In-Vitrodn-Vivo Correlation of Drug Liberation with an Extended Release Peroral Dosage form for Iloprost in Man

1995 ◽  
Vol 21 (20) ◽  
pp. 2339-2353 ◽  
Author(s):  
M. Hildebrand ◽  
C. Kraus ◽  
F. Windt-Hanke ◽  
B. Iffert ◽  
H. Scheuermann
Keyword(s):  
Dosage Form ◽  
Extended Release ◽  
Drug Liberation

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.

Development of Capsule containing Immediate Release Tablet and Extended Release Floating Tablet for Monitoring Release of Atenolol

2021 ◽  
pp. 2216-2220
Author(s):  
Mahesh Hari Kolhe ◽  
Ritu Mehra Gilhotra ◽  
Govind Sarangdhar Asane
Keyword(s):  
Dosage Form ◽  
Extended Release ◽  
Heart Diseases ◽  
Immediate Release ◽  
High Plasma ◽  
Release Behavior ◽  
Dose Frequency ◽  
Floating Tablet ◽  
Formulation Parameters ◽  
Single Dosage

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.

scholarly journals Formulation of Extended-Release Ranolazine Tablet and Investigation Its Stability in the Accelerated Stability Condition At 40⁰C And 75 % Humidity

2021 ◽  
pp. 1-3
Author(s):  
Farzad Khajavi ◽  
Keyword(s):  
Stability Condition ◽  
Dosage Form ◽  
Extended Release ◽  
Chemical Characteristics ◽  
Physical And Chemical Characteristics ◽  
Eudragit L100 ◽  
Accelerated Stability ◽  
Physical And Chemical ◽  
Extended Release Tablet ◽  
Release Tablet

Formulation of Ranolazine in the form of extended-release tablet in 500 mg dosage form was performed using Eudragit L100-55 as a retarding agent. Drugrelease profiles were investigated in comparison with the reference Ranexa extended-release 500 mg tablet. F2 and f1 were calculated as 64.16 and 8.53, respectively. According to Peppas equation, the release of drug is controlled by diffusion (n=0.5). The tablets were put into accelerated stability condition (40⁰C, 75% humidity) for 3 and 6 months. The dissolution release profiles and other physical and chemical characteristics of the tablets confirmed the robustness and stability of formulation in this condition.

Techniques of Mucilage and Gum Modification and their Effect on Hydrophilicity and Drug Release

2020 ◽  
Vol 14 ◽  
Author(s):  
Rishabha Malviya ◽  
Vandana Tyagi ◽  
Dharmendra Singh
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Extended Release ◽  
Release Mechanism ◽  
Release Agent ◽  
Drug Release Mechanism ◽  
Polymer Relaxation ◽  
Hydrophilic Matrices ◽  
The Matrix ◽  
High Degree

Aim: The manuscript aims to describe the techniques of modification of gums and mucilages and their effect on hydrophilicity and drug release. Discussion: The interest is increased in the fields of polymers which is obtained from natural origin and used in the preparation of pharmaceuticals. Mucilage and gum are natural materials, widely used in the preparation of novel dosage form and conventional dosage form. They are used in the pharmaceutical industry for various purposes like suspending, emulsifying, bio-adhesive, binding, matrix-forming, extended release and controlled release agent. Gum and mucilage are biodegradable, less toxic, cheap and easily available. Moreover, mucilage and gum can be changed to acquire tailored materials for the delivery of drugs and allow them to compete with commercially available synthetic products. These polysaccharides have unique swellability in an aqueous medium that can exert a retardant effect on drug release or act as a super disintegrant, depending on the concentration utilized in the preparation. Drug release mechanism from hydrophilic matrices consisting of gums and mucilages is based on solvent penetration-induced polymer relaxation, diffusion of entrapped drug followed by degradation or erosion of the matrix. Conclusion: The present manuscript highlight the advantages, modifications of gum and mucilage, their effects on hydrophilicity and drug release as well as aspects of the natural gums which can be assumed to be bifunctional excipient because of their concentration-dependent effect on drug release and their high degree of swellability.

Formulation and Evaluation of Novel Enteric Coated Extended Release Multiparticulates of Model NSAID Ketoprofen

2010 ◽  
Vol 3 (2) ◽  
pp. 994-999
Author(s):  
Lotlikar V ◽  
S Shidhaye ◽  
U Kedar ◽  
V Kadam
Keyword(s):  
Rheumatoid Arthritis ◽  
Dosage Form ◽  
Extended Release ◽  
In Vitro Dissolution ◽  
Ph Responsive ◽  
Model Drug ◽  
Enteric Coated ◽  
Pan Coater ◽  
Barrier Coat

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.

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