Dissolution and pharmacokinetics of baicalin–polyvinylpyrrolidone coprecipitate

Li, Bibo; He, Mei; Li, Wei; Luo, Zhibin; Guo, Ying; Li, Yajun; Zang, Chunbao; Wang, Bo; Li, Fang; Li, Shaolin; Ji, Ping

doi:10.1111/jphp.12146

Cited by 23 publications

(16 citation statements)

References 17 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…However, the phase behaviour of solid dispersion can be extremely complicated. Drug and polymer may be miscible, partially miscible or immiscible …”

Section: The Role Of Interactions In Drug–polymer Miscibilitymentioning

confidence: 99%

Interactions between drugs and polymers influencing hot melt extrusion

Pang

Guo

et al. 2014

Journal of Pharmacy and Pharmacology

119

View full text Add to dashboard Cite

Objectives Hot melt extrusion (HME) as a technique for producing amorphous solid dispersion (ASD) has been widely used in pharmaceutical research. The biggest challenge for the application of HME is the thermal degradation of drug, poor physical stability of ASD and precipitation of drug during dissolution. Interactions between drugs and polymers may play an important role in overcoming these barriers. In this review, influence of drug-polymer interactions on HME and the methods for characterizing the drug-polymer interactions were reviewed. Key findings Strong drug-polymer interactions, especially ionic interactions and hydrogen bonds, are helpful to improving the thermal stability of drug during HME, enhancing the physical stability of ASD during storage and maintaining supersaturated solution after dissolution in gastrointestinal tract. The interactions can be quantitatively and qualitatively characterized by many analysing methods. Conclusions As many factors collectively determine the properties of HME products, drug-polymer interactions play an extremely important role. However, the action mechanisms of drug-polymer interactions need intensive investigation to provide more useful information for optimizing the formulation and the process parameters of HME.

show abstract

“…However, the phase behaviour of solid dispersion can be extremely complicated. Drug and polymer may be miscible, partially miscible or immiscible …”

Section: The Role Of Interactions In Drug–polymer Miscibilitymentioning

confidence: 99%

Interactions between drugs and polymers influencing hot melt extrusion

Pang

Guo

et al. 2014

Journal of Pharmacy and Pharmacology

119

View full text Add to dashboard Cite

show abstract

“…It has attracted increasing attention from worldwide researchers mainly because of its various therapeutic benefits, such as anti‐inflammatory, antiviral, antioxidant and antitumour activities . However, because of the glycosyl group on the ring, BCL is low hydrophilic and poorly absorbed in the small intestine and colon, only moderately absorbed in the stomach, leading to low bioavailability, while its hydrolysate, baicalein was well‐absorbed in the gastrointestinal tract and then restored to BCL in the body . The oral bioavailability of BCL and baicalein was 2.2% and 27.8% in rats respectively .…”

Section: Introductionmentioning

confidence: 99%

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Jiang

Deng

et al. 2017

Journal of Pharmacy and Pharmacology

Self Cite

View full text Add to dashboard Cite

show abstract

“…These have included microspheres, 11 microcapsules, 12 nanoemulsions, 13 inclusion complexes, 14,15 solid lipid nanoparticles, 16 BA-polyvinylpyrrolidone coprecipitate, and a BA-phospholipid complex. 17,18 Indeed, the studies have shown an increased solubility and improvement of oral bioavailability in the preclinical phase. However, the currently marketed preparations, including BA capsules and tablets, have to be administered at a large dose to obtain effective drug plasma concentration, due to low oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

View full text Add to dashboard Cite

Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi , a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween ® 80, Phospholipon ® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of −20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1−Q)) =0.609 lnt −1.230 ( r =0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA.

show abstract

Dissolution and pharmacokinetics of baicalin–polyvinylpyrrolidone coprecipitate

Abstract: From these observations of improved dissolution and pharmacokinetic behaviours, a good relationship was found in vitro and in vivo, indicating that the coprecipitate could be a promising formulation strategy for insoluble baicalin.

Cited by 23 publications

References 17 publications

Interactions between drugs and polymers influencing hot melt extrusion

Interactions between drugs and polymers influencing hot melt extrusion

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Contact Info

Product

Resources

About