Solid Form Research Articles

One Part Method for Making Geopolymer Paste using Flocculated Sidoarjo Mud

Some efforts have proposed the utilization of Sidoarjo mud for geopolymer paste. However, the original dry mud in geopolymer concrete showed decreased compressive strength and increased required water. In this paper, the one-part method is proposed to reduce the water in the mixture. First, the mud was chemically flocculated. Then, the dry mud was mixed with fly ash, activated geothermal silicate, and sodium hydroxide mixture in solid form before then the distilled water was added. This reduced the required water to 50% compared to the two-part method. The flocculant sedimented heavy metal that resulted in higher compressive strength at a later age. At 28 days, dry flocculated mud showed higher compressive strength than the original dry mud, with a compressive strength of 13 MPa and 11 MPa, respectively. This is because of the increase of silica, alumina, and iron content from 70% in dry LUSI to 75% in dry flocculated mud.

Investigation of Avocado Pear (<i>Persea americana</i>) Seed Starch as Binder and Disintegrant in the Formulation of Paracetamol Tablet

<i>Background</i>: Avocado pear seeds are usually discarded as agricultural waste, the need arises therefore, to investigate their potentials as pharmaceutical excipients. Objective: The objective of this research was to extract, characterize, formulate and do in-vitro evaluation of the formulated paracetamol tablets. <i>Methods</i>: Ripe avocado (<i>Persea americana</i>) fruits were harvested in the month of April from a farm at Okada town. The seeds were authenticated by a taxonomist at the Department of Plant Biology, University of Benin, with Harbarium number UB/PB/24 0201. The seeds were prepared, dried and milled to fine powder and extracted using a standard procedure by Silva <i>et al</i>., 2013. The powder was subjected to phytochemical analysis and characterized for its micromeritic properties, and high-resolution analyses using differential scanning calorimetry, fourier transform infrared spectroscopy, scanning electron microscopy and x-ray diffractometry. Batches of paracetamol granules were prepared with avocado starch powder as disintegrant (2.5 - 15%w/w) and starch mucilage as binder (5.0 – 15 %w/v) using the wet granulation method. Granule flow properties were investigated before compression into tablets. Tablets were evaluated for physicochemical properties and drug-excipient interaction was investigated using DSC and FTIR. <i>Results</i>: Phytochemistry shows presence of saponins, flavonoids, tannins, alkaloids and glycosides. The starch was light-brown, odorless, tasteless and smooth in texture. Slightly soluble in water at room temperature, melting point range 102 - 114°C, moisture content 22.7 ± 2.40%; hydration capacity 2.76 ± 1.20 (g/g), swelling and moisture sorption capacities of 46.43 ± 1.50% and 115.34 ± 1.55%, respectively. Thermogram exhibited a single sharp peak of the extracted starch, FTIR shows no interactions, SEM and XRD results confirmed semi-crystalline powder with fluffy discrete particles. Granules exhibited fair to good flow properties; the tablets were uniform in weight, mean hardness values ≥ 58.84 N, friability 0.14 -1.56 %, disintegration times 0.50 – 11.12 mins and variable drug release 72.78 - 90.67% in 1.0 h. sss<i>Conclusion</i>: Tablets formulated with the extracted starch as disintegrant gave superior tablet properties, hence a viable local substitute that can be employed at higher concentrations as super-disintegrant and good mucilage binder at higher %w/v concentrations for oral solid dosage formulations.

The Properties of Waste Cooking Oil Soap with Avocado Waste Extract as Filler

The research investigated the production of bar soap formulation using waste cooking oil (WCO) and avocado waste extract as a filler to enhance its functional properties and provide additional benefits for human skin. The research involved refining WCO, extracting avocado seed and peel bioactive compounds, preparing the solid soap formulation, and conducting various tests to evaluate its pH, cleansing ability, organoleptic properties, and irritation potential. The results indicated that all of the soap formulations met Indonesia National Standard (SNI) for pH and exhibited comparable cleansing power to commercial soaps. Organoleptic tests revealed moderate levels of hardness, foam, odor, texture, and tight impression. Irritation tests identified WCO bar soap that four of six formulations did not cause skin irritation. Overall, the WCO bar soap containing 10% (w/w) avocado peel extract, demonstrated promising properties and met all the established criteria. Future research should focus on characterizing specific chemical compounds in the soap, exploring additional natural extracts with antioxidant and anti-allergic activities, and further analysis quantitatively is required to ensure the product's quality and clinical efficacy.

Enhancing 3D-Printed Chocolate Drug Delivery: The Role of Soy Lecithin in Improving Formulation Printability and Consistency

Abstract Objectives This study explores the potential of extrusion-based 3D printing to improve medication adherence by developing chocolate-based oral dosage forms incorporating active pharmaceutical ingredients such as paracetamol and ibuprofen, while using soy lecithin as an emulsifier to enhance the flow properties of the chocolate formulation, enabling consistent and reliable 3D printing of the dosage forms. Methods Extrusion-based 3D printing was used to obtain drug-loaded solid oral dosage forms. The formulation components as well as the printing design and conditions were optimised, to enhance the appearance and patient acceptability of the final products. Techniques such as spectroscopy, thermal analysis, rheology, mechanical analysis and in-vitro dissolution were employed to assess the physicochemical properties of these formulations. Key Findings: Soy lecithin was essential in obtaining robust and consistent dosage forms. The formulations showed good physicochemical stability of the components and demonstrated consistent drug release. Conclusions The findings suggest that extrusion-based 3D printing, with the aid of emulsifiers such as soy lecithin, is a viable method for producing personalised, chocolate-based drug delivery systems, potentially improving adherence through customizable dosage forms. Further research could enhance understanding of factors such as particle size, crystallinity, and the impact of chewing on drug release, to optimise therapeutic outcomes.

An invitro investigation on the physicochemical properties of different quercetin formulations.

Quercetin is a naturally occurring plant flavonoid commonly used as a nutritional supplement due to its antioxidant and anti-inflammatory properties. Its well-known low bioavailability has led to the design of different quercetin formulations by various commercial entities seeking to market a highly bioavailable quercetin product. This study investigates four different commercially available quercetin formulations (LMQ, QUX, QUO, and QUV) for their physicochemical properties that influence bioavailability. LMQ and QUX are liquid-based formulations while QUO and QUV are solid powder-based formulations. Studies were conducted on particle size using a particle size analyzer; solubility (in water, simulated gastric and intestinal fluid) using Ultra High Performance Liquid Chromatography (UHPLC) to quantify the quercetin content; intestinal permeability and toxicity using Caco-2 cells and HepG2 liver cells. LMQ and QUX had the narrowest particle size distribution as well as the highest solubility while QUO and QUV had the widest particle size distribution but the poorest solubility. One formulation (QUO) exhibited a significant reduction in cell viability with HepG2 and Caco-2 cells including a significant decrease in TEER value change (-39.0 %; p<0.01); its higher Caco-2 cell permeability (Papp 2.85×10-4±4.22×10-5; p<0.05) likely resulted from reduced membrane integrity. The other formulations significantly increased the TEER value within the first 4 h (≥22.7 %; p<0.05). The particle size distribution of each of the individual formulations reflected their solubilities in water and gastrointestinal fluids. Despite QUO having the highest permeability, its negative change in TEER value over time revealed its evident cytotoxic effects. QUV performed poorly in terms of solubility, and permeability. LMQ and QUX were the most consistent across each study with LMQ performing better than QUX overall. Findings of this study present one formulation (LMQ) with superior intestinal absorption while maintaining high cell viability, thus making it one of the safer and more effective quercetin formulations.

Rapidly Generated, Ultra-Stable, and Switchable Photoinduced Radicals: A Solid-State Photochromic Paradigm for Reusable Paper Light-Writing.

Although photochromic molecules have attracted widespread interest in various fields, solid-state photochromism remains a formidable challenge, owing to the substantial conformational constraints that hinder traditional molecular photoisomerization processes. Benefiting from the significant color change upon radical generation, chemical systems enabling a photoinduced radical (PIR) behavior through photoinduced electron transfer (PET) could be ideal candidates for solid-state photochromism within minimized need of conformational freedom. However, the transient nature of radicals causes a dilemma in this Scheme. Herein, we present a general crystal engineering strategy for rapidly generated (7-s irradiation to saturation) and ultra-stable (lasting 12 weeks) PIRs in the solid state, based on the anti-parallel alignment of para-hydroxyphenyl groups of persulfurated arenes to form a strong non-covalent network for efficient PET and radical stabilization. Using this strategy, a PIR platform was constructed, with a superior photochromic behavior remaining in different solid forms (even in the fully-ground sample) due to their transcendent crystallization ability. On this basis, our compounds can be further processed into reusable papers for light-writing, accompanied by water fumigation for modulating the reversible process. This work provides new insights into addressing solid-state photochromism and can inspire a wide range of optical material design from the switchable radical perspective.

Ketoconazole-Fumaric Acid Pharmaceutical Cocrystal: From Formulation Design for Bioavailability Improvement to Biocompatibility Testing and Antifungal Efficacy Evaluation.

Development of cocrystals through crystal engineering is a viable strategy to formulate poorly water-soluble active pharmaceutical ingredients as stable crystalline solid forms with enhanced bioavailability. This study presents a controlled cocrystallization process by cooling for the 1:1 cocrystal of Ketoconazole, an antifungal class II drug with the Fumaric acid coformer. This was successfully set up following the meta-stable zone width determination in acetone-water 4:6 (V/V) and pure ethanol. Considering the optimal crystallization data, laboratory scale-up processes were carried out at 1 g batch size, efficiently delivering the cocrystal in high yields up to 90% pure and single phase as revealed by powder X-ray diffraction. Biological assays in vitro showed improved viability and oxidative damage of the cocrystal over Ketoconazole on human dermal fibroblasts and hepatocarcinoma cells; in vivo, on Wistar rats, the cocrystal increased oral Ketoconazole bioavailability with transient minor biochemical transaminases increases and without histological liver alterations. Locally on Balb C mice, it induced no epicutaneuous sensitization. A molecular docking study conducted on sterol 14α-demethylase (CYP51) enzyme from the pathogenic yeast Candida albicans revealed that the cocrystal interacts more efficiently with the enzyme compared to Ketoconazole, indicating that the coformer enhances the binding affinity of the active ingredient.

Review: Biomacromolecules‐based encapsulation technologies for the protection of oxygen‐sensitive next‐generation probiotics

AbstractIn the recent years, various strains of the gut microbiota have been discovered to possess significant therapeutic potential, they are defined as next‐generation probiotics (NGPs). Akkermansia, Faecalibacterium, Bacteriodes, Eubacterium, and Bifidobacteria are among the typical NGP strains which exhibit several interesting bioactivities as live biotherapeutics. However, some strains of NGP are extremely sensitive to oxygen, such as Faecalibacterium prausnitzii. This hinders their cultivation and large‐scale production. Therefore, it is essential to develop a strategy to protect them during production, storage, and colonic administration. This review, highlights key NGP strains developed in recent years, alongside the encapsulation strategies used to protect them. The primary criterion for selecting encapsulating techniques is their feasibility to be performed under strictly anaerobic conditions. Various processes have been selected according to the physical forms of the products, including liquid, gel, and solid forms, as well as the final shaping of the product. The critical factors for selecting encapsulation materials include biocompatibility, safety, effective oxygen barrier properties, and an optimal release profile in the gastrointestinal tract. This review discusses protection strategies aimed at improving the survival and thereby effectiveness of NGPs.

N-Phenylphenothiazine Radical Cation with Extended π-Systems: Enhanced Heat Resistance of Triarylamine Radical Cations as Near-Infrared Absorbing Dyes

N-Phenylphenothiazine derivatives extended with various aryl groups were designed and synthesized. These derivatives have bent conformation in crystal and exhibit high solubility. Radical cations obtained by one-electron oxidation of these derivatives gave stable radical cations in solution and showed absorption in the near-infrared region. A radical cation was isolated as a stable salt, which exhibited heat resistance up to around 200 °C. A design strategy for radical cation-based near-infrared absorbing dyes, which are easily oxidized and stable not only as a solution but in solid form, is described.

RESEARCH INSIGHTS ON AJAMODADI CHURNA: A COMPREHENSIVE REVIEW

Churna Kalpana is an important solid dosage form in Ayurvedic pharmaceutics. In this preparation, clean, dry drugs are powdered finely and sieved through cloth or sieve. Ajamodadi churna, a classical Ayurvedic formulation, is widely used by Ayurvedic practitioners. Significant number of research has been carried out on Ajamodadi churna. A thorough literary search through various portals like Research gate, DHARA, PubMed and other journals to gather research conducted on Ajamodadi churna revealed twenty-eight research articles and two review articles. Among twenty eight research articles, eight were pharmaceutical and analytical studies, six were pre-clinical and fourteen were clinical studies. Pharmaceutical studies have provided information on the purity, safety and quality of in-house and market-available Ajamodadi churna formulations. Pre-clinical studies have put light on safety and pharmacological activities. Clinical studies have demonstrated that Ajamodadi churna is beneficial in the said conditions either alone or in combination with other treatment depending on the pathology. Based on these researches conducted, it is established that Ajamodadi churna is useful in different conditions like Shvayathu, Amavata, Sandhi peeda, Gridhrasi.

Safety as a determining factor in the pharmaceutical drug development for patients of the pediatric population

Patients in the pediatric population are characterized by differences in the pharmacokinetics and pharmacodynamics of drugs and the range of acceptable dosage forms compared to adult patients. The development of safe drugs is designed to reduce the incidence of adverse reactions in this group. Aim. To highlight physiological features of the body of patients in the pediatric population, the corresponding differences in the pharmacological characteristics of drugs, and approaches to minimizing the risks of pharmacotherapy at the stage of pharmaceutical drug development. Materials and methods. Such general scientific theoretical methods as system analysis, generalization, and system approach, as well as the bibliographic method consisted in processing scientific sources of information on drug use in pediatrics and developing pediatric dosage forms were used. Results. When prescribing drugs to pediatric patients, the physiological features of the child’s body development should be considered, using a flexible approach to pharmacotherapy. Many drugs used in pediatrics have not been officially studied in pediatric clinical trials, and therefore, children often receive them off-label. The use of drugs in pediatrics requires special knowledge about the influence of age-related aspects of the child’s physiology on the absorption, distribution, metabolism and excretion of a drug, as well as on its interaction with receptors and organs. This article discusses approaches to the pharmaceutical development of drugs for use in the pediatric population. Conclusions. In pharmaceutical development of drugs for use in pediatric practice, it is necessary to keep in mind the features of drugs due to age and physiological factors in this category of patients, as well as to take into account the route of administration, the choice of the optimal dosage form, the safety profile of excipients, taste and ease of use of drugs. The development of new medicinal products, including multiparticulate solid dosage forms, is designed to improve the safety profile of drugs in children.

Research on Waterless Cosmetics in the Form of Scrub Bars Based on Natural Exfoliants

Scrub bars are an innovative alternative to traditional liquid, semi-liquid, and oily body scrubs. Through the elimination of water from their formulas, they align with the current ‘waterless’ trend in the cosmetics market. The aims of this study were to create anhydrous formulations for body scrub bars and to assess their physical, chemical, and sensory characteristics depending on the type of exfoliant added. A total of five solid body scrub formulations were developed using different natural exfoliants: sugar, microcrystalline cellulose, ground coffee beans, corn granules, and sodium chloride. The shape and dimensions of the exfoliant particles were characterized by scanning electron microscopy (SEM). The formulations were subjected to texturometric tests. The final products underwent color assessment along with a consumer evaluation of sensory appeal. The test results showed that the body scrubs exhibiting the highest hardness and adhesive force were those containing exfoliants with small particles, either angular (sodium chloride) or subrounded (Coffea arabica seed powder) in shape. Conversely, the lowest hardness was determined for the product formulated with the addition of an exfoliant with well-rounded particles (microcrystalline cellulose). Among the exfoliants tested, microcrystalline cellulose proved to be the most suitable for body scrubs, demonstrating superior texture and exfoliating effectiveness. However, cosmetics containing ground coffee received the highest esthetic ratings. Coffee gave the product a natural color and an appealing scent, as judged by the testers.

Preparation, Characterization and In Vitro Anticancer Activity of Sulforaphene-Loaded Solid Lipid Nanoparticles.

Sulforaphane (SFE) extracted from radish seeds has garnered significant research attention in recent years due to its notable biological activities, particularly its anticancer properties. However, SFE is highly sensitive to the environment; therefore, solid lipid nanoparticles (SLNs) were used to embed SFE to enhance its stability. SFE-SLNs were characterized and compared with free SFE to assess the impact of SLNs on SFE. The SFE-SLNs exhibited a spherical shape with a uniform and stable distribution. FTIR analysis suggested that SLNs might distribute SFE both within and on their surface. The SLNs effectively protected free SFE from breaking down at high temperatures, in water with pH levels between 2.0 and 9.0, and while being stored for over 8 weeks at 25 °C. In addition, the SFE in SFE-SLNs exhibited a sustained release compared to a sudden release of free SFE, leading to enhanced absorption in the intestine and improved bioavailability. Embedding SFE in SLNs did not make it less effective at killing cancer cells. This study provides an effective approach to improving the efficiency and stability of SFE, which could aid in incorporating its beneficial characteristics into products such as beverages, dairy products, solid formulations, and dietary supplements.

Scientific opinion on the extension of uses of quillaia extract (E 999) as a food additive.

The EFSA Panel on Food Additives and Flavourings (FAF Panel) evaluated the safety of the extension of uses of quillaia extract (E 999) as a food additive in food supplements supplied in a solid or liquid form, excluding food supplements for infants and young children. Quillaia extract (E 999) was re-evaluated in 2019 by the EFSA FAF Panel, which derived an acceptable daily intake (ADI) of 3 mg saponins/kg bw per day for E 999, while in 2024 a follow-up of the re-evaluation was published by the FAF Panel, recommending some modifications of the existing EU specifications for quillaia extract (E 999). Currently, quillaia extract (E 999) is authorised in two food categories (FCs) i.e. FC 4.1.4 'Flavoured drinks' and FC 14.2.3 'Cider and perry' (excluding cidre bouché, cydr jakościowy, perry jakościowe, cydr lodowy, perry lodowe). A 'food supplements consumers only' scenario was calculated for this opinion considering the proposed extension of uses, together with the current authorised uses at both the maximum permitted level (MPLs) and the typical reported use levels of quillaia extract (E 999) at the time of the 2019 re-evaluation. The Panel concluded that the exposure estimates using the typical reported use levels for the currently authorised food categories and considering the proposed extension of uses for E 999 in FC 17.1 'Food supplements supplied in a solid form, excluding food supplement for infants and young children' and FC 17.2 'Food supplements supplied in a liquid form, excluding food supplement for infants and young children', if authorised, would not result in an exceedance of the ADI in any population group.

Comparison of Solid Self-Nanoemulsifying Systems and Surface-Coated Microspheres: Improving Oral Bioavailability of Niclosamide.

This study aimed to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) and surface-coated microspheres to improve the oral bioavailability of niclosamide. A solubility screening study showed that liquid SNEDDS, prepared using an optimized volume ratio of corn oil, Cremophor RH40, and Tween 80 (20:24:56), formed nanoemulsions with the smallest droplet size. Niclosamide was incorporated into this liquid SNEDDS and spray-dried with calcium silicate to produce solid SNEDDS. Surface-coated microspheres were prepared using sodium alginate and poloxamer 407 and optimized through solubility and dissolution tests. Scanning electron microscopy, differential scanning calorimetry, and X-ray diffraction were used to evaluate the physicochemical properties of the prepared solid SNEDDS, surface-coated microspheres, and the drug alone. The solubility, dissolution, and oral bioavailability were also assessed. Physicochemical evaluation demonstrated that niclosamide was converted to an amorphous state in the Solid SNEDDS formulation, with enhanced solubility and oral bioavailability. In comparison to niclosamide alone, solid SNEDDS exhibited an increase in drug solubility (approximately 2500-fold vs 158-fold) and oral bioavailability (approximately 10-fold vs 1.65-fold), significantly outperforming surface-coated microspheres. This solid SNEDDS formulation may be an excellent candidate for niclosamide with improved oral bioavailability for repurposing.

Enhancing physicochemical properties of Hydrochlorothiazide with zwitterionic L-proline and 5-Fluorocytosine cocrystals through mechanochemical synthesis.

Hydrochlorothiazide (HTZ) is a thiazide-type diuretic drug approved by the FDA in 1959 for treatment of hypertension and peripheral edema and has been used since. HTZ exhibits low solubility and low permeability, leading to variable oral bioavailability and limited intestinal drug permeability. For this reason, several attempts to improve HTZ physicochemical properties have been made during the past decades. In the broad frame of molecular crystal engineering, significant efforts and promising results in the quest for more effective solid/dosage forms of HTZ, including studies on polymorphism and cocrystals, are being developed. As part of these efforts, we report here two new cocrystals of HTZ with the zwitterionic L-proline and the prodrug 5-Fluorocytosine. Both cocrystals show improvement in solubility and permeability, suggesting that these new solid forms could be used as new drug candidates to deliver HTZ in the antihypertensive therapy.

Recent Advances in Drying and Development of Solid Formulations for Stable mRNA and siRNA Lipid Nanoparticles.

Current RNA lipid nanoparticle (LNP) based products are typically liquid formulations that require ultra-cold storage temperatures for stability. To address this limitation, recent efforts have focused on enhancing stability and enabling room temperature storage by converting these formulations into solid forms through drying processes such as lyophilization, spray drying, and spray-freeze drying. Nevertheless, the drying process itself can influence the stability of RNA/LNP formulations. Therefore, understanding the factors that contribute to instability during drying is essential. The choice of drying technique for LNPs depends on factors such as the mode of delivery, lipid components, and desired final product characteristics. Additionally, the drying mechanism and associated stresses must also be carefully considered. Drying methods involve a range of process parameters related to formulation, process settings, and the manufacturing environment. It is essential to understand how these parameters influence the final solid-state products' attributes, including appearance, moisture content, flow properties, and reconstitution time, as these can significantly affect the physical and chemical stability of the formulation. This review focuses on various drying techniques and their impact on the stability of RNA/LNP-based systems.

Computer-Aided formulation design for pharmaceutical drug product development, part 01: Materials exploration through a visualization tool

An interactive tool has been developed to help design oral solid dosage form formulations. The tool enables quantitative explorations and comparisons of physical, bulk, and mechanical properties, and takes into account functional characteristics as well. In this manner, comparisons and clustering of both excipients and APIs can be carried out. These comparisons enable the generation of alternatives as well as surrogate identification, so as to spare resources and material.Multiple data sources were merged to create a “joint” data table with all relevant properties. Four main workflow activities are supported: Explore Materials, Search Similar APIs, Search Similar Excipients and Search Material Clusters.Multi-dimensional filtering can be superimposed to each functionality. Suggested visualizations are made particularly accessible by providing them as “standard plots”.The underlying philosophy is to empower formulation scientists to explore options, rather than prescribe decisions on exclusively mathematical grounds. The tool described here is the first step towards a holistic optimization incorporating predictions of mixture properties. Methodology of use is illustrated through three material selection application examples.

Recent Advances in Orally Disintegrating Tablet: Properties, Formulation and Production

: Healthcare practitioners, patients, and consumers widely recognize the convenience as-sociated with administering oral tablets. The emergence of orally disintegrating tablets (ODTs) represents a significant advancement in solid dosage forms, facilitating more convenient oral de-livery while maintaining medication safety, effectiveness, and quality. The ODTs market is ex-pected to experience continuous growth in the coming years despite the internal challenges faced by commercial manufacturers. This paper initiates a comprehensive discussion of the properties of ODTs, including palatability and taste, drug content, disintegration, mechanical strength, mois-ture content, safety, and efficacy. The formulation factors that affect each of these qualities are also discussed. Additionally, this review delves into the processes of the production of ODTs, en-compassing the approaches and technologies from the mixing of active ingredients and recipients to the formation and packaging of ODTs. This review provides valuable insights into the ad-vancement in ODTs technology, aiming to equip researchers with the knowledge necessary to improve quality and optimize efficiency, ultimately receiving high acceptance from patients or consumers.

The impact of volume of dissolution medium for biopredictive dissolution/permeation studies of enabling formulations: A comparison of two brands of telmisartan / amlodipine tablets.

For compendial dissolution testing of solid dosage forms, media volumes of 500 to 900 mL are used in apparatus I and II to ensure sink conditions. However, these volumes are considerably larger than those in the gastrointestinal tract. Thus, the experiments are not biomimetic and possibly not suitable for biopredictive dissolution testing. The present study investigates the influence of volumes of dissolution media in non-compendial dissolution/permeation settings. Dissolution/permeation studies of two commercial bilayer tablets (Twynsta® and Arrow) containing the active pharmaceutical ingredients telmisartan (40 mg) and amlodipine (10 mg) were evaluated using the MacroFlux tool with various biomimetic media mimicking fasted and fed states as well as biological variability ("biorelevant"). Particularly, the two-stage dissolution process of telmisartan from the tablets is interesting because the compound has a pH-dependent solubility, and 2-stage dissolution leads to supersaturation and precipitation upon pH shift. For telmisartan, lower dissolution volumes significantly induced precipitation, leading to lower permeation, while no precipitation was observed in the larger volume. The permeation of telmisartan was overly sensitive to both pH and micelle concentrations in the biomimetic media. Amlodipine showed complete dissolution under any conditions, which correlates with its known complete absorption in vivo. In conclusion, volumes of dissolution media (and their compositions) are key parameters and play a significant role for designing relevant biomimetic experiments used to predict the bioavailability of supersaturating systems.