The influence of various factors on the kinetics of polycondensation of betulin (a triterpene alcohol of the lupane series) with adipic acid was studied.

The release of several nonsteroidal anti-inflammatory drugs (NSAIDs) including analgin, paracetamol, orthofen, naproxen, aspirin, and sodium salicylate from various lipophilic suppository bases has been investigated in vitro. Individual release patterns of NSAIDs from suppositories and the significant dependence of this process on the chemical nature of the base and surfactant were shown. It was found that a determining factor in the selection of a rational suppository base is the completeness of drug release from the suppositories because the correspondence of most of the studied suppositories to pharmacopoeial requirements for melting point and total deformation time did not guarantee that the drugs had high bioavailability. The optimum bases from a biopharmaceutical viewpoint for production of suppositories of the aforementioned NSAIDs were found. The results can be used by scientific and commercial laboratories for the creation of the optimum base for production of suppositories and other NSAID medicinal forms and for the development of a common approach to evaluating the quality of suppositories.

The melting point of lipophilic base mixtures for suppositories comprising confectionary fats with various surfactants including emulsifying cetostearyl alcohol type B (1 -10%), emulsifier T-2 (1 -5%), sodium lauryl sulfate (0.2 -5%), and phospholipid concentrate (0.1 -1%) has been investigated. It is established that these surfactants added in the indicated concentrations lead to depression of the melting point of confectionary fat. Introduction of suspended nonsteroidal anti-inflammatory drugs (NSAIDs) such as diclofenac sodium, analgin, paracetamol, naproxen, acetylsalicylic acid, and sodium salicylate to the aforementioned mixtures changed their melting points within 0.5 -3°C depending on the nature of the drug and excipient. The melting points of all investigated suppositories fell within 31.0 -36.3°C, thus obeying pharmacopoeial requirements. The softening time of all anti-inflammatory suppositories varied within 2 -11 min depending on the particular types of components and was within the pharmacopoeial limits. A comparative analysis of the variation of melting point and softening time of the NSAID suppositories showed no clear correlation between the two parameters in the indicated limits. The reported data can be used for selecting the optimum bases for suppositories and developing a common approach to the evaluation of the quality and performance characteristics of suppositories.

В статье приведены результаты многолетней работы по созданию ректальных и вагинальных суппозиториев для лечения инфекционно-воспалительных заболеваний и сформулированы подходы к выбору рационального состава и технологии изготовления суппозиториев, в том числе с использованием теста «Растворение». Разработаны однокомпонентные суппозитории с пропранололом, офлоксацином, флуконазолом, азитромицином, а также комбинированные суппозитории, содержащие метронидазол и фуразолидон; клотримазол и нитрофурал; клотримазол и цефазолин; парацетамол, дифенгидрамин и папаверин; метамизол натрия и напроксен. Ключевые слова: ректальные и вагинальные суппозитории, рациональный состав и технология, инфекционновоспалительные заболевания, тест «Растворение».