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Introduction. Prevention and treatment of periodontal diseases remains one of the urgent problems of modern medicine. According to WHO, the prevalence of dental diseases among adults is 90–95 %, among adolescents – 80–83 %. The health of the body as a whole largely depends on the state of the oral cavity. It is important for the effective treatment of diseases to have a properly selected dosage form, which provides both convenience of use and purposeful use of the action of the pharmacologically active drug contained in it. Medicinal pencils as a dosage form are very limited on the pharmaceutical market, so their development is relevant. As a local anesthetic component, anilocaine is included in the composition of pencils at a concentration of 5 %, antimicrobial action is provided by the introduction of metronidazole in a concentration of 1 % in order to prevent the occurrence of infection.Aim. Substantiation of the composition and technology of the medicinal pencil for the treatment and prevention of infectious and inflammatory diseases of the oral cavity.Materials and methods. For the study, we used medicinal pencils with an active pharmaceutical substance – anilocaine (FS 42-2846-97, LLC "Perm Chemical Company", Perm, shelf life of 5 years), metronidazole (FS 42-0257-07, JSC "Medisorb", Perm, shelf life of 3 years); basic components – PEO-400 (FS 42-1242-96, LLC "Neftegazkhimkomplekt", Moscow, shelf life of 3 years), PEO-1500 (FS 42-1885-96, LLC "Neftegazkhimkomplekt", Moscow, shelf life of 3 years), PEO-4000 (FS 42-3337-96, LLC "Neftegazkhimkomplekt", Moscow, shelf life 3 years), second ingredient – purified water (FS.2.2.0020.18), the UVOI-"MF" 1812S6 obtained at the reverse osmosis plant (JSC "NPK Median-Filter", Russia). In the course of the research, technological, structural-mechanical and biopharmaceutical methods were used.Results and discussion. Based on technological, structural-mechanical and biopharmaceutical studies, the composition of medicinal pencils with anesthetic, anti-inflammatory and antimicrobial effects for the treatment and prevention of infectious and inflammatory diseases of the oral cavity is proposed and justified for the first time. Biopharmaceutical availability of medicinal pencils is determined by the conductometric method.Conclusion. The conducted complex of studies will expand the range of domestic medicines for the treatment and prevention of infectious and inflammatory diseases of the oral cavity.
The results of technological and biopharmaceutical investigations of the domestic local anesthetic anilocaine (possessing significant surface anesthetic, antiinf1ammatory, and moderate antimicrobial properties) were used to develop compositions of new promising multifunctional medicinal forms, including biodegradable films for the treatment of disorders in the maxillofacial area.An analysis of the state of urgent dental aid in Russia for the last five years showed that extensive prophylactic measures improved the situation with diseases and injuries to the oral cavity. More complete solution of these problems depends on the further implementation of effective, simple, and readily available prophylactic and therapeutic means. Enhanced development of research in biopharmacy showed that the correct choice of a medicinal form, providing convenient use and targeted delivery of the active substance, is extremely important for effective therapy. From this standpoint, new possibilities for the treatment of disorders in the maxillofacial area are offered by the use of multifunctional delayed-release medicinal forms, in particular, biodegradable medicinal films (BMFs).Taking into account that the treatment of such disorders involves the need for both relieving pain and inhibiting inflammation, it was expedient to develop such a medicinal form using anilocaine -a new domestic local anesthetic possessing significant surface anesthetic properties [1]. An advantage of anilocaine in comparison to the other local anesthetics widely used in practice [2] is that its anesthetic effect is combined with antiinf1ammatory activity and moderate antimicrobial properties. EXPERIMENTAL PARTMaterials. The drugs anilocaine (Pharmacopoeial Article FS 42-2846-97) and dioxidine (FS 42-2308-97) were of the pharmacopoeial quality; the film-forming components were sodium carboxymethylcellulose (NaCMC, State Standard OST 6-55-39-90), sodium alginate (medical grade, FS 42-3383-97), Blanose cellulose gum (Int. biodegradable polymer (VFS 42-439-75), and agar-agar (RSP-10, p. 866); the plasticizers were glycerin (FS 42-2202-99), citric acid (GOST 908-70), and polyethylelene glycol PEG-400 (VFS 42-1242-49).Experimental techniques. The average molecular weight of a 1´2 cm film sample (corresponding to the mean therapeutic dose) was determined by simultaneously weighing ten samples with an accuracy of 0.0002 g. The weight of individual films was determined by separately weighing 20 samples, each with an accuracy of 0.0002 g. The deviation for films with an average weight not exceeding 0.1 g must not exceed ± 10% [3]. The film thickness was determined using an MKS-25 pycnometer (according to GOST 6507-78).The film dissolution time was determined by keeping a 1´2 cm film sample in a tube with 2.5 ml of purified water at room temperature, with periodic shaking so as to eliminate adhesion of the film to the tube wall and measuring the time (in seconds) required for complete dissolution. The aqueous solution pH was determined potentiometrically (RSP-XI, Vol. ...
Introduction. Soft gelatin capsules are a promising dosage form comprising essential oils as active agents. Joint research of the staff of the Perm State Pharmaceutical Academy, the Research Institute of Nutrition of the Ministry of Energy and Industry of the Republic of Tajikistan have proposed the composition of gelatin mass for encapsulation by the rotary matrix method. The mechanical and physical-technological parameters required to preserve the strength and elasticity of the capsule shell during the production process and storage are determined.Aim. Study of the rheological properties of gelatin masses based on gelatin of different grades, as well as the migration of essential oils through capsule shells.Materials and methods. Pharmaceutical active substances "Lipovitol" and "Limoneol" obtained in the Republic of Tajikistan were used as active substances introduced into the composition of soft gelatin capsules. Sunflower oil was used as the solvent. Gelatin samples were used to obtain gelatin masses: 1 – Foodchem (China), 2 – Brodnickie Zaklady Zelatyny Sp. zo.o. (Poland), 3 - Italgelatine s.p.a. (Italy), 4 – Ewald-Gelatine GmbH (Germany), 5 – Weishardt International (France); glycerol; sunflower oil. Gelatin mass for manufacturing soft capsules was prepared in a closed reactor. Capsules were prepared on an automatic encapsulation line RJWJ – 115 Soft Gelatin Encapsulator Machine (China). The structural and mechanical properties of soft gelatin masses were determined on a rotary viscometer RV type "Reotest 2" (Germany). The dynamics of the process of migration of essential oils and its components were studied by changing their amount in a capsule by chromato-mass spectrometry method on a chromatograph Varian CP 3800 with a quadrupole mass spectrometer 4000 MS as a detector (USA).Results and discussion. When studying the rheological properties of model compositions, it was found that for all samples of gelatin masses there is a decrease in values of effective viscosity when the shear rate increases, which characterizes the tested samples as a structured dispersion system. Additional studies have shown that the gelatin masses have thixotropic properties. Samples of gelatin masses 3–5 had narrower hysteresis loops, while sample 5 the narrowest, restoration of the structure took place quite quickly. Capsules obtained from gelatin mass 3 and 4 samples had a strong seam and were well cut out of the tape. From the mass of sample 5, high strength ribbons were obtained, a high temperature was required to seal the capsules, in some capsules the seam was not glued on one side, as a result, the capsules were rigid and brittle. As a result of the study, the rheological optimum of the gelatin mass suitable for preparing capsules by a rotary matrix method was determined, which has boundaries in the ranges of shear rates of 0.556–243 s-1 and viscosity ranges of 11.46-5028.76 Pa ⋅ s and shear stress of 2788–2808 Pa developing at these rates. When studying the migration of active substances through the capsule shell, it was found that over three years of storage of capsules in a closed polymer can, the content of essential oil in Lipovitol capsules decreased by 4.88 %, in Limoneol capsules by 5 %, which indicates partial migration of oil through the gelatin shell. The content remained within the permissible deviations (±10 %). The content of essential essential oil components also remained within acceptable deviations throughout the shelf life.Conclusion. The optimal composition of the shell for producing soft capsules by a rotary matrix method is justified. It was found that the rheological optimum of gelatin mass is characterized by viscosity ranges of 11.46-5028.76 Pa ⋅ s and shear stress of 2788–2808 Pa. According to the results of the study of the migration of essential oils through the shell, has been established the shelf life of soft gelatin capsules in glass jars made of dark glass and a temperature of 15 to 25 °C – 3 years.
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