A kind of preparation technology of desonide cream

Abstract

The invention discloses a preparation process of a desonide cream, wherein desonide is dissolved in an aqueous solution containing a surfactant to form an aqueous phase, and then the aqueous phase is emulsified with an oil phase and stirred and cooled, so that desonide crystals can be stably precipitated and uniformly dispersed in a cream matrix, with a small particle size, uniform content, high penetration rate, and good therapeutic effect. The invention has the advantages that the proportion and preparation method are reasonably designed, and the quality problems of the prior art that desonide does not crystallize after being dissolved or the crystals are too large can be effectively solved, and the content is uniform and the properties are smooth and not rough.

Description

Technical Field

[0001] The invention relates to a preparation process of desonide cream. Background Art

[0002] Desonide is a hydrophobic drug. In order to improve its bioavailability as much as possible, it needs to be dispersed in a cream in a solid form. However, in the prior art, it is difficult to disperse it evenly.

[0003] Specifically, desonide is dispersed in a cream base in solid form and needs to be added in the form of a dispersion or dissolved and then precipitated.

[0004] When the API dispersion is dispersed in the cream matrix, the main component content is extremely low and it is difficult to disperse it evenly directly; on the other hand, when dissolved in other types of solvents, it is difficult to precipitate, or the precipitated crystal particle size is too large to meet the pharmacopoeia standards or the properties are poor.

[0005] CN107260656A desonide cream and its preparation method, in which all purified water in the components is added in one step, it is impossible to precipitate desonide crystals in the preparation, and the skin penetration rate and therapeutic effect are still not ideal. Summary of the invention

[0006] The invention provides a preparation process of a desonide cream, the purpose of which is to overcome the above-mentioned shortcomings of the prior art and effectively improve the dispersion uniformity of desonide in the cream matrix.

[0007] The technical solution of the present invention is as follows: desonide is dissolved in an aqueous solution containing a surfactant to form an aqueous phase, which is emulsified with an oil phase and then stirred and cooled, so that desonide crystals can be stably precipitated and evenly dispersed in a cream matrix, with a small particle size, uniform content, high penetration rate and good therapeutic effect.

[0008] Specifically, a preparation process of desonide cream comprises:

[0009] 1) Water phase preparation:

[0010] Weigh glycerol, aluminum sulfate, calcium acetate, dextrin, methylparaben, sodium lauryl sulfate, desonide and purified water into a preparation pot, wherein the mass percentage of sodium lauryl sulfate is 2%, the mass percentage of desonide is 0.05%, and the mass percentage of purified water is 42.43-49.5%. Set the temperature of the preparation pot to 70° C. and the stirring speed to 70 rpm. Stir to dissolve. Adjust the pH of the aqueous phase to 4.8-5.2 with sodium citrate in the mass percentage as shown in the following table; cool down and control the temperature of the aqueous phase to 50° C., keep warm for later use, and obtain an aqueous phase.

[0011] 2) Oil phase preparation:

[0012] Weigh synthetic beeswax, white vaseline, light liquid paraffin and cetostearyl alcohol in a beaker, set the water bath temperature to 70°C, the stirrer speed to 500 rpm, and stir to melt; cool down, control the oil phase temperature to 50°C, keep warm for later use, and obtain the oil phase.

[0013] 3) Mixing:

[0014] Set the stirring speed of the preparation pot containing the water phase in step 1) to 70 rpm and the homogenization speed to 3000 rpm, add the oil phase in step 2), and vacuum homogenize and mix for 20 min.

[0015] 4) Cooling:

[0016] The mixture was cooled to 30-40°C with stirring, and the remaining mass percentage of purified water as shown in the following table was added to the preparation pot in step 3), and the mixture was homogenized and mixed under vacuum for 20 min; the desired desonide cream was obtained.

[0017] The invention has the advantages that the proportion and the preparation method are reasonably designed, and the quality problems of the prior art that desonide does not crystallize or the crystals are too large after being dissolved are effectively solved, and the content is uniform and the property is smooth and not rough. BRIEF DESCRIPTION OF THE DRAWINGS

[0018] Figure 1 This is a 400-fold microscope image of the desonide cream in Example 1 of the present invention.

[0019] Figure 2 This is a 400-fold microscope image of the desonide cream of Example 2 of the present invention.

[0020] Figure 3 This is a 400-fold microscope image of the desonide cream of Example 3 of the present invention.

[0021] Figure 4 It is a 400-fold microscope image of the desonide cream of Example 4 of the present invention.

[0022] Figure 5 This is a 400-fold microscope image of the desonide cream of Example 5 of the present invention.

[0023] Figure 6 It is a 400-fold microscope image of the desonide cream of Example 6 of the present invention.

[0024] Figure 7 This is a 400-fold microscope image of the desonide cream of Example 7 of the present invention.

[0025] Figure 8 This is a 400-fold microscope image of the desonide cream of Example 8 of the present invention.

[0026] Fig. 9 It is a comparison chart of the in vitro skin permeation of desonide cream of Examples 1-8 of the present invention. DETAILED DESCRIPTION

[0027] The present invention is further described in detail below with reference to examples and specific implementation methods.

[0028] Examples 1-4

[0029] A preparation process of desonide cream comprises:

[0030] 1) Water phase preparation:

[0031] Weigh glycerol, aluminum sulfate, calcium acetate, dextrin, methylparaben, sodium lauryl sulfate, desonide and part of purified water (the aqueous phase in the table below) in the following mass percentages into a preparation pot, set the temperature of the preparation pot to 70°C and the stirring speed to 70 rpm, stir to dissolve, adjust the pH of the aqueous phase to 4.8-5.2 with sodium citrate in the following mass percentages; cool down, control the temperature of the aqueous phase to 50°C, keep warm for later use, and obtain the aqueous phase.

[0032] 2) Oil phase preparation:

[0033] Weigh synthetic beeswax, white vaseline, light liquid paraffin and cetostearyl alcohol in the following mass percentages into a beaker, set the water bath temperature to 70°C and the stirrer speed to 500 rpm, and stir to melt; cool down to control the oil phase temperature to 50°C, keep warm for later use, and obtain the oil phase.

[0034] 3) Mixing:

[0035] Set the stirring speed of the preparation pot containing the water phase in step 1) to 70 rpm and the homogenization speed to 3000 rpm, add the oil phase in step 2), and vacuum homogenize and mix for 20 min.

[0036] 4) Cooling:

[0037] The mixture was cooled to 30-40°C with stirring, and the remaining purified water in the mass percentage shown in the following table was added to the preparation pot of step 3), and the mixture was homogenized and mixed under vacuum for 20 min; thus, the desonide cream was obtained.

[0038] Example 5

[0039] A preparation process of desonide cream, which is different from that of embodiments 1-4 in that all purified water in the following mass percentage is added in step 1), and desonide cream is obtained after stirring and cooling to 30-40° C. in step 4).

[0040] Example 6

[0041] A preparation process of desonide cream, which is different from that of embodiments 1-4 in that step 4) is stirred and cooled to 40-50°C.

[0042] Example 7

[0043] A preparation process of desonide cream, which is different from that of Examples 1-4 in that the desonide as a water phase preparation component in step 1) is changed to be added as an oil phase preparation component in step 2) according to the mass percentage in the following table.

[0044] Example 8

[0045] A preparation process of a desonide cream is different from that of embodiments 1-4 in that the aqueous phase preparation component desonide in step 1) is changed to step 4) after stirring and cooling to 30-40° C., and then the aqueous dispersion of desonide is prepared with the remaining purified water according to the mass percentage in the following table, and then added to the preparation pot in step 3), and vacuum homogenized and mixed for 20 min to obtain the desonide cream.

[0046]

[0047]

[0048] The content uniformity and crystallization of the desonide cream obtained in the above examples were tested, and the results are shown in the following table:

[0049]

[0050] From the above table and attached Figure 1-9 ( Fig. 9 As shown in the in vitro transdermal comparison of the above embodiments, desonide is dissolved in an aqueous phase containing 42.43-49.5% purified water. After preparation, desonide crystals can be stably precipitated and evenly dispersed in the cream matrix, with a small particle size, uniform content, high penetration rate and good therapeutic effect.

[0051] The above is only a preferred embodiment of the present invention. It should be pointed out that a person skilled in the art can make several modifications and improvements without departing from the inventive concept of the present invention, which all belong to the protection scope of the present invention.

Claims

1. A preparation process of desonide cream, characterized in that, The specific steps include: 1) Water phase preparation: Weigh 5% of glycerol, 0.09% of aluminum sulfate, 0.06% of calcium acetate, 0.03% of dextrin, 0.15% of methylparaben, 2% of sodium lauryl sulfate, 0.05% of desonide and 42.43-49.5% of purified water in a preparation pot, set the temperature of the preparation pot to 70° C. and the stirring speed to 70 rpm, stir and dissolve, and adjust the pH of the aqueous phase to 4.8-5.2 with 0.1% of sodium citrate in mass percentage, accounting for the total mass of the cream; cool down, control the temperature of the aqueous phase to 50° C., keep warm for standby use, and obtain an aqueous phase; 2) Oil phase preparation: Weigh 3.5% of synthetic beeswax, 3.5% of white vaseline, 4.3% of light liquid paraffin and 11.5% of cetostearyl alcohol in a beaker, set the water bath temperature to 70°C, the stirring speed of the stirrer to 500 rpm, stir to melt; cool down, control the oil phase temperature to 50°C, keep warm for standby use, and obtain the oil phase; 3) Mixing: Set the stirring speed of the preparation pot containing the water phase in step 1) to 70 rpm and the homogenization speed to 3000 rpm, add the oil phase in step 2), and mix homogenously under vacuum for 20 minutes; 4) Cooling: Stir and cool to 30-40°C, add the remaining purified water into the preparation pot in step 3), the amount of purified water in the entire prescription is 70.72% of the total mass of the cream by mass percentage, and mix homogenously in vacuum for 20 minutes; then the desonide cream is obtained.

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