Fibrosing colonopathy associated with treatment with enteric-coated mesalazine pills

2009 ◽  
Vol 15 (10) ◽  
pp. 1452-1453 ◽  
Author(s):  
Gerardo Prieto ◽  
Begoña Pérez-Moneo ◽  
Manuel Molina ◽  
Esther Ramos ◽  
Jesús Sarría ◽  
...  
Keyword(s):  
Enteric Coated ◽  
Fibrosing Colonopathy

Knowledge, Perceptions and Practices on Modified Release Tablets among Prescribers: A Preliminary Study

2020 ◽  
Vol 01 (01) ◽  
pp. 05-14
Author(s):  
M.G.K.M. Fernando ◽  
K.I.J. Priyadarshi ◽  
L.G.T. Shanika ◽  
N.R. Samaranayake
Keyword(s):  
Online Survey ◽  
Product Information ◽  
Response Rate ◽  
Immediate Release ◽  
State Universities ◽  
Modified Release ◽  
Validated Questionnaire ◽  
Therapeutic Outcomes ◽  
Medical Faculties ◽  
Enteric Coated

Introduction: Modified release tablets (MRTs) are developed to achieve different therapeutic outcomes and are frequently prescribed. This study aims to evaluate the knowledge, perceptions and practices on using MRTs among a selected cohort of prescribers. Methods: A self administered online survey was conducted using a pre-validated questionnaire, prepared in-house to assess knowledge, perceptions and practices on using MRTs, among academics with an MBBS degree in medical faculties of State universities in Sri Lanka. Results: The response rate was 15.5% among 375 prescribers. Most were females (53.4%) and were 46-55 years (29.3%). Over 50% correctly expanded abbreviations related to MRTs. Most defined enteric coated (87.9%) and targeted release (77.6%) forms accurately. However, 87.0% mixed-up definitions of sustained release with controlled release. Most believed that inability to split tablets (70.7%) and high cost (70.7%), as disadvantages of MRTs. Nearly half did not identify the risk of dose dumping (53.5%) and inflexible dosing schedule (44.8%) as disadvantages. For frequency of administering MRTs, 86.2% referred the product information leaflet (PIL) while 29.0% depended on the frequency of the corresponding immediate release tablet. Most (79.3%) prescribed MRTs to increase patient compliance while 12.1% prescribed them to reduce cost. When problems regarding MRTs were encountered, most referred PILs (81.0%) and clarified with experts (75.9%). Conclusions: Although the response rate was low, a clear gap in knowledge, perceptions and practices on using MRTs were identified among prescribers who responded. Interventions are needed to improve the knowledge, perceptions, and practices on using MRTs among prescribers.

Has the Time Come to Employ Population and Individual Bioequivalence for the Evaluation of Generics?

2020 ◽  
Vol 21 (2) ◽  
pp. 112-125
Author(s):  
Francis Micheal ◽  
Mohanlal Sayana ◽  
Rajendra Prasad ◽  
Balamurali Musuvathi Motilal
Keyword(s):  
Therapeutic Index ◽  
Bioequivalence Study ◽  
Open Label ◽  
Statistical Parameters ◽  
Population Mean ◽  
Average Bioequivalence ◽  
Individual Bioequivalence ◽  
Population Bioequivalence ◽  
Enteric Coated ◽  
Bioequivalence Assessment

Background: Bioequivalence studies are a vital part of drug development. The average bioequivalence approach is the standard method of assessment to conclude whether the generic product is bioequivalent to the innovator product. Of late, debates are on whether the average bioequivalence approach adequately addresses drug interchangeability as it considers only population mean for the evaluation especially when highly variable drug products and narrow therapeutic index drugs are dealt with. Hence, the alternative approaches like population bioequivalence and individual bioequivalence assessment approaches emerge as they consider inter/intra-subject variance and subject- by-formulation variance along with population mean. Objectives: The objective of the study was to apply different bioequivalence assessment approaches in a replicate bioequivalence study to evaluate the drug interchangeability. Methods: This was an open-label, single-dose, randomized, balanced, two-treatment, three-period, three-sequence, partial replicate crossover bioequivalence study of omeprazole enteric-coated tablet 20 mg conducted on 48 normal healthy subjects under fed conditions. The plasma concentration of omeprazole was analyzed by a validated bioanalytical method to determine the pharmacokinetic and statistical parameters to assess average bioequivalence, population bioequivalence, and individual bioequivalence. Results: In this study, test formulation was shown to be bio-inequivalent to the reference formulation by average bioequivalence, population bioequivalence, and individual bioequivalence approaches. Conclusion: The outcome of the evaluation clearly states that the bioequivalence outcome of all these approaches are the same. Obviously, it does not mean that these three approaches provide the same outcome though the consideration of variances varies. Certainly, population bioequivalence and individual bioequivalence approach will be more accurate for the assessment of drug interchangeability.

A Review on Enteric Coated Pellets Composed of Core Pellets Prepared by Extrusion-Spheronization

2019 ◽  
Vol 13 (2) ◽  
pp. 83-90 ◽  
Author(s):  
Hetal Patel ◽  
Mukesh Gohel
Keyword(s):  
Dosage Form ◽  
Extended Release ◽  
Rapid Onset ◽  
Enteric Coating ◽  
Onset Of Action ◽  
The Core ◽  
Current State ◽  
Enteric Coated ◽  
Extrusion Spheronization ◽  
Acid Labile

Enteric coated dosage form bypasses the stomach and releases the drug into the small intestine. Advantages of enteric coated pellets in comparison with enteric coated tablets are a) Pellets provide rapid onset of action and faster drug release due to the smaller size than tablets and b) Pellets exhibit less residence time of acid-labile drugs in the stomach compared to tablets. Dosage form coat can be damaged by longer resistance time in the stomach. The present review summarizes the current state of enteric coated pellets where core pellets are prepared by extrusion-spheronization technique and the enteric coating is applied in a fluidized bed processor. Two approaches are involved in the preparation of core pellets. In the first approach, a mixture of drug and excipient(s)/co-processed excipient is passed through extruders to prepare core pellets. In the second approach, excipient core pellets are prepared by extrusion technique and the drug is layered onto it before the enteric coating. The excipients present in the core pellets decide immediate or extended release of drug in the intestine. The coprocessed excipient pellets provide less batch variability and provide a platform for layering of many drugs before enteric coating. Some patents included enteric coating pellets [CN105456223 (A), CN105596310 (A), CN105616371 (A), CN105663095 (A), CN101611766B, CN106511862 (A), CN106668018 (A), CN106727381 (A), CN106924222 (A), TW200624127 (A), US 2017/0165248A1, US 2017/0224720A1] are discussed.

scholarly journals In-vitro and in-vivo metabolism of different aspirin formulations studied by a validated liquid chromatography tandem mass spectrometry method

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Michele Dei Cas ◽  
Jessica Rizzo ◽  
Mariangela Scavone ◽  
Eti Femia ◽  
Gian Marco Podda ◽  
...  
Keyword(s):  
Oral Administration ◽  
Whole Blood ◽  
Serum Levels ◽  
Reversed Phase ◽  
Weekly Treatment ◽  
Low Dose Aspirin ◽  
Liquid Chromatography Tandem Mass ◽  
Enteric Coated

AbstractLow-dose aspirin (ASA) is used to prevent cardiovascular events. The most commonly used formulation is enteric-coated ASA (EC-ASA) that may be absorbed more slowly and less efficiently in some patients. To uncover these “non-responders” patients, the availability of proper analytical methods is pivotal in order to study the pharmacodynamics, the pharmacokinetics and the metabolic fate of ASA. We validated a high-throughput, isocratic reversed-phase, negative MRM, LC–MS/MS method useful for measuring circulating ASA and salicylic acid (SA) in blood and plasma. ASA-d4 and SA-d4 were used as internal standards. The method was applied to evaluate: (a) the "in vitro" ASA degradation by esterases in whole blood and plasma, as a function of time and concentration; (b) the "in vivo" kinetics of ASA and SA after 7 days of oral administration of EC-ASA or plain-ASA (100 mg) in healthy volunteers (three men and three women, 37–63 years). Parameters of esterases activity were Vmax 6.5 ± 1.9 and Km 147.5 ± 64.4 in plasma, and Vmax 108.1 ± 20.8 and Km 803.2 ± 170.7 in whole blood. After oral administration of the two formulations, tmax varied between 3 and 6 h for EC-ASA and between 0.5 and 1.0 h for plain-ASA. Higher between-subjects variability was seen after EC-ASA, and one subject had a delayed absorption over eight hours. Plasma AUC was 725.5 (89.8–1222) for EC-ASA, and 823.1(624–1196) ng h/mL (median, 25–75% CI) for plain ASA. After the weekly treatment, serum levels of TxB2 were very low (< 10 ng/mL at 24 h from the drug intake) in all the studied subjects, regardless of the formulation or the tmax. This method proved to be suitable for studies on aspirin responsiveness.

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