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Preparation method of anti-thyroid ointment for external application

An anti-thyroid and ointment technology, applied in ointment delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Active Publication Date: 2014-10-29
陈凌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation has lower local skin adverse reactions than the preparation of Patent 1, but preclinical studies have found that the stability of glucocorticoid, one of its main ingredients, is not good, which affects the efficacy and shelf life of the preparation. In addition, more According to the clinical application of the population and a long period of time, there are still many local skin adverse reactions, which affect the patient's compliance with the treatment.

Method used

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  • Preparation method of anti-thyroid ointment for external application
  • Preparation method of anti-thyroid ointment for external application
  • Preparation method of anti-thyroid ointment for external application

Examples

Experimental program
Comparison scheme
Effect test

example 8

[0049] Example 8. This example adopts the formula of implementing 1 to prepare

[0050] (1) Put the original drug of prednisolone and 10 times (mass ratio) of povidone in 50 times (mass ratio) of ethanol, stir and dissolve on a constant temperature water bath at 60°C, evaporate the solvent, collect the solids, and dry Finally, pulverize and pass through an 80-mesh sieve to obtain prednisone-povidone solid dispersion powder.

[0051] (2) Put antithyroid drugs, preservatives, antioxidants and emulsifiers into distilled water and mix well, heat to 80°C, mix well to obtain the water phase;

[0052] (3) Heat the oil-soluble matrix and penetration enhancer to 80°C to melt, and mix well to obtain the oil phase;

[0053] (4) Pour the oil phase obtained in step (3) into the water phase obtained in step (2), heat to 80°C, and stir evenly;

[0054] (5) When the temperature drops to 40°C, add the prednisolone-povidone solid dispersion powder prepared in step (1);

[0055] (6) Stir full...

example 9

[0057] Example 9. This example adopts the formula of implementing 2 to prepare

[0058] (1) Weigh 8.0 g of β-cyclodextrin, add 100 ml of water, and heat to 61°C to make a saturated solution. Add the original drug of fluocinolone to 50 times boiling ethanol to dissolve, then slowly add it dropwise to the cyclodextrin aqueous solution which is equimolar to the drug, and stir at constant temperature for an appropriate time. Place in a -4°C refrigerator to precipitate the solid, and filter after 24 h. First wash the precipitated solid with a small amount of ethanol for 3 times, then wash with distilled water for 3 times, drain and dry at 60°C to obtain the prednisolone-β-cyclodextrin inclusion compound;

[0059] (2) Put antithyroid drugs, preservatives, antioxidants and emulsifiers into distilled water and mix well, heat to 80°C, mix well to obtain the water phase;

[0060] (3) Heat the oil-soluble matrix and penetration enhancer to 80°C to melt, and mix well to obtain the oil p...

Embodiment 10

[0065] Embodiment 10, this example adopts the formula of implementing 3 to prepare

[0066] (1) Dissolve the former drug of hydrocortisone in 30 times (mass ratio) of boiling ethanol. Then heat and melt 10 times (mass ratio) polyethylene glycol (4000) of hydrocortisone in a water bath, then mix the two liquids evenly, evaporate the solvent under constant stirring, and then transfer to an ice-water bath to cool and solidify. Move it to a desiccator, dry it in vacuum, make it embrittled, and pulverize it to obtain the hydrocortisone-polyethylene glycol solid dispersion;

[0067] (2) Put antithyroid drugs, preservatives, antioxidants and emulsifiers into distilled water and mix well, heat to 80°C, mix well to obtain the water phase;

[0068] (3) Heat the oil-soluble matrix and the penetration enhancer to 80°C to melt, and mix well to obtain the oil phase;

[0069] (4) Pour the oil phase obtained in step (3) into the water phase obtained in step (2), heat to 80°C, and stir evenl...

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Abstract

The invention relates to a preparation method of an anti-thyroid ointment for external application. The preparation method comprises the following steps: mixing glucocorticoid with a drug carrier material to make the glucocorticoid be evenly dispersed on the drug carrier material; adding an anti-thyroid drug into distilled water, evenly mixing, heating to 80 DEG C, evenly stirring so as to obtain a water phase; heating an oil-soluble substrate and a penetration promoter to a temperature of 80 DEG C so as to melt the substrate and the penetration promoter, evenly mixing the substrate and the penetration promoter so as to obtain an oil phase; pouring the oil phase into the water phase at a constant temperature of 80 DEG C, evenly stirring; adding a glucocorticoid component when the temperature is cooled to 40 DEG C; and finally stirring and cooling so as to obtain an ointment. The drug stability and solubility are improved, and the drug quality, curative effect, and service life are guaranteed and enhanced. The skin adverse reactions are reduced, the patients' paints are prominently reduced, the patients' compliance of drug application is improved, and thus the effect on treating hyperthyroidism is improved. The preparation is stable and safer, has a better curative effect, and is benefit for large-scale promotion and application.

Description

technical field [0001] The invention belongs to the field of antithyroid ointment drugs for external application, in particular to a preparation method of antithyroid ointment for external application. Background technique [0002] Hyperthyroidism (hereinafter referred to as hyperthyroidism) is a common disease. Over the past seventy years, oral imidazole and thiourea antithyroid drugs (hereinafter referred to as oral antithyroid drugs) have been the first choice and main treatment method for hyperthyroidism. This method is slow to control hyperthyroidism, the curative effect is not stable enough, some systemic adverse reactions may occur, and the remission rate after drug withdrawal is low. For this reason, in 1993, Chen Ling et al. developed and applied for the invention patent "anti-thyroid cream for external application", which was authorized, and its patent number is ZL93111370.9. The patent discloses an oil-in-water cream containing antithyroid drugs and glucocorticoi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/06A61K47/22A61K47/14A61K47/12A61K47/34A61P5/16
CPCA61K45/06A61K47/22A61K9/06A61K47/12A61K47/26A61K47/14A61K47/20A61K47/44A61K31/58A61K31/573A61K31/4164A61K31/513A61P43/00A61P5/16A61K2300/00A61K47/30A61K31/4172A61K31/56A61K47/10A61K47/34
Inventor 陈凌
Owner 陈凌
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