Development and Characterization of Enteric-Coated Immediate-Release Pellets of Aceclofenac by Extrusion/Spheronization Technique Using κ-Carrageenan as a Pelletizing Agent

With the purpose of evaluating the behavior of different polymers employed as binders in small-diameter pellets for oral administration, we prepared formulations containing paracetamol and one of the following polymers: PVP, PEG 1500, hydroxypropylmethylcellulose and methylcellulose, and we evaluated their different binding properties. The pellets were obtained by the extrusion/spheronization process and were subsequently subjected to fluid bed drying. In order to assess drug delivery, the United States Pharmacopeia (USP) apparatus 3 (Bio-Dis) was employed, in conjunction with the method described by the same pharmacopeia for the dissolution of paracetamol tablets (apparatus 1). The pellets were also evaluated for granulometry, friability, true density and drug content. The results indicate that the different binders used are capable of affecting production in different ways, and some of the physicochemical characteristics of the pellets, as well as the dissolution test, revealed that the formulations acted like immediate-release products. The pellets obtained presented favorable release characteristics for orally disintegrating tablets. USP apparatus 3 seems to be more adequate for discriminating among formulations than the basket method.

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In vivo and in vitro characterization of immediate release dosage forms containing n-acetylcysteine using the dynamic open flow-through test apparatus

10.26226/morressier.57d6b2b7d462b8028d88dd29 ◽

2016 ◽

Author(s):

Maximilian Sager

Keyword(s):

Immediate Release ◽

Dosage Forms ◽

Test Apparatus ◽

Open Flow ◽

In Vitro Characterization ◽

Flow Through

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

Journal of Health Sciences and Innovative Research ◽

10.31357/jhsir.v1i01.4769 ◽

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.

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Faculty of 1000 evaluation for Intragastric acidity and omeprazole exposure during dosing with either PA32540 (enteric-coated aspirin 325 mg + immediate-release omeprazole 40 mg) or enteric-coated aspirin 325 mg + enteric-coated omeprazole 40 mg - a randomised, phase 1, crossover study.

F1000 - Post-publication peer review of the biomedical literature ◽

10.3410/f.718016185.793478839 ◽

2013 ◽

Author(s):

Ian Beales

Keyword(s):

Crossover Study ◽

Phase 1 ◽

Immediate Release ◽

Intragastric Acidity ◽

Enteric Coated Aspirin ◽

Enteric Coated

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

Recent Patents on Drug Delivery & Formulation ◽

10.2174/1872211313666190212115139 ◽

2019 ◽

Vol 13 (2) ◽

pp. 83-90 ◽

Cited By ~ 1

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.

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Development and characterization of enteric-coated microparticles of biochanin A for their beneficial pharmacological potential in estrogen deficient-hypertension

Drug Delivery ◽

10.3109/10717544.2015.1114046 ◽

2015 ◽

Vol 23 (6) ◽

pp. 2044-2057 ◽

Cited By ~ 11

Author(s):

Chinu Sachdeva ◽

Neeraj Mishra ◽

Saurabh Sharma

Keyword(s):

Biochanin A ◽

Enteric Coated ◽

Pharmacological Potential

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Impact of pharmaceutical dosage form on stability and dissolution of roxithromycin

Open Medicine ◽

10.2478/s11536-009-0113-7 ◽

2010 ◽

Vol 5 (1) ◽

pp. 83-90 ◽

Cited By ~ 2

Author(s):

Michał Ostrowski ◽

Ewa Wilkowska ◽

Tomasz Bączek

Keyword(s):

High Performance ◽

Bitter Taste ◽

Immediate Release ◽

Oral Suspension ◽

Pharmaceutical Dosage Form ◽

Dissolution Tests ◽

Ph Conditions ◽

Dispersible Tablets ◽

Enteric Coated

AbstractThe behavior of dispersible tablets containing enteric-coated pellets and oral suspension, both containing roxithromycin, was investigated using dissolution tests in different media. The dissolution test was performed under different pH conditions. For both dosage forms investigated, the test was conducted at pH 1.2, 4.5, and 6.8. Additionally, for dispersible tablets, the test involving increasing pH was performed at pH 1.2 (acid stage) and afterwards at pH 6.8 (buffer stage). The extent of dissolution was measured using high-performance liquid chromatography (HPLC). In all cases tested, roxithromycin underwent rapid degradation at pH 1.2. Dispersible tablets displayed the features of modified release preparations with a non-complete dissolution during the test times in all media. Conversely, the oral suspension behaved as an immediate release preparation, with degradation at pH 1.2. However, the dissolution of the oral suspension at pH 4.5 and 6.8 was rapid and complete. The role of enteric-coated pellets is to mask the bitter taste of the active substance upon administration. However, the coating showed lack of resistance to media at pH 1.2. Therefore, dispersible tablets containing enteric-coated pellets are not pharmaceutically equivalent to the immediate-release oral suspension.

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