keyword
MENU ▼
Read by QxMD icon Read
search

Excipient

keyword
https://www.readbyqxmd.com/read/27915006/predicting-optimal-wet-granulation-parameters-for-extrusion-spheronisation-of-pharmaceutical-pellets-using-a-mixer-torque-rheometer
#1
Manuel Kuhs, John Moore, Gayathri Kollamaram, Gavin Walker, Denise Croker
Mixer torque rheometry (MTR) was evaluated as a pre-production (pre-formulation and optimization) tool for predicting ideal liquid-to-solid ratios (L/S) for extrusion-spheronisation of a wide range of APIs using 10g formulations. APIs of low, medium and high solubility were formulated at low and high loadings (15 and 40% w/w, respectively) with PVP as binder (5%) and MCC as the major excipient. L/S corresponding to the maximum torque produced during wet massing in the MTR, L/S(maxT), was 0.8 for the low solubility APIs, which decreased to 0...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27914235/hyaluronan-as-a-promising-excipient-for-ocular-drug-delivery
#2
REVIEW
Michaela Guter, Miriam Breunig
Hyaluronan (HA) is a naturally occurring polysaccharide and well known for its exceptional properties such as high biocompatibility and biodegradability, along with a low immunogenicity. Besides its use for various biomedical applications it recently came into focus as a favorable excipient for the formulation of various ocular therapeutics. This review article summarizes the ocular distribution of HA and its most heavily investigated binding protein "cluster of differentiation 44" (CD44) which is the rationale for the clinical use of HA, primarily as an additive in ocular applications ranging from eye drops to contact lenses...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27913241/evaluation-of-highly-branched-cyclic-dextrin-in-inhalable-particles-of-combined-antibiotics-for-the-pulmonary-delivery-of-anti-tuberculosis-drugs
#3
Kazunori Kadota, Arisa Senda, Hideaki Tagishi, John Oluwasogo Ayorinde, Yuichi Tozuka
This work aims to identify a suitable formulation for the pulmonary delivery of combinations of inhalational drugs using highly branched cyclic dextrin (HBCD) macromolecules. We compared the effectiveness between powders prepared from HBCD with those prepared from five alternative excipients (lactose, maltose, sucrose, β-cyclodextrin and methyl β-cyclodextrin) in the pulmonary delivery of a single-dosage form of two anti-tuberculosis drugs (isoniazid and rifampicin). Fine particles of untreated active pharmaceutical ingredients (APIs) and combination products using excipients were prepared by spray drying...
November 29, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27911829/supramolecular-pegylation-of-biopharmaceuticals
#4
Matthew J Webber, Eric A Appel, Brittany Vinciguerra, Abel B Cortinas, Lavanya S Thapa, Siddharth Jhunjhunwala, Lyle Isaacs, Robert Langer, Daniel G Anderson
The covalent modification of therapeutic biomolecules has been broadly explored, leading to a number of clinically approved modified protein drugs. These modifications are typically intended to address challenges arising in biopharmaceutical practice by promoting improved stability and shelf life of therapeutic proteins in formulation, or modifying pharmacokinetics in the body. Toward these objectives, covalent modification with poly(ethylene glycol) (PEG) has been a common direction. Here, a platform approach to biopharmaceutical modification is described that relies on noncovalent, supramolecular host-guest interactions to endow proteins with prosthetic functionality...
November 28, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27908675/effect-of-polymers-in-moisture-sorption-and-physical-stability-of-polymorphic-olanzapine
#5
Maria C Paisana, Martin A Wahl, F João
The study aims to elucidate the transformations of anhydrous olanzapine Form I (OLZ FI) into the hydrate forms, when stored at a high relative humidity or suspended in an aqueous media, in the presence of polymers. OLZ FI and physical mixtures (3:1 and 1:1, as powders or compacts) of olanzapine with polyethylene glycol (PEG-6000), polyvinylpyrrolidone (PVP K25) and hydroxypropylcellulose (HPC-LF) were stored (75%RH/25°C, 75%RH/40°C and 93%RH/25°C) for 28days. OLZ FI and the physical mixtures were also suspended in water under stirring (200rpm/60min)...
November 28, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27904076/amorphous-amorphous-phase-separation-of-freeze-concentrated-protein-and-amino-acid-excipients-for-lyophilized-formulations
#6
Ken-Ichi Izutsu, Hiroyuki Yoshida, Hiroko Shibata, Yukihiro Goda
The objective of this study was to elucidate the mixing state of proteins and amino acid excipients concentrated in the amorphous non-ice region of frozen solutions. Thermal analysis of frozen aqueous solutions was performed in heating scans before and after a heat treatment. Frozen aqueous solutions containing a protein (e.g., recombinant human albumin, gelatin) or a polysaccharide (dextran) and an amino acid excipient (e.g., L-arginine, L-arginine hydrochloride, L-arginine monophosphate, sodium L-glutamate) at varied mass ratios showed single or double Tg' (glass transition temperature of maximally freeze-concentrated solutes)...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27903454/effects-of-frequently-used-pharmaceutical-excipients-on-the-organic-cation-transporters-1-3-and-peptide-transporters-1-2-stably-expressed-in-mdckii-cells
#7
Marcus Otter, Stefan Oswald, Werner Siegmund, Markus Keiser
There is ample evidence that pharmaceutical excipients, which are supposed to be pharmacologically inactive, have an impact on drug metabolism and efflux transport. So far, little is known whether they also modulate uptake transporter proteins. We have recently shown that commonly used solubilizing agents exert significant effects on the function of organic anion uptake transporting polypeptides. Therefore, we investigated in this study the influence of frequently used pharmaceutical excipients on the transport activity of organic cation transporters OCT1, OCT2 and OCT3 and the peptide transporters PEPT1 and PEPT2...
November 26, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27898331/cleaning-verification-exploring-the-effect-of-the-cleanliness-of-stainless-steel-surface-on-sample-recovery
#8
Imad A Haidar Ahmad, James Tam, Xue Li, William Duffield, Thomas Tarara, Andrei Blasko
The parameters affecting the recovery of pharmaceutical residues from the surface of stainless steel coupons for quantitative cleaning verification method development have been studied, including active pharmaceutical ingredient (API) level, spiking procedure, API/excipient ratio, analyst-to-analyst variability, inter-day variability, and cleaning procedure of the coupons. The lack of a well-defined procedure that consistently cleaned coupon surface was identified as the major contributor to low and variable recoveries...
November 18, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27896684/use-of-spray-dried-dispersions-in-early-pharmaceutical-development-theoretical-and-practical-challenges
#9
Jinjiang Li, Dhaval Patel, George Wang
Spray-dried dispersions (SDDs) have become an important formulation technology for the pharmaceutical product development of poorly water-soluble (PWS) compounds. Although this technology is now widely used in the industry, especially in the early-phase development, the lack of mechanistic understanding still causes difficulty in selecting excipients and predicting stability of SDD-based drug products. In this review, the authors aim to discuss several principles of polymer science pertaining to the development of SDDs, in terms of selecting polymers and solvents, optimizing drug loading, as well as assessing physical stability on storage and supersaturation maintenance after dissolution, from both thermodynamic and kinetic considerations...
November 28, 2016: AAPS Journal
https://www.readbyqxmd.com/read/27894968/crystallographic-structure-intermolecular-packing-energetics-crystal-morphology-and-surface-chemistry-of-salmeterol-xinafoate-form-i
#10
Alexandru A Moldovan, Ian Rosbottom, Vasuki Ramachandran, Christopher M Pask, Oboroghene Olomukhoro, Kevin J Roberts
Single crystals of salmeterol xinafoate (form I), prepared from slow cooled supersaturated propan-2-ol solutions, crystallise in a triclinic P‾1 symmetry with two closely related independent salt pairs within the asymmetric unit, with an approximately double unit cell volume compared to the previously published crystal structure(1). Synthonic analysis of the bulk intermolecular packing confirms the similarity in packing energetics between the two salt pairs. The strongest synthons, as expected, are dominated by coulombic interactions...
November 25, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27894967/role-of-buffers-in-protein-formulations
#11
REVIEW
Teddy J Zbacnik, Ryan E Holcomb, Derrick S Katayama, Brian M Murphy, Robert W Payne, Richard C Coccaro, Gabriel J Evans, James E Matsuura, Charles S Henry, Mark Cornell Manning
Buffers comprise an integral component of protein formulations. Not only do they function to regulate shifts in pH, they also can stabilize proteins by a variety of mechanisms. The ability of buffers to stabilize therapeutic proteins whether in liquid formulations, frozen solutions or the solid state is highlighted in this review. Addition of buffers can result in increased conformational stability of proteins, whether by ligand binding or by an excluded solute mechanism. In addition they can alter the colloidal stability of proteins and modulate interfacial damage...
November 25, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27890621/nasal-drug-delivery-design-of-a-novel-mucoadhesive-and-in-situ-gelling-polymer
#12
Claudia Menzel, Max Jelkmann, Flavia Laffleur, Andreas Bernkop-Schnürch
The aim of the present study was to establish a novel polymeric excipient for liquid nasal dosage forms exhibiting viscosity increasing properties, improved mucoadhesion and stability towards oxidation in solution. In order to achieve this goal, 2-mercaptonicotinic acid was first coupled to L-cysteine by disulfide exchange reaction and after purification directly attached to the polymeric backbone of xanthan gum by carbodiimide mediated amide bond formation. The resulting conjugate was characterized with respect to the amount of coupled ligand, the in situ gelling behavior, mucoadhesive properties and stability towards oxidation...
November 24, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27890595/the-formation-and-physical-stability-of-two-phase-solid-dispersion-systems-of-indomethacin-in-supercooled-molten-mixtures-with-different-matrix-formers
#13
Kristian Semjonov, Karin Kogermann, Ivo Laidmäe, Osmo Antikainen, Clare J Strachan, Henrik Ehlers, Jouko Yliruusi, Jyrki Heinämäki
Amorphous solid dispersions (SDs) are a promising approach to improve the dissolution rate of and oral bioavailability of poorly water-soluble drugs. In some cases multi-phase, instead of single-phase, SD systems with amorphous drug are obtained. While it is widely assumed that one-phase amorphous systems are desirable, two-phase systems may still potentially exhibit enhanced stability and dissolution advantages over undispersed systems. The objective of the present study was to understand the solid-state properties of two-phase SDs with amorphous drug and their relation to physical stability...
November 23, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27890244/development-and-optimization-of-a-wet-granulation-process-at-elevated-temperature-for-a-poorly-compactible-drug-using-twin-screw-extruder-for-continuous-manufacturing
#14
Anuprabha K Meena, Divyakant Desai, Abu T M Serajuddin
The objective of this study was to enhance tabletability of a poorly compactible drug, acetaminophen, by wet granulation using twin screw extruder at high temperature. It was desired that there would be minimum amounts of excipients used and the granules obtained after extrusion would be dry and fall within a size range suitable for tableting without any further processing. Mixtures of acetaminophen (95%) with binders (5% povidone or partially pregelatinized starch) were wet granulated through twin screw extruder at 70°C by adding 7% w/w water...
November 24, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27889669/physicochemical-analysis-in-the-evaluation-of-reconstituted-dry-emulsion-tablets
#15
Noémi Anna Niczinger, Barnabás Kállai-Szabó, Miléna Lengyel, Péter Gordon, Imre Klebovich, István Antal
The aim of this study was to characterize the formation of emulsions by droplet size analysis and turbidimetry during reconstitution from a solid dosage form, namely from dry emulsion systems, which carry an oil phase for poorly soluble active ingredients. For the dry emulsion systems tablets were prepared either from oil-in-water systems using a freeze-drying process or through direct compression containing the same oil and excipients. The ratios of oil to emulgents and oil to xanthan gum were equal in both methods...
November 18, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27888143/dissolution-behavior-of-co-amorphous-amino-acid-indomethacin-mixtures-the-ability-of-amino-acids-to-stabilize-the-supersaturated-state-of-indomethacin
#16
Rami Ojarinta, Aki T Heikkinen, Elina Sievänen, Riikka Laitinen
Arginine, phenylalanine, and tryptophan have been previously shown to improve the solid-state stability of amorphous indomethacin. The present study investigates the ability of these amino acids to prolong the supersaturation of indomethacin in both aqueous and biorelevant conditions either when freely in solution or when formulated as co-amorphous mixtures. The co-amorphous amino acid-indomethacin mixtures (molar ratio 1:1) and amorphous indomethacin were prepared by cryomilling. Dissolution and precipitation tests were performed in buffer solutions (pH 5 and 6...
November 22, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27887722/the-effect-of-specific-surface-area-of-chitin-metal-silicate-coprocessed-excipient-on-the-chemical-decomposition-of-cefotaxime-sodium
#17
Suhair S Al-Nimry, Khouloud A Alkhamis, Kawthar Z Alzarieni
Chitin-metal silicates are multifunctional excipients used in tablets. Previously, a correlation between the surface acidity of chitin-calcium and chitin-magnesium silicate and the chemical decomposition of cefotaxime sodium was found but not with chitin-aluminum silicate. This lack of correlation could be due to the catalytic effect of silica alumina or the difference in surface area of the excipients. The objective of this study was to investigate the effect of the specific surface area of the excipient on the chemical decomposition of cefotaxime sodium in the solid state...
November 22, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27886514/sugar-based-novel-niosomal-nanocarrier-system-for-enhanced-oral-bioavailability-of-levofloxacin
#18
Muhammad Imran, Muhammad Raza Shah, Farhat Ullah, Shafi Ullah, Abdelbary M A Elhissi, Waqas Nawaz, Farid Ahmad, Abdul Sadiq, Imdad Ali
CONTEXT: Vesicular systems have attracted great attention in drug delivery because of their amphiphilicity, biodegradability, non-toxicity and potential for increasing drug bioavailability. OBJECTIVE: A novel sugar-based double-tailed surfactant containing renewable block was synthesized for preparing niosomal vesicles that could be exploited for Levofloxacin encapsulation, aiming to increase its oral bioavailability. MATERIALS AND METHODS: The surfactant was characterized by (1)H NMR, mass spectroscopy and Fourier transform infrared spectroscopy (FT-IR)...
November 2016: Drug Delivery
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
#19
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 (SD) of artemether were prepared using; artemether and polyethyleneglycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESD) 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). SESD's were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3)...
November 25, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27882559/lipiodol-does-not-affect-the-tissue-distribution-of-intravenous-doxorubicin-infusion-in-pigs
#20
Elsa Lilienberg, Ilse R Dubbelboer, Erik Sjögren, Hans Lennernäs
OBJECTIVES: In liver cancer treatment, lipiodol is used as a pharmaceutical excipient to improve delivery of the cytostatic drug doxorubicin (DOX). As DOX and its metabolite doxorubicinol (DOXol) cause serious off-target adverse effects, we investigated the effects of drug-free lipiodol or ciclosporin (CsA) on the tissue distribution (Kp ) of DOX and DOXol in relevant pig tissues. METHODS: Four treatment groups (TI-TIV) all received an intravenous DOX solution at 0 and 200 min...
November 23, 2016: Journal of Pharmacy and Pharmacology
keyword
keyword
82396
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"