Ultrasound-assisted preparation of novel ibuprofen-loaded excipient with improved compression and dissolution properties

• Published in: Drug development and industrial pharmacy Vol. 42; no. 10; pp. 1553 - 1563
• Main Authors: Gandhi, Paras, Patil, Sharvil, Aher, Suyog, Paradkar, Anant
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 02-10-2016
• Subjects: Crystallization; dicalcium phosphate; dissolution; Excipients - chemistry; ibuprofen; Ibuprofen - chemical synthesis; Ibuprofen - chemistry; Solubility; Solvents - chemistry; Tablets - chemistry; Ultrasonography, Interventional - methods; ibuprofen; solubility; Crystallization; dicalcium phosphate; dissolution
• ISSN: 0363-9045; 1520-5762
• DOI: 10.3109/03639045.2016.1151035

Context: Most of the active pharmaceutical ingredients (APIs) suffer from a drawback of poor aqueous solubility. In addition to the same, some APIs show poor tabletting behavior creating problems in formulation development. Crystal engineering can be an efficient tool in rectification of such problems associated with the APIs. Thus present work deals with crystallization of ibuprofen (a model drug) onto the surface of dicalcium phosphate (DCP) particles using different techniques.
Objective: The objective of the present work was to prepare ibuprofen-loaded DCP particles and further to analyze them for compressibility and dissolution behavior.
Materials and methods: Various crystallization techniques such as solvent evaporation (SE), melt crystallization (MC), melt sonocrystallization (MSC), antisolvent crystallization (AC), and antisolvent sonocrystallization (ASC) were screened for the preparation of ibuprofen-loaded DCP. Products obtained from different techniques were analyzed for physicochemical, micromeritic and compression properties.
Results and discussion: ASC technique was found to be suitable for preparing directly compressible ibuprofen-loaded DCP particles. The change in the crystal habit (needle to plate shape) of ibuprofen and its crystallization in miniscular form onto the surface of DCP particles showed significant improvement in the dissolution rate and compression properties of ibuprofen due to an increase in specific surface area when compared with ibuprofen crystallized by other techniques. Additionally, the tablets prepared from ASC powder did not require binder since ibuprofen acted as melt binder during compression.
Conclusion: Directly compressible ibuprofen-loaded DCP particles can serve as an alternative for conventional ibuprofen tablets prepared by wet granulation technique.