Microcapsules With Polymeric Coating Comprising A Lipid And An Active Agent
A polymer coating, microcapsule technology, used in the treatment of diarrhea or the prevention of colon cancer, the treatment or prevention of colon diseases, can solve the problem of dependence, butyric acid dose is difficult to determine and so on
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Embodiment 1
[0283] Example 1. General Procedure A for the Preparation of Microcapsules
[0284] a) Preparation of oil phase and determination of optimum oil phase composition
[0285] The oil phase was prepared by mixing lipids with tributyrin and heating the mixture to 60°C to melt the corresponding lipids if the lipids are solid at room temperature. Subsequently, lecithin is optionally added and dissolved during stirring with a spoon, wherein the mixture is heated to 60° C. if necessary to dissolve the lecithin. For the preparation of microcapsules, the oil phase was used without cooling at 60°C.
[0286] b) Preparation of the aqueous phase
[0287] currently using T25 Slowly add pectin powder to hot water preheated to above 90°C using a water heater while stirring at maximum speed. The mixing is carried out until the mixture is homogeneous. The homogeneous solution was then placed on a hot plate (150° C.), heated to boiling temperature and boiled for 5 minutes, wherein the mixtur...
Embodiment 2
[0299] Embodiment 2: Determination of the optimum oil phase composition
[0300] The oil phase was prepared following general procedure A, where X amount of lipid L was mixed with Y amount of liquid tributyrin. In order to achieve physical entrapment of tributyrin within the solid oil phase, it is desirable to obtain the solid oil phase at ambient temperature.
[0301] To identify suitable oil phase compositions, the prepared oil phases of different compositions were cooled to ambient temperature and their physical states were recorded, as summarized in Table 1.
[0302] Table 1 shows that when tributyrin was mixed with sunflower oil, solidification of the oil phase could not be obtained in the concentration range studied. However, when solid hydrogenated coconut kernel oil (Witocan 42 / 44) was mixed with tributyrin, solidification of the oil phase was achieved after cooling at 19% Witocan and higher concentrations.
Embodiment 3
[0303] Example 3. Determination of the optimum amount of lipid in microcapsules
[0304] For handling, it is desirable to obtain non-tacky, free-flowing microcapsules exhibiting efficient entrapment of the tributyrin-containing oil phase (ideally without oil leakage).
[0305] Microcapsules with different lipid contents having compositions according to entries 1 to 11 in Table 2 were prepared following general procedure A. Drying was performed at 30°C. The average diameter of the microcapsules is 1.3 mm. The dried microcapsules were visually inspected for free-flowing properties and possible oil leakage from the microcapsules. As can be deduced from the results summarized in Table 2, specifically, microcapsules with a pectin concentration of around 4% in the emulsion and a lipid phase content of around 4% to 5% in the emulsion proved to be stable in their free-flowing The properties, ie their non-adhesive aspect, are particularly advantageous. Furthermore, they showed no l...
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