Overview of the pharmacokinetics and pharmacodynamics of URAT1 inhibitors for the treatment of hyperuricemia and gout.

INTRODUCTION: Hyperuricemia is a common metabolic disease, which is a risk factor for gouty arthritis and ureteral stones and may also lead to cardiovascular and chronic kidney disease (CDK). Therefore, hyperuricemia should be treated early. Xanthine oxidase inhibitors (XOIs) and uricosuric agents (UAs), which target uric acid, are two types of medications that are used to treat gout and hyperuricemia. XOIs stop the body from producing excessive uric acid, while UAs eliminate it rapidly via the kidneys. Urate transporter 1 (URAT1) belongs to the organic anion transporter family (OAT) and is specifically localized to the apical membrane of the epithelial cells of proximal tubules. Unlike other organic anion transporter family members, URAT1 identifies and transports organic anions that are primarily responsible for urate transport. AREAS COVERED: This article reviews the pharmacokinetics and pharmacodynamics of the existing URAT1 inhibitors to serve as a reference for subsequent drug studies. EXPERT OPINION: The URAT1 inhibitors that are currently used as clinical drugs mainly include dotinurad, benzbromarone, and probenecid. Results indicate that RDEA3170 may be the most promising inhibitor, in addition to SHR4640, URC-102, and MBX-102, which are in the early stages of development.

The effects and underlying mechanisms of medicine and food homologous flowers on the prevention and treatment of related diseases.

The theory of medicine and food homology has a long history in China. Numerous traditional Chinese medicinal could be used as both medicine and food. Many flower medicinal materials also belong to the homology of medicine and food, such as Chrysanthemum morifolium, Lonicera japonica, Crocus sativus, and Lonicera macranthoides. They mainly contain flavonoids, organic acids, terpenoids, and other active ingredients, which have a variety of medicinal values, including anti-inflammatory, anti-tumor, and antioxidant. There are many formulations and functional foods containing these plants in Chinese medicine, which have a variety of nutritional and health effects on the human body. In this review, 10 widely used flowers were selected to review their pharmacological activities, prevention and treatment of related diseases and underlying mechanisms, and discussed the current limitations and future development prospects, hoping to provide references for the research on the development and utilization of natural medical flowers. PRACTICAL APPLICATIONS: The "homology of medicine and food" flowers have a wide range of uses and are of great research value. In this paper, we introduce 10 "homology of medicine and food" flowers. Their active ingredients, pharmacological activities, and treatments for related diseases are reviewed, and the limitations and development prospects of the "homology of medicine and food" flowers are discussed. It is hoped that this will contribute to the development of the food and pharmacological fields.

Preparation of an isorhamnetin phospholipid complex for improving solubility and anti-hyperuricemia activity.

To improve the solubility and anti-hyperuricemia activity of the insoluble natural flavonoid isorhamnetin (ISO), an isorhamnetin phospholipid complex (ISO-PC) was prepared. ISO-PC was prepared through solvent evaporation and its prescription process was optimized. The formation of ISO-PC was verified via multiple characterization methods. Parameters such as drug loading, solubility, octanol-water partition coefficient, stability, and in vivo anti-hyperuricemia activity of ISO-PC were investigated. The complexation efficiency of ISO-PC was 95.1% ± 0.56%. The characterization results confirmed that ISO-PC was bound by intermolecular interactions between ISO and phospholipids. Compared with ISO, the solubility of ISO-PC in water and 1-octanol increased by 122 and 16.5 times, respectively. In addition, the octanol-water partition coefficient decreased to 1.08. Pharmacodynamic studies have reported that ISO-PC has a more significant effect on reducing serum uric acid levels and renal protection. In conclusion, the findings of this study suggested that ISO-PC could be used as a promising formulation to improve the solubility and the anti-hyperuricemia activity of ISO.