Taste masking of bitter APIs by using hot melt extrusion (HME)
Maniruzzaman, M., Boateng, J. and Douroumis, D. (2011) Taste masking of bitter APIs by using hot melt extrusion (HME). In: AAPS Journal. American Association of Pharmaceutical Sciences, Arlington, VA, USA, T3273-T3273. ISSN 1550-7416 (on-line)
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To investigate the potential of Hot-melt Extrusion (HME) for masking the taste of bitter cationic APIs when incorporated into different anionic polymer formulations through a possible taste masking mechanism attributed to intermolecular drug/polymer ionic interactions.
The materials (Cetirizine HCl-CTZ, Propanolol HCl-PRP, Verapamil HCl-VRP, and Diphenhydramine HCl-DPD) and three polymers were mixed in 10/90, 20/80 (drug/polymer wt/wt) ratio in 100g batches (10 min in a Turbula TF2 Mixer). The Eudragit® polymers were processed by adding 20% triethyl citrate as plasticizer. Extrusion was performed using a Randcastle single-screw extruder (RCP0625) equipped with a 5-mm rod die. The resulting granules were characterized by XRPD, DSC, XPS, NMR and dissolution studies. The taste masking efficiency was evaluated in vivo with six healthy human volunteers (age 18 – 25). Bitterness intensity scale used from 1 to 5 where1, 2, 3, 4, and 5 indicate no, threshold, slight, moderate, and strong.
All formulations showed the presence of APIs in amorphous state with some showing only one glass transition (Tg), indicating molecularly dispersed APIs. The in vivo study for APIs and the extrudates showed significant suppression of the bitter taste for all actives (Fig 1a) and influence of the polymeric carriers (Fig 1b). The experimental findings form XPS analysis elucidated a possible taste masking mechanism attributed to intermolecular ionic interactions between amino and carboxylic groups of API’s and polymers respectively. NMR experiments also determined an oppositely charged drug/polymers interactions in all formulations. Dissolution studies of the HME granules showed rapid release within the first two hours for all APIs formulated with Eudragit L100 or Acryl-EZE. As expected, the APIs extruded with S100 showed slow release for the first two hours which increased at higher pH (6.8) values. The Eudragit S100 is soluble at pH>7 and thus drug release was retarded at low pH values.
The in vivo taste evaluation showed that the appropriate selection of drug-polymer combinations can achieve significant taste masking effect.
|Item Type:||Conference Proceedings|
|Title of Proceedings:||AAPS Journal|
|Additional Information:|| Paper presented at 2010 FIP Pharmaceutical Sciences World Congress (PSWC) in association with the AAPS Annual Meeting and Exposition, New Orleans, USA, Nov. 14-18, 2010  FIP is the International Pharmaceutical Federation|
|Uncontrolled Keywords:||HME, taste masking|
|Subjects:||R Medicine > RS Pharmacy and materia medica
T Technology > T Technology (General)
|Faculty / Department / Research Groups:||Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences|
|Last Modified:||17 Oct 2016 09:11|
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