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Preparation and characterisation of lornoxicam solid dispersion systems using hot melt extrusion technique

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Abstract

The aim of the research study was to investigate the ability of Soluplus® and surfactant individually as well as in combination to improve the solubility, subsequently the dissolution profile of lornoxicam (LORX). A laboratory size single screw rotating extruder with temperature and speed control parameters employed during hot melt extrusion (HME) processing of LORX along with polymer-surfactant blends. Soluplus® used as primary solubilizing agent for preparing solid dispersion (SD). Along with Soluplus® different concentrations of surfactants such as PEG 400, Lutrol F127, Lutrol F68 were used to solve the permeability issues related to LORX. Encapsulation of LORX particles inside the molten matrix of polymer-excipient blend was confirmed by DSC, XRD and FT-IR. Drug excipient microscopic interaction was further confirmed by scanning electron microscopy (SEM). Depending upon the ratio of the polymer and surfactants used, the solubility of the hot melt extruded LORX was improved and found to be in the range 35–86 μg/ml (actual aqueous solubility of LORX was found to be 0.0083 μg/ml). Dissolution profile of the extruded SD was improved and was found to be in the range of 98–104 % within 20 min (actual dissolution profile of LORX was found to be 8 % at the end of 1 h). SEM and Raman images suggest the formation of amorphous dispersion systems. SD was subjected to stability studies as per ICH guidelines and found to be stable after 6 months when analyzed by HPLC. SD prepared from HME significantly improves the solubility and dissolution profile of LORX—a BCS class II drug.

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Acknowledgments

The authors are thankful to Alkem Pharmaceuticals Ltd., India for providing the gift sample of LORX, BASF Ltd. Mumbai for the gift sample of Soluplus®, Lutrol® F127 and Lutrol® F68. The author is also thankful to UGC (SAP) for providing the research fellowship and Institute of Chemical Technology, ELITE status (Mumbai, India) for providing all facilities and guidance.

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None.

Compliance with ethical requirements

This article dose not contain any studies with human and animal subjects performed by any of the authors.

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Authors and Affiliations

  1. Department of Pharmaceutical Science and Technology, Institute of Chemical Technology (ELITE status), Nathalal Parekh Marg, Matunga (E), Mumbai, 400019, Maharashtra, India

    Ritesh Fule, Tarique Meer & Purnima Amin

  2. Department of Pharmaceutical Sciences, KLE University, Nehru Nagar, Belgaum, 590010, Karnataka, India

    Dinesh Dhamecha

  3. Research and Development, Alkem Laboratories Ltd., C-17/7 MIDC industrial estate, Taluka Panvel, District Raigad, Taloja, 410208, Maharashtra, India

    Shyam Ghadlinge

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  1. Ritesh Fule
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  2. Tarique Meer
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  5. Shyam Ghadlinge
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Correspondence to Ritesh Fule.

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Fule, R., Meer, T., Amin, P. et al. Preparation and characterisation of lornoxicam solid dispersion systems using hot melt extrusion technique. Journal of Pharmaceutical Investigation 44, 41–59 (2014). https://doi.org/10.1007/s40005-013-0099-7

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