Development of composition and technologies of dental film with ketorolac trometamine

The report presents the results of the development of dental films with ketorolac trometamine based on the natural biodegradable polymers from the groups of sodium alginates and xanthan gums in combination with lightly crosslinked acrylic polymer carbopo

Block Copolymers of Ethylene Oxide and Propylene Oxide: Prospects for Medical and Pharmaceutical Application in Russia

Block copolymers of ethylene oxide and propylene oxide (EO/PO block copolymers) are polymeric non-ionic surfactants with a high hydrophilic–lipophilic balance also referred to as pluronics, poloxamers, or proxanols. These compounds are among the most demanded modern excipients for the production of medicines. EO/PO block copolymers are used both in the production of traditional (liquid, semi-solid, and solid) dosage forms and as part of targeted delivery systems. The extensive application of EO/PO block copolymers is due to the diverse array of their properties, including not only solubilising, emulsifying, gelling, and other effects but also thermoreversibility, which is essential for developing in situ delivery systems and 3D printing technologies.The aim of the study was to evaluate the potential of EO/PO block copolymers for medicinal use and to assess the range of medicinal products approved in the Russian Federation that contain EO/PO block copolymers.This review presents an analysis of the register of poloxamer-containing medicines approved in the Russian Federation, a list of the largest manufacturers of EO/PO block copolymers in the world, and a study of the possibility to use copolymers for medical purposes. Currently, there are more than 10 chemical manufacturers producing EO/PO block copolymers for the pharmaceutical, biotechnology, and other industries around the world. EO/PO block copolymers are included in more than 60 medicinal products present in the Russian pharmaceutical market; this observation indicates the need to phase out the import of poloxamers

STUDY OF THE MATRIX STRUCTURE INFLUENCE ON THE RHEOLOGICAL CHARACTERISTICS OF NIMESULIDE ORAL GEL EXPERIMENTAL SAMPLES

The article presents the results of the studying rheological characteristics of nimesulide oral gel experimental samples on the basis of the combined matrix. We have investigated influence of rheological properties of the nimesulide release from oral gels. We have established a gel with optimal rheological and biopharmaceutical characteristics

THE DETERMINATION OF THE RHEOLOGICAL OPTIMUM OF OPHTHALMIC GELS. MODERN ASPECTS OF THE OPHTHALMIC DOSAGE FORMS DEVELOPMENT

The article describes the main requirements for ophthalmic gels and presents the study of the rheological properties of ophthalmic gels, registered in the Russian Federation: Korneregel®, Solcoseryl®, Vidisic®, Ophtagel®, Oftan-Timogel®, Systein gel®. The parameters of rheological measurements conducted for ophthalmic gels are substantiated. On the basis of the results obtained, optimum rheological characteristics are suggested, which can be recommended for use in the development of ophthalmic gels

JUSTIFICATION OF THE RHEOLOGICAL OPTIMUM IN THE DEVELOPMENT OF SEMISOLID FORMS. DENTAL GELS

The article presents the results of studying the rheological characteristics of dental preparations in the form of gels registered in the Russian Federation: Dentamet®, Kamistad®, Calgel®, Metragyl-Denta® and Holisal®. The parameters of rheological measurements conducted for dental soft medicinal forms are substantiated. On the basis of the results obtained, optimum rheological characteristics are suggested, which can be recommended for use in the development of dental gels

THE DETERMINATION OF RHEOLOGICAL OPTIMUM OF VAGINAL GELS

The article presents the results of rheological properties study of vaginal gels, registered in the Russian Federation. Was justified the optimal rheological characteristics, which can be recommended for use to the pharmaceutical development of vaginal gels. It is advisable to use the rheological optimum to select the type of packaging and method of dosing of vaginal gels according to their rheological characteristics

Technologic Considerations of Creation Dosage Form of Original Substance 3,7-diazabicyclo[3.3.1]nonane

Introduction. An innovative pharmaceutical substance based on the 3,7-diazabicyclo[3.3.1]nonane derivative provides long-term activation of AMPA receptors and the production of neurotrophic factors, which makes it possible to use it for the treatment of cognitive impairments and rehabilitation of patients who have undergone acute brain hypoxia. Given that this substance is able to be absorbed through the walls of the gastrointestinal tract and pass through the blood-brain barrier, there are no restrictions on the development of an oral dosage form. In addition, the oral dosage form has significant advantages when used in geriatric and pediatric practice.Aim. The aim of the work was to carry out a comparative study of the possibility of using gelatin and hypromellose capsules for the development of the composition and technology for obtaining a dosage form containing a pharmaceutical substance based on a 3,7-diazabicyclo[3.3.1]nonane derivative.Materials and methods. The study of the «Dissolution» test of gelatinous and hypromellose capsules was carried out on an ERWEKA DT 720 «Paddle stirrer» apparatus at a stirrer rotation speed of 50 rpm in three media: pH 1.2, pH 4.5 and pH 6.8. The content of the substance in each sample was determined by high performance liquid chromatography with UV detection.Results and discussion. The results of the development and testing of capsules containing an original pharmaceutical substance of nootropic action based on a derivative of 3,7-diazabicyclo[3.3.1]nonane, which has low pharmaceutical and technological characteristics and is practically insoluble in water, are presented. The D/S value was ≥250.00 ml in each physiological pH range. The results of determining the dissolution of the developed dosage form in three media at pH values of 1.2, 4.5 and 6.8 showed a positive effect of the technology used on the solubility of the substance.Conclusion. A significant increase in the solubility of the practically insoluble substance of the 3,7-diazabicyclo[3.3.1]nonane derivative in the developed dosage form was shown, which is the result of the use of a well-founded complex of excipients and the technology of moisture-activated granulation. According to the results obtained, (77.60 ± 2.50) % of the substance passes into the dissolution medium with a pH of 4.5 in 45 minutes. The research results are used to develop a technological scheme for obtaining a finished dosage form, its indicators and quality standards

Development of Thermoreversible Dental Gel with Berberine

Introduction. Dental gel is one of the modern dosage forms with optimal biopharmaceutical properties for the treatment and prevention of oral diseases An isoquinoline alkaloid berberine is the promising active substance with antibacterial and anti-inflammatory effect, capable of forming stable dispersed systems with gel-forming components. It is noteworthy that, despite the pronounced antimicrobial activity of the alkaloid berberine, there is currently no dental dosage form with this component on the pharmaceutical market, and therefore research in this direction is of great interest.Aim. Selection of the optimal technology for obtaining dental gel with berberine for the treatment of oral diseases.Materials and methods. Berberine bisulfate (manufactured by CJSC «Vifitech», Obolensk, Moscow region, RF), poloxamers P407 and P338 (EP, USP/N; BASF, Germany), propylene glycol (USP; BASF, Germany), sodium chloride (Sigma-Aldrich, Germany, Cat. No. S9888), mucin type II from a pig stomach (Sigma-Aldrich, Germany, Cat. No. M2378). In the development of the composition and technology for the preparation of gels, a magnetic stirrer with a temperature control function (C-MAG HS 7 from IKA, Germany) was used. Gels were prepared by the «hot method» and «cold method».Results and discussion. The production of the gel by the «hot method» provided a uniform dosage form. The obtained pH value is within the range of optimal diapason. Measurement of the specific peel force of the model gel sample showed pronounced mucoadhesive properties, which indicates that there is no need to adjust this parameter by introducing additional components into the formulation. The spectroscopic method is applicable for the analysis of berberine gel. It has been found that a significant dilution of the reference substance sample is required to develop an identification procedure.Conclusion. The production of a sample of the dosage form by the «hot method» is optimal, which is probably due to the effect of solubilization and better distribution of the active substance in the base

THE STUDY OF THE OSMOTIC ACTIVITY OF OPHTALMIC GELS

Studies of the osmotic activity of emoxypine and dalargine ophthalmic experimental gels samples based on various polymers and also studies of some marketed in Russia ophthalmic gels are presented in the article. Selection of the most promising for further study emoxypine and dalargine experimental gel compositions was based on the comparative study of Vidisic®, Solcoseryl®, Corneregel®, Oftagel® ophthalmic gels as well as 0,9% sodium chloride solution used as the standard of osmolality. Optimal values of osmotic activity have an experimental sample of an emoxypine ophthalmic gel containing Natrosol™ 250HHX at a concentration of 1%, as well as Oftagel® and Solcoseryl® gels