Development of Composition and Technologies of Dental Gel of Meloxicam

BACKGROUND: Dental gels have several advantages over other oral dosage forms. Being a viscoplastic dosage form, the gel, when applied to the damaged area of the gum or mucous membrane, creates a protective film, preventing mechanical irritation, and providing a localized effect of the drug components. AIM: The aim of this work was to develop the composition and technology of the dental gel of meloxicam, the study of the main technological and consumer characteristics, as well as the local irritating effect of the dosage form. METHODS: Dental gels were prepared using purified water, alcohol, glycerol, and buckthorn oil as solvents, gelling agents used were: Hydroxyethylcellulose Natrosol® 250 HHX Pharm, Carbopol® 974P NF Polymer, and solubilizer Poloxamer 407 (Lutrol® F 127). The bioadhesive component and Noveon® Polycarbophil component were used for dental gel preparation. Aspartame was used as sweetener. Menthol and ascorbic acid were used to correct the organoleptic properties of the pharmaceutical composition. The formulated dental gel of meloxicam at a concentration of 7.5% was evaluated for organoleptic properties, pH, rheological characteristics, bioadhesive properties, and stability under the accelerated aging period. The in vivo local irritant effect was evaluated using ten rabbits by cutaneous, subcutaneous, subconjunctival administration, as well as application to the upper palate. RESULTS: Based on the results of studying technological and organoleptic properties, the optimal composition based on the Natrosol® 250 HHX hydroxyethylcellulose gelling agent, glycerol solvent, and purified water in the ratio 1/5 was selected, the composition contains Noveon® bioadhesive in an amount of 2%. The composition has good taste, pH close to pH of saliva has high bioadhesive properties, satisfactory rheological characteristics. The shelf life of the experimental series by accelerated aging was 2 years. The selected composition does not have a local irritant effect. CONCLUSION: A new dosage form of meloxicam was developed – a gel for use in dental practice

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

The state pharmacopoeia in the system of higher education

The article provides with a brief historical background for the editions of the State Pharmacopoeia. It characterizes the Russian State Pharmacopoeia of the XIII edition. It was shown that the Russian State Pharmacopoeia, being an essential part of the drug standardization system, also carries an important educational function. Guality standards and methods of analysis, systematization of knowledge, definitions and classifications regulated by the Pharmacopoeia, not only form the knowledge base, but also define the scientific veiw for future experts

Stationary Solutions for the Cahn - Hilliard Equation Coupled with Neumann Boundary Conditions

The structure of stationary states of the one-dimensional Cahn - Hilliard equation coupled with the Neumann boundary conditions has been studied. Here the free energy is given by a fourth order polynomial. The bifurcation diagram for existence and uniqueness of monotone solutions for this problem has been constructed. Namely, we find the length of the interval on which the solution monotonically increases or decreases and has one zero for some fixed values of physical parameters. Under the non-uniqueness we understand a possibility of existence of more than one monotone solutions for the same values of physical parameters.Исследована структура стационарного состояния одномерного уравнения Кана - Хилларда в сочетании с граничными условиями Неймана. Здесь свободная энергия задается полиномом четвертого порядка. Была построена диаграмма бифуркации существования и единственности монотонных решений этой задачи. А именно, найдена длина интервала, на котором решение монотонно возрастает или убывает и имеет один нуль для некоторых фиксированных значений физических параметров. Под неоднозначностью понимается возможность существования более чем одного монотонного решения для некоторых значений физических параметров

Development of a Liposomal Dosage Form Based on Hydrophobic Derivative of Indolocarbazole

Introduction. An original N-glycoside derivative of indolocarbazole LHS-1269 with a carbohydrate xylose residue was synthesized at the N.N. Blokhin Russian Cancer Research Center Ministry of Health of Russia. It is characterized by high antitumor activity against a number of transferable ascitic and solid tumors in vivo experiments. Due to the hydrophobic properties of the substance LHS-1269, a method of solubilization by encapsulation in phospholipid vesicles - liposomes is proposed for creating an injectable dosage form.Aim. Development of the composition of a model of a liposomal dosage form for injection of an indolocarbazole derivative LHS-1269.Materials and methods. Substance LHS-1269 (N.N. Blokhin Russian Cancer Research Center Ministry of Health of Russia), egg phosphatidylcholine (PC, E PC S, Lipoid, Germany), cholesterol >99 % (Sigma-Aldrich, Japan), polyethylene glycol-2000-distearoylphosphatidylethanolamine (PEG-PE, Lipoid, Germany). To prepare phospholipid vesicles, the method of lipid film hydration with subsequent filtration and extrusion was used. The obtained liposomes were analyzed using the method of spectrophotometry, laser scattering spectroscopy, the method of determining the electrophoretic mobility of particles, and viscometry.Results and discussion. On the basis of lipid components and active substance in various molar ratios, compositions were made and experimental models of liposomal dispersion were obtained. The compositions were evaluated based on the effectiveness of LHS-1269 incorporation into liposomes and physical and chemical parameters - dispersion viscosity, vesicle size distribution, and zeta-potential. As a result of the analysis of 7 studied compositions, the optimal molar ratios of the drug form components - LHS-1269/PC 1:160 and PC/cholesterol/PEG-PE 1:0.33:0.003 were determined. The use of this composition allows us to obtain relatively stable (zeta-potential -33 mV) homogeneous liposomes with a diameter of 190 nm with a maximum level of encapsulation of the active substance of 98 %.Conclusions. As a result of technological and chemical-pharmaceutical research, the composition of a model of a liposomal dosage form for injection of the indolocarbazole derivative LHS-1269 has been developed

THE THE INFLUENCE OF THE EXCIPIENTS ON THE ANTI-INFLAMMATORY EMULGEL BIOPHARMACEUTICAL QUALITY PARAMETERS

Objective: Boswellia serrata dry extract (BSDE) has clinically proved its anti-inflammatory, anti-gout, and analgesic effect. In the course of this study, compositions and technologies of the emulgels, containing dry Boswellia extract, were developed. Materials and Methods: Rheological characteristics of gels were determined with rotational viscosity method using coaxial rotation viscometer Lamy Rheology RM 200. The stickiness was determined using a lever mechanism which separates two preprocessed glass plates of the same area from each other. Spreadability was determined with a weighted amount of gel placed on a glass plate (10 cm × 10 cm), covered with a cover glass of the same size and a 100 g measuring plane placed on top of it. Results: The composition containing 20% of turpentine oil was shown to have the highest yield strength, which can positively affect the aggregative stability of the dosage form. The spreadability of all samples lies within the average value of the spreadability of the commercial gels. The stickiness of all samples was determined to be in the range from 3.6 to 4.9 N. The composition containing turpentine oil showed maximum stickiness after application and its minimum decrease by 5 min. Conclusion: The advantages of the composition including turpentine oil as a solvent for BSDE were experimentally established

Государственная фармакопея в системе высшего профессионального образования

The article provides with a brief historical background for the editions of the State Pharmacopoeia. It characterizes the Russian State Pharmacopoeia of the XIII edition. It was shown that the Russian State Pharmacopoeia, being an essential part of the drug standardization system, also carries an important educational function. Guality standards and methods of analysis, systematization of knowledge, definitions and classifications regulated by the Pharmacopoeia, not only form the knowledge base, but also define the scientific veiw for future experts.В статье представлена краткая историческая справка изданий государственной фармакопеи России. Дана характеристика содержания Государственной фармакопеи Российской Федерации XIII издания. Показано, что Государственная фармакопея, являясь обязательным элементом системы стандартизации лекарственных средств, несет важнейшую образовательную функцию. Стандарты качества и методы анализа, систематизация знаний, определений и классификаций, регламентируемые фармакопеей, не только формируют багаж знаний, но и определяют профессиональное мировоззрение будущих специалистов

Intranasal Ion-Triggered In Situ Delivery System of Virus-like Particles: Development Using the Quality by Design Approach

The rapid growth in the prevalence of infectious diseases requires timely action from drug developers. In recent years, the COVID-19 pandemic has demonstrated the unpreparedness of the population for such emergencies. The introduction of modern methods of Design of Experiments (DoE) is required to accelerate the process of drug development and bring a drug to market. The main objective of this study was to develop an ion-triggered in situ system for intranasal delivery of VLP using a Quality by Design approach. Based on a literature review and initial studies, the key QTPP, CQA, CPP, and CMA were identified to develop a novel delivery system for virus-like particles. As a result of the studies on the quality attributes of the developed delivery system, an ion-triggered in situ gel meeting all the specified parameters was obtained using the Quality by Design method

OPTIMIZATION OF HPLC METHODS FOR QUANTITATIVE DETERMINATION OF GLYCYRRHIZIC ACID IN LICORICE ROOTS

Comparative evaluation of glycyrrhizic acid content in licorice roots by methods of UV-spectrophotometry (GF RF XIII) and high-performance liquid chromatography (HPLC) was carried out. Sample preparation for HPLC method of quantitative determination of glycyrrhizic acid in samples of domestic production is developed. Small selectivity of UV-spectrophotometry at determination of glycyrrhizic acid is experimentally established and perspective of HPLC method for standardization of licorice raw materials is shown

Антигепатотоксическая активность липосомального Силибинина

The liposomal form of silibinin was obtained, and its antihepatotoxic activity in mice was studied using a model of acute toxic hepatitis caused by injection of carbon tetrachloride or paracetamol. It was shown that the use of the drug in therapy or prevention regimens leads to normalization of levels of transaminases and total protein in the blood of experimental animals. The results of the study showed that liposomal silibinin when administered intravenously shows a more pronounced hepatoprotective effect compared to intragastric administration of free silibinin. Thus, the effectiveness of the therapeutic action of silibinin can be significantly increased by using its liposomal form. Liposomal drug, in contrast to native silibinin, can be injected directly into the blood that significantly increases its bioavailability.Была получена липосомальная форма силибинина и изучена его антигепатотоксическая активность на мышах с использованием модели острого токсического гепатита, вызванного инъекцией четыреххлористого углерода или парацетамола. Показано, что применение препарата в схемах терапии или профилактики приводит к нормализации уровня трансаминаз и общего белка в крови экспериментальных животных. Результаты исследования показали, что липосомальный силибинин при внутривенном введении проявляет более выраженный гепатопротекторный эффект по сравнению с внутрижелудочным введением свободного силибинина. Таким образом, эффективность лечебного действия силибинина может быть значительно повышена при использовании его липосомальной формы. Липосомальный препарат, в отличие от нативного силибинина, можно вводить непосредственно в кровь, что значительно повышает его биодоступность