scholarly journals Extended Release Enteric Coated Capsule Dosage Form

2020 ◽  
Author(s):  
2019 ◽  
Vol 13 (2) ◽  
pp. 83-90 ◽  
Author(s):  
Hetal Patel ◽  
Mukesh Gohel

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.


Author(s):  
Lotlikar V ◽  
S Shidhaye ◽  
U Kedar ◽  
V Kadam

The aim of this study was to develop a pH responsive enteric coated extended release multiparticulate dosage form containing a model drug ketoprofen, a nonsteroidal anti-inflammatory drug used for rheumatoid arthritis. The drug loaded pellets in matrix form were prepared by using extrusion/spheronization method. The optimized pelletization method revealed that extrusion using 1 mm sieve plate and spheronization friction disc of 2mm carried out at 700 rpm for 5-10 minutes resulted in good spherical pellets and uniformity in size. Evaluated core pellets were coated with polymer Eudragit® RS 30D on Fluid bed coater to achieve a sustainable release for 12 hours. Ketoprofen as like other NSAID have been reported for gastric mucosal irritation so a pH responsive barrier coat of Eudragit L®100-55 was employed on a pan coater for abstaining release in acidic media. The formulated pellets were characterized for shape and size uniformity, friability, surface morphology studies. The particle size of core and polymer coated pellets were found to be in the range of 0.95-1.2 mm and 1.32-1.51 mm respectively. The pellets were spherical in shape with smooth texture and uniformity in size. In-vitro dissolution tests were carried out for pellets in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the ketoprofen from formulated pellets was established in pH 1.2 for a period of 2 h, followed by pH 7.5 for rest of the study. The study concluded that the formulated multiparticulate dosage form of ketoprofen was able to relieve symptoms of rheumatoid arthritis.


Author(s):  
Mahesh Hari Kolhe ◽  
Ritu Mehra Gilhotra ◽  
Govind Sarangdhar Asane

Atenolol is beta blocker absorbed through GIT use for heart diseases. Single tablets, floating tablets and sustained released formulations studied are insufficient to produce effective dose to enhance bioavailability and effectiveness. Our study is focused on development of capsule dosage form containing immediate release (IR) and floating extended release (ER) tablets for monitoring release of atenolol in single dosage form. Two different tablets for IR and ER were prepared in three different combinations (Batch). Pre-formulation and post formulation parameters found to be within acceptable limits of formulation. Release behavior of individual tablets and capsule containing two tablets were studied. Among the batches, capsules containing smaller amount of atenolol in IR and large amount of Atenolol in ER (batch II) showed impressive drug release pattern. This formulation was stable even after a month and achieved optimum release behavior of immediate release and sustained release. This study could be used for effective treatment for different heart complications and reduce toxicity due to high plasma concentration in increased dose frequency.


2009 ◽  
Vol 1 ◽  
pp. CMT.S3049
Author(s):  
Alejandro Arenas-Pinto

Didanosine (ddl) has been used to treat HIV infection, in combination with other anti-retroviral drugs, for over 15 years. However, the use of the original formulation of ddI was limited by serious gastro-intestinal adverse effects, which were mainly attributable to the buffer used to protect ddI from the effect of gastric pH. Didanosine enteric-coated capsule (ddI-EC), a more recently introduced formulation, is less likely to cause gastrointestinal intolerance and its absorption might not be compromised by food intake. In this review we discuss efficacy of ddI-EC-containing anti-retroviral combinations (cART) both in naïve and previously treated patients. Because of its favorable resistance profile, ddI-EC has been shown to be potentially efficacious in rescuing patients in virological failure, even if they have nucleoside reverse transcriptase inhibitors (NRTI)-associated resistance mutations. However, ddI has been shown as a potent inducer of mitochondrial dysfunction. Peripheral neuropathy, severe hyperlactatemia and pancreatitis have all been described in patients exposed to ddI. Close monitoring of patients on ddI-EC-containing cART and low threshold for treatment modifications are required to prevent major complications. In the context of once daily cART, ddI-EC is a valid option, particularly when other agents are not available, or when other medical conditions preclude the use of drugs such as tenofovir or abacavir. The role of ddI-EC in second line cART may be even more important in resource-limited settings where additional options are lacking.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 805
Author(s):  
Daniel Zakowiecki ◽  
Maja Frankiewicz ◽  
Tobias Hess ◽  
Krzysztof Cal ◽  
Maciej Gajda ◽  
...  

Novel calcium phosphate-based starter pellets were used to develop a biphasic-release multiple-unit pellet system (MUPS) with diclofenac sodium as a model drug in the form of hard gelatin capsules. For comparative purposes, corresponding formulations based on the inert cores made of microcrystalline cellulose, sucrose and isomalt were prepared. The developed system consisted of two types of drug-layered pellets attaining different release patterns: delayed-release (enteric-coated) and extended-release. Dissolution characteristics were examined using both compendial and biorelevant methods, which reflected fed and fasting conditions. The results were collated with an equivalent commercial product but prepared with the direct pelletization technique.


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