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This review summarizes results of clinical studies of the efficacy and safety of topical dosage forms of non-steroidal anti-inflammatory drugs (NSAIDs). Examples of the delivery of active substances to target tissues after cutaneous application of the drugs are described. Literature data on reduced concentrations of active substances in the blood and reduced side effects of topical dosage forms of NSAIDs as compared with systemic agents are presented and show that local drug administration can reduce the number of side effects.

The role of dopaminergic transmission in the mechanism of analgesic action of the low-affinity NMDAreceptor antagonist hemantane [N-(2-adamantyl)hexamethyleneimine hydrochloride] was demonstrated experimentally. A single i.p. injection of hemantane at a dose of 20 mg/kg has the ability to inhibit dopamine reuptake and exhibits an analgesic effect in the somatic thermal pain model (tail-flick test) and visceral pain model (acetic-acid-induced writhing test) in ICR mice. The dopamine D1 receptor antagonist R(+)-SCH-23390 at a dose of 0.005 mg/kg and dopamine D2 receptor antagonist sulpiride at a dose of 5 mg/kg administered by a single i.p. injection 30 min before hemantane injection prevented manifestation of the antinociceptive activity of the NMDA receptor antagonist in the used methods, which was more pronounced for the spinal reflex (tail-flick test).

A methodological approach to selecting the optimal drying method for enisamium iodide, an antiviral agent with a broad spectrum of pharmacological activities, is considered. A vacuum drying method in an apparatus with a tape mixing device is proposed and verified based on studies of the main properties of the product. An industrial setup prototype and design features of the apparatus are described. The basic technological regimes of enisamium iodide drying ensuring the product quality are established. The kinetic drying and heating curves of the product, including those in the optimal regime, are presented. Test results were used to determine the specific technical parameters of the setup operation.

2-Isobutyl-4,6-dimethyl-5-hydroxypyrimidine (SNK-411) and its salt (SNK-578) were synthesized. Antitumor and antimetastatic activity of the new derivative 5-hydroxypyrimidine SNK-578 were studied in tests on male C57BL/6 mice using the B16 melanoma model. The standard grafted dose was 5 × 106 tumor cells mouse. SNK-578 was injected i.p. at doses of 10 and 25 mg/kg for two weeks from day 2 to day 15 of B16 melanoma development. Doxorubicin was injected to mice at a dose of 4 mg/kg on day 2 of tumor development to act as a positive control and to reveal an additive effect from combined single use of doxorubicin and injection of a course of SNK-578. The combination of i.p. injection of a course of SNK-578 at a dose of 10 mg/kg and a single i.p. injection of doxorubicin at a dose of 4 mg/kg revealed statistically significant tumor growth inhibition that was expressed as a decrease of tumor volume by 2.4, 1.9, and 1.5 times on day 11, 15, and 21 of the test as compared with the active control group that did not receive SNK-578. SNK-578 possessed pronounced antimetastatic activity at doses of 10 and 25 mg/kg for monotherapy and coadministration with doxorubicin at a dose of 4 mg/kg. The metastasis inhibition index (MII) after SNK-578 injection at a dose of 10 mg/kg was 75.8%; at 25 mg/kg, 92.3%. The most pronounced antimetastatic effect was observed after combined i.p. injection of SNK-578 at a dose of 10 mg/kg for 14 d and a single injection of doxorubicin at a dose of 4 mg/kg. Metastases were not observed in six of nine mice on day 21 of B16 melanoma development; the other three had 1, 2, and 3 very small metastases so that the MII was 98.9%.

2-Adamantylaminopropanol hydrochloride (ADK-971) and 5-hydroxyadamantan-2-ylaminopropanol hydrochloride (ADK-1013) were less active than hemantane in parkinsonian syndrome murine models. ADK-971 and AKD-1013, like hemantane at a dose of 20 mg/kg, exhibited comparable antiexudative effects in the mouse acetic peritonitis model. However, ADK-971 and ADK-1013 (20 mg/kg), in contrast to hemantane at the same dose, did not possess analgesic effects against visceral and thermal somatic pain in mice.

A selective enterosorbent (ES) based on natural silk fibroin with detoxification properties superior to those of traditional carbon sorbents (SKN-2K, SKN-4M) was proposed. The ES could be used as a matrix for drugs and a platform for new dosage forms to enhance the sanitizing effect of the proposed ES. Inclusion complexes of the ES with benzimidazolyl-2-methylcarbamate hydrochloride (I) were obtained and investigated. H-bonds were shown to form during the reaction of ES with I.

Hemantane is an antiparkinsonian drug with pronounced analgesic and anti-inflammatory properties. The present work evaluated topical gel dosage forms based on it for analgesic activity. It was found that gel batches 070916, 080916, and 090916 exhibited analgesic activity using the formalin test in rats and diminished behavior characteristic of pain in the inflammation-mediated tonic phase of formalin-induced pain. 5% hemantane gel batch 080916 exhibited the most distinct analgesic activity because this dosage form decreased pain indicators even in the acute phase related to the effect of formalin on primary pain afferents.

Dosage forms intended for ophthalmic use with declared and potential antioxidant properties were investigated. Antioxidant activity was determined using potentiometry with potassium hexacyanoferrate (III) as the oxidant. Antiradical activity was studied using the stable radical 2,2-diphenyl-1-picrylhydrazyl. The reaction half-lives of the investigated dosage forms were determined. Ratios of the experimental antioxidant activity to the content of main active ingredient were assessed.