums, often require oral care actives for applications such as tooth whitening, dental health, gum health, and bad breath. Consider, for example, antiplaque agents, antitartar agents, antigingivitis agents, antibacterial agents, bleaching agents, and the like. [0003] Such agents are typically administered from toothpastes and / or mouth rinses. Due to the typical environment of the oral cavity, such as the presence of saliva, a standard difficulty in the art is that active agents from toothpastes and mouth rinses will rapidly decrease in concentration after their application. They therefore do not protect the mouth for a long time, and therefore th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/11A61K8/22A61K8/37A61K8/43A61K8/73A61K8/81A61Q11/00
CPCA61K8/11A61K8/22A61K8/37A61K8/43A61K8/731A61K8/8152A61Q11/00A61P1/02A61K8/31A61K8/42A61K8/8111A61K2800/95
Inventor F·L·楚恩鲍-玛盖亚张志兵
Owner KONINKLJIJKE PHILIPS NV
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