Formulation and Evaluation of Polysaccharide Microparticles for the Controlled Release of Propranolol Hydrochloride.

Propranolol hydrochloride, a non-cardio-selective beta blocker, is used to treat several conditions in children, including hypertension, arrhythmias, hyperthyroidism, hemangiomas, etc. Commercial liquid formulations are available in Europe and the US, but they have disadvantages, such as limited stability, bitter taste, and the need for multiple daily doses due to the drug's short half-life. Considering these limitations, controlled-release solid formulations, such as microparticles, may offer a better solution for pediatric administration. The main objective of this study was to formulate an encapsulation system for propranolol hydrochloride, based on sodium alginate and other polysaccharide polymers, to control and prolong its release. Microparticles were prepared using the ionotropic gelation method, which involves instilling a polymer solution into a solution of gelling ions via the extrusion technique. Physicochemical characterization was conducted by assessing the entrapment efficiency, drug loading, swelling index, microparticle size, rheological properties, and surface tension. In order to improve the characteristics of the tested microparticles, selected formulations were coated with chitosan. Further experimental work included differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) analysis, and SEM imaging. This in vitro release study showed that chitosan-coated microparticles demonstrate favorable properties, suggesting a novel approach to formulating pediatric dosage forms, although further optimization is necessary.

Interchangeability of medications and biopharmaceutical implication of taking drugs with fluids other than water: ibuprofen case study

Abstract The aim of this study was to compare the dissolution properties of ibuprofen solid oral dosage forms commercially available in Bosnia and Herzegovina and to estimate the influence of dissolution medium composition on the drug release. Eight products (A-H) were subjected to in vitro dissolution test using experimental conditions described in USP42-NF37. Dissolution properties of one selected product were examined in the presence of alcohol (22.2% v/v) and fruit juice (22.2% v/v). Products marked B-H complied with the pharmacopeial criteria. Dissolution profile of product B was similar with dissolution profiles of products D, E, F and G and similarity was also found between products A-D, C-G, D-G and E-F. Drug release from most of the examined preparations fitted best to the Weibull kinetic model. In the presence of alcohol in the medium, higher amount of ibuprofen was dissolved. Contrary, ibuprofen dissolved in the presence of fruit juice was significantly lower. Differences in the dissolution profiles of investigated preparations suggest that their interchangeability should be additionally considered and demonstrated with in vivo bioequivalence studies. Presence of different substances in the medium can affect dissolution properties of ibuprofen, emphasizing the importance of the patient's compliance.

Phytotherapy and Dietotherapy of COVID-19-An Online Survey Results from Central Part of Balkan Peninsula.

Since the appearance of the novel coronavirus disease of 2019-COVID-19, various therapeutic approaches were attempted, with complementary and alternative medicine (CAM) taking an important place. The aim of this study was to investigate the use of CAM with the purpose of prevention or treatment of COVID-19 during the pandemics. A prospective, cross-sectional study, in the form of an on-line survey was conducted. A total of 1704 responses were collected. Among the respondents, 2.76% declared currently and 22.12% previously having COVID-19. Approximately one quarter of interviewees (23.24%) declared themselves as phytotherapy users. The most frequently used medicinal plants were garlic, ginger and chamomile. The majority of respondents stated that they expected positive effects on immune and respiratory system. Medicinal plants were frequently used, on a daily basis. The main sources of information for applied self-medication were populistic thematic literature, followed by the Internet. Approximately one-third of phytotherapy users (35.25%) consulted with a medical professional before the application of phytotherapy. Regarding dietotherapy, 41.14% of respondents reported using non-herbal dietary supplements, while only 7.16% reported specific diet. The presented results suggest that CAM is recognized and readily used as a potential alternative and complementary regimen in the fight against COVID-19.

An Investigation into the Factors Governing Drug Absorption and Food Effect Prediction Based on Data Mining Methodology.

Drug absorption is a complex process governed by a number of interrelated physicochemical, biopharmaceutical, and pharmacokinetic factors. In order to explore complex relationships among these factors, multivariate exploratory analysis was performed on the dataset of drugs with diverse bioperformance. The investigated dataset included subset of drugs for which bioequivalence between solid dosage form and oral solution has been reported, and subset of drugs described in the literature as low solubility/low permeability compounds. Discriminatory power of hierarchical clustering on principal components was somewhat higher when applied on the data subsets of drugs with similar bioperformance, while analysis of the integrated dataset indicated existence of two groups of drugs with the boundaries reflected in Peff value of approximately 2 × 10-4 cm/s and Fa and Fm values higher than 85% and 50%, respectively. Majority of the investigated drugs within the integrated dataset were grouped within their initial subset indicating that overall drug bioperformance is closely related to its physicochemical, biopharmaceutical and pharmacokinetic properties. Classification models constructed using the random forest (RF) and support vector machine with polynomial kernel function were able to predict food effect based on drug dose/solubility ratio (D/S), effective permeability (Peff), percent of dose metabolized (Fm), and elimination half-life (τ1/2). Although both models performed well during training and testing, only RF kept satisfying performance when applied on the external dataset (kappa value > 0.4). The results obtained indicate that data mining can be employed as useful tool in biopharmaceutical drug characterization which merits further investigation.

Application of data mining approach to identify drug subclasses based on solubility and permeability.

Solubility and permeability are recognized as key parameters governing drug intestinal absorption and represent the basis for biopharmaceutics drug classification. The Biopharmaceutics Classification System (BCS) is widely accepted and adopted by regulatory agencies. However, currently established low/high permeability and solubility boundaries are the subject of the ongoing scientific discussion. The aim of the present study was to apply data mining analysis on the selected drugs data set in order to develop a human permeability predictive model based on selected molecular descriptors, and to perform data clustering and classification to identify drug subclasses with respect to dose/solubility ratio (D/S) and effective permeability (Peff ). The Peff values predicted for 30 model drugs for which experimental human permeability data are not available were in good agreement with the reported fraction of drug absorbed. The results of clustering and classification analysis indicate the predominant influence of Peff over D/S. Two Peff cut-off values (1 × 10-4 and 2.7 × 10-4  cm/s) have been identified indicating the existence of an intermediate group of drugs with moderate permeability. Advanced computational analysis employed in the present study enabled the recognition of complex relationships and patterns within physicochemical and biopharmaceutical properties associated with drug bioperformance.