A review on the taste masking of bitter APIs: hot-melt extrusion (HME) evaluation

Abstract:: Hot melt extrusion (HME) is a continuous pharmaceutical manufacturing process that has been extensively inves-tigated for solubility improvement and taste masking of active pharmaceutical ingredients. Recently, it is being explored for its application in 3D printing. 3D printing of pharmaceuticals allows flexibility of dosage form design, customization of dosage form for personalized therapy and the possibility of complex designs with the inclusion of multiple actives in a sin-gle unit dosage form. Fused deposition modeling (FDM) is a 3D printing technique with a variety of applications in pharma-ceutical dosage form development. FDM process requires a polymer filament as the starting material that can be obtained by hot melt extrusion. Recent reports suggest enormous applications of a combination of hot melt extrusion and FDM technol-ogy in 3D printing of pharmaceuticals and need to be investigated further. This review in detail describes the HME process along with its application in 3D printing. The review also summarizes the published reports on the application of HME cou-pled with 3D printing technology in drug delivery.

Download Full-text

Hot-melt extrusion microencapsulation of quercetin for taste-masking

Journal of Microencapsulation ◽

10.1080/02652048.2017.1280095 ◽

2017 ◽

Vol 34 (1) ◽

pp. 29-37 ◽

Cited By ~ 21

Author(s):

Chia Miang Khor ◽

Wai Kiong Ng ◽

Parijat Kanaujia ◽

Kok Ping Chan ◽

Yuancai Dong

Keyword(s):

Hot Melt Extrusion ◽

Taste Masking ◽

Melt Extrusion ◽

Hot Melt

Download Full-text

A Review of Hot-Melt Extrusion: Process Technology to Pharmaceutical Products

ISRN Pharmaceutics ◽

10.5402/2012/436763 ◽

2012 ◽

Vol 2012 ◽

pp. 1-9 ◽

Cited By ~ 52

Author(s):

Mohammed Maniruzzaman ◽

Joshua S. Boateng ◽

Martin J. Snowden ◽

Dennis Douroumis

Keyword(s):

Drug Delivery ◽

Oral Drug Delivery ◽

Hot Melt Extrusion ◽

Pharmaceutical Products ◽

Taste Masking ◽

Oral Drug ◽

Melt Extrusion ◽

Process Technology ◽

Processing Technologies ◽

Hot Melt

Over the last three decades industrial adaptability has allowed hot-melt extrusion (HME) to gain wide acceptance and has already established its place in the broad spectrum of manufacturing operations and pharmaceutical research developments. HME has already been demonstrated as a robust, novel technique to make solid dispersions in order to provide time controlled, modified, extended, and targeted drug delivery resulting in improved bioavailability as well as taste masking of bitter active pharmaceutical ingredients (APIs). This paper reviews the innumerable benefits of HME, based on a holistic perspective of the equipment, processing technologies to the materials, novel formulation design and developments, and its varied applications in oral drug delivery systems.

Download Full-text

Taste masking of paracetamol by hot-melt extrusion: An in vitro and in vivo evaluation

European Journal of Pharmaceutics and Biopharmaceutics ◽

10.1016/j.ejpb.2011.10.019 ◽

2012 ◽

Vol 80 (2) ◽

pp. 433-442 ◽

Cited By ~ 97

Author(s):

Mohammed Maniruzzaman ◽

Joshua S. Boateng ◽

Marion Bonnefille ◽

Attila Aranyos ◽

John C. Mitchell ◽

...

Keyword(s):

Hot Melt Extrusion ◽

Taste Masking ◽

Melt Extrusion ◽

In Vivo Evaluation ◽

Hot Melt

Download Full-text

Taste Masking Using Hot-Melt Extrusion

Hot-Melt Extrusion: Pharmaceutical Applications ◽

10.1002/9780470711415.ch9 ◽

2012 ◽

pp. 201-221 ◽

Cited By ~ 2

Author(s):

Dennis Douroumis ◽

Marion Bonnefille ◽

Attila Aranyos

Keyword(s):

Hot Melt Extrusion ◽

Taste Masking ◽

Melt Extrusion ◽

Hot Melt

Download Full-text

TASTE ABATEMENT AND CHARACTERIZATION OF DISPERSIBLE TABLETS OF ARTEMETHER PREPARED BY HOT MELT EXTRUSION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i6.19555 ◽

2017 ◽

Vol 9 (6) ◽

pp. 28

Author(s):

Yogesh A. Sonar ◽

Mrudula H. Bele ◽

Nitin H. Sonar ◽

Vishal S. Bagul ◽

Prashik S. Shimpi

Keyword(s):

Sensory Evaluation ◽

Solid Dispersion ◽

In Vitro Release ◽

Hot Melt Extrusion ◽

Taste Masking ◽

Melt Extrusion ◽

Evaluation Panel ◽

Dispersible Tablets ◽

Hot Melt

Objective: The aim of this study was to formulate and evaluate a taste-masked formulation using hot melt extrusion approach for artemether.Methods: Taste masking of artemether was done by preparing solid dispersion with coating polymer kollicoatsmartseal 30D using hot melt extrusion. The prepared solid dispersion was subjected to taste masking evaluation like sensory evaluation parameters against five levels set for taste evaluation using artemether as control standard along with in vitro release studies in simulated salivery fluid. After taste evaluation of solid dispersion was subjected to the formulation of dispersible tablets by direct compression method. The final taste masking evaluation of dispersible tablets of solid dispersion containing artemether were done by a sensory evaluation panel of nine members along with in vitro release study in simulated salivary and gastric fluid.Results: The percent drug content was found 35.09±0.06 % in solid dispersion. The drug excipients compatibility studies performed with the help of FTIR instrument and DSC that indicates there were no interactions between drug and polymers. Solid dispersions (1:1, 1:2, 1:3 drug polymer ratio) of artemether were evaluated by sensory evaluation panel from which 1:3 drug: polymer solid dispersion was found more palatable. Release rate study in simulated salivary fluid shown no release but shows release of drug in simulated gastric fluids which indicates that the drug was taste masked. The optimized batch of dispersible tablets (F1) were subjected for evaluation parameters like dispersion time (70±1.90), wetting time (63±1.86), etc. Dissolution studies of optimized formulation indicated that the polymer does not allow drug to release in simulated salivery pH 6.8 but shows immediate release in simulated gastric pH which also confirms taste masking efficiency of polymer. Final optimized F1 batch evaluated for taste masking evaluation by sensory evaluation panel using pure drug as control standard found to be palatable.Conclusion: It may be concluded that kollicoatsmartseal 30D could mask the taste of the drug in salivary pH and shows drug release at gastric pH which confirms its efficiency for taste masking.

Download Full-text