International Journal of Pharmaceutics最新文献

{"title":"Rosuvastatin/calcium carbonate co-precipitated nanoparticles: A novel synergistic approach enhancing local bone regeneration in osteoporotic rat model.","authors":"Noha S El-Salamouni, Mennatallah A Gowayed, Samar El Achy, Maha El Shahawy, Doaa A Ghareeb, Shaymaa A Abdulmalek, Abeer A Kassem, Gihan S Labib","doi":"10.1016/j.ijpharm.2024.124977","DOIUrl":"10.1016/j.ijpharm.2024.124977","url":null,"abstract":"<p><p>This study aimed at preparing sustained release rosuvastatin (Ru) calcium carbonate (CC) co-precipitate nano-formulation for local intra-osseous application in osteoporotic rats. Nano-formulations were prepared by the co-precipitation method using different concentrations of polyvinyl alcohol (PVA) (0.2, 0.4, 0.6 %) as a stabilizer and equimolar ratios of calcium chloride and calcium carbonate (0.1, 0.3 or 0.5 M). Pre-formulation examination including; FTIR and X-ray diffraction confirmed the formation of CC nanoparticles in a crystalline structure that was preserved before and after loading with Ru. The optimized formula showing; PS of 105.71 ± 5.10 nm, PDI of 0.25 ± 0.02, ZP of -44.70 ± 0.09 mV, % EE of 60.16 ± 1.58 and a quasi-spherical nanoparticle with nano-deposition of Ru crystals adsorbed on them as seen under TEM and SEM, was then integrated in 20 % Pluronic gel. The Ru-gel exhibited good rheological behavior with a short gelation time of 20 sec and a sustained release pattern of 30 % for the optimized Ru/CC gel versus ≈ 90 % for the Ru/CC dispersion after 6 h. In-vivo, ovariectomy-induced osteoporotic rats were used to cause a bone defect in the tibial metaphysis. The drill-hole defects were then filled with the formulations under test and examined 30 days postoperatively. Through SEM-EDX scanning, histological assessments, and evaluation of bone metabolic markers, Ru/CC treatment significantly enhanced bone healing, improved bone microarchitecture, increased trabecular bone area, enhanced osteogenic gene expression, and reduced osteoclast activity. Experiments proved that Ru/CC successfully enhances osteogenesis and reduces osteoclastogenesis, proposing it as a promising therapeutic approach for enhancing bone regeneration in osteoporosis.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"124977"},"PeriodicalIF":5.3,"publicationDate":"2025-01-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142695376","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Vat photopolymerization 3D printing optimization: Analysis of print conditions and print quality for complex geometries and ocular applications.","authors":"Parvin Shokrollahi, Piyush Garg, David Wulff, Alex Hui, Chau-Minh Phan, Lyndon Jones","doi":"10.1016/j.ijpharm.2024.124999","DOIUrl":"10.1016/j.ijpharm.2024.124999","url":null,"abstract":"<p><p>3D printing, also known as additive manufacturing, continues to reshape manufacturing paradigms in healthcare by providing customized on-demand object fabrication. However, stereolithography-based 3D printers encounter a conflict between optimizing printing parameters, requiring more time, and print efficiency, requiring less time. Moreover, commonly used metrics to assess shape fidelity of 3D printed hydrogel materials like 'circularity' and 'printability' are limited by the soft nature of hydrogels, that can cause irregularities in their boundary. To unlock the full potential of 3D printing of biomaterials, it is also necessary to understand correlation between printing parameters and ink properties. In this work, a method based on curing depth, overcuring (cumulative cure), and print thickness was developed, which enables a time-efficient and reliable determination of printing conditions for complex geometries using gelatin methacrylate hydrogel biomaterial ink. We also examined the impact of printing direction on the print quality in terms of object/print thickness and aspect ratio. Moreover, the effects of dye concentration, exposure time, and layer thickness on print quality were evaluated, with discussions focused on the correlation between print dimension to layer thickness. Further evaluation was achieved by successfully printing bioinspired corneal stroma-like scaffold and delicate structures like a contact lens and a model eyeball, substantially expanding the scope of this method in producing high-quality prints with intricate details. We also demonstrate the effectiveness of 'Feret ratio,' another measure of object shape, in assessing the shape fidelity of different prints. Overall, the results highlight the practical potential of this method in enhancing the speed and reliability of the 3D printing processes involving complex geometries using a low-cost 3D printers.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"124999"},"PeriodicalIF":5.3,"publicationDate":"2025-01-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142716115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In vivo pharmacokinetic study and PBPK modeling: Comparison between 3D-printed nanocrystals and solid dispersions.","authors":"Lucia Lopez-Vidal, Mariano Tinti, Maria Elisa Melian, Lucila Canton, Matias Lorenzutti, Laureano Schofs, Maria Lina Formica, Alejandro J Paredes, Sergio Sanchez Bruni, Nicolas Litterio, Ricardo Faccio, Santiago Daniel Palma, Juan Pablo Real","doi":"10.1016/j.ijpharm.2024.125063","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2024.125063","url":null,"abstract":"<p><p>The solubility of drugs remains one of the most challenging aspects of formulation development. Several technologies exist to enhance the properties of poorly soluble drugs, with nanocrystal (NC) and solid dispersion (SD) technologies being among the most important. This work compared NCs and SDs under identical conditions using albendazole as a model drug and 3D printing technology as the delivery method. SDs were initially prepared and characterized, and then compared to the NCs system. Techniques such as TGA, DSC, XRD, FTIR, SEM, and Raman spectroscopy were employed to assess the solid-state properties and formulation homogeneity. Solubility and dissolution profiles were evaluated under simulated gastric and intestinal conditions. An in vivo pharmacokinetic study in dogs compared 3D-printed formulations (NC-3D and SD-3D) with a control group treated with the pure drug (ABZ-C) was carry out. A PBPK model was developed also in dogs to further analyse the results. While no statistically significant differences were observed in the in vitro dissolution profiles in 0.1 N HCl, differences emerged in precipitation time and solubility at intestinal pH (6.8). The pharmacokinetic study revealed improvements in the pharmacokinetic profile of both systems compared to the control, as expected. Between the NCs and the SD, the NC system demonstrated significantly superior pharmacokinetic parameters of interest. The PBPK model helped explain the differences observed in the in vivo study. The results suggest that nanocrystal technology is more effective at enhancing the in vivo performance of Class II drugs, at least when using albendazole as the model drug.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125063"},"PeriodicalIF":5.3,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142864127","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"How can language models assist with pharmaceuticals manufacturing deviations and Investigations?","authors":"Hossein Salami, Brandye Smith-Goettler, Vijay Yadav","doi":"10.1016/j.ijpharm.2024.125100","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2024.125100","url":null,"abstract":"<p><p>Large Language Models (LLM) such as the Generative-Pretrained-Transformer (GPT) and Large-Language-Model-Meta-AI (LLaMA) have attracted much attention. There is strong evidence that these models perform remarkably well in various natural language processing tasks. However, how to leverage them in domain-specific use cases and drive value remains an open question. Focusing on the digital transformation in the pharmaceutical manufacturing space, we propose that leveraging historical records of manufacturing deviations, as a mostly unstructured data source, in an organization can be beneficial for productivity, efficiency, quality, and compliance, specifically for addressing and closing new cases, or de-risking new manufacturing campaigns by identifying common themes and occurrences. Herein, by constructing an industrially relevant dataset, the ability of generative LLMs (e.g., GPT and Claude) and text embedding models in performing tasks related to pharmaceutical manufacturing deviations are studied. Generative models are evaluated for automating knowledge extraction from deviation reports in a mature organization, while embedding models are evaluated for identification of similar incidents from a large body of historical records using similarity analysis in vector space. Results show highly accurate outcomes for entity extraction tasks, especially with larger models, strong reasoning capabilities, as well as an interplay between the apparent reasoning and hallucination behavior of LLMs. Results also show the ability of embedding models for capturing semantics in certain deviation categories. Overall, these findings suggest significant potential for enhancing workflows in the pharmaceutical manufacturing through AI-driven tools, while also highlighting important questions that necessitate further research.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125100"},"PeriodicalIF":5.3,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142864125","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Intracellular mechanistic insights into cRGD-modified Bi₂Se₃ nanofoams for enhanced photothermal therapy via exocytosis inhibition.","authors":"Li Ding, Xinghua Yu, Shihao Cai, Azhar Mahmood, Wenjing Meng, Xiaotong Liu, Jiahan Liu, Jieyun Li, Xuejuan Zhang, Chuanbin Wu","doi":"10.1016/j.ijpharm.2024.125093","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2024.125093","url":null,"abstract":"<p><p>The cRGD peptide surface coating strategy for photothermal therapy nanoplatforms shows great promise in developing safe and effective cancer therapies. However, the precise intracellular mechanisms of these platforms remain unclear due to the complexity of intracellular trafficking and nano-bio interactions. This study investigates the nano-bio interactions of Bi₂Se₃ nanofoams, a representative photothermal therapy nanoplatform, coated with cRGD peptide in cancer cells, focusing on endocytosis, exocytosis, and cellular trafficking. Our findings reveal that the cRGD-coated Bi₂Se₃ nanofoams are internalized through three distinct endocytosis pathways: Rab34-mediated macropinocytosis, caveolae-dependent, and clathrin-dependent endocytosis. These nanofoams then accumulate in lysosomes via autophagy. Furthermore, inhibiting exocytosis reduces the loss of these nanofoams from cancer cells, enhancing photothermal and chemotherapy effects. This exocytosis-inhibiting strategy demonstrates significant potential for cancer therapy, validated by successful in vitro and in vivo results.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125093"},"PeriodicalIF":5.3,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142864143","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring the hydrate landscape using data mining on the Cambridge structural database (CSD).","authors":"Minqi Fu, Jiayu Dai, Jingtao Xu, Anders Østergaard Madsen, Jukka Rantanen","doi":"10.1016/j.ijpharm.2024.125075","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2024.125075","url":null,"abstract":"<p><p>With the continued relevance of drug hydrates in pharmaceutical sciences, a comprehensive understanding of hydrate and anhydrate forms is essential, not only through individual case studies but also from a broader, systematic perspective. The Cambridge Structural Database (CSD) is a well-established database for crystal structures of organic molecules and here, the structural features of pharmaceutically relevant compounds forming hydrates were explored. Drug anhydrate and hydrate subsets were generated and further classified into separate anhydrate and hydrate sets for free drug, cocrystal/solvate, salt, multicomponent cocrystal/solvate, and salt cocrystal/solvate systems. A thorough understanding of these sets was documented at molecular and structural levels. The CSD drug subset contains 24% of entries as hydrates and 76% as anhydrates. Only 6% of anhydrates have corresponding hydrate forms in the CSD drug subset. The formation of hydrates seems to be still less documented in multicomponent drug hydrates, as well as polymorphism of hydrates is less explored for these increasingly complicated systems with a high number of components. The presence of water molecules or additional components does not necessarily lead to a higher degree of crystal packing. Water is involved in 44% of hydrogen bonds (H-bond) in drug hydrate set, where water prefers to act as H-bond donor. H-bonds formed only by water show a relatively high bond strength. This work demonstrates the potential of data science in analyzing pharmaceutically relevant databases to uncover hidden patterns, and more specifically utilizing the CSD for understanding structural aspects and the role of water in H-bond patterns in drug hydrates.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125075"},"PeriodicalIF":5.3,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142864118","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Release-modulating mechanism and comparative pharmacokinetics in beagle dogs of bethanechol-loaded oral dosage forms.","authors":"Hyeong-Mo Jeong, Hansol Kim, Taeyeon Jang, Ayoung Choi, Jun-Bom Park, Chulhun Park, Beom-Jin Lee","doi":"10.1016/j.ijpharm.2024.125091","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2024.125091","url":null,"abstract":"<p><p>Bethanechol chloride (BTC), a quaternary ammonium compound used in bladder dysfunction treatment, requires challenges in developing optimal oral dosage forms due to its high water-solubility, short half-life, rapid elimination and four times a day administration. The aim of this study was to develop optimal BTC-loaded oral dosage forms that could provide both rapid onset and sustained therapeutic effects while reducing the frequency of conventional four-times-daily dosing (Mytonin® tablets). Four different BTC-loaded oral dosage forms were designed including gastro-retentive tablet (GRT), controlled-release tablet (CRT), bilayer tablet (BLT), and tablet-in-tablet (TIT). Then, release-modulating mechanism and in vivo pharmacokinetics in beagle dogs were compared. The release profiles of the four BTC-loaded dosage forms varied according to system design and formulation composition. The optimized GRT F-5 showed rapid buoyancy within 15 s and floated for 12 h, while continuously releasing the drug. CRT showed Fickian diffusion release, whereas BLT and TIT exhibited biphasic immediate and sustained release profiles. Polymer swelling behavior was analyzed using the Vergnaud model, where GRT F-5 and CRT showed n values < 0.5, confirming diffusion-controlled polymer hydration mechanism. In the instrumental analysis, the hydrogen bonding formation of BTC with release-modulating polymers, such as hydroxypropyl methylcellulose and polyethylene oxide and loosening of the polymer structure was crucial as the water influx increased. In pharmacokinetic studies in beagle dogs, the area under the plasma concentration-time curve (AUC) by normalizing dose for 48 h for GRT, CRT, BLT, and TIT were 90.2 %, 108.6 %, 83.8 %, and 76.4 %, respectively, compared with that of the reference drug (Mytonin® tablets, immediate release, four times a day). Interestingly, the plasma maximum concentration (C_max) and AUC)_0-12h of GRT F-5 and and Mytonin® tablets for the first 12-h period were much higher compared with that of other BTC-loaded CRT, BLT, and TIT. BTC was absorbed throughout the gastrointestinal tract, but is preferably absorbed in the stomach and upper intestinal sites. However, the GRT F-5 could provide more therapeutic potential for improving patient compliance in bladder dysfunction treatment by achieving both rapid onset and sustained drug release with reduced dosing frequency.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125091"},"PeriodicalIF":5.3,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142864146","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Intracorneal iontophoretic delivery of triamcinolone acetonide prodrugs: Physicochemical parameters guiding electrotransport.","authors":"Verena Santer, Deborah Chiara Minzaghi, César Eulogio Serna-Jiménez, Yogeshvar N Kalia","doi":"10.1016/j.ijpharm.2024.125096","DOIUrl":"10.1016/j.ijpharm.2024.125096","url":null,"abstract":"<p><p>Intracorneal delivery of ten amino acid (alanine, arginine, asparagine, glutamine, glycine, histidine, isoleucine, lysine, methionine and valine) ester prodrugs of triamcinolone acetonide (TA-AA) was investigated in vitro, using a corneal iontophoresis device (IONTOFOR-CXL; SOOFT Italia S.p.A.) approved for clinical use in the treatment of keratoconus. Short duration iontophoresis (1 mA for 5 min) was performed and intracorneal deposition of TA was quantified by HPLC-UV and UHPLC-MS/MS. The data evidenced the clear advantage of TA-AA prodrug iontophoresis compared to passive delivery and revealed unexpected and prodrug dependent deposition profiles. Despite their superior electrical mobility, intracorneal delivery of dications, TA-Arg and TA-Lys, did not outperform that of TA-Ala and TA-Gly. In silico investigations to relate the TA-AA prodrugs' physicochemical properties to their electrotransport confirmed that increased lipophilicity potential did not favour iontophoretic transport. For TA-Ala and TA-Gly, it was hypothesized that the greater charge distribution and decreased tendency to interact with the corneal tissue via electrostatic and H-bonds contributed to their successful iontophoretic delivery. Intracorneal biodistribution of TA confirmed that TA-Gly iontophoresis resulted in supratherapeutic concentrations in deep corneal stroma, exceeding TA IC₅₀ by ∼ 10⁴-fold. The results clearly demonstrated the successful combination of the clinically approved SOOFT iontophoretic device and the TA-AA prodrugs for targeted corneal iontophoretic delivery.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125096"},"PeriodicalIF":5.3,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854127","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Multiple hour antifibrotic drug release enabled by a thermosensitive quadpolymer.","authors":"Friederike L Jayes, Ria D Corder, Robert B Vachieri, Saad A Khan, Darlene K Taylor","doi":"10.1016/j.ijpharm.2024.125097","DOIUrl":"10.1016/j.ijpharm.2024.125097","url":null,"abstract":"<p><p>Injectable drug delivery for uterine fibroid therapy is an ambitious, possibly fertility-preserving concept, that could meet the challenges associated with the structure of these tumors and their location in the uterus. This study was conducted to advance a thermosensitive injectable quadpolymer for effective sustained release of anti-fibrotic drug formulations and to evaluate the feasibility of its use for delivery of the anti-fibrotic drug pirfenidone as a therapy to reduce fibroid cell proliferation. A series of quadpolymers were prepared by free radical polymerization of N-isopropylacrylamide (NIPAM) with different amounts of polylactic acid functionalized hydroxyethyl methacrylate (HEMA-PLA), acrylic acid (AAc), and methacrylate functionalized hyperbranched polyglycerol (HPG-MA) to optimize the sol-gel phase transition temperature and mechanical stiffness. Poly(NIPAM-co-HEMA-PLA-co-AAc-co-HPG-MA) with feed ratio (83-7-1-9), at 17% w/v, readily formed an aqueous solution that could be manipulated by syringe at room temperature. The quadpolymer also rapidly formed a stable gel at physiological body temperature, and partially biodegraded over time as confirmed by several spectroscopic characterization techniques. To evaluate the potential range of utility, quadpolymer 83-7-1-9 was loaded in-vitro with caffeine (a prototype hydrophilic drug) or the hydrophobic drug pirfenidone. Pirfenidone-loaded quadpolymer 83-7-1-9 formulations released 50% of drug loaded in double the time as compared to other reported liposome and nanoparticle injectable pirfenidone formulations. Furthermore, treatment of cultured fibroid cells with pirfenidone-loaded quadpolymer 83-7-1-9 formulations confirmed that activity of pirfenidone was preserved and proliferation of fibroid cells was inhibited. These results support that quadpolymer 83-7-1-9 is a promising candidate to be further developed for localized delivery of drugs for uterine fibroid therapy.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125097"},"PeriodicalIF":5.3,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854137","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Using in-line measurement and statistical analyses to predict tablet properties compressed using a Styl'One compaction simulator: A high shear wet granulation study.","authors":"Issa Munu, Andrei L Nicusan, Jason Crooks, Kendal Pitt, Christopher Windows-Yule, Andrew Ingram","doi":"10.1016/j.ijpharm.2024.125098","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2024.125098","url":null,"abstract":"<p><p>High shear wet granulation (HSWG) is widely used in tablet manufacturing mainly because of its advantages in improving flowability, powder handling, process run time, size distribution, and preventing segregation. In-line process analytical technology measurements are essential in capturing detailed particle dynamics and presenting real-time data to uncover the complexity of the HSWG process and ultimately for process control. This study is to find relationships between Lenterra in-line measurements and granule properties and tablet properties. The Styl'One Evolution compaction simulator was used to produce tablets that mimic an industrial rotary tablet press, which is different from the Gamlen used in our previous study. Furthermore, this research provided an understanding of the granule growth mechanisms during the granulation process, revealing that an induction granule growth mechanism occurs. This is specific to the material and process conditions studied. The model developed using data from a Gamlen tabletting press demonstrated high predictability for data generated using the Styl'One Evolution compaction simulator, with an R² value of 0.9535 and a RMSE of 0.4040 MPa. This finding highlights the ability of the model to predict tablet tensile strength independently of the compaction machine used, suggesting industrial-scale applications. The findings of this research provide substantial advances in understanding and monitoring the granulation process, with promising implications for scalable industrial processes.</p>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"125098"},"PeriodicalIF":5.3,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}