Desloratadine external preparation and preparation method thereof

Abstract

The invention relates to a desloratadine external preparation and a preparation method thereof. The external preparation takes desloratadine as a main drug and is used for treating allergic skin inflammation. The desloratadine external preparation can increase the concentration of free drug in skin local tissues of the part with the allergic skin inflammation of a body through percutaneous absorption, have an effective histamine sensitization antagonism role, better play local antianaphylaxis and anti-inflammation efficacies and reduce adverse reactions. The external formulation does not pass through the gastrointestinal tract, thereby avoiding the first pass effect and reduce the probability of occurrence of adverse reactions. The external preparation can be directly applied at the affected side, and the onset of action is rapid. Furthermore, the dose and the coverage area of the external preparation can be selected according to the area and the severity of the affected site, and the external preparation is convenient to use and convenient to carry.

Description

Technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a desloratadine external preparation and a preparation method thereof. Background technique

[0002] Desloratadine is a non-sedative long-acting tricyclic antihistamine and the active metabolite of loratadine. It can selectively block peripheral H1 receptors and inhibit various allergic inflammations. The release of chemical mediators, such as inhibiting the release of histamine, prostaglandins, and leukocyte mediators from mast cells and basophils, to relieve symptoms related to allergic rhinitis or chronic idiopathic urticaria.

[0003] At present, the dosage forms of desloratadine on the market are mainly oral dosage forms such as tablets, dispersible tablets, and syrups. When these oral dosage forms are taken orally, the gastrointestinal tract will have a first-pass effect on the drug, and the metabolic effects of food and gastric emptying on the drug. Moreover, the oral...

Examples

Embodiment 1

[0024] Example 1: The following prescription was used to prepare desloratadine ointment:

[0025] Magnesium stearate 9.7g white petrolatum 4.8g

[0026] Liquid paraffin 7.3g glyceryl monostearate 4.8g

[0027] Tween-80 1.4g Azone 0.9g

[0028] Ethyl paraben 0.1g glycerin 14.6g

[0029] Sodium lauryl sulfate 0.1g desloratadine 2.4g

[0030] β-cyclodextrin 4.8g purified water 48.6g

[0031] Preparation Process:

[0032] First, add sodium lauryl sulfate and β-cyclodextrin into water, stir to dissolve, add desloratadine, stir to dissolve, add glycerin, stir and disperse uniformly to obtain an aqueous solution; heat and stir the remaining materials in a water bath at 80°C To dissolve, slowly add the water phase solution, stirring while adding, continue to heat and stir in a water bath for 4 hours after all the addition is complete, and then get desloratadine ointment after cooling.

Embodiment 2

[0033] Example 2: Preparation of desloratadine gel, the prescription is as follows:

[0034] Deloratadine 1g β-cyclodextrin 2g

[0035] Azone 1g Carbomer 1g

[0036] Liquid paraffin 2g EDTA-Na 0.05g

[0037] Isopropanol 20g PEG-400 3g

[0038] Isopropyl myristate 6g decyl oleate 6g

[0039] Purified water 61.95g

[0040] Preparation Process:

[0041] First, add β-cyclodextrin to water and stir to dissolve, then slowly add desloratadine, stirring while adding until all is dissolved to obtain desloratadine-β-cyclodextrin solution; add PEG-400, myristic acid Isopropyl ester, sunflower oleate, azone, liquid paraffin, EDTA-Na, and isopropanol are heated in a 70℃ water bath and stirred to dissolve, then add the desloratadine-β-cyclodextrin solution and stir while adding , Make it uniformly dispersed, and then add carbomer to make it swell and disperse uniformly to obtain desloratadine gel.

Embodiment 3

[0042] Example 3: The following prescription was used to prepare desloratadine ointment:

[0043] Magnesium stearate 8.1g white petrolatum 5.6g

[0044] Liquid paraffin 8.0g glyceryl monostearate 5.2g

[0045] N-methyl-pyrrolidone 1.0g

[0046] Ethyl paraben 0.1g propylene glycol 14.2g

[0047] Sodium lauryl sulfate 0.1g Deloratadine 2.8g

[0048] β-cyclodextrin 2.8g purified water 49g

[0049] Preparation Process:

[0050] First, add sodium lauryl sulfate and β-cyclodextrin into water, stir to dissolve, add desloratadine, stir to dissolve, add propylene glycol, stir and disperse uniformly to obtain an aqueous solution; heat and stir the remaining materials in a water bath at 80°C To dissolve, slowly add the water phase solution, stirring while adding, continue to heat and stir in a water bath for 4 hours after all the addition is complete, and then get desloratadine ointment after cooling.

Technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a desloratadine external preparation and a preparation method thereof. Background technique

[0002] Desloratadine is a non-sedative long-acting tricyclic antihistamine and the active metabolite of loratadine. It can selectively block peripheral H1 receptors and inhibit various allergic inflammations. The release of chemical mediators, such as inhibiting the release of histamine, prostaglandins, and leukocyte mediators from mast cells and basophils, to relieve symptoms related to allergic rhinitis or chronic idiopathic urticaria.

[0003] At present, the dosage forms of desloratadine on the market are mainly oral dosage forms such as tablets, dispersible tablets, and syrups. When these oral dosage forms are taken orally, the gastrointestinal tract will have a first-pass effect on the drug, and the metabolic effects of food and gastric emptying on the drug. Moreover, the oral...

Examples

Embodiment 1

[0024] Example 1: The following prescription was used to prepare desloratadine ointment:

[0025] Magnesium stearate 9.7g white petrolatum 4.8g

[0026] Liquid paraffin 7.3g glyceryl monostearate 4.8g

[0027] Tween-80 1.4g Azone 0.9g

[0028] Ethyl paraben 0.1g glycerin 14.6g

[0029] Sodium lauryl sulfate 0.1g desloratadine 2.4g

[0030] β-cyclodextrin 4.8g purified water 48.6g

[0031] Preparation Process:

[0032] First, add sodium lauryl sulfate and β-cyclodextrin into water, stir to dissolve, add desloratadine, stir to dissolve, add glycerin, stir and disperse uniformly to obtain an aqueous solution; heat and stir the remaining materials in a water bath at 80°C To dissolve, slowly add the water phase solution, stirring while adding, continue to heat and stir in a water bath for 4 hours after all the addition is complete, and then get desloratadine ointment after cooling.

Embodiment 2

[0033] Example 2: Preparation of desloratadine gel, the prescription is as follows:

[0034] Deloratadine 1g β-cyclodextrin 2g

[0035] Azone 1g Carbomer 1g

[0036] Liquid paraffin 2g EDTA-Na 0.05g

[0037] Isopropanol 20g PEG-400 3g

[0038] Isopropyl myristate 6g decyl oleate 6g

[0039] Purified water 61.95g

[0040] Preparation Process:

[0041] First, add β-cyclodextrin to water and stir to dissolve, then slowly add desloratadine, stirring while adding until all is dissolved to obtain desloratadine-β-cyclodextrin solution; add PEG-400, myristic acid Isopropyl ester, sunflower oleate, azone, liquid paraffin, EDTA-Na, and isopropanol are heated in a 70℃ water bath and stirred to dissolve, then add the desloratadine-β-cyclodextrin solution and stir while adding , Make it uniformly dispersed, and then add carbomer to make it swell and disperse uniformly to obtain desloratadine gel.

Embodiment 3

[0042] Example 3: The following prescription was used to prepare desloratadine ointment:

[0043] Magnesium stearate 8.1g white petrolatum 5.6g

[0044] Liquid paraffin 8.0g glyceryl monostearate 5.2g

[0045] N-methyl-pyrrolidone 1.0g

[0046] Ethyl paraben 0.1g propylene glycol 14.2g

[0047] Sodium lauryl sulfate 0.1g Deloratadine 2.8g

[0048] β-cyclodextrin 2.8g purified water 49g

[0049] Preparation Process:

[0050] First, add sodium lauryl sulfate and β-cyclodextrin into water, stir to dissolve, add desloratadine, stir to dissolve, add propylene glycol, stir and disperse uniformly to obtain an aqueous solution; heat and stir the remaining materials in a water bath at 80°C To dissolve, slowly add the water phase solution, stirring while adding, continue to heat and stir in a water bath for 4 hours after all the addition is complete, and then get desloratadine ointment after cooling.