Objective: To substantiate the possibility of using polarimetry to control the quality of tinctures as an additional pharmacopoeial method. Methods: The polarimetric method (POL-1/2, Atago, Japan, the measurement accuracy of±0.002 °) was used to measure the optical activity (α °) of motherwort, valerian and hawthorn tinctures. The dynamic light scattering method (DLS; Zetasizer Nano ZS, Malvern, UK) was used to assess the stability of alcoholic and aqueous dilutions of tinctures according to the intensity of dynamic light scattering dependent on the size (d, nm) of the dispersed phase particles and the values of the electrokinetic potential (ξ, mV). Results: For the first time in this investigation, the polarimetry approach was proposed to evaluate the cardiotonic and hypotensive tinctures' quality and for their identification. Valerian tincture, dilution 1:40,-0.10°<α°<-0.89°; motherwort, tincture-dilution 1:10,-0.10°<α°<-2.21°; hawthorn, tincture without dilution,-0.76°<α°<-1.55°-these are the acceptable ranges of optical activity (α°) of their alcohol dilutions. Beyond these intervals, the use of the polarimetric approach is impossible. Values of optical activity below 0.1 correspond to too low a content of optically active components. Tinctures with optical activity above the upper value of the interval were unstable dispersed systems with low values of the electrokinetic potential (|ξ|≪25mV) and micron particle sizes. Reference tinctures were made from raw materials (Leonurus cardiaca L.) to verify the results. The quality parameters: optical activity (α°), spectra of dynamic light scattering by intensity, volume, and number ("I-d"; "V-d"; "N-d"), electrokinetic potential (ξ) values, and photon pulse count per second (Count Rate, kcps) corresponded to the results obtained for pharmaceutical dosage forms. Conclusion: The permissible intervals of optical activity (α°) of their ethanol dilutions, as well as their relationships with the particle size of the dispersed phase and the values of the electrokinetic potential, were established for the first time to evaluate the quality of tinctures. The obtained results show that polarimetry can be recommended as an additional pharmacopoeial quality control method for tinctures.
Objective: To prove the benefits of biopharmaceutical parameters of cannabinoids over NSAIDs using quantitative structure and activity relationships (QSAR). Methods: The topological indices of Wiener (W) and Balaban (J) were calculated using the previously developed original program ChemicDescript (certificate no. 2003612305). Results: It was shown that the calculated topological indices were in one-to-one correspondence with such biopharmaceutical parameters as the constants of equilibrium binding to cannabinoid receptors CB1 and CB2, toxicity, and lipophilicity. For example, it was shown that when the Wiener index changes from 480 to 530 LogK increases from 1.0 to 3.5. The LD50-W/J and logP-W/J diagrams demonstrate that cannabinoids are less toxic and more lipophilic than NSAIDs. Cannabidiol and cannabinol, having close values of their topological indices and insignificant psychoactivity, have the highest LD50 values, i.e. they are the least toxic. Moreover, for synthetic cannabinoids–nabilone and THJ-2201–the Wiener index is approximately 2 times higher than for plant analogues. Conclusion: In connection with the successful promotion of cannabinoid analgesics in the global pharmaceutical market, the results obtained are important for demonstrating their advantages over NSAIDs in terms of toxicity and lipophilicity. The results demonstrate the possibility of predicting the cannabinoid receptor binding energy of synthetic and newly identified plant cannabinoids, as well as assessing their toxicity and lipophilicity.
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