Abstract
Introduction. Direct compression technology is one of the most common tablet technologies. As known, many active pharmaceutical ingredients are not suitable for this technology without the addition of special excipients. A useful tool for determining the suitability of powdered materials for direct compression technology is the Sediment Delivery Model (SeDeM) method, based on the concept of Quality by Design. The presented method allows not only to assess the suitability of a material for direct compression, but also helps to predict the composition of a solid dosage form in the form of a tablet, which, in turn, leads to a significant reduction in experimental work carried out in the development of a new drug.Aim. Prediction of the compositions of matrix tablets based on sodium 4,4'-(propanediamido)dibenzoate with prolonged release, obtained by direct compression using the method of mathematical modeling SeDeM.Materials and methods. The objects of the study were the original substance sodium 4,4'-(propanediamido)dibenzoate, as well as a number of auxiliary substances, which included polymers used for dosage forms with prolonged release, a dusting component – magnesium stearate, and a filler – lactose monohydrate. Physicochemical and technological properties of APIs, explosives, obtained tablet mixtures and tablets were studied in accordance with the requirements of the State Pharmacopoeia of the Russian Federation XIV ed. and EP 9th ed.Results and discussion. The properties of the substance and excipients were assessed in accordance with the SeDeM method. It was found that the substance 4,4'-(propanediamido) sodium dibenzoate is not suitable for direct pressing due to poor flowability and low compressibility. Hypromellose Methocel K4M had good compressibility, but it did not have sufficient flowability. The other tested polymers had satisfactory properties for the direct compression technology. The composition of the tablet mixtures was calculated using the SeDeM method, the obtained tablet mixtures had satisfactory technological characteristics for obtaining tablets by direct compression. The tablets obtained as a result of the experiment also met the pharmacopoeial requirements.Conclusion. Prediction of the composition of sustained-release tablets based on the original substance sodium 4,4'-(propanediamido)dibenzoate was carried out using the SeDeM method. It was found that this method is suitable for the development of the composition of tablets based on sodium 4,4'-(propanediamido)dibenzoate.
Highlights
Direct compression technology is one of the most common tablet technologies
The objects of the study were the original substance sodium 4,4'-(propanediamido)dibenzoate, as well as a number of auxiliary substances, which included polymers used for dosage forms with prolonged release, a dusting component – magnesium stearate, and a filler – lactose monohydrate
Physicochemical and technological properties of APIs, explosives, obtained tablet mixtures and tablets were studied in accordance with the requirements of the State Pharmacopoeia of the Russian Federation XIV ed. and EP 9th ed
Summary
Объектами исследования являлась оригинальная АФС 4,4’-(пропандиамидо)дибензоат натрия, а также вспомогательные вещества:. Kollicoat IR – сополимер полиэтиленгликоля и поливинилового спирта (BASF, Германия);. Kollicoat MAE 100P – сополимер метакриловой кислоты и этилакрилата (BASF, Германия);. Eudragit L100-55 – сополимер метакриловой кислоты и этилакрилата (Evonik, Германия);. В качестве ЛФ для представленной АФС были выбраны матричные таблетки с пролонгированным высвобождением. Физико-химические и технологические свойства АФС, ВВ, полученных модельных таблеточных смесей, а также свойства полученных таблеток были изучены в соответствии с требованиями ГФ РФ XIV изд. Гигроскопичность субстанции 4,4’-(пропандиамидо)дибензоата натрия определяли в соответствии с требованиями EP 9th ed. Измерение насыпной плотности (Da) и насыпной плотности после уплотнения (Dc) порошка проводили с использованием тестера насыпной плотности ERWEKA SVM 221 (ERWEKA GmbH, Германия) в соответствии с требованиями ОФС.1.4.2.0016.15 «Степень сыпучести порошков». Пористость между частицами рассчитывается по формуле 3: Ie
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