Lactobacilli use in treatment and prevention of the vaginal microflora disorders, such as bacterial vaginosis and vulvovaginal candidiasis, is highly promising. The objective of this study was is to develop formulation and technology of the extemporal Lactobacillus casei (L. casei) ІМВ В-7280-containing medicinal product in the form of vaginal pessaries. The quality control parameters were defined in accordance with the State Pharmacopeia of Ukraine (2nd edition) and included appearance, uniformity of texture, uniformity of mass and disintegration test. Lactobacilli assay was determined after preparation and within the storage period. Thus, feasible formulation and technology were selected for vaginal pessaries with an expected 6-month shelf life. The results of the hereby described research will be used for technological instruction development for extemporaneous vaginal pessaries with defined probiotic activity.

• Keywords
• Lactobacilli, vaginal dysbiosis, vaginal pessaries,
• MeSH
• Vaginosis, Bacterial therapy   MeSH
• Humans MeSH
• Pessaries * MeSH
• Drug Compounding * MeSH
• Probiotics pharmacology   MeSH
• Check Tag
• Humans MeSH
• Female MeSH
• Publication type
• Journal Article MeSH

The aim of this work was to develop anti-stress compressed lozenges containing 100 mg of glycine and 250 mg of magnesium citrate obtained by the direct compression method. To choose optimal excipient composition providing the sufficient pharmaco-technical properties of the tablet blend, mechanical strength of tablets and non-disintegrating, slow-dissolving behavior of compressed lozenges during sucking, 27 experimental formulations according to fractional factorial Latin cube design were prepared and tested. The excipients used in the study were: Mannogem® EZ, Cellactose® 80 and GalenIQ 721 (fillers); Plasdone S-630, Kollidon® 90 F and Avicel® PH-101 (dry binders); Metolose® 90SH-4000SR and guar gum (gel-forming binders); PRUV®, Neusilin® US2, and Compritol® 888 CG ATO (antifriction excipients). The following parameters were investigated as responses: bulk density, Carrs index, friability, resistance to crushing, and in vitro disintegration time. ANOVA approach was applied for statistical processing, which allowed to reveal the individual effects of each excipient and several interaction effects observed for the excipient amounts used in this study. Isomalt (GalenIQ 721), copovidone (Plasdone S-630), and glyceryl behenate (Compritol® 888 CG ATO) were selected to be incorporated in the final formulation of compressed lozenges.

• Keywords
• Analysis of variance, compressed lozenges, design of experiment, formulation development, glycine, magnesium citrate, stress-protective activity,
• MeSH
• Analysis of Variance MeSH
• Cellulose * MeSH
• Excipients * MeSH
• Solubility MeSH
• Tablets MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• Cellulose * MeSH
• Excipients * MeSH
• Tablets MeSH

PURPOSE: The purpose of this study was formulation and optimization of vaginal film formulation containing abacavir (ABC), a potent nucleoside reverse transcriptase inhibitor. METHODS: Vaginal films were prepared by solvent evaporation method using hydroxypropyl methylcellulose (HPMC) blended with polyvinyl pyrrolidone (PVP). Various physicochemical parameters of the prepared films such as drug content, thickness, tensile strength, percentage elongation at break, drug polymer interaction, swelling capacity, folding endurance, bio-adhesion, pH, and moisture content were evaluated with morphological studies. In vitro release study and in vivo release study were also performed. RESULTS: Films exhibited favorable physicochemical properties. The in vitro study showed that HPMC-PVP combination can control the release of abacavir through vaginal films with higher amount of PVP in the formulation resulting in an enhanced drug release rate. During the in vivo study in rabbits, systemic absorption of the drug was noted and the films remained intact for long in vagina without causing any sort of irritations. CONCLUSION: Thus, in a nutshell, the findings of our experimental work indicate that such films can be considered as a novel drug carrier system for the treatment of AIDS and other sexually transmitted diseases (STDs), and are suitable for local as well as systemic effects.

• MeSH
• Administration, Intravaginal MeSH
• Chemical Phenomena MeSH
• Dideoxynucleosides administration & dosage   pharmacokinetics   MeSH
• Rabbits MeSH
• Anti-HIV Agents administration & dosage   pharmacokinetics   MeSH
• Dosage Forms * MeSH
• Drug Carriers administration & dosage   chemistry   MeSH
• Drug Compounding * MeSH
• Drug Liberation * MeSH
• Animals MeSH
• Check Tag
• Rabbits MeSH
• Female MeSH
• Animals MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• abacavir MeSH Browser
• Dideoxynucleosides MeSH
• Anti-HIV Agents MeSH
• Dosage Forms * MeSH
• Drug Carriers MeSH

This study reports the development and validation of a new, simple, and accurate high-performance thin-layer chromatography (HPTLC)-densitomeric method for the determination of nandrolone decanoate in a commercially available injection formulation. Chromatographic analysis was performed on glass CN modified silica gel 60F254 plates developed using n-hexane-ethyl acetate in volume ratio 42.5:7.5 as the mobile phase. Densitometric scanning was carried out at the wavelength of 245 nm. This chromatographic system gave compact spot and a symmetrical peak of nandrolone decanoate with retardation factor (RF) value at 0.57 (±0.02). The linearity of this method with the high correlation coefficient of calibration plot ranges from 0.780 to 12.500 μg/spot. The developed method is characterized by good precision (coefficient of variation CV < 2%) and high accuracy close to 100.3% (R = 99.0%). Values of limits of detection and quantification equal to 0.231 and 0.700 μg/spot, respectively, confirm the sensitivity of the developed method. The analysis of the pharmaceutical formulation of nandrolone decanoate indicates drug content of 50.5 mg/mL and 101.0% in relation to the label claim. This is in good agreement with the recommendation of the International Council for Harmonisation (ICH) guidelines as well as the pharmacopoeial requirements. The low CV value (<1%) of nandrolone decanoate content in the tested injection formulation confirms the suitability of the proposed HPTLC-densitometric method for routine control of this compound in examined pharmaceuticals.

• Keywords
• HPTLC, densitometry, nandrolone decanoate, steroids,
• MeSH
• Chromatography, Thin Layer * methods   standards   MeSH
• Densitometry * methods   standards   MeSH
• Pharmaceutical Preparations analysis   MeSH
• Nandrolone Decanoate analysis   MeSH
• Drug Compounding MeSH
• Reproducibility of Results MeSH
• Sensitivity and Specificity MeSH
• Chromatography, High Pressure Liquid * methods   standards   MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• Pharmaceutical Preparations MeSH
• Nandrolone Decanoate MeSH

The bioavailability of rivaroxaban at the higher doses (15 and 20 mg) is considerably reduced when the drug is administered on an empty stomach. This can lead to inadequate anticoagulant effect, and therefore, it is recommended to use the higher doses at fed state. However, proper posology may represent a barrier for some patients. Therefore, the aim of this study was to evaluate innovative rivaroxaban-containing formulations designed to eliminate the food effect to ensure reliable absorption and thus to improve patient adherence with the treatment. Three prototypes (Cocrystal, HPMCP and Kollidon) with rivaroxaban were developed and their bioavailability and food effect in comparison to the reference product was tested in open label, randomized, single oral dose, crossover studies, where test products were administered under fasting and fed conditions and the reference product was administered under fed conditions. Comparable bioavailability for all tested prototypes both under fed and fasting conditions was demonstrated as the 90% confidence intervals of the geometric mean ratios for area under the concentration-time curve remained within the standard acceptance range of 80.00%-125.00%. An innovative immediate release form of rivaroxaban with no food effect on drug bioavailability has been developed, which may represent an important step toward increasing adherence, improving treatment outcome and reducing health care costs.

• MeSH
• Administration, Oral MeSH
• Biological Availability * MeSH
• Adult MeSH
• Factor Xa Inhibitors pharmacokinetics   administration & dosage   MeSH
• Food-Drug Interactions * MeSH
• Meals MeSH
• Cross-Over Studies * MeSH
• Middle Aged MeSH
• Humans MeSH
• Young Adult MeSH
• Fasting * MeSH
• Drug Compounding methods   MeSH
• Rivaroxaban * pharmacokinetics   administration & dosage   MeSH
• Check Tag
• Adult MeSH
• Middle Aged MeSH
• Humans MeSH
• Young Adult MeSH
• Male MeSH
• Female MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH
• Randomized Controlled Trial MeSH
• Names of Substances
• Factor Xa Inhibitors MeSH
• Rivaroxaban * MeSH

Persistence of Bacillus thuringiensis is an important factor in determining the success of this product as a pest control agent. In this report we present the development of a highly active mosquitocidal formulation with high resistance to UV. LLP29-M19 strain of Bt, selected by repeated exposure to UV was found to be highly resistant to UV. The product was optimized and the methods used were statistically analyzed. Using single-factor experiments it was determined that the optimal concentration of sodium alginate, CaCl2 and hollow glass beads in the formulation were 1.0%, 2.0% and 3.5%, respectively. Plackett-Burman design was used to screen the interaction of the three factors, CaCl2, sodium alginate and hollow glass beads in the sustained-release formulation. The best combined concentration and mutual effects of the three factors were optimized by response surface methodology. The results showed that the most favorable composition was sodium alginate 0.78%, CaCl2 4.52%, hollow glass bead 3.12%, bacterial powder 3.0%, melanin 0.015%, sodium benzoate 0.2%, and mouse feed 0.5%, resulting in the immobilization time of 4.5 h, at which time the corrected sustained-release virulence rose 2391.67 fold, which was 6.07-fold higher than the basic formulation and deviated only 5.0% from the value predicted by RSM.

• MeSH
• Alginates pharmacology   MeSH
• Bacillus thuringiensis physiology   MeSH
• Bacterial Proteins pharmacology   MeSH
• Pest Control, Biological methods   MeSH
• Biological Control Agents pharmacology   MeSH
• Culicidae drug effects   MeSH
• Chemistry, Pharmaceutical methods   MeSH
• Glucuronic Acid pharmacology   MeSH
• Hexuronic Acids pharmacology   MeSH
• Larva drug effects   MeSH
• Delayed-Action Preparations pharmacology   MeSH
• Mosquito Control methods   MeSH
• Ultraviolet Rays MeSH
• Animals MeSH
• Check Tag
• Animals MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH
• Names of Substances
• Alginates MeSH
• Bacterial Proteins MeSH
• Biological Control Agents MeSH
• Glucuronic Acid MeSH
• Hexuronic Acids MeSH
• Delayed-Action Preparations MeSH

Inhalation drug administration is increasingly used for local pharmacotherapy of lung disorders and as an alternative route for systemic drug delivery. Modern inhalation powder systems aim to target drug deposition in the required site of action. Large porous particles (LPP), characterized by an aerodynamic diameter over 5 μm, density below 0.4 g/cm3, and the ability to avoid protective lung mechanisms, come to the forefront of the research. They are mostly prepared by spray techniques such as spray drying or lyophilization using pore-forming substances (porogens). These substances could be gaseous, solid, or liquid, and their selection depends on their polarity, solubility, and mutual compatibility with the carrier material and the drug. According to the pores-forming mechanism, porogens can be divided into groups, such as osmogens, extractable porogens, and porogens developing gases during decomposition. This review characterizes modern trends in the formulation of solid microparticles for lung delivery; describes the mechanisms of action of the most often used porogens, discusses their applicability in various formulation methods, emphasizes spray techniques; and documents discussed topics by examples from experimental studies.

• Keywords
• Microparticles, inhalation, porogens, porosity, porous particles, spray drying,
• MeSH
• Administration, Inhalation MeSH
• Chemistry, Pharmaceutical methods   MeSH
• Drug Delivery Systems * methods   MeSH
• Humans MeSH
• Lung * metabolism   drug effects   MeSH
• Porosity MeSH
• Powders MeSH
• Drug Compounding methods   MeSH
• Particle Size * MeSH
• Animals MeSH
• Check Tag
• Humans MeSH
• Animals MeSH
• Publication type
• Journal Article MeSH
• Review MeSH
• Names of Substances
• Powders MeSH

Injectable depot formulations are aimed at providing long-term sustained release of a drug into systemic circulation, thus reducing plasma level fluctuations and improving patient compliance. The particle size distribution of the formulation in the form of suspension is a key parameter that controls the release rate. In this work, the process of wet stirred media milling (ball milling) of a poorly water-soluble substance has been investigated with two main aims: (i) to determine the parametric sensitivity of milling kinetics; and (ii) to develop scale-up methodology for process transfer from batch to flow-through arrangement. Ball milling experiments were performed in two types of ball mills, a batch mill with a 30ml maximum working volume, and a flow-through mill with a 250ml maximum working volume. Milling parameters were investigated in detail by methodologies of QbD to map the parametric space. Specifically, the effects of ball size, ball fill level, and rpm on the particle breakage kinetics were systematically investigated at both mills, with an additional parameter (flow-rate) in the case of the flow-through mill. The breakage rate was found to follow power-law kinetics with respect to dimensionless time, with an asymptotic d50 particle size in the range of 200-300nm. In the case of the flow-through mill, the number of theoretical passes through the mill was found to be an important scale-up parameter.

• Keywords
• Ball milling, Ball size, Particle size distribution, Power-law kinetics, Surfactant,
• MeSH
• Chemistry, Pharmaceutical methods   MeSH
• Injections MeSH
• Delayed-Action Preparations administration & dosage   chemical synthesis   MeSH
• Nanoparticles chemistry   MeSH
• Solubility MeSH
• Suspensions MeSH
• Particle Size MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• Delayed-Action Preparations MeSH
• Suspensions MeSH

This review aims at the current trends in chocolate ganache production and recipe formulation. Ganache is a blend of chocolate, sugars, dairy, and other ingredients commonly used to fill pralines, pastries, etc. In spite of ganache's popularity in the food industry, a comprehensive review focused on the application of functional substances and ganache processing has not been discussed in the scientific literature. This review addresses the new ways of applying special ingredients, such as vegetable fats and seeds, flavor infusions, oleogels, hemp products, etc., which can be added to the ganache matrix to achieve desirable properties. In particular, the application of sterols and sterol esters as functional substances of oleogels seems to be a very promising method, enhancing the ganache fat profile. The elevated caloric content that is characteristic of ganache can be substantially attenuated through the application of hydrocolloids and/or fruit-based components, thereby offering the potential for caloric reduction without compromising on taste. The various alterations to ganache formulations by the application of natural substances offer a large base for the development of novel ganache variants and relevant food products.

• Keywords
• chocolate, emulsion, ganache, ganache processing, hydrocolloids, oleogels, pralines, recipe formulation,
• Publication type
• Journal Article MeSH
• Review MeSH

Monoglycerides (MGs) such as glycerol monolaurate (GML) and glycerol monostearate (GMS) have been used as excipients in oral formulations because of their emulsifying effect as well as their ability to inhibit the precipitation and intestinal efflux of drugs. Excipient-drug compatibility studies, however, have been underexplored. In this study, benznidazole (BNZ) was selected as a drug model due to the difficulty in improving its solubility and because of the potential impact on public health (it is the only drug currently used to treat Chagas disease). The effect of different processing conditions (maceration, ball milling, and melting) on the physical-chemistry properties of BNZ/MGs mixtures was investigated to guide the rational development of new solid formulations. GML was more effective in improving the solubility of BNZ, which could be due to its more malleable structure, less hydrophobic nature, and greater interaction with BNZ. The formation of hydrogen bonds between the imidazole group of BNZ and the polar region of GML was confirmed by spectroscopy analyses (IR, 1H NMR). The higher the monoglyceride content in the mixture, the higher the BNZ solubility. Regardless of the method of processing the mixture, the drug was found to be crystalline. Polarized light microscopy analysis showed the presence of spherulites. Overall, these findings suggest that preparation methods of BNZ:MGs formulations that involve thermal or/and mechanical treatment have a low impact on the solid properties of the material, and this allows for the production of formulations with reproducible performance.

• Keywords
• Benznidazole, Compatibility study, Monoglycerides, Solubility,
• MeSH
• Glycerides MeSH
• Monoglycerides * MeSH
• Nitroimidazoles * MeSH
• Excipients MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• benzonidazole MeSH Browser
• Glycerides MeSH
• Monoglycerides * MeSH
• Nitroimidazoles * MeSH
• Excipients MeSH