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1.
Eur J Pharm Sci ; 191: 106601, 2023 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-37783379

RESUMEN

The aim of this work is to develop a novel simultaneous in vitro dissolution - in situ perfusion system (SDPS) as a potential tool to evaluate the in vivo performance of solid oral formulation in rat. The innovative nitrendipine (NTD) tablet of Bayotensin mite® made in Germany was used as reference listed drug (RLD), and five generic products from Chinese market were compared with RLD using the in vitro dissolution test method specified by the orange book and the SDPS method developed in this study. Four self-prepared NTD tablets with different proportions of microcrystalline cellulose/starch were employed to investigate the discriminatory ability of the SDPS for formulation. In addition, the predictivity of the SDPS in relation to data from in vivo pharmaceutics studies was evaluated. The 45-min dissolution test and multiple-pH dissolution profiles of generic product 1 and 2 have no difference compared with the RLD, but their dissolution profiles from the SDPS showed statistically significant differences. A biexponential formula successfully described the concentration profiles of self-prepared formulations in SDPS experiments. The kdis (0.08 ± 0.01 ∼ 0.2 ± 0.03 min-1) and ka (about 2.30 × 10-3 min-1) values calculated by the formulas of F1-F3 suggested that the used excipients had no effect on the intestinal absorption of NTD, and it might be the property of active pharmaceutical ingredient that led to the difference among the generics. Furthermore, the in vivo rat pharmacokinetics study results of F1-F3 showed a good correlation (R2 = 0.99) with the SDPS data. In summary, the SDPS is a promising tool to detect the unexpected quality changes of pharmaceutical products in weakly regulated markets, facilitate formulation screening, and potentially reduce animal testing for estimating the in vivo absorption behavior of solid oral formulations. The absorption performance of generic drugs in vivo should be further investigated.


Asunto(s)
Biofarmacia , Excipientes , Animales , Ratas , Solubilidad , Comprimidos/química , Excipientes/química , Perfusión , Administración Oral
2.
J Mech Behav Biomed Mater ; 146: 106081, 2023 10.
Artículo en Inglés | MEDLINE | ID: mdl-37651758

RESUMEN

Bacterial infection caused by trauma and chronic wounds in the most mobile area remains a challenge in clinic. It is difficult to achieve the synergistic effects of antibacterial capacity and skin regeneration using conventional therapeutic methods. Developing a multi-functional hydrogel dressing that can cope with the complex wound environment will contribute to the healing and therapeutic effects. In this work, a novel Cur@PAM/TA-Cu photothermal hydrogel delivery system was prepared by engineering tannic acid (TA) into covalent cross-linked polyacrylamide (PAM) on which the chelating tannic acid-copper metal-polyphenolic network (TA-Cu MPN) was imposed to form dual-crosslinked networks, and the natural medicine curcumin was loaded eventually. The molecularly engineered dual-crosslinked networks resulted in enhanced mechanical properties including bio-adhesion, tensile strength and self-healing, which made the hydrogel suitable for dynamic wound and various application scenarios. In addition, the excellent photothermal capacity, antioxidant effect and biocompatibility of the hydrogel were demonstrated. Notably, this curcumin loaded photothermal hydrogel exhibited superior antibacterial capacity (almost 100% killing ratio to E. coli and S. aureus) under 808 nm laser irradiation. Meanwhile, the in vivo wound healing experiment results revealed that the anti-inflammation and proangiogenic effect of Cur@PAM/TA-Cu hydrogel successfully shortened the healing time of wound and the reconstruction of skin structure and function. Thus, this dual-crosslinked multi-functional hydrogel delivery system is a promising wound dressing for accelerating wound healing.


Asunto(s)
Curcumina , Hidrogeles , Hidrogeles/farmacología , Cobre/farmacología , Curcumina/farmacología , Escherichia coli , Staphylococcus aureus , Cicatrización de Heridas , Antibacterianos/farmacología
3.
Med Gas Res ; 8(4): 135-143, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30713665

RESUMEN

Expending a considerable amount of physical energy inevitably leads to fatigue during both training and competition in football. An increasing number of experimental findings have confirmed the relationship between the generation and clearance of free radicals, fatigue, and exercise injury. Recently, hydrogen was identified as a new selective antioxidant with potential beneficial applications in sports. The present study evaluated the effect of 2-month consumption of hydrogen-rich water on the gut flora in juvenile female soccer players from Suzhou. As demonstrated by enzyme linked immunosorbent assay and 16S rDNA sequence analysis of stool samples, the consumption of hydrogen-rich water for two months significantly reduced serum malondialdehyde, interleukin-1, interleukin-6, tumour necrosis factor-α levels; then significantly increased serum superoxide dismutase, total antioxidant capacity levels and haemoglobin levels of whole blood. Furthermore, the consumption of hydrogen-rich water improved the diversity and abundance of the gut flora in athletes. All examined indices, including the shannon, sobs, ace, and chao indices, were higher in the control group than those proposed to result from hydrogen-rich water consumption prior to the trial, but these indices were all reversed and were higher than those in the controls after the 2-month intervention. Nevertheless, there were some differences in the gut flora components of these two groups before the trial, whereas there were no significant changes in the gut flora composition during the trial period. Thus, the consumption of hydrogen-rich water for two months might play a role modulating in the gut flora of athletes based on its selective antioxidant and anti-inflammatory activities. The study protocol was approved by the ethics committee of the Suzhou Sports School (approved number: SSS-EC150903).

4.
J Pharm Anal ; 3(6): 429-433, 2013 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29403850

RESUMEN

A high-speed counter-current chromatography (HSCCC) method was successfully developed for the preparative separation and purification of deoxyschizandrin from Schisandrae Sphenantherae Fructus in one step. The purity of deoxyschizandrin was 98.5%, and the structure was identified by MS, UV and NMR. This method was simple, fast, convenient and appropriate to prepare pure compound as reference substances for related research on Schisandrae Sphenantherae Fructus.

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