A kind of acyclovir hydrocortisone cream and preparation method thereof

Abstract

The invention relates to the technical field of medicinal preparations, and in particular relates to acyclovir hydrocortisone cream and a preparation method thereof. The acyclovir hydrocortisone cream comprises acyclovir, hydrocortisone, an oil-phase matrix, an emulsifier, a co-solvent, an acid-alkaline buffer system, a humectant and water, wherein the oil-phase matrix is a mixture consisting of liquid paraffin, cetostearyl alcohol and albolene; the co-solvent is poloxamer, and the acid-alkaline buffer system is a citric acid-sodium hydroxide system. By improving the formula and combining the improvement of the preparation process, the acyclovir hydrocortisone can be uniformly dispersed in the cream matrix in a tiny crystal manner, so that the cream has the advantage of simple preparation method, the industrial production is facilitated, and the stability of the prepared cream is better.

Description

Technical field

[0001] The invention relates to the technical field of compound pharmaceutical preparations, in particular to a aciclovir hydrocortisone cream and a preparation method thereof. Background technique

[0002] Acyclovir is a synthetic purine nucleoside analog that inhibits herpes simplex type 1 (HSV-1), type 2 (HSV-2) and varicella-zoster virus (VZV) in vivo and in vitro effect. Cell culture results show that the activity against herpes simplex virus type I (HSV-1) and type II (HSV-2) is the strongest: against varicella-zoster virus (VZV) and African lymphoma virus (EBV) second; against giant Cellular virus (CMV) has a weak effect and has drug resistance, and has a certain effect on hepatitis B virus (HBV). After this product enters herpes virus-infected cells, it competes with deoxynucleosides for viral thymidine kinase or cellular kinase, and the drug is phosphorylated into activated acyclovir triphosphate, and then inhibits virus replication in two ways: ①Interf...

Examples

Embodiment 1

[0044] A kind of acyclovir hydrocortisone cream, its raw material formula is as follows:

[0045] Acyclovir 5.0%

[0046] Hydrocortisone 1.0wt%

[0047] Poloxamer 188 1wt%

[0048] Citric acid 0.75wt%

[0049] Sodium hydroxide 0.25wt%

[0050] Cetearyl alcohol 12wt%

[0051] White Vaseline 7.5wt%

[0052] Liquid paraffin 7.5wt%

[0053] Sodium lauryl sulfate 1wt%

[0054] Propylene glycol 20wt%

[0055] Purified water balance

[0056] The steps of the method for preparing acyclovir hydrocortisone cream from the raw materials of the above formula are as follows:

[0057] (1) Weigh the oil phase components cetearyl alcohol, white petrolatum and liquid paraffin respectively according to the raw material formula, and heat to 75-80°C and mix to obtain the oil phase.

[0058] (2) Dissolve sodium hydroxide, poloxamer 188 and sodium lauryl sulfate in purified water, heat to 75-80°C, and then add acyclovir to dissolve to obtain an aqueous phase.

[0059] (3) Add the water phase to the oil phase, stir and ...

Embodiment 2

[0064] A kind of acyclovir hydrocortisone cream, its raw material formula is as follows:

[0065] Acyclovir 5.0%

[0066] Hydrocortisone 1.0wt%

[0067] Poloxamer 188 0.5wt%

[0068] Citric acid 0.3wt%

[0069] Sodium hydroxide 0.1wt%

[0070] Cetearyl alcohol 8wt%

[0071] White Vaseline 5wt%

[0072] Liquid paraffin 5wt%

[0073] Sodium lauryl sulfate 0.5wt%

[0074] Propylene glycol 10wt%

[0075] Purified water balance

[0076] The preparation method is the same as in Example 1.

[0077] The prepared cream is milky white, pH 5.2, microscopic observation, the bulk drug crystals are less than 20 μm, evenly dispersed in the cream matrix; the particle size of the emulsion droplets are all less than 8 μm, centrifuged at 3000 rpm for 30 minutes, without layering or breaking.

Embodiment 3

[0079] A kind of acyclovir hydrocortisone cream, its raw material formula is as follows:

[0080] Acyclovir 5.0wt%

[0081] Hydrocortisone 1.0wt%

[0082] Poloxamer 188 2wt%

[0083] Citrate 3wt%

[0084] Sodium hydroxide 1wt%

[0085] Cetearyl alcohol 16wt%

[0086] White Vaseline 10wt%

[0087] Liquid paraffin 10wt%

[0088] Sodium lauryl sulfate 2wt%

[0089] Propylene glycol 10wt%

[0090] Purified water balance

[0091] The preparation method is the same as in Example 1.

[0092] The prepared cream is milky white, pH 5.1, microscopic observation, the bulk drug crystals are less than 20 μm, evenly dispersed in the cream matrix; the particle size of the emulsion droplets are all less than 8 μm, centrifuged at 3000 rpm for 30 minutes, without layering or breaking.

Technical field

[0001] The invention relates to the technical field of compound pharmaceutical preparations, in particular to a aciclovir hydrocortisone cream and a preparation method thereof. Background technique

[0002] Acyclovir is a synthetic purine nucleoside analog that inhibits herpes simplex type 1 (HSV-1), type 2 (HSV-2) and varicella-zoster virus (VZV) in vivo and in vitro effect. Cell culture results show that the activity against herpes simplex virus type I (HSV-1) and type II (HSV-2) is the strongest: against varicella-zoster virus (VZV) and African lymphoma virus (EBV) second; against giant Cellular virus (CMV) has a weak effect and has drug resistance, and has a certain effect on hepatitis B virus (HBV). After this product enters herpes virus-infected cells, it competes with deoxynucleosides for viral thymidine kinase or cellular kinase, and the drug is phosphorylated into activated acyclovir triphosphate, and then inhibits virus replication in two ways: ①Interf...

Examples

Embodiment 1

[0044] A kind of acyclovir hydrocortisone cream, its raw material formula is as follows:

[0045] Acyclovir 5.0%

[0046] Hydrocortisone 1.0wt%

[0047] Poloxamer 188 1wt%

[0048] Citric acid 0.75wt%

[0049] Sodium hydroxide 0.25wt%

[0050] Cetearyl alcohol 12wt%

[0051] White Vaseline 7.5wt%

[0052] Liquid paraffin 7.5wt%

[0053] Sodium lauryl sulfate 1wt%

[0054] Propylene glycol 20wt%

[0055] Purified water balance

[0056] The steps of the method for preparing acyclovir hydrocortisone cream from the raw materials of the above formula are as follows:

[0057] (1) Weigh the oil phase components cetearyl alcohol, white petrolatum and liquid paraffin respectively according to the raw material formula, and heat to 75-80°C and mix to obtain the oil phase.

[0058] (2) Dissolve sodium hydroxide, poloxamer 188 and sodium lauryl sulfate in purified water, heat to 75-80°C, and then add acyclovir to dissolve to obtain an aqueous phase.

[0059] (3) Add the water phase to the oil phase, stir and ...

Embodiment 2

[0064] A kind of acyclovir hydrocortisone cream, its raw material formula is as follows:

[0065] Acyclovir 5.0%

[0066] Hydrocortisone 1.0wt%

[0067] Poloxamer 188 0.5wt%

[0068] Citric acid 0.3wt%

[0069] Sodium hydroxide 0.1wt%

[0070] Cetearyl alcohol 8wt%

[0071] White Vaseline 5wt%

[0072] Liquid paraffin 5wt%

[0073] Sodium lauryl sulfate 0.5wt%

[0074] Propylene glycol 10wt%

[0075] Purified water balance

[0076] The preparation method is the same as in Example 1.

[0077] The prepared cream is milky white, pH 5.2, microscopic observation, the bulk drug crystals are less than 20 μm, evenly dispersed in the cream matrix; the particle size of the emulsion droplets are all less than 8 μm, centrifuged at 3000 rpm for 30 minutes, without layering or breaking.

Embodiment 3

[0079] A kind of acyclovir hydrocortisone cream, its raw material formula is as follows:

[0080] Acyclovir 5.0wt%

[0081] Hydrocortisone 1.0wt%

[0082] Poloxamer 188 2wt%

[0083] Citrate 3wt%

[0084] Sodium hydroxide 1wt%

[0085] Cetearyl alcohol 16wt%

[0086] White Vaseline 10wt%

[0087] Liquid paraffin 10wt%

[0088] Sodium lauryl sulfate 2wt%

[0089] Propylene glycol 10wt%

[0090] Purified water balance

[0091] The preparation method is the same as in Example 1.

[0092] The prepared cream is milky white, pH 5.1, microscopic observation, the bulk drug crystals are less than 20 μm, evenly dispersed in the cream matrix; the particle size of the emulsion droplets are all less than 8 μm, centrifuged at 3000 rpm for 30 minutes, without layering or breaking.

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