Objectives: The present study investigates the effect of particle engineering technique on powder properties and pharmacokinetics of piroxicam (PXM).
Methods: PXM was subjected to melt sonocrystallization to obtain product designated as MSCPXM and characterized for various pharmacotechnical parameters, performance characteristics and pharmacokinetic evaluation.
Results: Micromeritic and rheological properties were found to be superior to the original form (OFPXM). On melt sonocrystallization, solubility and intrinsic dissolution rate were enhanced by 76.45% and 33.33%, respectively. Solid state evaluation by DSC and XRPD ruled out possibilities of polymorph formation but confirmed decreased crystallinity index. SEM analysis revealed uniformly shaped smaller drug particles of MSCPXM as compared to PXM. The thermodynamic stability of MSCPXM was monitored by XRPD and the sample was stable even after 3 months of storage at 40 ± 2°C and 75 ± 5% RH. The MSCPXM was formulated as immediate release tablets (F1 - F4) and evaluated with reference tablets of OFPXM (F0). F2 was identified as best formulation with suitable tablet characteristics and in-vitro drug release profile. Pharmacokinetic evaluation of F2 in rats supported the in-vitro data with 2.08-fold increase in bioavailability achieved at 4.8 ± 1.7 h with MSCPXM as compared to OFPXM.
Conclusions: Conclusively, melt sonocrystallization offered an efficient, solvent-free technique that can be exploited for particle designing of drugs with favorable pharmaceutical properties.
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http://dx.doi.org/10.1517/17425247.2013.736961 | DOI Listing |
Proc Natl Acad Sci U S A
April 2016
Institute for Complex Molecular Systems, Eindhoven University of Technology, 5600 MB Eindhoven, The Netherlands; Laboratory of Macromolecular and Organic Chemistry, Department of Chemical Engineering and Chemistry, Eindhoven University of Technology, 5600 MB Eindhoven, The Netherlands; Laboratory of Physical Chemistry, Department of Chemical Engineering and Chemistry, Eindhoven University of Technology, 5600 MB Eindhoven, The Netherlands
Antifreeze proteins (AFPs) are a unique class of proteins that bind to growing ice crystal surfaces and arrest further ice growth. AFPs have gained a large interest for their use in antifreeze formulations for water-based materials, such as foods, waterborne paints, and organ transplants. Instead of commonly used colligative antifreezes such as salts and alcohols, the advantage of using AFPs as an additive is that they do not alter the physicochemical properties of the water-based material.
View Article and Find Full Text PDFDrug Dev Ind Pharm
October 2016
b Centre for Pharmaceutical Engineering Science, University of Bradford, Bradford , UK.
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.
View Article and Find Full Text PDFCurr Pharm Des
September 2016
Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, TX 78712, Austin, USA.
This review is intended to provide a critical account of the current goals and technologies of particle engineering regarding the production of crystalline and amorphous particles. The technologies discussed here cover traditional crystallization technologies, supercritical fluid technologies, spray drying, controlled solvent crystallization, and sonocrystallization. Also recent advancements in particle engineering including spray freezing into liquid, thin-film freeze-drying, PRINT technology are presented.
View Article and Find Full Text PDFPharmaceutics
April 2015
Department of Pharmaceutics, Rajiv Academy for Pharmacy, N.H. #2, Delhi Mathura Road, P.O. Chhattikara, Mathura-281001, India.
Curcumin suffers from the limitation of poor solubility and low dissolution that can lead to limited applications. The investigation was aimed to substantiate the potentiality of melt sonocrystallized gastroretentive tablets of curcumin. Melt sonocrystallized curcumin (MSC CMN) was developed and its therapeutic potential was validated by in vitro cytotoxicity studies against Human oral cancer cell line KB.
View Article and Find Full Text PDFJ Ultrasound
March 2014
Suresh Gyanvihar University, Jaipur, 302025 Rajasthan India.
The poor solubility and low dissolution rate in gastro-intestinal fluid, especially for class-II drugs according to Biopharmaceutics Classification System (BCS) the bioavailability enhanced by increasing the solubility and dissolution rate. A novel melt sonocrystallization technique of particle engineering to enhance solubility as well as dissolution of hydrophobic drug and to study its effect on crystal properties of drug. The present study leads to use investigate solubility of melt sonocrystallization technique to modify the undesirable properties of Rosiglitazone is antidiabetic drug in thiozolidione category with (BCS II) to forms agglomerates with number of shallow circular pits on the surface leads to increase solubility.
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