Changsha Jingyi Pharmaceutical Technology Co., Ltd

Imidafenacin tablets are the first-line drug for the treatment of overactive bladder (OAB). However, the tablets need to be taken twice daily for up to 3-6 months, which highly reduces patient compliance. This study aimed to develop a long-acting imidafenacin transdermal patch (LAITP) with high drug loading using amorphous solid dispersion technology (ASD). ASD, consisting of polyvinyl pyrrolidone and imidafenacin, not only significantly increased the drug loading in the patch, but also inhibited drug crystallization. Furthermore, the formation mechanism of ASD was systematically elucidated using SEM, XRD, DSC, FT-IR, and molecular docking. The LAITP was optimized through single-factor investigations and ternary phase diagram analysis. It was confirmed by SEM and confocal Raman microscopy that ASD was a spherical microparticle with a size of 28.62 ± 8.91 µm in LAITP. Notably, under long-term and accelerated conditions of 3 months, the LAITP exhibited excellent stability to ensure the reliability of quality. Importantly, human pharmacokinetic studies demonstrated that LAITP with low skin irritation and favorable adhesion properties prolonged sustained effective plasma concentration in comparison to commercial tablets (Staybla®), reducing the frequency of administration and thereby improving patient compliance, which is expected to be a promising treatment option for patients with OAB.

Diabetes foot (DF) is one of the most serious chronic complications of diabetes. This study explored the relationship between serum interleukin-6 (IL-6), intercellular adhesion molecule-1 (ICAM-1) and soluble suppression of tumorigenicity 2 (sST2) and wound prognosis in 210 DF patients between January 2019 and January 2024. 210 DF patients were divided into the good prognosis (n = 147) and poor prognosis (n = 63) group according to the prognosis. Comparative analysis revealed that levels of serum IL-6, ICAM-1 and sST2 in the poor prognosis group were all higher than those in the good prognosis group significantly (P < .05). Multivariate logistic regression identified these 3 biomarkers as independent risk factors for poor wound healing (P < .05). Positive correlations between serum IL-6 (r = 0.269), ICAM-1 (r = 0.302), sST2 (r = 0.289) levels and poor prognosis were confirmed through Pearson's correlation analysis. A prediction model was established to analyse their predictive value. The training and validation sets ROC curves had AUCs of 0.79 (0.71-0.87) and 0.75 (0.59-0.91) respectively. Calibration curves were plotted to evaluate the consistency of the model, and the results showed that the predictive value of the nomogram model was similar to that of the actual one. Decision curves were plotted, which showed that the nomogram had higher positive net benefit in the range of 20% to 60%. This study suggest that serum IL-6, ICAM-1, and sST2 levels may serve as valuable prognostic indicators for wound healing progression in DF patients, with combined biomarker assessment showing potential clinical utility for outcome prediction. The total sample size (n = 210), with validation set (n = 63) of this study are relatively limited and the representativeness is restricted, which may affect the universality of the research conclusions.

The microstructures of pharmaceutical preparations play a pivotal role in determining their critical quality attributes (CQAs), such as drug release, content uniformity, and stability, which greatly impact the safety and efficacy of drugs. Unlike the inherent molecular structures of active pharmaceutical ingredients (APIs) and excipients, the microstructures of pharmaceutical preparations are developed during the formulation process, presenting unique analytical challenges. In this review, we primarily focus on presenting the research methods used to elucidate the microstructures of pharmaceutical preparations, including X-ray imaging (XRI), scanning electron microscopy (SEM), atomic force microscopy (AFM), Raman spectroscopy, infrared (IR) spectroscopy, and rheometer technology. Subsequently, we highlight the applications, advantages, and limitations of these methods. Finally, we discuss the current challenges and future perspectives in this field. This review aims to provide a comprehensive reference for understanding the microstructures of pharmaceutical preparations, offering new insights and potential advancements in their development.