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Crushed Tablet Formulations

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https://www.readbyqxmd.com/read/28070847/role-of-water-sorption-in-tablet-crushing-strength-disintegration-and-dissolution
#1
M Sacchetti, R Teerakapibal, K Kim, E J Elder
Drugs formulated as tablets are subjected to accelerated stability conditions with the goal of identifying a stable formulation that will exhibit a sufficiently long shelf life. Water sorption at a condition such as 40°C/75% RH can result in significant changes in tablet properties such as a decrease in dissolution rate, the cause of which may be difficult to interpret, given the complex nature of ingredients and their interactions in a tablet. In this research, three drugs, displaying a wide range of physicochemical properties, were formulated with commonly used diluents, disintegrants, and binders, using a design of experiments approach...
January 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28053581/optimization-of-formulation-and-processing-of-moringa-oleifera-and-spirulina-complex-tablets
#2
Yi Zheng, Fan Zhu, Dan Lin, Jun Wu, Yichao Zhou, Bohn Mark
Objective: To prepare a more comprehensive nutrition, more balanced proportion of natural nutritional supplement tablets with Moringa oleifera leaves and spirulina the two nutrients which have complementary natural food ingredients. Method: On the basis of research M. oleifera leaves with spirulina nutrient composition was determined on M. oleifera leaves and spirulina ratio of raw materials, and the choice of microcrystalline cellulose, sodium salt of caboxy methyl cellulose(CMC),magnesium stearate excipient, through single factor and orthogonal experiment, selecting the best formula tablets prepared by powder direct compression technology, for preparation of M...
January 2017: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/28053507/riluzole-5-mg-ml-oral-suspension-for-optimized-drug-delivery-in-amyotrophic-lateral-sclerosis
#3
Ann Margaret Dyer, Alan Smith
The aim of the present work is to extensively evaluate the pharmaceutical attributes of currently available riluzole presentations. The article describes the limitations and risks associated with the administration of crushed tablets, including the potential for inaccurate dosing and reduced rate of absorption when riluzole is administered with high-fat foods, and the advantages that a recently approved innovative oral liquid form of riluzole confers on amyotrophic lateral sclerosis (ALS) patients. The article further evaluates the patented and innovative controlled flocculation technology used in the pseudoplastic suspension formulation to reduce the oral anesthesia seen with crushed tablets, resulting in optimized drug delivery for riluzole...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28040560/a-systematic-review-of-the-use-of-dosage-form-manipulation-to-obtain-required-doses-to-inform-use-of-manipulation-in-paediatric-practice
#4
REVIEW
Roberta H Richey, Clare Hughes, Jean V Craig, Utpal U Shah, James L Ford, Catrin E Barker, Matthew Peak, Anthony J Nunn, Mark A Turner
This study sought to determine whether there is an evidence base for drug manipulation to obtain the required dose, a common feature of paediatric clinical practice. A systematic review of the data sources, PubMed, EMBASE, CINAHL, IPA and the Cochrane database of systematic reviews, was used. Studies that considered the dose accuracy of manipulated medicines of any dosage form, evidence of safety or harm, bioavailability, patient experience, tolerability, contamination and comparison of methods of manipulation were included...
December 28, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27956191/effects-of-excipients-and-curing-process-on-the-abuse-deterrent-properties-of-directly-compressed-tablets
#5
Ziyaur Rahman, Ahmed S Zidan, Maxwell Korang-Yeboah, Yang Yang, Akhtar Siddiqui, Diaa Shakleya, Mansoor A Khan, Celia Cruz, Muhammad Ashraf
The objective of the present investigation was to understand the effects of excipients and curing process on the abuse deterrent properties (ADP) of Polyox™ based directly compressible abuse deterrent tablet formulations (ADFs). The excipients investigated were lactose (monohydrate or anhydrous), microcrystalline cellulose and hydroxypropyl methylcellulose. The ADPs studied were tablet crush resistance or hardness, particle size distribution following mechanical manipulation, drug extraction in water and alcohol, syringeability and injectability...
December 9, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27923700/continuous-monitoring-of-api-content-api-distribution-and-crushing-strength-after-tableting-via-near-infrared-chemical-imaging
#6
P R Wahl, I Pucher, O Scheibelhofer, M Kerschhaggl, S Sacher, J G Khinast
Near-infrared chemical imaging (NIR-CI) with high-speed cameras based on the push-broom acquisition principle is a rapidly-evolving and can be used for a variety of purposes, from classification (and sorting) of products to mapping spatial distribution of materials. The present study examined if NIR-CI is suitable for tablet manufacturing. To that end, the tablets were introduced into the CI system via a flat belt conveyor. A formulation, which consisted of 4wt.%-6wt.% caffeine, 5wt.% crospovidone as a disintegrant, 88wt...
December 5, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27904079/application-of-response-surface-methodology-to-estimate-the-design-space-of-pharmaceutical-diluents-for-dispensing-powdered-formulations
#7
Yasunori Miyazaki, Kozo Takayama, Tomonobu Uchino, Yoshiyuki Kagawa
Scientific approaches for dispensation are important for the quality and efficacy of drug treatments. Therefore, for the dispensation of powdered medicines, we have developed a powder blending method using a planetary centrifugal mixer (PCM) to replace the empirical manual method involving a mortar and pestle. The aim of this study was to optimize the formulation of pharmaceutical diluents for dispensing powdered medicines, using PCM. The diluents, composed of powdered lactose, crystalline lactose, and corn starch were assigned to a {3,2}-Simplex Lattice design...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27875913/development-and-optimization-of-a-meloxicam-%C3%AE-cyclodextrin-complex-for-orally-disintegrating-tablet-using-statistical-analysis
#8
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/27773347/chewed-ticagrelor-tablets-provide-faster-platelet-inhibition-compared-to-integral-tablets-the-inhibition-of-platelet-aggregation-after-administration-of-three-different-ticagrelor-formulations-ipaad-tica-study-a-randomised-controlled-trial
#9
Dimitrios Venetsanos, Sofia Sederholm Lawesson, Eva Swahn, Joakim Alfredsson
AIMS: To provide pharmacodynamic data of crushed and chewed ticagrelor tablets, in comparison with standard integral tablets. METHODS: Ninety nine patients with stable angina were randomly assigned, in a 3:1:1 fashion, to one of the following 180mg ticagrelor loading dose (LD) formulations: A) Integral B) Crushed or C) Chewed tablets. Platelet reactivity (PR) was assessed with VerifyNow before, 20 and 60min after LD. High residual platelet reactivity (HRPR) was defined as >208 P2Y12 reaction units (PRU)...
January 2017: Thrombosis Research
https://www.readbyqxmd.com/read/27540214/a-really-wheezy-way-to-save-money
#10
Grace Li, Ofran Almossawi, Hasna Dulfeker, Vicky Jones, Felicity Taylor
AIM: To compare the palatability of oral non-soluble and oral soluble prednisolone tablets in paediatric patients admitted to the general paediatric wards in an acute London Trust. METHOD: As part of ongoing quality improvement initiatives, the Paediatric and Pharmacy departments compared tolerability of soluble versus non-soluble prednisolone in a group of 27 patients. Using a modified 5 point hedonic scale with 'smiley' faces we measured palatability and tolerance (swallowed versus refusal or vomiting) over two three week periods: the first period whilst soluble prednisolone was dispensed (n=17) and the second period after the switch to non-soluble prednisolone had been made (n=10)...
September 2016: Archives of Disease in Childhood
https://www.readbyqxmd.com/read/27492017/oral-dosage-form-administration-practice-in-children-under-6-years-of-age-a-survey-study-of-paediatric-nurses
#11
A C Walch, E Henin, J Berthiller, X Dode, B Abel, B Kassai, A Lajoinie
The purpose of this study was to interview paediatric nurses on administration issues using extemporaneous capsules and marketed capsules and tablets in children younger than 6 years old, based on most frequently administered drugs in six participating wards. The 59 responding nurses estimated respectively at 7.7±1.7 and 7.3±1.8years the age from which children would properly swallow extemporaneous capsules and marketed solids, with 33% and 37% of nurses considering that children under 6 would not get their prescribed treatment using these dosage forms...
September 25, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27473278/new-multifunctional-pharmaceutical-excipient-in-tablet-formulation-based-on-citric-acid-cyclodextrin-polymer
#12
Maria José Garcia-Fernandez, Nicolas Tabary, Feng Chai, Frédéric Cazaux, Nicolas Blanchemain, Marie-Pierre Flament, Bernard Martel
A β-cyclodextrin (β-CD) polymer obtained by crosslinking β-CD with citric acid in its water-insoluble (PCD-I) and soluble (PCD-S) forms was used as a multifunctional direct compression excipient for tablet designing. PCD-I powder was obtained after grinding the solid fraction through a 200μm grid. PCD-S powder was recovered after lyophilization or spray drying of the PCD-S aqueous solutions, eventually followed by a wet granulation step. Both PCD-I and PCD-S powders were characterized, separately and mixed in variable ratios, based on dynamic water vapor sorption, SEM, particle size distribution, tapped density, compressibility, and flowability...
September 25, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27467117/deterred-drug-abuse-using-superabsorbent-polymers
#13
David J Mastropietro, Srinath Muppalaneni, Hossein Omidian
OBJECTIVE: This study aimed to determine whether selected superabsorbent polymers (SAPs) could be used as a suitable alternative to thwart extraction, filtration, and syringeability attempts for abuse. Many abuse-deterrent formulations (ADFs) rely on high molecular weight polymers such as poly(ethylene oxide) to provide crush and extraction resistance. However, these polymers suffer from slow dissolution kinetics, and are susceptible to a variety of abuse conditions. METHODS: Several commercially available SAPs were evaluated for swelling behavior in extraction solvents, and tableting properties...
November 2016: Expert Opinion on Drug Delivery
https://www.readbyqxmd.com/read/27402156/crush-resistance-and-insufflation-potential-of-poly-ethylene-oxide-based-abuse-deterrent-formulations
#14
Srinath Muppalaneni, David J Mastropietro, Hossein Omidian
OBJECTIVES: This study was conducted to evaluate suitable methods of testing crush-resistant tablets composed largely of thermoplastic polymers. The objectives were, i) to evaluate the effect of thermal processes on crush resistance, ii) to develop test method(s) to indicate whether a crush-resistant tablet is susceptible to tampering by insufflation based on generated particle sizes, and iii) to find an appropriate analytical tool for discriminatory studies. METHODS: We investigated the crush-resistance properties of poly(ethylene oxide) (PEO) tablets using three manual and four electrical devices...
October 2016: Expert Opinion on Drug Delivery
https://www.readbyqxmd.com/read/27349946/the-milky-way-paediatric-milk-based-dispersible-tablets-prepared-by-direct-compression-a-proof-of-concept-study
#15
Samuel E F Orubu, Nicholas J Hobson, Abdul W Basit, Catherine Tuleu
OBJECTIVES: Dispersible tablets are proposed by the World Health Organization as the preferred paediatric formulation. It was hypothesised that tablets made from a powdered milk-base that disperse in water to form suspensions resembling milk might be a useful platform to improve acceptability in children. METHODS: Milk-based dispersible tablets containing various types of powdered milk and infant formulae were formulated. The influence of milk type and content on placebo tablet properties was investigated using a design-of-experiments approach...
June 28, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27346282/an-integrated-quality-by-design-qbd-approach-for-design-development-and-optimization-of-orally-disintegrating-tablet-formulation-of-carbamazepine
#16
Saurabh M Mishra, Bhagwan D Rohera
The objective of the present study was to design and develop a formulation for orally disintegrating tablets (ODTs) of carbamazepine using quality by design principles. The target product profile (TPP) and quality target product profile (QTPP) of ODTs were identified. Risk assessment was carried out by leveraging prior knowledge and experience to define the criticality of factors based on their impact by Ishikawa fishbone diagram and preliminary hazard analysis tool. Box-Behnken response surface methodology was used to study the effect of critical factors on various attributes of ODTs...
June 27, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27344987/comparison-between-self-formulation-and-compounded-formulation-dexamethasone-mouth-rinse-for-oral-lichen-planus-a-pilot-randomized-cross-over-trial
#17
Jessica L Hambly, Alison Haywood, Laetitia Hattingh, Raj G Nair
AIM: There is a lack of appropriate, commercially-available topical corticosteroid formulations for use in oral lichen planus (OLP) and oral lichenoid reaction. Current therapy includes crushing a dexamethasone tablet and mixing it with water for use as a mouth rinse. This formulation is unpleasant esthetically and to use in the mouth, as it is a bitter and gritty suspension, resulting in poor compliance. Thus, the present study was designed to formulate and pilot an effective, esthetically-pleasing formulation...
June 26, 2016: Journal of Investigative and Clinical Dentistry
https://www.readbyqxmd.com/read/27330154/abuse-potential-with-oral-route-of-administration-of-a-hydrocodone-extended-release-tablet-formulated-with-abuse-deterrence-technology-in-nondependent-recreational-opioid-users
#18
Mona Darwish, Mary Bond, Yuju Ma, William Tracewell, Philmore Robertson, Lynn R Webster
OBJECTIVE: To compare the oral abuse potential of hydrocodone extended-release (ER) tablet developed with CIMA(®) Abuse-Deterrence Technology with that of hydrocodone immediate release (IR). DESIGN: Randomized, double-blind, placebo-controlled, crossover study. SETTING AND PATIENTS: One study site in the United States; adult nondependent, recreational opioid users. METHODS: After confirming their ability to tolerate and discriminate hydrocodone IR 45 mg from placebo, eligible participants were randomized to receive each of the following oral treatments once: finely crushed placebo, hydrocodone IR 45-mg powder, intact hydrocodone ER 45-mg tablet, and finely crushed hydrocodone ER 45-mg tablet...
June 21, 2016: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/27183705/physicochemical-characterisation-of-fluids-and-soft-foods-frequently-mixed-with-oral-drug-formulations-prior-to-administration-to-children
#19
E Kersten, A Barry, S Klein
Oral drug administration to children poses specific pharmaceutical challenges that are often not seen to the same extent in adults, and whose occurrence may also be age dependent. When an age-appropriate dosage form is not available, manipulation of adult dosage forms (e.g., splitting and crushing of tablets or opening of capsules) has been reported as a means to facilitate administration to children. To enhance swallowability and/or mask an unpleasant taste of the dosage form to be administered, crushed/split tablets or the contents of capsules are often mixed with food or drinks or suspended in a vehicle prior to administration...
March 2016: Die Pharmazie
https://www.readbyqxmd.com/read/27162630/bioavailability-pharmacokinetics-and-safety-of-riociguat-given-as-an-oral-suspension-or-crushed-tablet-with-and-without-food
#20
Soundos Saleh, Reiner Frey, Corina Becker, Sigrun Unger, Georg Wensing, Wolfgang Mück
Riociguat is approved for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. Some patients have difficulty swallowing tablets; therefore, 2 randomized, nonblinded, crossover studies compared the relative bioavailability of riociguat oral suspensions and immediate-release (IR) tablet and of crushed-tablet preparations versus whole IR tablet. In study 1, 30 healthy subjects received 5 single riociguat doses: 0.3 and 2.4 mg (0.15 mg/mL suspensions), 0.15 mg (0.03 mg/mL), and 1...
March 2016: Pulmonary Circulation
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