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Drug Development and Industrial Pharmacy

Kristin Forner, Carl Roos, David Dahlgren, Filippos Kesisoglou, Moritz A Konerding, Johanna Mazur, Hans Lennernäs, Peter Langguth
CONTEXT: Prediction of the in vivo absorption of poorly soluble drugs may require simultaneous dissolution/permeation experiments. In vivo predictive media have been modified for permeation experiments with Caco-2 cells, but not for excised rat intestinal segments. OBJECTIVE: The present study aimed to improve the setup of dissolution/permeation experiments with excised rat intestinal segments by assessing suitable donor and receiver media. METHODS: The regional compatibility of rat intestine in Ussing chambers with modified Fasted and Fed State Simulated Intestinal Fluids (Fa/FeSSIFmod) as donor media was evaluated via several parameters that reflect the viability of the excised intestinal segments...
October 20, 2016: Drug Development and Industrial Pharmacy
Juilee A Kulkarni, Amelia M Avachat
Asenapine maleate (AM) is used in the treatment of schizophrenia. Its oral and sublingual bioavailability is <2% and 35%, respectively, due to first pass metabolism and poor solubility. To avoid first pass metabolism and to enhance solubility at all nasal pH conditions, thermo-responsive in situ nasal gel containing asenapine maleate-hydroxyl propyl β cyclodextrin inclusion complex (AM-HPβCD) was prepared in the present study. Inclusion complex (1:1 molar ratio) was characterized using UV spectroscopy, FITR and XRD techniques...
October 16, 2016: Drug Development and Industrial Pharmacy
Darjan Košir, Franc Vrečer
CONTEXT: The flow and compaction properties of a compaction mixture or powder and the drug-release profile of final tablets are important critical quality attributes (CQAs) that have an impact on the overall performance of hydrophilic matrix tablets. The selection of granulation method can importantly affect these CQAs. OBJECTIVE: This study investigates various agglomeration methods of sustained-release formulation using HPMC K4M as a release polymer with various wet- and dry-granulation techniques...
October 14, 2016: Drug Development and Industrial Pharmacy
Daniela D'Almeida Peres, Maira Bueno Ariede, Thalita Marcilio Candido, Tania Santos de Almeida, Felipe Rebello Lourenço, Vladi Olga Consiglieri, Telma Mary Kaneko, Maria Valéria Robles Velasco, André Rolim Baby
Multifunctional formulations are of great importance to ensure better skin protection from harm caused by ultraviolet radiation (UV). Despite the advantages of Quality by Design and Process Analytical Technology approaches to the development and optimization of new products, we found in the literature only a few studies concerning their applications in cosmetic product industry. Thus, in this research work, we applied the QbD and PAT approaches to the development of multifunctional sunscreens containing bemotrizinol, ethylhexyl triazone, and ferulic acid...
October 13, 2016: Drug Development and Industrial Pharmacy
Amit Arya, Dipak K Majumdar, Dharam Pal Pathak, Anil K Sharma, Alok R Ray
Colon-targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid-butyl methacrylate copolymers. Microparticles were prepared by oil-in-oil solvent evaporation method using Span 80 as emulsifier. Microparticles were found to be spherical in shape, hemocompatible and anionic with zeta potential of -27.4 and -29.0 mV. Entrapment of drug in the microparticles was confirmed by Fourier transform infrared (FTIR) spectroscopy. However, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) revealed amorphous nature of microparticles due to the dilution effect of amorphous polymer...
October 6, 2016: Drug Development and Industrial Pharmacy
Amnon C Sintov, Giora Enden
The purpose of this study was to investigate a new polymeric system and production process in which self-assembled doxorubicin-loaded nanoparticles were synthetized by using a water-in-oil microemulsion as a template and calcium ions as cross-linkers. The manufacturing process combined cross-linking of carbomer within a W/O microemulsion followed by a phase-separation technique to avoid using organic solvents for extraction. To assess the sustained release behavior of doxorubicin from the nanoparticles, we have developed a new simple method based on the permeability coefficient of a synthetic membrane mounted on Franz diffusion cell system...
October 6, 2016: Drug Development and Industrial Pharmacy
Mahendra Shukla, Swati Jaiswal, Abhisheak Sharma, Pradeep Kumar Srivastava, Abhishek Arya, Anil Kumar Dwivedi, Jawahar Lal
OBJECTIVE: Curcumin, the golden spice from Indian saffron, has shown chemoprotective action against many types of cancer including breast cancer. However, poor oral bioavailability is the major hurdle in its clinical application. In the recent years, self-nanoemulsifying drug delivery system (SNEDDS) has emerged as a promising tool to improve the oral absorption and enhancing the bioavailability of poorly water-soluble drugs. In this context, complexation with lipid carriers like phospholipid has also shown the tremendous potential to improve the solubility and therapeutic efficacy of certain drugs with poor oral bioavailability...
October 6, 2016: Drug Development and Industrial Pharmacy
Xinnuo Xiong, Kailin Xu, Shanshan Li, Peixiao Tang, Ying Xiao, Hui Li
Solid-state amorphization of crystalline rebamipide (RBM) was realized by ball milling and spray drying. The amorphous content of samples milled for various time was quantified using X-ray powder diffraction. Crystalline RBM and three amorphous RBM obtained by milling and spray drying were characterized by morphological analysis, X-ray diffraction, thermal analysis and vibrational spectroscopy. The crystal structure of RBM was first determined by single-crystal X-ray diffraction. In addition, the solubility and dissolution rate of the RBM samples were investigated in different media...
October 6, 2016: Drug Development and Industrial Pharmacy
Martina Hotujac Grgurević, Marina Juretić, Anita Hafner, Jasmina Lovrić, Ivan Pepić
OBJECTIVE: To evaluate the compatibility of commercially available eye drop surface tension with the tear film physiological range and to characterize commonly used ophthalmic excipients in terms of their surface activity under eye-biorelevant conditions. SIGNIFICANCE: There are a number of quality requirements for the eye drops (e.g. tonicity, pH, viscosity, refractive index) that needs to comply with the physiological parameters of the eye surface. However, the adjustment of surface tension properties of the eye drops to the normal range of surface tension at the air/tear fluid interface (40-46 mN/m) has received rather less attention thus far...
October 6, 2016: Drug Development and Industrial Pharmacy
Julien P Maincent, Laura K Najvar, William R Kirkpatrick, Siyuan Huang, Thomas F Patterson, Nathan P Wiederhold, Jay I Peters, Robert O Williams
Previously, modified release itraconazole in the form of a melt-extruded amorphous solid dispersion based on a pH dependent enteric polymer combined with hydrophilic additives (HME-ITZ), exhibited improved in vitro dissolution properties. These properties agreed with pharmacokinetic results in rats showing high and sustained itraconazole (ITZ) systemic levels. The objective of the present study was to better understand the best choice of rodent model for evaluating the pharmacokinetic and efficacy of this orally administered modified release ITZ dosage form against invasive Aspergillus fumigatus...
October 5, 2016: Drug Development and Industrial Pharmacy
Ioannis Nikolakakis, Kyriakos Kachrimanis
A simple and highly reproducible procedure was established for the study of orthorhombic paracetamol crystallization kinetics, comprising melting, quench-cooling of the melt and scanning the formed glass by DSC at different heating rates. Results were analyzed on the basis of the mean as well as local values of the Avrami exponent, n, the energy of activation, as well as the Šesták-Berggren two-parameter autocatalytic kinetic model. The mean value of the Avrami kinetic exponent, n, ranged between 3 and 5, indicating deviation from the nucleation and growth mechanism underlying the Johnson-Mehl, Avrami-Kolmogorov (JMAK) model...
October 2, 2016: Drug Development and Industrial Pharmacy
Feng Zhang, Fan Meng, Zhi Yuan Wang, Watson Na
The interaction between copovidone and Carbopol 907 is pH dependent. When the pH of an aqueous solution fell below pH 4.5, a water-insoluble complex began to form and precipitate. This complex resulted from a hydrogen-bond-induced interaction between the carboxylic groups in Carbopol 907 and the carbonyl groups of N-vinylpyrrolidone repeat units in copovidone. Consisting of these two polymers at an approximate 1:1 weight ratio, the complex was an amorphous material with a glass transition temperature of 157 °C...
October 2, 2016: Drug Development and Industrial Pharmacy
Soad Ali Yehia, Sally Adel Abdel-Halim, Mary Yosry Aziz
The objective of this study is to formulate biodegradable in situ microparticles (ISM) containing lornoxicam for post operative and arthritic pain management. ISM emulsions were prepared according to 2(5) full factorial experimental design to investigate the influence of formulation variables on the release profile of the drug. The independent variables studied are the polymer type, polymer inherent viscosity, polymer concentration, oil type and polymer: oil ratio. In vitro drug release, microscopical examination, particle size determination, and syringeability measurement, were selected as dependent variables...
September 27, 2016: Drug Development and Industrial Pharmacy
Mohit Dwivedi, Vijay Sharma, Kamla Pathak
CONTEXT: Eosinophilic pustular folliculitis is a secondary symptom associated with HIV infection appears as levels of CD4 lymphocyte cells and T4 lymphocyte cell. Isotretinoin, an analogue of vitamin A (retinoid) alters the DNA transcription mechanism and interferes in the process of DNA formation. It also inhibits the eosinophilic chemotactic factors present in sebaceous lipids and in the stratum corneum of patients suffering from this ailment. OBJECTIVE: The present research was aimed to formulate isotretenoin loaded invasomal gel to deliver and target the drug to pilosebaceous follicular unit...
September 21, 2016: Drug Development and Industrial Pharmacy
Janne Olsen Frenvik, Knut Dyrstad, Solveig Kristensen, Olav B Ryan
Targeted Thorium Conjugates (TTCs) are being explored as a potential future platform for specific tumour targeting pharmaceuticals. In TTCs the alpha emitting radionuclide thorium-227 ((227)Th) with a half-life of 18.697 days is labelled to targeting moieties, such as monoclonal antibodies (mAbs). The amount of daughter nuclide radium-223 ((223)Ra, t1/2 = 11.435 days) will increase during manufacture and distribution, and so a technology for purification is required to assure an acceptable level of (223)Ra is administrated to the patient...
September 15, 2016: Drug Development and Industrial Pharmacy
A A Karatzas, S N Politis, D M Rekkas
The purpose of this study was the development of novel, fast disintegrating, effervescent pellets by employing the direct pelletization technique as a single step process. In line with the Quality by Design (QbD) regulatory framework, statistical experimental design was extensively applied to correlate significant formulation and process variables with the critical quality attributes of the product. Pellets were studied with regards to sphericity, size and size distribution. In contrast to the existing multiparticulate platforms, this development integrated only water-soluble excipients to facilitate the multifunctional use of the final dosage form...
September 13, 2016: Drug Development and Industrial Pharmacy
F H Xavier-Junior, C Vauthier, A R V Morais, E N Alencar, E S T Egito
Natural oils are extremely complex mixtures containing compounds of different chemical nature. Some of them have physiological or therapeutic activities that may act either alone or in synergy. Therefore, they are used in the pharmaceutical, agronomic, food, sanitary, and cosmetic industries. Today, the interest in bioactive natural oils is growing due to their immense potential to prevent and treat numerous human diseases. Formulation in microemulsions (MEs) containing natural oils appeared suitable to improve pharmaceutical and biopharmaceutical properties of bioactive compounds derivate from these oils...
September 13, 2016: Drug Development and Industrial Pharmacy
Soraya Hengsawas Surasarang, Justin M Keen, Siyuan Huang, Feng Zhang, James W McGinity, Robert O Williams Iii
The purpose of this study was to enhance the dissolution properties of albendazole (ABZ) by the use of amorphous solid dispersions. Phase diagrams of ABZ-polymer binary mixtures generated from Flory-Huggins theory were used to assess miscibility and processability. Forced degradation studies showed that ABZ degraded upon exposure to hydrogen peroxide and 1 N NaOH at 80°C for 5 min, and the degradants were albendazole sulfoxide (ABZSX), and ABZ impurity A, respectively. ABZ was chemically stable following exposure to 1 N HCl at 80°C for one hour...
September 12, 2016: Drug Development and Industrial Pharmacy
A Michael Rajesh, Kiritkumar Mangaldas Popat
OBJECTIVE: The objective was to evaluate taste masking of azithromycin (AZI) by ion exchange resins (IERs) and the formation of covalent semi interpenetrating polymer network (IPN) beads using chitosan (CS) and sodium carboxylated agarose (SCAG) for sustained release of drug. METHODS: Methacrylic acid (MAA)-based IERs were prepared by suspension polymerization method. Drug release complexes (DRCs) were prepared by different drug:resin ratios i.e. 1:1, 1:2 and 1:4...
September 7, 2016: Drug Development and Industrial Pharmacy
Zhihe Lu, Jingrong Su, Zhengrong Li, Yuzhu Zhan, Decai Ye
CONTEXT: Gemcitabine (GEM) and Baicalein (BCL) are reported to have anti-tumor effects including pancreatic cancer. Hyaluronic acid (HA) can bind to over-expressed receptors in various kinds of cancer cells. OBJECTIVE: The aim of this study is to develop prodrugs containing HA, BCL and GEM, and construct nanomedicine incorporate GEM and BCL in the core and HA on the surface. This system could target the cancer cells and co-deliver the drugs. METHODS: GEM-stearic acid lipid prodrug (GEM-SA) and hyaluronic acid-amino acid-baicalein prodrug (HA-AA-BCL) were synthesized...
September 6, 2016: Drug Development and Industrial Pharmacy
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