Formulation, characterization, pharmacokinetics and antioxidant activity of phloretin oral granules.

Phloretin (PHL), a flavonoid of the dihydrogen chalcone class, is reported to have low oral bioavailability due to its poor solubility and absorption. A common approach to enhance the solubility of such flavonoids is solubilization in a polymeric or lipidic matrix which would help in enhance dissolution rate and solubility. Accordingly, in the current study PHL was dissolved in Gelucire® 44/14 by melt-fusion technique and the viscous semisolid melt was adsorbed on a solid carrier to obtain free flowing granules. SeDeM-SLA (Solid-Liquid Adsorption) expert system was employed to select the most suitable carrier. This study achieved positive outcomes through the successful development of formulated oral PHL granules. The granules exhibited good stability, and favourable pharmacokinetic properties. In addition, the selected carrier effectively retained the antioxidant properties of PHL.

A concise summary of powder processing methodologies for flow enhancement.

The knowledge of powder properties has been highlighted since the 19th century since most formulations focus on solid dosage forms, and powder flow is essential for various manufacturing operations. A poor powder flow may generate problems in the manufacturing processes and cause the plant's malfunction. Hence these problems should be studied and rectified beforehand by various powder flow techniques to improve and enhance powder flowability. The powder's physical properties can be determined using compendial and non-compendial methods. The non-compendial practices generally describe the powder response under the stress and shear experienced during their processing. The primary interest of the current report is to summarize the flow problems and enlist the techniques to eliminate the issues associated with the powder's flow properties, thereby increasing plant output and minimizing the production process inconvenience with excellent efficiency. In this review, we discuss powder flow and its measurement techniques and mainly focus on various approaches to improve the cohesive powder flow property.

Determination of Microstructural Impact on the Release of Drug from Hydroxypropyl Cellulose Gel by Validated In Vitro Release Test Method.

Microstructure of a semisolid system is greatly influenced by the formulation composition and the processing parameters. Different polymers exhibit different three-dimensional structure and these have a great impact on the drug release properties. The current research focuses on studying the impact of hydroxypropyl cellulose gel microstructure on the release properties of chlorhexidine gluconate (CHX G). The two main investigating methods of microstructure were used namely, rheology and texture analysis to determine the differences in the formulations studied. The CHX G drug release study was performed using a developed and validated in vitro release test method, which is reproducible, discriminative, and robust to detect the formulation differences. The drug release results showed that there was appreciable difference in the release rates of the different formulations. The rheology and texture analysis data correlated well with the difference in the release rates. The formulations differences were further confirmed by a statistical approach using analysis of variance.

Insights on the Critical Parameters Affecting the Probiotic Viability During Stabilization Process and Formulation Development.

Probiotics have gained a lot of interest in recent years as an alternative as well as adjuvant therapy for several conditions owing to their health benefits. These live microorganisms have proven efficacy for treating gut disorders, inflammation, bacterial vaginosis, hepatic and depressive disorders, and many more. There are conventional as well as non-conventional formulations available for the delivery of probiotics with the latter having fewer regulatory guidelines. The conventional formulations include the pharmaceutical formulations specifically designed to deliver an efficacious number of viable microorganisms. Studies have indicated 108-109 CFU/g as an ideal dose of probiotics for achieving health benefits, and hence, all the formulations must at least contain the said number of viable bacteria to show a therapeutic effect. The most crucial feature of probiotic formulations is that the bacteria are prone to several environmental and processing factors which all together reduce the viability of the bacteria in the final formulation. These factors include processing parameters like temperature, humidity, pressure, and storage conditions. Thus, the present review primarily focuses on the critical process parameters affecting the probiotic viability during stabilization process and formulation development. Understanding these factors prior to processing helps in delivering probiotics in the required therapeutic numbers at the target site.

Characterization and evaluation of tea bag papers.

The infusion kinetics of tea bags containing black tea or green tea has been studied in detail in the past. However, the tea bag papers have never been characterized and evaluated earlier to understand their contribution towards tea bag infusion. In the present work, papers used for making tea bags were characterized for thickness, wettability, surface topography, pore size, porosity and permeance to understand their influence on infusion kinetics of tea bags. Scanning electron microscopy studies highlighted the pore structure and porous nature of tea bag papers. The porosity of tea bag paper was quantified using image processing and permeance was determined experimentally. Besides, a relationship between porosity and permeance of tea bag papers has been perceived. A general trend of increase in permeance with increasing porosity was observed. Woven nylon paper showed the highest permeance (23.9 × 10-5 m/s) when compared with other tea bag papers. Furthermore, an initial infusion rate was determined using initial infusion data of tea bag infusion for different tea bag papers. The influence of permeance on the initial infusion rate of tea bag papers has also been investigated.

Thermodynamic aspects of the preparation of amorphous solid dispersions of Naringenin with enhanced dissolution rate.

Amorphous ternary solid dispersions of poorly water-soluble Naringenin (NRG) in Poloxamer 188 (POX) and Neusilin US2 (NSL) were prepared in a Hot- Melt Extruder (HME) using the principle of Low-Temperature Solubilization (LTS). Before HME, the NRG-POX solid-state interaction was investigated using Flory Huggins (F-H) theory. Construction of the composition-phase diagram showed Gibbs free energy to be negative close to the melting temperature of NRG, indicating a miscible system. The temperature-composition phase diagram provided insights on the phase behavior of the active-polymer solid dispersion system. The interactions and phase behavior predicted within the framework of the F-H theory were further investigated using Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), Hot Stage Microscopy (HSM) and Fourier-transform infrared spectroscopy (FT-IR). Based on the findings, amorphous solid dispersions of NRG were prepared via HME, which demonstrated a significant increase in the dissolution rate (p ≤ 0.05). The enhancement of the dissolution rate is due to conversion from crystalline to amorphous form, as confirmed by DSC and XRD. The amorphous NRG prepared in the current study exhibited a release of 77% at the end of 2 h, which is an increment of 250% from that of pure crystals.