TRANSDERMAL THERAPEUTIC SYSTEM WITH ANTIHISTAMINE EFFECT AND METHOD FOR ITS PREPARATION Russian patent published in 2024 - IPC A61K31/4545 A61K47/10 A61K47/14 A61K47/58 A61K9/70 A61P37/08 

Abstract RU 2816908 C1

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention refers to pharmacology and medicine, namely to new medicinal preparations for use in prevention of allergic diseases. Disclosed is a transdermal therapeutic system (TTS) for an antihistamine effect, obtained from a mixture containing desloratadine, methanol, polyvinylpyrrolidone, polyethylene glycol, polysorbate 80 and water with the following ratio of components, wt.%: desloratadine 0.725–0.75, methanol 12.56–15.71, polyvinylpyrrolidone 34.53–36.35, polyethylene glycol 4.545–4.773, polysorbate 80 8.645–9.1, dialyzed water – balance, while evaporating said mixture by 50% and lyophilizing it to remove methanol residues. Method of producing said TTS involves preparing an organic phase by mixing desloratadine in powder form with methanol until complete dissolution, adding a weighed portion of polyethylene glycol to the obtained solution, stirring the entire mixture for 20 minutes until complete dissolution, mixing the aqueous and organic phases to form micelles, for this, polysorbate 80 is added to the dialyzed water with constant stirring, the organic phase is added to the aqueous phase after 20 minutes at rate of 1 ml/min, mixing solution for 10 minutes, dissolving polyvinylpyrrolidone in methanol and adding the obtained solution to the aqueous-organic phase, obtained mixture is transferred to thermal vacuum drying for 2 hours until evaporation by 50%, solution is poured onto a paraffin substrate and placed in a lyophilic drying at -80 °C and pressure of 46.6 Pa for 6 hours to remove residual methanol.

EFFECT: group of inventions makes it possible to increase the antihistamine effect, reduce side effects, increase the time of maintaining a constant concentration of the preparation due to encapsulation of desloratadine in micelles.

2 cl, 2 dwg, 1 tbl, 1 ex

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RU 2 816 908 C1

Authors

Shlyapkina Vasilisa Igorevna

Kulikov Oleg Aleksandrovich

Ageev Valentin Pavlovich

Zharkov Mikhail Nikolaevich

Yakobson Denis Eduardovich

Pyataev Nikolaj Anatolevich

Dates

2024-04-08Published

2023-06-01Filed