Combined application of extrusion-spheronization and hot-melt coating technologies for improving moisture-proofing of herbal extracts

Chen, Hao; Shi, Shuai; Liu, Aina; Tang, Xing

doi:10.1002/jps.21990

Cited by 19 publications

(7 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Due to the hydrophobic character of HMC excipients, a prolonged-release from the coated material is achieved and can be modified towards an immediate release by the combination with surfactants or other more hydrophilic components [26]. Apart from the modification of release profiles, lipid coatings are widely used for taste masking [27], swallowability improvement, and moisture protection of oral formulations [28].…”

Section: Introductionmentioning

confidence: 99%

Hot Melt Coating of Amorphous Carvedilol

et al. 2020

View full text Add to dashboard Cite

The use of amorphous drug delivery systems is an attractive approach to improve the bioavailability of low molecular weight drug candidates that suffer from poor aqueous solubility. However, the pharmaceutical performance of many neat amorphous drugs is compromised by their tendency for recrystallization during storage and lumping upon dissolution, which may be improved by the application of coatings on amorphous surfaces. In this study, hot melt coating (HMC) as a solvent-free coating method was utilized to coat amorphous carvedilol (CRV) particles with tripalmitin containing 10% (w/w) and 20% (w/w) of polysorbate 65 (PS65) in a fluid bed coater. Lipid coated amorphous particles were assessed in terms of their physical stability during storage and their drug release during dynamic in vitro lipolysis. The release of CRV during in vitro lipolysis was shown to be mainly dependent on the PS65 concentration in the coating layer, with a PS65 concentration of 20% (w/w) resulting in an immediate release profile. The physical stability of the amorphous CRV core, however, was negatively affected by the lipid coating, resulting in the recrystallization of CRV at the interface between the crystalline lipid layer and the amorphous drug core. Our study demonstrated the feasibility of lipid spray coating of amorphous CRV as a strategy to modify the drug release from amorphous systems but at the same time highlights the importance of surface-mediated processes for the physical stability of the amorphous form.

show abstract

Section: Introductionmentioning

confidence: 99%

Hot Melt Coating of Amorphous Carvedilol

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Some alternative formulations and processes have been proposed to cope with the unfavorable characteristics of DHEs, and may provide a means of addressing these issues [8]. For example, in general, the addition of disintegrants to the tablet formulation or high amount of magnesium stearate blended with the granules can promote the tablet integration, and the dry granulation of hygroscopic herbal extracts can improve their poor compressibility [9].…”

Section: Introductionmentioning

confidence: 99%

Multivariate Statistical Optimization of Tablet Formulations Incorporating High Doses of a Dry Herbal Extract

Kim

Lee

et al. 2019

Pharmaceutics

View full text Add to dashboard Cite

The development of oral tablet formulation for herbal medicines has been restricted by large drug loadings and the poor physicochemical and mechanical properties of dry herbal extracts (DHEs). Herein, statistical experimental designs were applied to herbal tablet formulation development and optimization using Wuzi Yanzong dry extract (WYE). The tablet disintegration time and hardness were identified as the critical quality attributes (CQAs) of the product. The tablet formulation was designed to achieve a high drug loading (50% or higher of WYE), shorter tablet disintegration time (less than 30 minutes), and suitable hardness (6.0 to 7.5 kp). A D-optimal mixture design was used to evaluate the effects of excipients on CQAs to minimize the risk compression failure and improve the tabletability in formulations containing WYE at 50% and 65% by weight. A partial least squares model was used to elucidate the multivariate relationships between a large number of formulation variables and product CQAs, and determine the maximum possible WYE loading. From overlaid plots of the effects of formulation variables on CQAs, it was found that a maximum WYE loading of 67% in tablet formulation satisfied the acceptance criteria of CQAs. In conclusion, this study shows that multivariate statistical tools are useful for developing tablet formulations containing high doses of herbal extracts and establishing control strategies that ensure product quality.

show abstract

“…Luo et al (2013) describe an application wherein the dissolution and bioavailability of Ginsenosides is improved by melt extrusion and cogrinding. These findings are indicative that in the future, melt extrusion will find broader applications to improving herbal drug attributes and not just be limited to areas such as moisture proofing of herbal extracts (Chen et al 2010). …”

Section: Clinical and Therapeutic Potentialmentioning

confidence: 92%

Melt Extrusion in Drug Delivery: Three Decades of Progress

Shah

Repka

2013

AAPS Advances in the Pharmaceutical Sciences Series

View full text Add to dashboard Cite

This chapter appraises the role of melt extrusion as a solubilization and bioavailability enhancement technique. The introductory chapter highlights major aspects of hot melt extrusion (HME) technology as applied in the pharmaceutical industry, particularly processing techniques, material considerations, recent innovative applications of melt extrusion in drug delivery system design, and a review of current HME-based formulations (marketed or under commercial development). The chapter also focuses on key development aspects of HME processes, such as material sparing screening approaches, process formulation relationships, and stability evaluation of prototype formulations, which emphasize the clinical and biological significance of this technique. In addition, it displays the journey and evolution of this important processing technology into an established pharmaceutical manufacturing platform. The chapter describes several case studies wherein melt extrusion has been utilized to develop commercial drug products.Early-stage development in melt extrusion encompasses various critically interdependent areas involving process considerations, stability assessment of prototype formulations, and performance evaluation (with respect to intended applications) of prototype formulations. Processing ConsiderationsProcessing considerations is a rather broad terminology covering material properties, instrument considerations, and process-formulation interplay. Systematic research over the last couple of decades has revealed that critical product quality attributes are directly dependent on both "formulation" and the "process" employed. It is important to note that the interplay between these determines the finished product attributes. Material PropertiesAll of the materials used in melt extrusion (drugs, carriers, processing aids, release modifiers, etc.) should meet certain minimal pharmaceutical criteria, which

show abstract

Combined application of extrusion-spheronization and hot-melt coating technologies for improving moisture-proofing of herbal extracts

Cited by 19 publications

References 21 publications

Hot Melt Coating of Amorphous Carvedilol

Hot Melt Coating of Amorphous Carvedilol

Multivariate Statistical Optimization of Tablet Formulations Incorporating High Doses of a Dry Herbal Extract

Melt Extrusion in Drug Delivery: Three Decades of Progress

Contact Info

Product

Resources

About