Biopharmaceutical investigations of biodegradable medicinal films containing anilocaine

Abstract

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. ...