Precise adaptation of the greenhouse lighting spectrum to basic photophysiological processes can effectively and directionally stimulate plant growth and development. The optimal spectrum depends on the plant species and the stage of development and could be assessed empirically. The aim of this study is to determine the LED illumination spectrum that provides a significant improvement in the growth rate and accumulation of biologically active compounds for basil plants (Ocimum basilicum L.) under hydroponic cultivation compared to more traditional lighting sources. The following light sources with various emission spectra were used: an LED lamp within a spectral range of 400–800 nm (B:G:R 15%:5%:80%); a high-pressure sodium lamp (HPS) (B:G:R 5%:45%:50%); a compact fluorescent lamp (B:G:R 20%:40%:40%); a grow LED strip (B:G:R 15%:40%:45%); a white LED lamp (B:G:R 30%:45%:25%); a customized LED lighting setup in color ratios 100%B, 75%B + 25%R, 50%B + 50%R, 25%B + 75%R, 100%R, and natural lighting. A photosynthetic photon flux density (PPFD) of 150 μmol∙m⁻²∙s⁻¹ was provided with all the sources. It was demonstrated reliably that employing the LED strip as an illumination device gives a 112% increase in basil plant yield compared to the HPS; the transpiration coefficient for the LED strip is six times lower than for the HPS. The content of flavonoids in the basil aerial parts on the 30th, 50th, and 70th days of development is 3.2 times higher than for the HPS; the metabolite composition is also more uniform for LED strip lighting.

Introduction. The solubility of an active pharmaceutical ingredient plays a major role in drug absorption. Hot melt extrusion is a batch or continuous process that allows creating solid dispersion systems based on various carriers in order to increase solubility and bioavailability of active substances. Development of effective and safe analgesics is one of the most vital tasks of organic and medicinal chemistry. An innovative non-opioid analgesic with very low toxicity and low dosage, but practically insoluble in water, was used in this work. It was suggested to obtain a solid dispersion by hot melt extrusion in order to increase bioavailability.Aim. Development a hot melt extrusion technology for production of a solid dispersion system of PAV-0056 as an active substance and Plasdone™ S-630 as a polymeric carrier to increase the solubility.Materials and methods. PAV-0056 (methyl-2-(7-nitro-2-oxo-5-phenyl-3-propoxy-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)acetate) (JSC "Organica", Russia) Figure 1; Plasdone™ S-630 (Boai NKY Pharmaceuticals Ltd., China); PEG-1500 (Clariant, Switzerland); acetonitrile for chromatography (Thermo Fisher Scientific, Germany). Extrudates were obtained using a HAAKE™ MiniCTW co-rotating twin-screw laboratory extruder (Thermo Fisher Scientific, Germany). Extrudates were examined by optical microscopy and differential scanning calorimetry, and time of water solution stability was determined. The quantitative content of the active substance and related impurities in the 2.5 % solid dispersion of PAV-0056 was determined by HPLC-UV.Results and discussion. Hot melt extrusion process conditions were established for a mixture of 2.5 % PAV-0056 and Plasdone™ S-630. Stability of the extrudate solution in water was studied, the content of the active substance and impurities in the extrudates was determined. Based on the binary mixture, a composition containing 10 % of PEG-1500 was developed. The optimal conditions for the extrusion process were chosen for obtaining a solid dispersion system that meets the requirements of the regulatory documentation for the content of the active substance and impurities.Conclusion. The binary mixture proved to be unsuccessful for the creation of SDS by hot melt extrusion due to significant accumulation of impurities during the extrusion process. By adding PEG-1500 to the composition, it was possible to considerably lower the operating temperature of the process, reduce the impurity content in the extrudate, and maintain satisfactory stability of the PAV-0056 solution in water.

Introduction. Arterial hypertension is one of the main risk factors for the development of cardiovascular diseases. Drug treatment of arterial hypertension is associated with a number of difficulties: often requires combination therapy, also a possible change in either dosages or drugs during treatment during the patient's life. Three-dimensional printing allows to create individual medicines on-demand.Aim. Study suitability of Kollidon® VA 64 as a matrix-polymer for the preparation of immediate release ramipril printing tablets.Materials and methods. Substance: ramipril; excipients: Kollidon® VA 64, Kollidon® CL-F, Soluplus®, PEG 1500, sodium carbonate anhydrous, Poloxamer 188, sodium stearyl fumarate, mannitol; reagents: hydrochloric acid, acetonitrile for ultra-HPLC, sodium octanesulfonate for HPLC, orthophosphoric acid 85 %, sodium perchlorate analytical grade, triethylamine, standard: ramipril USP (№1598303). Ramipril filaments were prepared by hot melt extrusion on the extruder Haake™ miniCTW (Thermo Fisher Scientific). The tablets were printed on a hand-made 3D printer. The printlets were studied for friability and hardness. Uniformity and quantitative determination of ramipril and impurities in tablets and filaments were determined by high performance liquid chromatography on a Shimadzu Prominence LC liquid chromatograph. Stability of ramipril was studied on a DSC 3+ Mettler Toledo by differential scanning calorimetry. Also, the stability of ramipril was determined by the Raman spectroscopy on an analytical system ORTES-785TRS-2700.Results and discussion. Ramipril filaments with a diameter of 1.75 mm were obtained by melt extrusion at a temperature of 105 °C. They were homogeneous in quantitative content of the active substance. From the resulting filaments, tablets were printed in five configurations with three filling densities: 30 %, 50 % and 100 %. Degradation of ramipril in filaments and tablets is not observed. The melting point of the selected mixture is lower than the melting point of matrix-polymer. It makes possible to lower the processing temperature. Tablets with 100 % filling provide an immediate release of ramipril.Conclusion. Kollidon® VA 64 is suitable as a matrix-polymer for the development of immediate release ramipril printlets. Kollidon® VA 64 provides the necessary physical and processing properties of the filament required for FDM printing.

Introduction. Ebastine is a second-generation antihistamine drug available in the form of orally disintegrating tablets and film-coated tablets. Ebastine substance exhibits high bioavailability, but low solubility in water and gastrointestinal tract media. The technology of solid dispersions based on polymer carriers by hot melt extrusion is proposed to solve the problem of ebastine low solubility.Aim. Composition development of extrudate and its production technology to create an amorphous solid dispersion of ebastine in oder to increase the recovery rate and bioavailability.Materials and methods. Ebastin micronized (JSC "Active Component", Russia); ebastin crystalline (Arevipharma GmbH, Germany); VIVAPHARM® PVP/VA 64 (JRS Pharma GMbH & Co. KG, Germany). Extrudates were obtained on a HAAKE™ miniCTW co-rotating twin-screw laboratory extruder (Thermo Fisher Scientific, Germany). Extrudates were studied by differential scanning calorimetry, synchronous thermal analysis, powder X-ray diffraction and FTIR-spectroscopy. The quantitative content of the active ingredient was determined by spectrophotometry. The content of related impurities in the amorphous solid dispersion of ebastine was determined by HPLC.Results and discussion. The technology of amorphous solid dispersion of ebastine by hot melt extrusion was developed. The pharmacokinetic properties of ebastine were significantly improved. The process of obtaining solid dispersion with 20 % of ebastine was optimized in order to reduce the content of impurities in the extrudate.Conclusion. The maximum concentration of ebastine for proper quality amorphous solid dispersion based on PVP/VA64 amounted to 20 %. Obtaining a solid dispersion by hot melt extrusion with ebastine content in PVP/VA64 higher than 30 % is impossible because the melt does not possess the glass transition property.

Introduction. Flavonoids, despite their pronounced therapeutic benefits, are limitedly used in medicine as active pharmaceutical ingredients (API) owing to a complex of unsatisfactory physicochemical properties. In order to study the mentioned problem, we decided to use quercetin as model compound with extremely low water solubility and dissolution in gastrointestinal (GI) tract media. Therefore, the main idea appears to study the possibility and prospects of hot melt extrusion (HME) application for enhancement the solubility properties of quercetin in the composition of solid dispersion system (SDS) based on hydrophilic polymeric carrier (polyvinylpyrrolidone vinyl acetate, PVP/VA). Consequently, there is a necessity to select effective drug-to-polymer ratio in solid dispersion for providing better solubility and dissolution properties.Aim. Assessment of PVP/VA effect on quercetin solubility properties in binary solid dispersion prepared by HME.Materials and methods. Quercetin substance with purity 98 % was purchased from Molekula Limited, United Kingdom. PVP/VA (copolymer of polyvinylpyrrolidone with vinyl acetate in the ratio of 60 : 40, VIVAPHARM® PVP/VA 64) as carrier was procured from JRS PHARMA (JRS PHARMA GmbH & Co. KG, Germany). Quercetin SDS were prepared using micro-conical twin screw compounder HAAKE™ MiniCTW (Thermo Fisher Scientific, Germany). The obtained samples were analyzed by phase-contrast microscopy, FTIR spectroscopy and differential scanning calorimetry (DSC). Quercetin quantitative content in SDS were determined by UV-spectrophotometry.Results and discussion. The improvement of water solubility and dissolution rates of quercetin SDS in comparison with pure substance was observed for all solid dispersion compositions irrespective to drug-to-polymer ratio. Notably, with reduction of quercetin content in SDS compositions the PVP/VA contribution was increased. We found partial or even complete amorphization of API in formulations with 1 % and 5 % quercetin content, resulting in the improvement of water solubility properties, stability of solutions and increased dissolution rates in GI tract media. Water solubility of 1 % SDS relative to pure substance was enhanced by 353-fold. At the same time, the complete release of quercetin from 1 % SDS was achieved in 40 minutes in the hydrochloric acid and citrate buffer, and also quercetin dissolution of 90 % in 60 minute was observed in phosphate buffer.Conclusion. 1 % quercetin SDS based on PVP/VA appears to be the most promising for solid dosage forms development.

Introduction. 3D printing has shown its usefulness as a drug manufacturing technology over the past decade. However, the lack of regulated methods for quality control of finished printed drugs imposes a limitation on the widespread use of 3D printing methods in pharmaceutical practice. Thus, the development of methods for the analysis of printed dosage forms is of interest in pharmaceutical development.Aim. To develop a specific method for the determination of ramipril in filaments and printlets by HPLC.Materials and methods. Substance: ramipril. Excipients: Kollidon® VA 64, Kollidon® CL-F, PEG-1500, sodium carbonate anhydrous, Poloxamer-188, sodium stearyl fumarate. Reagents: hydrochloric acid, acetonitrile for ultra-HPLC, sodium octanesulfonate for HPLC, orthophosphoric acid 85 %, sodium perchlorate analytical grade, triethylamine. Standard: ramipril USP (No 1598303).Results and discussion. A special HPLC method in accordance with an ion-pair reagent (sodium octanesulfonate) for the determination of ramipril in the composition of filaments and printets was proposed.Conclusion. The developed chromatographic method should be adapted for ramipril release determination. This method can be used to quantify ramipril in further studies.