Facile fabrication of an extended‐release tablet of Ticagrelor using three dimensional printing technology
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Abstract:
The objective of the study was to fabricate tailored extended-release tablets of blood thinner Ticagrelor as once-daily dosing using additive manufacturing for better compliance in heart failure therapy. The solid work design of the tablet was printed using hot melt extrusion (HME) based 3D printing by optimized mixture of Eudragit RS-100, plasticizer and drug for producing extrudable and printable filaments. FTIR and TGA results showed no covalent interaction among ingredients and no decomposition during HME process, respectively. Friability, weight variation, assay and content uniformity tests met USP requirements, while the mean hardness of the tablets was calculated in a value between 40 and 50 kg. According to DSC and XRD results, the crystallinity state of the Ticagrelor was converted to an amorphous one in the tablet matrix. Smooth surfaces with multiple deposited layers were observed using SEM. In comparison, the maximum Ticagrelor release of 100% after 120 min from Brilinta® tablets was decreased to 97% in 400 min from the 3D tablet at infill of 90%. Korsmeyer-Peppas kinetic model showed the drug release mechanism is affected by diffusion and swelling. In general, fabrication of the extended-release 3D printed tablet of Ticagrelor using HME-based-additive manufacturing has the potential to provide specific doses with tailored kinetic release for personalized medicine, improving adherence at point-of-care.Keywords:
Friability
The influence of various temperature and relative humidity conditions on changes in hardness and friability of five commercial brands of packaged paracetamol tablets stored over a period of six months has been investigated. At 75% RH all sample show deterioration in hardness at 25 degrees (5-10%) and at 45 degrees (10-39%). At 100% RH there is a little difference in deterioration in hardness at 25 degrees (16-24%) and 45 masculine (20-28%) suggesting that once the critical moisture content is reached by the tablets, further increase in relative humidity has little effect on changes in hardness. Under the same conditions, all tablets show an increase in friability ranging from 2.83 to 8.02%. The overall increase in friability with an increase in temperature from 25 degrees to 45 degrees at 75% and 100% RH is 0.0 to 25.2%. The results indicate that moisture sorption by tablet matrix through certain packaging materials may adversely affect the hardness and friability characteristics.
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The demand for fast dissolving tablet (FDT) has been growing during the last decade especially for elderly, children and patients who have swallowing difficulties. This dosage form is placed in the mouth, allowed to disperse or dissolve in the saliva, and then swallowed without the need of water. The problem of certain FDT is their low resistance and high friability. FDT having alone superdisintegrant have slow disintegration and high friability. The purpose of this study was to prepare and evaluate the coprocessed superdisintegrant in promoting tablet disintegration and having low friability. Attempt was made to develop FDT of Prochlorperazine Maleate with the help of coprocessed superdisintegrant. The tablets were evaluated for its percentage friability, disintegration time, wetting time, and hardness. In the investigation, a 32 full factorial design was used to investigate the combined influence of two formulation variables: amount of sodium starch glycolate and crospovidone. The results of multiple linear regression analysis revealed that for obtaining a hard and rapidly disintegrating dosage form. A checkpoint batch was also prepared to prove the validity of the evolved mathematical model. The concentration was optimized at which FDT disintegrate within 30 seconds and having friability 0.60%. A response surface plot is also presented to graphically represent the effect of the independent variables on the disintegration time and percentage friability. Optimized FDT should be prepared using an optimum concentration of sodium starch glycolate and crospovidone. Short-term stability studies indicated that there are no significant changes in drug content and in vitro disintegration time. The optimized tablet was found to be stable and shelf life is predicted more than two years.
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AbstractThe tablet friability resulting from manufacturing process variations was studied for two differently sized tablets using the same formulation. Granulations containing lower moisture contents required higher compression and ejection forces to manufacture a tablet at a given hardness, although this did not influence friability. Increased tablet hardness (and to a lesser extent decreased tablet thickness) decreased the tablet friability of the larger tablet. An increase in the quantity of granulating fluid increased the granulation particle size and slightly improved compactibility without significantly affecting friability. Tablet dissolution increased as the quantity of granulating fluid was decreased. There was a strong interaction, with respect to dissolution, between moisture content and the amount of granulating fluid. Tablet hardness did not significantly influence dissolution. Doubling the quantity of magnesium stearate in the granulation in one tablet strength decreased the maximum tablet hardness that could be obtained, and for the other tablet strength increased friability. It also resulted in slower tablet dissolution.
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Ticagrelor is a reversible P2Y12 receptor antagonist that is more potent than clopidogrel. When used in combination with aspirin, it reduces cardiovascular events in patients with acute coronary syndrome. However, unbiased review of 5 randomised controlled trials indicates that although statistically significant, the clinical superiority of ticagrelor over clopidogrel is modest. Thus, identification of patients who benefit the most from ticagrelor is a priority. Besides bleeding issues, ticagrelor can frequently cause bouts of dyspnoea, which requires ticagrelor replacement by another P2Y12 receptor antagonist, with a loading dose.
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Ticagrelor, acting as a reversible platelet aggregation inhibitor of P2Y12 receptors (P2Y12R), is regarded as one of the first-line antiplatelet drugs for acute cardiovascular diseases. Though the probability of ticagrelor resistance is much lower than that of clopidogrel, there have been recent reports of ticagrelor resistance. In this review, we summarized the clinical application of ticagrelor and then presented the criteria and current status of ticagrelor resistance. We further discussed the potential mechanisms for ticagrelor resistance in terms of drug absorption, metabolism, and receptor action. In conclusion, the incidences of ticagrelor resistance fluctuated between 0 and 20%, and possible mechanisms mainly arose from its absorption and receptor action. Specifically, a variety of factors, such as the drug form of ticagrelor, gut microecology, and the expression and function of P-glycoprotein (P-gp) and P2Y12R, have been shown to be associated with ticagrelor resistance. The exact mechanisms of ticagrelor resistance warrant further exploration, which may contribute to the diagnosis and treatment of ticagrelor resistance.
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This chapter focuses on photomechanical responses observed in photoresponsive polymeric materials that employ photochromic constituents to transduce light into macroscopic mechanical responses. It also focuses on photomechanical effects in amorphous and semicrystalline polymers that are polymers in the bulk solid states. In the numerous literature reports to date, photomechanical effects in amorphous and semicrystalline polymeric materials have shown strong dependence on the morphology, free volume, and other variables. Researchers at the Air Force Research Laboratory have recently completed a series of systematic investigations focused on elucidating the relationship of photomechanical effects in amorphous and semicrystalline polymeric materials to a variety of factors including crystallinity, segmental mobility, and cross-linking. Ordered crystalline regions have a denser molecular packing, leading to high bulk density of semicrystalline polymers versus amorphous polymers. In addition to the molecular packing effect, the proximity between polymer segments of crystalline region promotes stronger intermolecular secondary bonding, due to the reduction in intermolecular distance.
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