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Pharmaceutical Development and Technology

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https://www.readbyqxmd.com/read/28058866/the-influence-of-thermal-treatment-and-type-of-insoluble-poly-meth-acrylates-on-dissolution-behavior-of-very-soluble-drug-from-hypromellose-matrix-tablets-evaluated-by-multivariate-data-analysis
#1
Katerina Kubova, Daniel Peček, Kristýna Hasserová, Petr Doležel, Miroslava Pavelková, Jakub Vyslouzil, Jan Muselík, David Vetchy
Hypromellose matrices exhibit extended burst effect immediately after contact with aqueous medium, especially when a water-soluble drug is incorporated. The objective of this study was to reduce burst effect and maintain complete dissolution of a very soluble levetiracetam over 12 h period from hypromellose K4M matrices to obtain zero-order kinetics. Desired changes were achieved by applying water dispersions of insoluble Eudragits(®) (NE, NM, RL, RS) as a granulation liquid to the drug/microcrystalline cellulose mixture during high-shear granulation (non-thermal treated set) and consequently by thermally treating granules or final tablets (TT), respectively...
January 6, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27879163/a-study-of-critical-functionality-related-characteristics-of-hpmc-for-sustained-release-tablets
#2
Darjan Košir, Tadej Ojsteršek, Saša Baumgartner, Franc Vrečer
The drug release profile from hydrophilic matrix tablets can be crucially affected by the variability of physicochemical properties of the controlled release agent. This study investigates and seeks to understand the functionality-related characteristics (FRCs) of hydroxypropyl methylcellulose (HPMC) type 2208, K4M grade, that influence the release rate of the model drug carvedilol from hydrophilic matrix tablets during the entire dissolution profile. The following FRCs were examined: particle size distribution, degree of substitution, and viscosity...
December 23, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27910726/the-effect-of-deuterium-oxide-on-the-conformational-stability-and-aggregation-of-bovine-serum-albumin
#3
Mouhamad Reslan, Veysel Kayser
Protein aggregation is a significant problem affecting the integrity of proteins, and is a major hindrance to the development of biopharmaceutical products. Deuterium oxide (D2O), widely used in protein characterization studies, has been shown to promote protein aggregation when used as a substitute for water in most buffered protein solutions; however, a few studies have reported minor improvements in melting point temperatures for some proteins. Our study aims to investigate the effect of D2O on protein stability, using bovine serum albumin (BSA) as a model...
December 21, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27915492/preparation-and-in-vitro-evaluation-of-melatonin-loaded-ha-pva-gel-formulations
#4
Sakine Tuncay Tanrıverdi, Catalina Natalia Cheaburu-Yilmaz, Sonia Carbone, Özgen Özer
Melatonin-loaded hyaluronic acid (HA) and poly(vinyl alcohol) (PVA) gels were prepared by using freeze-thaw technique and an emulsion method followed by freeze-thaw technique to produce a new synergistic system for topical application. Freeze-thaw hydrogels and emulgels were characterized by means of Fourier transform infrared spectroscopy, rheology and swelling tests. The porous structure of the hydrogels was shown by scanning electron microscopy observations and thermal properties were tested by differential scanning calorimetry measurements...
December 20, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27884084/losartan-loaded-liposomes-improve-the-antitumor-efficacy-of-liposomal-paclitaxel-modified-with-ph-sensitive-peptides-by-inhibition-of-collagen-in-breast-cancer
#5
Tai Xia, Qin He, Kairong Shi, Yang Wang, Qianwen Yu, Li Zhang, Qianyu Zhang, Huile Gao, Lifang Ma, Ji Liu
The dense collagen network in tumors restricts the penetration of drugs into tumors. Free losartan could inhibit collagen, but it would cause hypotension at the dosage of 10 mg/kg/d. In this study, losartan was encapsulated in liposomes (LST-Lip) and the collagen inhibition ability of LST-Lip was investigated. Our results showed the blood pressure was not affected by LST-Lip at the dosage of 2.5 mg/kg every other day. The amount of Evans Blue in tumor in LST-Lip group was 1.98 times of that in control group...
December 15, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27879156/enhancing-tablet-disintegration-characteristics-of-a-highly-water-soluble-high-drug-loading-formulation-by-granulation-process
#6
Preetanshu Pandey, Christopher Levins, Steve Pafiakis, Brian Zacour, Dilbir S Bindra, Jade Trinh, David Buckley, Shruti Gour, Shasad Sharif, Howard Stamato
The objective of this study was to improve the disintegration and dissolution characteristics of a highly water-soluble tablet matrix by altering the manufacturing process. A high disintegration time along with high dependence of the disintegration time on tablet hardness was observed for a high drug loading (70% w/w) API when formulated using a high-shear wet granulation (HSWG) process. Keeping the formulation composition mostly constant, a fluid-bed granulation (FBG) process was explored as an alternate granulation method using a 2((4-1)) fractional factorial design with two center points...
December 15, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27973975/solution-stability-of-captisol-stabilized-melphalan-evomela-versus-propylene-glycol-based-melphalan-hydrochloride-injection
#7
Ramsharan Singh, Jin Chen, Teresa Miller, Michael Bergren, Rangan Mallik
PURPOSE: The objective of this study was to compare the stability of recently approved Captisol-stabilized propylene glycol-free melphalan injection (Evomela™) against currently marketed propylene glycol-based melphalan injection. The products were compared as reconstituted solutions in vials as well as admixture solutions prepared from normal saline in infusion bags. METHODS: Evomela and propylene glycol-based melphalan injection were reconstituted in normal saline and organic custom diluent, respectively, according to their package insert instructions...
December 14, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27881046/preparation-and-characterization-of-bee-venom-loaded-plga-particles-for-sustained-release
#8
Min-Ho Park, Hye-Suk Jun, Jong-Woon Jeon, Jin-Kyu Park, Bong-Joo Lee, Guk-Hyun Suh, Jeong-Sook Park, Cheong-Weon Cho
Bee venom-loaded poly(lactic-co-glycolic acid) (PLGA) particles were prepared by double emulsion-solvent evaporation, and characterized for a sustained-release system. Factors such as the type of organic solvent, the amount of bee venom and PLGA, the type of PLGA, the type of polyvinyl alcohol, and the emulsification method were considered. Physicochemical properties, including the encapsulation efficiency, drug loading, particle size, zeta-potential and surface morphology were examined by Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD)...
December 14, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27937049/agglomeration-of-celecoxib-by-quasi-emulsion-solvent-diffusion-method-without-stabilizer-effect-of-good-solvent
#9
Maryam Maghsoodi, Ali Nokhodchi
AIM: The aim of the present research is to investigate the feasibility of agglomeration of crystals by the quasi emulsion solvent diffusion method without using a stabilizer. METHOD: Two solvent systems comprising a solvent and an antisolvent (water) were used to prepare celecoxib agglomerates. To this end, seven solvents including propanol, methyl acetate, methyl ethyl ketone, butanol, ethyl acetate, isopropyl acetate and pentanol were examined. The agglomerates were evaluated by micromeritic properties (e...
December 12, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27882805/free-radical-formation-in-chloramphenicol-heated-at-different-temperatures-and-the-best-thermal-sterilization-conditions-application-of-epr-spectroscopy-and-uv-spectrophotometry
#10
Paweł Ramos, Barbara Pilawa
Free radicals in thermally treated chloramphenicol were examined by electron paramagnetic resonance (EPR) spectroscopy. The parameters and shape of EPR spectra were analysed and free radical concentrations were obtained in the tested drug samples. Chloramphenicol was thermally sterilized at pharmacopeia conditions: 100 °C (120 min). Sterilization was also carried out at different conditions, 110 °C (60 min) and 120 °C (30 min), for comparison with pharmacopeia settings. Microbiological analysis was performed on the samples to confirm sterility...
December 12, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27882815/approaches-to-developing-fast-release-pellets-via-wet-extrusion-spheronization
#11
Yu Xia, Chun-Yang Shi, Jian-Guo Fang, Wen-Qing Wang
Microcrystalline cellulose (MCC) is widely regarded as the excellent choice to manufacture pellets via wet extrusion-spheronisation (ES) process due to its excellent water uptake capability, water holding capacity, desirable rheological properties, cohesiveness and plasticity etc. Nevertheless, in spite of all these advantages, limitations associated with the application of MCC also have been reported. The most prevailing limitation is prolonged or incomplete drug release profile due to the lack of disintegration as pellet contracts significantly during the drying process, especially when in combination with poorly soluble drug at a high level...
December 9, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27871215/formulation-characterization-and-in-vitro-ex-vivo-evaluation-of-quercetin-loaded-microemulsion-for-topical-application
#12
Azar Kajbafvala, Alireza Salabat, Anayatollah Salimi
The aim of this study was to develop a new microemulsion formulation for topical application of poorly soluble drug named quercetin. In order to design suitable microemulsion system, the pseudo-ternary phase diagrams of microemulsion systems were constructed at different surfactant/co-surfactant ratios using tween 80 as surfactant, transcutol(®) P as a co-surfactant and oleic acid as an oil phase. Some physicochemical properties such as droplet size, density, refractive index, electrical conductivity, pH, surface tension, and viscosity of the microemulsion systems were measured at 298...
December 9, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27885872/improvement-of-solubility-dissolution-and-stability-profile-of-artemether-solid-dispersions-and-self-emulsified-solid-dispersions-by-solvent-evaporation-method
#13
Muhammad Tayyab Ansari, Muhammad Sohail Arshad, Altaf Hussain, Zeeshan Ahmad
The purpose of this study was to investigate changes in the water solubility of artemether; a poorly soluble drug used for the treatment of malaria. Different solid dispersions (SDs) of artemether were prepared using artemether and polyethylene glycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESDs) containing artemether, polyethylene glycol 6000, cremophor-A-25, olive oil, hydroxypropylmethylcellulose and transcutol in the ratio 12:75:5:4:2:2, respectively (Group 2). SESDs were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3)...
December 8, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27875913/development-and-optimization-of-a-meloxicam-%C3%AE-cyclodextrin-complex-for-orally-disintegrating-tablet-using-statistical-analysis
#14
Ahmad Ainurofiq, Syaiful Choiri
The purpose of this research was to develop an inclusion complex of meloxicam (MEL)/β-cyclodextrin (β-CD) incorporated into an orally disintegrating tablet (ODT), using statistical analysis to optimize the ODT formulation based on a quality by design (QbD) approach. MEL/β-CD complexation was performed by kneading, co-precipitation and spray drying methods under different molar ratios. Fourier transform infrared spectroscopy, X-ray diffraction and thermal analysis were utilized to evaluate the complexes. A central composite design (α = 2) was applied to optimize and assess the influence of Primojel, Primellose and crushing strength (CS) as independent variables on tablet friability, disintegration behavior, wicking properties and drug release...
December 8, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27919197/correction-to-novel-platens-to-measure-the-hardness-of-a-pentagonal-shaped-tablet
#15
(no author information available yet)
No abstract text is available yet for this article.
December 5, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27876425/how-can-lipid-nanocarriers-improve-transdermal-delivery-of-olanzapine
#16
Nimra Iqbal, Carla Vitorino, Kevin M G Taylor
The development of a transdermal nanocarrier drug delivery system with potential for the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder, is described. Lipid nanocarriers (LN), encompassing various solid:liquid lipid compositions were formulated and assessed as potential nanosystems for transdermal delivery of olanzapine. A previously optimized method of hot high pressure homogenization (HPH) was adopted for the production of the LN, which comprised solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsions (NE)...
November 23, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27824281/on-the-inherent-properties-of-soluplus-and-its-application-in-ibuprofen-solid-dispersions-generated-by-microwave-quench-cooling-technology
#17
Nian-Qiu Shi, Hong-Wei Lai, Yong Zhang, Bo Feng, Xiao Xiao, Hong-Mei Zhang, Zheng-Qiang Li, Xian-Rong Qi
Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, or Soluplus(®), is a relatively new copolymer and a promising carrier of amorphous solid dispersions. Knowledge on the inherent properties of Soluplus(®) (e.g. cloud points, critical micelle concentrations, and viscosity) in different conditions is relatively inadequate, and the application characteristics of Soluplus(®)-based solid dispersions made by microwave methods still need to be clarified. In the present investigation, the inherent properties of a Soluplus(®) carrier, including cloud points, critical micelle concentrations, and viscosity, were explored in different media and in altered conditions...
November 16, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27808590/correlation-between-the-viscoelastic-properties-of-the-gel-layer-of-swollen-hpmc-matrix-tablets-and-their-in-vitro-drug-release
#18
Rania Hamed, Tamadur Al Baraghthi, Suhair Sunoqrot
Drug release from hydroxypropyl methylcellulose (HPMC) hydrophilic matrix tablets is controlled by drug diffusion through the gel layer of the matrix-forming polymer upon hydration, matrix erosion, or combination of diffusion and erosion mechanisms. In this study, the relationship between viscoelastic properties of the gel layer of swollen intact matrix tablets and drug release was investigated. Two sets of quetiapine fumarate (QF) matrix tablets were prepared using the high viscosity grade HPMC K4M at low (70 mg/tablet) and high (170 mg/tablet) polymer concentrations...
November 3, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27808578/a-new-polymorph-of-isoimperatorin
#19
Jing Fu, Xiaoxv Dong, Xinbing Yin, Chunjing Yang, Wenping Wang, Xueying Du, Xin Zhang, Jian Ni
Isoimperatorin is a naturally occurring furocoumarin and is being considered as a potential chemoprevention. Only one crystal form of isoimperatorin (Form I) was reported during previous research so that an investigation of polymorphism of isoimperatorin was successfully undertaken. A new polymorph of isoimperatorin was discovered through comprehensive polymorph screening experiments. Their structures were elucidated by single-crystal structure analysis and extensively characterized by XRPD, DSC, FT-IR and SEM...
November 3, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27808002/enhancement-of-levodopa-stability-when-complexed-with-%C3%AE-cyclodextrin-in-transdermal-patches
#20
Rana Obaidat, Nizar Al-Shar'i, Bassam Tashtoush, Tamara Athamneh
Levodopa is a promising candidate for administration via the transdermal route because it exhibits a short plasma half-life and has a small window of absorption in the upper section of the small intestine. The aim of this study was to prepare stable levodopa transdermal patches. Both xanthan gum and Carbopol 971 polymers were selected with ethylcellulose constituting the backing layer of the prepared patches. The effect of adding β-cyclodextrin on the prepared patches was investigated. The uniformity in thickness, weight and content of the studied patches was acceptable...
November 3, 2016: Pharmaceutical Development and Technology
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