Percutaneous delivery system for nicotinamide transdermal therapeutic system

E. G. Kuznetsova, V. A. Ryzhikova, L. A. Salomatina, O. M. Kuryleva, V. Sevastianov
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Abstract

Recently, antioxidants, one of which is nicotinamide, have often been used in the treatment of a number of chronic cardiovascular, autoimmune, skin diseases, and diabetes mellitus. Taking into account the frequent and long-term use of nicotinamide, it seems appropriate to the authors to create a new dosage form of a transdermal therapeutic system (TTS) capable of maintaining the required level of the drug concentration in the blood for a long time. The aim of the work was to develop and to study the functional properties of a system for percutaneous delivery of nicotinamide in vitro. Four compositions of the percutaneous delivery emulsion system for the nicotinamide TTS were suggested, in which the amount of the percutaneous carrier of sodium docusate was varied. Studies of the diffusion of nicotinamide in vitro through unconserved rabbit skin have shown that an increase in the concentration of sodium docusate by three times (from 3.3 % to 9.8 %) significantly increases the amount of the diffused drug substance by 15% and decreases the amount of nicotinamide remaining in the TTS. The amount of the antioxidant founded in the skin flap was lower than the therapeutic dose (~ 1.46 % of its initial amount in TTS) 24 hours after the start of the in vitro experiment. It indicates the absence of a possible aftereffect of nicotinamide TTS in its clinical use after detaching from the patient’s skin.
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用于烟酰胺透皮治疗系统的经皮给药系统
近年来,抗氧化剂(其中之一是烟酰胺)已被广泛用于治疗多种慢性心血管疾病、自身免疫性疾病、皮肤病和糖尿病。考虑到烟酰胺的频繁和长期使用,作者似乎应该创建一种新的透皮治疗系统(TTS)剂型,能够长时间维持血液中所需的药物浓度水平。本研究的目的是开发和研究经皮烟酰胺体外给药系统的功能特性。提出了烟酰胺TTS经皮给药乳剂体系的四种组成,其中docusate钠的经皮载体量不同。烟酰胺在体外通过未保存的兔皮肤扩散的研究表明,将docusate钠的浓度增加三倍(从3.3%增加到9.8%),可使扩散的原料药的量显著增加15%,并减少残留在TTS中的烟酰胺的量。体外实验开始24小时后,皮瓣中抗氧化剂的含量低于治疗剂量(约为TTS初始量的1.46%)。这表明烟酰胺TTS在临床使用中从患者皮肤分离后没有可能的后遗症。
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