Optimization of the Composition of the Ointment with Phytoecdysteroids Serpisten

Abstract

Introduction. Phytoecdysteroids are a group of natural compounds related in structure and physiological effect to ecdysone - the hormone of insect molting. Phytoecdisteroids have been found to have an antiflammatory effect, which suggests that they have regenerative properties. The development of a soft dosage form containing phytoecdysteroids is of interest.Aim. Improvement of ointment compositions with phytoecdysteroids by optimizing the composition of base adjuvants.Materials and methods. As an active substance was used Serpisten, containing the sum of phytoecdysteroids, the main of which is 20-hydroxyecdysone and obtained from the leaves of Serratulaecoronatae. Raw materials "Serpukhi crowned leaves" were registered by the Federal Service Rospotrebnadzor (Moscow) for the production of dietary supplements (Gr. No. 77.99.23.3.U.1922.3.08), substance Serpisten (Gr. No. 77.99.23.3.U.1923.3.08. TU 9369-002-15092611-2008). In work were used the excipients allowed for medical use: the monoglycerides distilled, T-2 emulsifier, tween 80, sodium - carboxymethylcellulose, polyvinyl alcohol, hydroxide of aluminum, aero forces, vaseline, oil vaseline, sunflower oil. Optimization of ointment auxiliary substances composition was carried out according to the Greco-Latin 4 x 4 square plan with repeated observations. The concentration of hydrogen ions from aqueous ointments was evaluated as process parameters; acid number; release of serpistene from ointment into agar gel, thermal stability of structure. The structural and mechanical properties of the optimal composition ointment composition were determined on a RV type REOTEST 2.1 rotary viscometer (RHEOTEST Medingen GmbH, Germany). Ointment Bepanten (GP Grenzach Produktions GmbH, Germany) was used as a comparison preparation.Results and discussion. During optimization of the composition of the diphilic ointment with serpistene, was found that the ratio of hydrophobic and hydrophilic phases should be 1 : 1, it is advisable to introduce into the ointment base an emulsifier T-2, aerosil and a mixture of vaseline and vaseline oil in the proportion of 1 : 1. As a result of the carried out studies on the optimization of ointment compositions, the following serpisten ointment composition is proposed: serpisten - 0.02; emulsifier T-2 - 3.0; aerosil - 3.0; vaseline - 23.0; vaseline oil - 23.0; ethyl alcohol 40 % - 1 ml; purified water to 100.0. Comparative analysis of effective viscosity showed that the proposed composition is as close as possible to the Bepanten ointment.Conclusion. A set of technological studies was carried out to optimize the composition of the Serpisten, 0.02 % ointment on a diphilic basis. The developed composition and technology made it possible to obtain a composition with thermal stability, bring the hydrogen index of the ointment closer to the pH of human skin and achieve the parameters included in the rheological optimum for dermatological ointments (0.34-108 Pa • s).

Keywords

• ointment
• phytoecdysteroids
• excipients
• quality indicators
• rheological characteristics