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AAPS PharmSciTech

Shaban A Khaled, Morgan R Alexander, Derek J Irvine, Ricky D Wildman, Martin J Wallace, Sonja Sharpe, Jae Yoo, Clive J Roberts
An extrusion-based 3D printer was used to fabricate paracetamol tablets with different geometries (mesh, ring and solid) from a single paste-based formulation formed from standard pharmaceutical ingredients. The tablets demonstrate that tunable drug release profiles can be achieved from this single formulation even with high drug loading (> 80% w/w). The tablets were evaluated for drug release using a USP dissolution testing type I apparatus. The tablets showed well-defined release profiles (from immediate to sustained release) controlled by their different geometries...
August 10, 2018: AAPS PharmSciTech
Long Xi, Hang Song, Yunzhi Wang, Haoshi Gao, Qiang Fu
The present study aimed to increase the in vitro dissolution rate of lacidipine, a poorly water-soluble drug, by formulating amorphous solid dispersions (ASDs) using hot-melt extrusion (HME). Differential scanning calorimetry, powder X-ray diffraction, polarized light microscopy, and Fourier transform infrared were used to characterize the optimal formulations and evaluate the physical stability for the stress test. Film-casting method and hot-stage microscopy were applied to study the miscibility of lacidipine and the drug carriers...
August 9, 2018: AAPS PharmSciTech
Changmin Kang, Ju-Hyun Lee, Dong-Wook Kim, Beom-Jin Lee, Jun-Bom Park
The purpose of this study was to prepare sustained release (SR) matrix tablets using a direct compression incorporated with a post-heating process. Allopurinol was selected due to the water-soluble property and Compritol 888 ATO® (also known as glyceryl behenate) was used as an SR matrix-forming agent. The API, SR material, microcrystalline cellulose, and magnesium stearate (lubricant) were mixed and prepared into a tablet by a direct compression method. The compressed tablets were stored in a dry oven at four temperatures (60, 70, 80, and 90°C) and for three time periods (15, 30, 45 min)...
August 9, 2018: AAPS PharmSciTech
Wen-Ting Wang, Hua Zhang, Yuan Yuan, Ya Guo, Shi-Xin He
Raman spectroscopy is a spectroscopic analysis technique that enables rapid qualitative and quantitative detection based on inelastic collision and Raman scattering intensity. This review detailed the generation principle, instrument composition, influencing factors, and common classifications of Raman spectrum. Furthermore, it summarized and forecast the research progress of Raman spectroscopy in the field of drug analysis simultaneously over the past decade, including the identification of active pharmaceutical ingredients (APIs), qualitative and quantitative studies of pharmaceutical preparations, detection of illicit drugs, the identification of Chinese herbal medicines, and the combination with other technologies...
August 8, 2018: AAPS PharmSciTech
Ling Dong, Feifei Yang, Zhihong Zhu, Yue Yang, Xiaoyu Zhang, Mingzhu Ye, Weisan Pan, Hao Pan
The objective of this study was to prepare ibuprofen enteric-coated sustained-release pellets (IB-SRPs) and codeine phosphate immediate-release pellets (CP-IRPs) to play a synergistic role in analgesia. The pellets were developed by extrusion-spheronization and fluidized bed coating technology. The single-factor investigation was used to determine the optimal prescription and process. The sustained-release membrane of IB-SRPs was water-insoluble ethyl cellulose (EC), triethyl citrate (TEC) was used as plasticizer, and hydroxypropyl methylcellulose (HPMCP) was chose as porogen...
August 8, 2018: AAPS PharmSciTech
Turki Al Hagbani, Sami Nazzal
Medicated chewing gums (MCGs) represent a unique platform for drug delivery. They have been defined as solid single-dose preparations, which may contain more than one active pharmaceutical ingredient (API) with base consisting primarily of gum that has to be chewed for a certain period of time. They mainly contain a tasteless masticatory gum base as the core with other minor nonmasticatory ingredients, such as flavors and sweeteners. Despite their advantages in drug delivery, MCGs remain a niche product due to the complexity of their formulation, lack of acceptable testing methods, and intricacy of their manufacturing...
August 7, 2018: AAPS PharmSciTech
Yutaka Inoue, Ayumi Nanri, Isamu Murata, Ikuo Kanamoto
The aim of the current study was to evaluate the physicochemical properties of a solid dispersion of coenzyme Q10 (CoQ10)/cyclodextrin metal organic frameworks-1 (CD-MOF-1). As a result of the powder X-ray diffraction (PXRD), it was confirmed that the CD-MOF-1 was changed from the α form to the β form by evaporation (EVP). A diffraction peak due to melting of CoQ10 disappeared the EVP (CoQ10/CD-MOF-1 = 1/2). The structure of this complex is presumed to be similar to the β form of CD-MOF-1. As a result of the differential scanning calorimetry (DSC), the endothermic peak due to the melting of CoQ10 disappeared the EVP (CoQ10/CD-MOF-1 = 1/2)...
August 7, 2018: AAPS PharmSciTech
Patricia Inês Back, Luisa Rodrigues Furtado, Marina Cardoso Nemitz, Lucélia Albarello Balestrin, Flávia Nathiely Silveira Fachel, Henrique Mautone Gomes, Roselena Silvestri Schuh, José Cláudio Moreira, Gilsane Lino von Poser, Helder Ferreira Teixeira
Soybean isoflavone-rich extracts have been considered as promising skin antiaging products due to their antioxidant activity. This study investigates the effect of soybean isoflavone forms on porcine ear skin permeation/retention from topical nanoemulsions and their potential in protecting skin against oxidative damage caused by UVA/UVB light. Soybean non-hydrolyzed (SNHE) and hydrolyzed (SHE) extracts, mainly composed of genistin and genistein, were produced. Nanoemulsions containing SNHE (NESNHE ) and SHE (NESHE ) were prepared by spontaneous emulsification procedure and yielded monodispersed nanoemulsions...
August 6, 2018: AAPS PharmSciTech
Soo Hyeon Shin, Jukkarin Srivilai, Sarah A Ibrahim, Caroline Strasinger, Dana C Hammell, Hazem E Hassan, Audra L Stinchcomb
Chemical penetration enhancers (CPEs) are frequently incorporated into transdermal delivery systems (TDSs) to improve drug delivery and to reduce the required drug load in formulations. However, the minimum detectable effect of formulation changes to CPE-containing TDSs using in vitro permeation tests (IVPT), a widely used method to characterize permeation of topically applied drug products, remains unclear. The objective of the current exploratory study was to investigate the sensitivity of IVPT in assessing permeation changes with CPE concentration modifications and subsequently the feasibility of IVPT's use for support of quality control related to relative CPE concentration variation in a given formulation...
August 6, 2018: AAPS PharmSciTech
Vaishnavi Parikh, Suhas G Gumaste, Shivaji Phadke
Surfactants are commonly incorporated in conventional and enabled formulations to enhance the rate and extent of dissolution of drugs exhibiting poor aqueous solubility. Generally the interactions between the drug and excipients are systematically evaluated, however, limited attention is paid towards understanding the effect of interaction between functional excipients and its impact on the performance of the product. In the current study, the effect of potential interaction between a nonionic polymer binder, povidone, and anionic surfactant docusate sodium on the rate and extent of dissolution of a drug exhibiting poor aqueous solubility was evaluated by varying the proportions of the binder and the surfactant in the formulation...
August 6, 2018: AAPS PharmSciTech
Débora Priscila de Campos, Neila Márcia Silva-Barcellos, Renata Rodrigues Lima, Ranylson Marcello Leal Savedra, Melissa Fabíola Siqueira, Maria Irene Yoshida, Wagner da Nova Mussel, Jacqueline de Souza
The recommended method for the biopharmaceutical evaluation of drug solubility is the shake flask; however, there are discrepancies reported about the solubility of certain compounds measured with this method, one of them is candesartan cilexetil. The present work aimed to elucidate the solubility of candesartan cilexetil by associating others assays such as stability determination, polymorphic characterization and in silico calculations of intrinsic solubility, ionized species, and electronic structures using quantum chemistry descriptors (frontier molecular orbitals and Fukui functions)...
July 30, 2018: AAPS PharmSciTech
Sangeetha Mathavan, Nigel Chen-Tan, Frank Arfuso, Hani Al-Salami
When we administered orally a mixture of the anti-diabetic drug, gliclazide (G) and a primary bile acid, they exerted a hypoglycemic effect in a rat model of type 1 diabetes (T1D), but stability of mixture was limited. We aimed to develop and characterize microcapsules incorporating G with a microcapsule-stabilizing bile acid, ursodeoxycholic acid (UDCA). Sodium alginate (SA)-based microcapsules were prepared with either G or G with UDCA and analyzed in terms of morphological, physico-chemical, and electro-chemical characteristics at different pH and temperatures...
July 30, 2018: AAPS PharmSciTech
Ravikumar Rramaswamy, Ganesh Mani, Senthil Venkatachalam, Ramesh Venkata Yasam, J C Bose Rajendran, Jang Hyun Tae
A simple composite electrospun nanofiber of cellulose acetate phthalate (CAP)-polyethylene glycol (PEG) loaded with tetrahydrocurcumin (THC) was developed in this study, and the in vitro diffusion of THC was evaluated. The nanofibers were characterized by scanning electron microscopy, powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC). The formulated nanofiber (NF) with THC has smooth morphology with diameter of around 300-500 nm. The complete entrapment and dispersion of THC was observed from the results of PXRD and DSC due to the loss of THC crystalline property...
July 25, 2018: AAPS PharmSciTech
Jun Soo Chae, Bo Ram Chae, Dong Jun Shin, Yoon Tae Goo, Eun Seok Lee, Ho Yub Yoon, Chang Hyun Kim, Young Wook Choi
To overcome the poor dissolution of telmisartan (TMS) at weak acidic pH, amorphous alkalinized TMS (AAT) was prepared by introducing sodium hydroxide as a selective alkalizer. AAT-containing polymeric solid dispersions were prepared by a solvent evaporation method; these solid dispersions were AAT-PEG, AAT-PVP, AAT-POL, and AAT-SOL for the polymers of PEG 6000, PVP K30, Poloxamer 407, and Soluplus, respectively. The characteristics of the different formulations were observed by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy...
July 24, 2018: AAPS PharmSciTech
Samaneh Ghassemi, Azadeh Haeri, Soraya Shahhosseini, Simin Dadashzadeh
The purpose of the current study was to develop a novel liposomal formulation to improve the oral bioavailability of carvedilol, a Biopharmaceutics Classification System class II with poor aqueous solubility and extensive presystemic metabolism. Conventional and various surfactant-enriched carvedilol-loaded liposomes were prepared by thin film hydration technique and physicochemical properties of liposomes (including size, encapsulation efficiency, release behavior, and morphology) were evaluated. To assess the oral bioavailability, in vivo studies were carried out in eight groups of male Wistar rats (n = 6) and the drug plasma concentration was determined...
July 20, 2018: AAPS PharmSciTech
Nikolaos Naziris, Natassa Pippa, Dimitris Stellas, Varvara Chrysostomou, Stergios Pispas, Costas Demetzos, Marcin Libera, Barbara Trzebicka
Chimeric/mixed stimuli-responsive nanocarriers are promising agents for therapeutic and diagnostic applications, as well as in the combinatorial field of theranostics. Herein, we designed chimeric nanosystems, composed of natural phospholipid and pH-sensitive amphiphilic diblock copolymer, in different molar ratios and assessed the polymer lyotropic effect on their properties. Initially, polymer-grafted bilayers were evaluated for their thermotropic behavior by thermal analysis. Chimeric liposomes were prepared through thin-film hydration and the obtained vesicles were studied by light scattering techniques, to measure their physicochemical characteristics and colloidal stability, as well as by imaging techniques, to elucidate their global and membrane morphology...
July 20, 2018: AAPS PharmSciTech
Hesham M Tawfeek, Matthew Roberts, Mohamed A El Hamd, Ahmed A H Abdellatif, Mahmoud A Younis
In an attempt to decrease the dose, anticipated side effects, and the cost of production of glibenclamide, GLC, a potent oral hypoglycemic drug, the enhancement of the dissolution and hence the oral bioavailability were investigated. Adsorption and co-adsorption techniques using carriers having a very large surface area and surface active agents were utilized to enhance the drug dissolution. Moreover, the Langmuir adsorption isotherms were constructed to identify the type and mechanism of adsorption. The optimized formulation showing the highest in vitro release was compressed into mini-tablet to facilitate drug administration to elderly patients and those having swallowing difficulties...
July 19, 2018: AAPS PharmSciTech
Ellen Hackl, Joseph Darkwah, Geoff Smith, Irina Ermolina
The current paper continues our study on the ability of L-arginine to prevent/reduce the aggregation of proteins that results from the various stresses during the lyophilisation and/or storage of lyophilized protein-based products. The first part of our study, i.e. formulation development, was devoted to the rational design and optimization of an L-arginine containing lyophilized formulation which can resist the natural tendency of L-arginine to absorb atmosphere moisture. Mannitol and trehalose were chosen among other excipients to be included in the protein-based formulation, as mannitol in a combination with L-arginine has been shown to reduce moisture sorption while trehalose provides a degree of lyoprotection...
July 6, 2018: AAPS PharmSciTech
Monika Lavan, Gregory Knipp
During the production process, an editorial error occurred where the label numbering for the first two tables were inadvertently switched. The original article has been corrected.
June 28, 2018: AAPS PharmSciTech
Regina G Kelmann, Mariana Colombo, Ricardo J Nunes, Cláudia M O Simões, Letícia S Koester
The aim of this study is to describe the development of nanoemulsion-loaded hydrogels to deliver pentyl gallate (PG), a gallic acid n-alkyl ester, through the skin. PG is an antioxidant agent; however, it seems to be a promising agent for herpis labialis treatment. Aristoflex AVC® and chitosan were used as gelling agents for nanoemulsion thickening. The developed formulations presented suitable PG content (94.4-100.3% w/w), nanometric droplet sizes (162-297 nm), high zeta potentials, and a non-Newtonian pseudoplastic behavior...
June 25, 2018: AAPS PharmSciTech
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