Current Issue : April-June Volume : 2026 Issue Number : 2 Articles : 5 Articles
Background/Objectives: This study aimed to perform a comparative analysis of the original Viagra® product and sildenafil-containing tablets obtained from illegal sources (the darknet). Specifically, the analyzed material consisted of samples seized by Polish law enforcement authorities from unverified vendors operating within the Central European darknet market. The study utilized thermal methods, specifically Thermogravimetry (TG), Derivative Thermogravimetry (DTG), and calculated Differential Thermal Analysis (c-DTA), as well as colorimetric analysis based on the International Commission on Illumination (CIE) L*a*b* system. Methods: Thermal analyses enabled the assessment of the thermal stability of the tested samples, identification of characteristic stages of thermal decomposition, and determination of differences in thermal behavior between the pure substance, the original preparation, and darknet samples. In turn, color measurements in the CIE L*a*b* space allowed for an objective comparison of tablet appearance and determination of the degree of color similarity to the original product. Results: The obtained results showed that only a few samples (V1, V3, V4, V6, V8) exhibited features similar to the original Viagra®, both in terms of thermal profile and color. Most of the tested tablets were characterized by significant variability in physicochemical properties, indicating a lack of quality control and inconsistency in formulation. Samples V2 and V7 deviated particularly strongly—both thermally and visually—suggesting that they might not contain the original active substance or contained it in a different chemical form. Conclusions: The use of combined thermal and colorimetric methods proved to be an effective tool in the identification of counterfeit pharmaceutical products, enabling simultaneous evaluation of their composition and authenticity. The results confirm the validity of employing integrated physicochemical analyses for the detection of falsified medicines present on the illegal market....
Background/Objectives: This study explores the integration of Design of Experiments (DoE) with Physiologically Based Biopharmaceutics Modeling (PBBM) to streamline the development of extended-release (XR) formulations. Using donepezil (DPZ) as a model drug, we developed an optimized XR formulation exhibiting a dissolution profile comparable to the reference product, Aricept® (Eisai GmbH, Frankfurt, Germany). Methods: A Box–Behnken experimental design was applied to systematically evaluate how formulation variables—HPMC 100, HPMC 4000, and NaCMC—affect drug release kinetics, tablet hydration, and erosion. This strategy enabled the identification of optimal excipient concentrations with minimal experimental effort. Results: The in vitro dissolution data were then integrated into a PBBM framework to simulate drug release and pharmacokinetics, enabling virtual bioequivalence (VBE) assessments. The combined approach provided robust predictive insights into formulation performance, substantially reducing reliance on resource-intensive in vivo studies. Beyond its successful application with DPZ, this integrated methodology offers a scalable and generalizable strategy for efficiently developing bioequivalent XR formulations for various clinically relevant drugs. Conclusions: Our findings highlight the importance of leveraging advanced statistical methods and in silico modeling to overcome contemporary pharmaceutical development challenges, paving the way for innovative, cost-effective solutions that significantly accelerate time-to-market....
Saffron (Crocus sativus L.) is one of the most valued spices worldwide, rich in bioactive apocarotenoids such as crocins, picrocrocin, and safranal, which display antioxidant, neuroprotective, and anticancer properties. Saffron’s chemical composition is critical for its therapeutic efficacy and a combination of components appears essential to reach the best protection and increase tissue resilience, so stigmas were subjected to hydroalcoholic extraction followed by purification via solid-phase extraction to enriched crocin and picrocrocin fractions. The extracts were included in liposomes to enhance their bioavailability and gastrointestinal absorption by oral administration while protecting them in the harsh gastric environment, increasing their permeation and sustaining their release in the gastrointestinal tract. Liposomes were prepared by the reverse-phase evaporation method using saturated or unsaturated lipids extracted from soy. Encapsulation efficiency was determined by HPLC monitoring of trans-4GG crocin, cis-4GG crocin, and picrocrocin. The results indicate that liposomes show greater encapsulation capacity for hydrophilic apocarotenoids such as crocins (≈90% for cis-4GG, ≈50% for trans-4GG crocin) with respect to picrocrocins (<20%). These findings support the application of liposomal carriers to improve the stability, shelf-life, and potential bioavailability of saffron’s bioactive properties for nutraceutical, pharmaceutical, and functional food applications....
(1) Background: Fixed-dose combination (FDC) improves patient convenience and therapeutic adherence by combining suitable drugs in a single dose form. This study examined the in vitro dissolution of an ibuprofen-loratadine FDC oral suspension to commercial reference formulations. (2) Methods: The FDC suspension (ibuprofen 200 mg/5 mL, loratadine 5 mg/5 mL) was tested against Fenbro 8 Plus and Lorid on USP Apparatus II at 50 rpm and 37 ± 0.5 ◦C. Dissolution testing was carried out in 900 mL of phosphate buffer (pH 7.2) for ibuprofen and 0.1 N HCl (pH 3.3) for loratadine. Quantification was performed using validated high-performance liquid chromatography linked with ultraviolet detector (HPLCUV) procedures complying with the ICH Q2 (R2) guidelines. (3) Results: The linearity of the HPLC methods for ibuprofen and loratadine was (R2 > 0.99), accuracy (99.6–100.18%), and precision (%RSD < 2). For both loratadine and ibuprofen, the FDC suspension’s Q15, Q30, T50, T90, and DE% values nearly matched those of the commercial products. Over 95% of both drugs were released within 60 min. The dissolution equivalence between the FDC and the reference formulations was demonstrated by the calculated similarity (f 2) and difference (f 1) factors, which were f 1 = 3 and f 2 = 70 for ibuprofen, and f 1 = 4 and f 2 = 64 for loratadine. (4) Conclusions: The FDC suspension of ibuprofen and loratadine showed dissolving behavior comparable to commercial formulations, confirming its applicability for the practical and efficient treatment of allergy symptoms and inflammatory pain....
Freeze-drying has been a workhorse for the pharmaceutical industry to enable long-term storage and longdistance transport of drug products that are unstable in liquid or frozen form. The importance of freeze-drying was particularly evident in the development and storage of life-saving medicines such as mRNA-based vaccines during the COVID-19 pandemic. In response to growing demand for improved manufacturing efficiency, emerging freeze-drying technologies spurred by the U.S. Food and Drug Administration (FDA) Pharmaceutical Quality for the 21st Century Initiative have been introduced with the aim to modernize the pharmaceutical manufacturing sector. Here, we provide regulatory considerations for emerging technologies in pharmaceutical freeze-drying from a manufacturing perspective. We also present an analysis of current trends in freeze-drying and in-process controls submitted in human drug applications—24 New Drug Applications, 118 Abbreviated New Drug Applications, and 20 Biologics License Applications assessed between 2020 and 2023—seeking FDA approval. Additionally, we analyzed the Form FDA-483 Inspection Observations educed from 201 inspections conducted at manufacturing facilities performing freeze-dried parenteral operations between 2015 and 2019, to identify common compliance challenges and provide regulatory insights for the pharmaceutical industry....
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