tacrolimus topical preparation
A technology for tacrolimus and external preparations, which is applied in the field of external preparations and can solve problems such as inapplicability of ointments
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Embodiment 1
[0043] formula:
[0044]
[0045] Preparation:
[0046] Weigh the prescribed amount of beeswax and white petroleum jelly into the emulsification tank, heat and melt at 70°C and keep warm at 65±5°C for later use;
[0047] Weigh the prescribed amount of glycerol triacrylate (propylene carbonate / triacetin) and place it in the liquid preparation container, add the prescribed amount of tacrolimus and stir until completely dissolved;
[0048] Add the raw material solution into the emulsification tank, and rinse the dosing container with part of the light liquid paraffin, add it into the emulsification tank together with the remaining light liquid paraffin, and stir evenly;
[0049] Turn on the homogenizer, and homogenize the milk at a speed of 3500rpm for 60-90 minutes, then cool down slowly, and continue stirring until the temperature drops to 30±2°C;
[0050] Composite hoses are used for filling and sealing, and the filling temperature is controlled at 30±5°C.
[0051] In ad...
Embodiment 2
[0067] Example 2 Anhydrous gel (water-soluble gel)
[0068] 1.02 g of tacrolimus hydrate was dissolved in 3 g of glycerol triacrylate under heating, and polyethylene glycol 400 (85.98 g) and polyethylene glycol 4000 (10 g) were added thereto. The mixture was further heated for mixing and then cooled to provide an anhydrous gel. (Here and hereinafter, % refers to percentage by weight)
[0069] In addition, glyceryl triacetate (Comparative Example 2) was used as a substitute for glyceryl triacrylate to provide another ointment (Reference Control).
[0070] stability test
[0071]The example and control ointments were stored at 3°C or 36°C for 10 days. Then, changes in appearance were observed and the amounts of tautomers (decomposition products of tacrolimus) and other related substances were determined.
[0072] Table 4 Stability test results
[0073]
[0074] The results showed that compared with the control containing propylene carbonate and glyceryl triacetate, the...
Embodiment 3
[0075] Example 3 Hydrogel
[0076] 0.15g methyl p-hydroxybenzoate and 0.1g propyl p-hydroxybenzoate are dissolved in purified water under heating, after cooling to 40°C or lower, 10g glycerin, 0.5g citric acid (or acetic acid (Example 3- 2) or phosphoric acid (Example 3-3)) and Carbopol 980 (0.5g) were dissolved. 1.02 g of tacrolimus hydrate was dissolved in 20 g of glycerol triacrylate under heating, and added to the solution, and dispersed with a stirrer. Aqueous sodium hydroxide solution was added dropwise with stirring to adjust the pH to pH 4 to 7 to form a gel. Purified water was added to adjust the total amount to 100 g to provide a hydrogel. And, a lotion can be prepared by using 0.1 g to 0.2 g of Carbopol 980.
[0077] In addition, glyceryl triacetate (Comparative Example 3) was used as a substitute for glyceryl triacrylate to provide another ointment (Reference Control).
[0078] stability test
[0079] The example and control ointments were stored at 3°C or 3...
PUM
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