Influence of excipients and processing conditions on the development of agglomerates of racecadotril by crystallo-co-agglomeration

• Published in: International Journal of Pharmaceutical Investigation Vol. 2; no. 4; pp. 189 - 200
• Main Authors: Garala, Kevin, Patel, Jaydeep, Patel, Anjali, Raval, Mihir, Dharamsi, Abhay
• Format: Journal Article
• Language: English
• Published: India Medknow Publications Pvt Ltd 01.10.2012; Medknow Publications and Media Pvt. Ltd; Medknow Publications & Media Pvt Ltd
• Subjects: Original; India; crushing strength; flowability; Crystallo-co-agglomeration; racecadotril
• ISSN: 2230-973X; 2230-9713
• DOI: 10.4103/2230-973X.106996

Purpose: The purpose of the present investigation was to improve the flow and mechanical properties of racecadotril by a crystallo-co-agglomeration (CCA) technique. Direct tableting is a requirement of pharmaceutical industries. Poor mechanical properties of crystalline drug particles require wet granulation which is uneconomical, laborious, and tedious. Materials and Methods: The objective of this work was to study the influence of various polymers/excipients and processing conditions on the formation of directly compressible agglomerates of the water-insoluble drug, racecadotril, an antidiarrheal agent. The agglomerates of racecadotril were prepared using dichloromethane (DCM)-water as the crystallization system. DCM acted as a good solvent for racecadotril as well as a bridging liquid for the agglomeration of the crystallized drug and water as the nonsolvent. The prepared agglomerates were tested for micromeritic and mechanical properties. Results: The process yielded ~90 to 96% wt/ wt spherical agglomerates containing racecadotril with the diameter between 299 and 521 μ. A higher rotational speed of crystallization system reduces the size of the agglomerates and disturbs the sphericity. Spherical agglomerates were generated with a uniform dispersion of the crystallized drug. CCA showed excellent flowability and crushing strength. Conclusion: Excipients and processing conditions can play a key role in preparing spherical agglomerates of racecadotril by CCA, an excellent alternative to the wet granulation process to prepare intermediates for direct compression.