Vol 68, No 4 (2019)

Introduction. Wild bergamot ( Monarda fistulosa L.) is a North American species of the plant of the family Lamiaceae . The relevance of the study of wild bergamot is due to the high bactericidal effect exceeding that of some antibiotics. In addition, the wild bergamot raw material has anti-inflammatory, fungicidal, anthelmintic, antispasmodic, immunomodulatory, and antiseborrheic activities. Despite a variety of pharmacological effects, the wild bergamot raw material is not pharmacopoeial in both Russia and foreign countries. For introduction of wild bergamot herb into the State Pharmacopoeia of the Russian Federation, it is necessary to conduct a set of pharmacognostic studies, including the development of regulatory documentation confirming the quality of medicinal plant raw material. Objective: to develop a procedure for the quantitative determination of the amount of flavonoids in the wild bergamot herb. Material and methods. The object of the investigation was wild bergamot herb harvested in the Samara University Botanical Garden in July 2016-2018. The UV spectra of its extracts were spectrophotometrically measured and obtained on a Specod 40 spectrophotometer (Analytik Jena, Germany). Results. A procedure was developed to quantify the amount of flavonoids in the wild bergamot herb with the differential spectrophotometric method using the state standard sample of cynaroside at an analytical wavelength of 394 nm. The error of a measurement at a 95% confidence interval is ±2.23%. The developed procedure was used to analyze a number of wild bergamot herb samples. The amount of flavonoids in the raw material samples ranged from 3.92±0.4% to 4.28±0.1% (in terms of cynaroside). Conclusion. A spectrophotometric method for quantifying the amount of flavonoids was proposed for the standardization of wild bergamot herb. The flavonoid amount of less than 3.0% was recommended as the lower limit.

Introduction. Alcoholic plant extracts are widely used in the therapy of many diseases. However, this formulation has a number of disadvantages that can be eliminated by transferring the liquid extract to the solid state. In this case, the adsorption technique allows one to preserve the entire complex of biologically active substances of the extract and does not affect its therapeutic efficacy. Objective: to select the optimal adsorbent for converting a liquid plant extract to the solid state, by using the drug Rotocan as an example. Materials and methods. The investigation object was the combined plant remedy Rotokan that is a mixture of liquid extracts from wild chamomile (Matricaria chamomilla) flowers, marigold (Calendula) flowers, and milfoil (Achillea) herb (hereinafter referred to as the extract). The investigators used solid carriers having sorption activity, such as microcrystalline cellulose (MCC), colloidal silicon dioxide (CSD), and microcapsules (MC) of vaterite, which were prepared extempore. Adsorption was carried out at room temperature in a glider mixer at different ratios of the extract and solid carriers. The technological characteristics of the adsorbents before and after adsorption were established according to the requirements of the Russian Federation State Pharmacopoeia, 13th edition (RF SP, 13th Edition) by using an electronic GTB flow tester and a SWM 102 bulk density tester. A Cary-100 UV spectrophotometer was used to spectrophotometrically determine flavonoids calculated with reference to luteolin. Results. It was established that the technological characteristics of the microcapsules of vaterite before and after the adsorption of the extract did not meet the requirements of the RF SP, 13th Edition. When desorbed from MCC and CSD powders, the biologically active substances of the extract were transferred to a desorbate, unlike MC, the desorbate from which failed to react to flavonoids and to quantify the latter. Conclusion. To convert the amount of plant extracts from wild chamomile flowers, marigold flowers, and milfoil herb from a liquid formulation to the solid phase by adsorption, it is promising to use microcellulose and colloidal silicon dioxide.

Introduction. Alteplase (recombinant tissue plasminogen activator (rtPA)) is the main thrombolytic agent recommended for the therapy of ischemic stroke and myocardial infarction. Alteplase is obtained by a recombinant DNA technique in CHO cell culture. Revelyse® manufactured by AO «GENERIUM» is the first registered Actilyse (alteplase, Boehringer Ingelheim) biosimilar. The existing technologies to obtain alteplase are involved and have a low yield. Objective: to develop a highly efficient procedure for purification of alteplase. Material and methods. Alteplase-containing culture fluid (CF) (AO «GENERIUM»), Actilyse® (alteplase, Boehringer Ingelheim), the affinity sorbent CaptureSelect tPA (ThermoScientific). Results. A commercial alteplase purification procedure based on the affinity sorbent CaptureSelect tPA (Thermo Scientific) was developed and scaled. Conclusion. The developed alteplase purification procedure allows one to obtain a drug that is biosimilar to Actilyze® and meets the requirements of the Pharmacopoeia.

Introduction. The development of intestinal dysbiosis is one of the components in the pathogenesis of inflammatory bowel diseases. A zinc-containing biocomposite (L15) has been designed, which is a hydrophobic rectal ointment. Its composition contains a zinc-containing metal complex dihydroquercetin derivative that has antimicrobial and prebiotic properties. Objective: to assess the qualitative and quantitative changes in the composition of the parietal microflora of the animal colon after rectal administration of the zinc-containing biocomposite in the presence of induced ulcerative colitis. Material and methods. The study was conducted on 54 male Wistar rats divided into 2 groups. Ulcerative colitis was induced by the original procedure. The animals underwent general clinical observation and determination of the quantitative and qualitative composition of the parietal microflora of the distal colon. Results. The rectal administration of a zinc-containing biocomposite to the animals with simulated ulcerative colitis after 10 days led to maintenance of a high level of the representatives of obligate bacteria, such as Bifidobacterium spp. and Lactobacillus spp., which was 47.6% each in progressive disorders with the development of dysbiosis in the parietal microflora of the colon in the control group. Conclusion. In all experimental periods, the changes in the qualitative and quantitative composition of the parietal microflora of the colon in the experimental animals treated with the test zinc-containing biocomposite for a simulated ulcerative lesion of the colon mucosa were positive compensatory as a significant increase in the concentration of Bifidobacterium spp. at 10 days of the experiment and proceeded without the opportunistic microflora.