Ekaterinburg, Ekaterinburg, Russian Federation
Nearly 40% of novel chemical entities show evidence of low solubility in water and low bioavailability. Self-emulsifying formulations have showed the power to improve the bioavailability of hydrophobic drugs. Self-emulsifying formulations belong to lipid formulations, and their size range from 100 nm in case of self-emulsifying drug delivery systems and less than 50 nm in case of self-microemulsifying drug delivery systems. In general self-emulsifying formulations s represent isotropic mixtures of oils, surfactants and co-surfactants, which emulsify spontaneous in aqueous media under conditions of gentle stirring. Usually self-emulsifying formulations presented liquids, which fill the soft gelatinous capsules. However, the dosage form has drawbacks, especially in the production process. In this regard, the use of the methodology of solidification of liquid or semi-solid components of self-emulsifying formulations and their transformation into powders for the preparation of solid dosage forms is relevant. This paper summarizes the main features, a classification of lipid forms, auxiliary substances for the preparation of self-emulsifying formulations, techniques of solidification, the phases of the development of self-emulsifying formulations, evaluation of parameters of quality of liquid and solid self-emulsifying formulations, approaches to development of medicinal forms on the basis of the self-emulsifying formulations, as well as an overview of the drugs, presented on the market in the form of self-emulsifying formulations.
self-emulsifying formulations, self-emulsifying drug delivery system, self-microemulsifying drug delivery system.
Большинство новых химических соединений (около 40%) имеют низкую растворимость в воде и, как следствие, низкую биодоступность. Самоэмульгирующиеся композиции (self-emulsifying formulations – SELF) – это класс липидных систем доставки лекарственных веществ (ЛВ), включающих масло, одно или более поверхностно-активное вещество (ПАВ) и косурфактант, которые спонтанно эмульгируются до образования эмульсии или микроэмульсии типа масло-в-воде при слабом перемешивании в среде желудочно-кишечного тракта (ЖКТ). Данные системы показали большую перспективу в увеличении растворимости и биодоступности плохорастворимых в воде ЛВ [7].
При разработке любой лекарственной формы (ЛФ) ЛВ, а особенно для форм, включающих функциональные вспомогательные вещества (ВВ), важно иметь представление о физико-химических и биофармацевтических свойствах ЛВ. В случае липидных систем доставки ЛВ, выбор липидных ВВ и типа системы доставки ЛВ во многом определяется свойствами ЛВ.
Чтобы охарактеризовать и оценить липидные системы доставки ЛВ, в 2000 г. профессор C. Pouton опубликовал Классификационную систему липидных форм (Lipid Formulation Classification System), представленную в табл. 1 [2].
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