26. March 2017
Aim: The therapeutic efficiency of a formulation will depend on various crucial parameters such as solubility of the drug, stability of the compound, excipients used in the formulation of finished dosage form, and the manufacturing technology used for the fabrication of finished dosage form. This research work is an attempt to enhance the solubility and dissolution rate by fabricating solid dispersion (SD) of the bosentan using hydrophilic polymers, soluplus, and kollidon VA 64. SDs of...
22. February 2017
Abstract Mannitol is a commonly used bulking agent in lyophilized formulations. It can crystallize into multiple solid forms during lyophilization thereby exhibiting phase heterogeneity and variability in product performance. In this manuscript, we studied the effect of cyclophosphamide (CPA), an anticancer drug, on the solid form of mannitol during lyophilization from aqueous solutions. Freeze-concentration studies were performed in the DSC while lyophilization was performed in a lab scale...
21. December 2016
Abstract Synergetic role of polymer blending on dissolution of amorphous solid dispersion was investigated. Dissolution rates of hypromellose (HPMC) and methacrylic acid copolymer (EUD) from the HPMC/EUD spray-dried sample (SPD) were improved compared to those of each single polymer SPD. Differential scanning calorimetry measurements revealed that the structural change in HPMC following heating was inhibited by co-spray-drying with EUD, suggesting an intermolecular interaction between the...
27. October 2016
Abstract The positively charged amino acids are commonly used excipients in biopharmaceutical formulations for stabilization of therapeutic proteins, yet the mechanisms for their modulation of protein stability are poorly understood. In this study, both lysine and histidine are shown to affect the thermal stability of myoglobin, bovine serum albumin, and lysozyme through a combination of mechanisms governed by their respective functional side chains and glycine, similar to arginine. This study...
08. October 2016
Abstract The number of topical fungal infections is growing, mostly owing to immunosuppressive therapy. Several topical fungal infections, such as eye mycoses, can be treated by local administration of antimycotic drugs. One major group of the antifungal agents is triazole, such as voriconazole (VCZ), which is used as the first line treatment of aspergillosis. A disadvantage of VCZ is its low water solubility making the drug difficult to administer in a liquid preparation. The lipid-based...
17. June 2016
Abstract Three granulation processing methods; Hot melt extrusion (HME), Roller compaction Dry granulation (RCDG) and Moisture assisted dry granulation (MADG) are assessed to evaluate different polymeric binders for preparation of a high dose immediate release tablet of acetaminophen drug. Different characterization techniques were used to enumerate poor physical property characteristic for drug (paracetamol) including hygroscopicity, low solubility and bulk density, and poor powder...
28. May 2016
Microscale freeze-drying makes rapid process cycles possible for early-stage formulation development. To investigate the effects of equipment scale and cooling rate on the solid state properties and the protein’s secondary structure of a sample, three binary formulations of catalase were prepared and freeze-dried with sucrose, mannitol, or (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD). The protein’s secondary structure was assessed using attenuated total reflection Fourier transform infrared...
16. May 2016
Paracetamol (PAR), phenylephrine hydrochloride (PHE) and chlorpheniramine maleate (CPM) are commonly used in clinical practice as antipyretic and analgesic drugs to ameliorate pain and fever in cold and flu conditions. The present work describes the use of thermal analysis for the characterization of the physicochemical compatibility between drugs and excipients during the development of solid dosage forms. Thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC) were used...
25. April 2016
This study consists of two experimental designs. Within the first one, suitable technique for application of model drug onto inactive pellets was evaluated and formulation and process parameters with greatest impact to process efficency and useful yield were determined. Results of experiments showed that formulation characteristics were the ones with the greatest impact on coating efficiency and that suspension layering technique was signifficantly better for drug application onto inactive...
05. March 2016
This study explored the effect of nano-crystalline cellulose (NCC) on Meloxicam (MX) solid dispersion (SD) prepared by co-grinding technique compared to micro-crystalline cellulose (MCC) in presence of lactose. MX-tablets were prepared by direct compression of different co-ground SDs or physical mixtures. The solubility, dissolution, SEM and DSC of different preparations were studied. Flow-through cell apparatus (FTC) was used to study the dissolution of MX from tablets at pH 7.4. Generally,...