Potentiometric Electronic Tongue for the Evaluation of Multiple-Unit Pellet Sprinkle Formulations of Rosuvastatin Calcium.

Sprinkle formulations represent an interesting genre of medicinal products. A frequent problem, however, is the need to mask the unpleasant taste of these drug substances. In the present work, we propose the use of a novel sensor array based on solid-state ion-selective electrodes to evaluate the taste-masking efficiency of rosuvastatin (ROS) sprinkle formulations.

The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium.

Sprinkle formulations represent an interesting concept of medicinal products aimed at the steadily growing population of patients suffering from swallowing difficulties (dysphagia). In the present work, immediate-release sprinkle MUPS (multiple-unit pellet system) containing rosuvastatin calcium as a model drug substance was successfully developed. The formulation was prepared by drug layering technique using novel calcium phosphate-based starting pellets (PharSQ Spheres CM) of three different particle sizes.

Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator.

Continuous manufacturing is becoming the new technological standard in the pharmaceutical industry. In this work, a twin-screw processor was employed for the continuous production of liquisolid tablets containing either simethicone or a combination of simethicone with loperamide hydrochloride. Both active ingredients present major technological challenges, as simethicone is a liquid, oily substance, and loperamide hydrochloride was used in a very small amount (0.

Development of Safirinium dyes for new applications: fluorescent staining of bacteria, human kidney cells, and the horny layer of the epidermis.

Low-molecular synthetic fluorophores are convenient tools in bioimaging applications. Several derivatives of Safirinium dyes as well as their reactive N-hydroxysuccinimide (NHS) esters bearing diverse substituents were synthesized and evaluated experimentally in terms of their lipophilicity by means of reverse-phase and immobilized artificial membrane high-performance liquid chromatography. Subsequently, the selected compounds were employed as novel cellular imaging agents for staining Gram-positive and Gram-negative bacteria, human kidney cell line, as well as human skin tissue.

Comparative study of the percutaneous permeation and bioaccumulation of a cyclic siloxane using frozen-thawed and nonfrozen ex vivo human skin.

Literature shows contradictory information regarding the effect of freezing the excise skin ex vivo on the diffusion of substances into the skin. Few studies indicate that storing the human or animal skin in a frozen state decreases the barrier properties after thawing. Therefore, to understand the properties of frozen skin, we evaluated the effect of storage of ex vivo human skin (2 weeks at -20 °C) on the penetration of stratum corneum and permeation into deeper skin layers (epidermis, and dermis) as well as to the receptor fluid by octamethylcyclotetrasiloxane (D4) a representative test compound of cyclic siloxanes.

Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate.

Reliable and stable tablet formulations for rosuvastatin calcium (RSC) in four strengths: 5 mg, 10 mg, 20 mg, and 40 mg have been developed. Rosuvastatin is a cholesterol-lowering statin drug and is known to be unstable during storage. The possibility of its stabilization with inorganic salts of multivalent metals has already been reported in the literature.

Mangiferin and Hesperidin Transdermal Distribution and Permeability through the Skin from Solutions and Honeybush Extracts ( sp.)-A Comparison Ex Vivo Study.

Polyphenolic compounds-mangiferin and hesperidin-are, among others, the most important secondary metabolites of African shrub sp. (honeybush). The aim of this study was to compare the percutaneous absorption of mangiferin and hesperidin from solutions (water, ethanol 50%, ()) and extracts obtained from green and fermented honeybush (water, ethanol 50%, ()).

Development of a Biphasic-Release Multiple-Unit Pellet System with Diclofenac Sodium Using Novel Calcium Phosphate-Based Starter Pellets.

Novel calcium phosphate-based starter pellets were used to develop a biphasic-release multiple-unit pellet system (MUPS) with diclofenac sodium as a model drug in the form of hard gelatin capsules. For comparative purposes, corresponding formulations based on the inert cores made of microcrystalline cellulose, sucrose and isomalt were prepared. The developed system consisted of two types of drug-layered pellets attaining different release patterns: delayed-release (enteric-coated) and extended-release.

Transdermal transport of collagen and hyaluronic acid using water in oil microemulsion.

Collagen and hyaluronic acid (HA) are biopolymers that affect the appearance and condition of the skin. Delivery of these compounds into the skin is highly challenging since have a number of disadvantageous properties, such as high molecular weight and hydrophilicity. Here, we evaluated the transdermal penetration of low and high molecular weight collagen and HA from microemulsions.

The consequences of overcoming the human skin barrier by siloxanes (silicones) Part 1. Penetration and permeation depth study of cyclic methyl siloxanes.

Dynamic production of cyclic siloxanes: octamethylcyclotetrasiloxane D4, decamethylcyclopentasiloxane D5 and dodecamethylcyclohexasiloxane D6 increases their concentrations in environment. It is considered that both environmental pollution and the usage of personal care products and cosmetics containing cyclic siloxanes can be the main source of the human exposure by transdermal route. The aim of the study was to verify the possibility to overcome the skin barrier by cyclic siloxanes (ATR-FTIR and GC-FID), evaluation of diffusion pathway to stratum corneum SC (Fluorescence microscopy), and determination of depth of permeation to deeper skin layers: epidermis and dermis (ATR-FTIR) and also of potential interaction with SC lipids and proteins (Fluorescence microscopy, ATR-FTIR) and the cytotoxicity studies against HaCaT cells (MTT test).

Dissolution studies of metamizole sodium and pseudoephedrine sulphate dosage forms - comparison and correlation of electronic tongue results with reference studies.

This work reports a critical evaluation of the results of the release of active substances (APIs) from novel pharmaceutical formulations provided by an electronic tongue system (ET). Detailed dissolution studies of modified-release granules used in pharmacotherapy containing metamizole sodium and pseudoephedrine sulphate were carried out. The impact of the dissolution-modifying excipients (carmellose sodium and hypromellose) on the dissolution process as well as on the outcomes of the sensor array of ion-selective electrodes was investigated.

The effect of mangiferin on skin: Penetration, permeation and inhibition of ECM enzymes.

Mangiferin (2-C-β-D-glucopyranosyl-1,3,6,7-tetrahydroxyxanthone) is a polyphenol with strong antioxidant properties. Mangiferin is obtained from the mango tree (Mangifera indica L., Anacardiaceae).

Influence of dissolution-modifying excipients in various pharmaceutical formulations on electronic tongue results.

The overall performance of a potentiometric electronic tongue (ET) as well as the sensitivity and selectivity pattern of particular ion-selective electrodes forming the array towards exemplary APIs (metamizole sodium, pseudoephedrine sulphate) and excipients (hypromellose, carmellose, Eudragit E) was determined. Simultaneous sensing of both API and the encapsulating excipient in their physical mixture was noticed using potentiometric sensors. Usually, such altering of chemical image is treated as an evidence of taste masking/modified release effect (linked with chemical entrapment of API in polymer matrix), while the observed "mixture effect" can also take place which may complicate the interpretation of ET results.

The effect of a lipid composition and a surfactant on the characteristics of the solid lipid microspheres and nanospheres (SLM and SLN).

Solid lipid microparticles (SLM) were produced by a two-step process that, firstly, involved the emulsification of the molten lipid phase in a heated aqueous phase and, secondly, the system cooling. Compritol 888 ATO and Precirol ATO 5, including their mixtures with Miglyol 812 or Witepsol H15 were used as lipid components (10-30% w/w). The average size of the SLM prepared with Compritol and Tween 80 as an emulsifier was 3-7μm and the influence of lipid concentration and thermal sterilization was not large.

Roxithromycin-loaded lipid nanoparticles for follicular targeting.

Particulate drug carriers e.g. nanoparticles (NPs) have been shown to penetrate and accumulate preferentially in skin hair follicles creating high local concentration of a drug.

The improvement of the dissolution rate of ziprasidone free base from solid oral formulations.

This work aims at increasing solubility and dissolution rate of ziprasidone free base-Biopharmaceutics Classifaction System (BCS) class II compound. The authors describe a practical approach to amorphization and highlight problems that may occur during the development of formulations containing amorphous ziprasidone, which was obtained by grinding in high-energy planetary ball mills or cryogenic mills. The release of ziprasidone free base from the developed formulations was compared to the reference drug product containing crystalline ziprasidone hydrochloride-Zeldox® hard gelatin capsules.

Polymeric nanoparticles-embedded organogel for roxithromycin delivery to hair follicles.

Drug delivery into hair follicles with the use of nanoparticles (NPs) is gaining more importance as drug-loaded NPs may accumulate in hair follicle openings. The aim was to develop and evaluate a pluronic lecithin organogel (PLO) with roxithromycin (ROX)-loaded NPs for follicular targeting. Polymeric NPs were evaluated in terms of particle shape, size, zeta potential, suspension stability, encapsulation efficiency and in vitro drug release.

Determination of API content in a pilot-scale blending by near-infrared spectroscopy as a first step method to process line implementation.

Near infrared (NIR) spectroscopy was used for estimation of powder blend homogeneity and manufacturing control of a medicinal product powder mixture containing active pharmaceutical ingredient (API). Aiming at initiating a Process Analytical Technology (PAT) activity, the first step was a stationary mode at-line evaluation. In this, the content of pharmaceutical active compound in the powder mixtures intended to the direct tabletting was estimated based on recorded NIR spectra.

Development of rapid and robust stability-indicating method for analysis of ziprasidone (hydrochloride and freebase) as drug substance and in medicines by UPLC.

Ultra Performance Liquid Chromatography (UPLC) was employed to develop a rapid and robust method for the analysis of ziprasidone, both as a drug substance and in the final dosage forms. The application of this method in stability analyses was verified. Tests were carried out according to ICH/FDA guidelines, European Pharmacopeia, and United States Pharmacopeia rules, which take into account factors such as specificity, linearity, accuracy, and precision.

Taste masking of roxithromycin by spray drying technique.

The spray drying technique was used to obtain the roxithromycin containing microcapsules with high taste masking efficiency. Eudragit L30D-55 was chosen as a barrier coating. The taste was evaluated by an electronic tongue, and taste-masking effect in water lasted at least several dozen hours.

Electronic tongue for the detection of taste-masking microencapsulation of active pharmaceutical substances.

Electronic tongues can produce chemical images of samples, whose changes can be correlated with general properties, e.g. taste sensations.

Advanced tools for in vivo skin analysis.

A thorough examination of the skin is essential for accurate disease diagnostics, evaluation of the effectiveness of topically applied drugs and the assessment of the results of dermatologic surgeries such as skin grafts. Knowledge of skin parameters is also important in the cosmetics industry, where the effects of skin care products are evaluated. Due to significant progress in the electronics and computer industries, sophisticated analytic devices are increasingly available for day-to-day diagnostics.

Targeting to the hair follicles: current status and potential.

The pilosebaceous unit is a complex structure that undergoes a specific growth cycle and comprises a few important drug targeting sites. For example, drugs can be targeted to the bulge region with stem cells or to the sebaceous glands. Interest in pilosebaceous units is directed towards their utilization as reservoirs for localized therapy and also as a transport pathway for systemic drug delivery.