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.

Recent Developments in Medicated Lozenges: A Promising Dosage Form for the Effective Delivery of Therapeutic Agents

2021 ◽  
Vol 11 ◽  
Author(s):  
Deepak Sharma ◽  
Dinesh Kumar ◽  
Gurmeet Singh
Keyword(s):  
Retention Time ◽  
Drug Targeting ◽  
Dosage Form ◽  
Base Material ◽  
Rapid Onset ◽  
Oral Route ◽  
Therapeutic Agents ◽  
Oral Dosage ◽  
Onset Of Action ◽  
Pharmaceutical Industries

Background: The delivery of therapeutic agents through the oral route remains the most favorable one as compared to other routes of drug administration. However, numerous disadvantages are encountered in conventional formulations such as low bioavailability, first-pass metabolism, gastric irritation, delayed onset of action, bitter taste, low retention time, frequent dosing, and non-localized drug targeting. All these problems encountered guide the various pharmaceutical industries to manufacture and develop a novel solid oral dosage form called lozenges. Lozenges are solid oral dosage forms of medicament, meant to be dissolved within the mouth or pharynx. It may consist of one or more than one medicinal agent contained in a sweetened and flavored base material. Objective: The present review is focused on various types, compositions, methodologies used to prepare the medicated lozenges and on different evaluation parameters that establish its safety and efficacy. It also put a light on different commercially available and reported medicated lozenges formulation. Method: The various review and research articles reported by different researchers were studied extensively by using the databases of Google Scholar, Pubmed, Scopus, Web of Science and various commercial websites that were also investigated for information regarding new products. Results: Lozenges provides various advantages in terms of patient compliance, rapid onset of action, prolonged retention time, enhancement of bioavailability, ease of manufacturing, localized drug targeting, sustained or controlled effect, and reduced dosing frequency. It has also the ability to incorporate the drugs belong to different therapeutic classes for treating various disorders related to oral cavities like gingivitis, dental plaque, mouth ulcers, throat pain, oral thrush, throat infection, periodontitis, and pharyngitis. However, its applicability is not only limited to localized action, but it has also been employed to deliver the drug systemically for the conditions such as cough, decongestion, runny nose, nausea, vomiting, allergy, low immunity, fever, body ache, the killing of worms and smoking cessation. Conclusion: It was concluded that it has been played an important role in the field of drug delivery and will continue to perform in the same way in the future as well.

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.

scholarly journals Sublingual Tablets : An Overview

2020 ◽  
pp. 333-339
Author(s):  
Rohit S. Nikam ◽  
Smita P Borkar ◽  
Prakash D Jadhav ◽  
Vishal D. Yadav ◽  
Apurva V Jadhav
Keyword(s):  
Drug Delivery ◽  
Oral Cavity ◽  
Mucous Membrane ◽  
Dosage Form ◽  
Rapid Onset ◽  
Oral Route ◽  
Mouth Area ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Oral Mucous Membrane

Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a useful when rapid onset of action is desired with better patient compliance than oraly ingested tablets. In terms of permeability, the sublingual area of the oral cavity (i.e. the floor of the mou) is more permeable than the buccal (cheek) area, which in turn is more permeable than the palatal (roof of the mouth) area. A rapid onset of pharmacological effect is often desired for some drugs, especially those used in the treatment of acute disorders. Sublingual tablets disintegrate rapidly and the small amount of saliva present is usually sufficient for achieving disintegration of the dosage form coupled with better dissolution and increased bioavailability.

Oral Disintegrating Tablets – An Updated Patent Perspective

2020 ◽  
Vol 14 ◽  
Author(s):  
Shailesh Sharma ◽  
Kuljit Singh
Keyword(s):  
Dosage Form ◽  
Rapid Onset ◽  
Wet Granulation ◽  
Patent Citations ◽  
Onset Of Action ◽  
Solid Dosage ◽  
Alternative Approach ◽  
Cotton Candy ◽  
Improve Patient ◽  
Advantageous Effect

Abstract:: Current development in drug delivery system has been employed with an endeavour of enhancing the bioavailability, mask the taste of drug, rapid onset of action and improve patient compliance. An alternative approach of conventional dosage form is being employed to triumph over all these issues named as Orodispersible system. Over past three decades this novel dosage form gain a considerable attention as compared to other conventional solid dosage form such as tablet and capsules. ODTs dissolved or disintegrate within few seconds to a minute when put on the tongue, without need of water. ODT has an advantageous effect on paediatrics and geriatrics patients with dysphagia. Over the last decade, widespread advances in the formulation of ODTs have been executed in academia and industry that resulted in the emerging of a large number of patents. Products developed from ODT mechanics launched in the market in the 1980s, have grown bit by bit in demand and their product are rapidly escalating. Expanding in the technology forum for industrialized these systems include the use of lyophilization, cotton candy, sublimation, melt extrusion and direct compression in addition the conventional wet granulation processes and patent techniques. The present study focused on non-patent and patent citations concerning to ODT along with active ingredients, technique used and results of the innovations.

scholarly journals FORMULATION AND EVALUATION OF AN INJECTABLE SOLUTION AS A DOSAGE FORM

2018 ◽  
Vol 8 (5) ◽  
pp. 81-87 ◽  
Author(s):  
Sneha Thomas ◽  
S Mahendran ◽  
R Selvakumar
Keyword(s):  
Dosage Form ◽  
Scale Up ◽  
Clinical Effectiveness ◽  
Rapid Onset ◽  
Drug Release Profile ◽  
Onset Of Action ◽  
Production Scale ◽  
Proper Form ◽  
Injectable Dosage ◽  
Systemic Drug

The present study will outline formulation and the evaluation methods of injectable dosage form. The various initial formulations of the developed and those are examined for drug release profile, bioavailability, and clinical effectiveness and for the pilot plant studies and production scale-up. The drug that we need should be most convenient and in proper form then only it reaches to the desired site of action. This is greatly influenced by which the type of dosage form of the drug. Since, injections include much variety of therapeutic agents. Injections are sterile, pyrogen limited, that is, bacterial endotoxin units limit, preparations intended to be administered parenterally. It is well recognized that the advantages of parenteral injections are immediate systemic drug availability and rapid onset of action. Keywords: Injectable, Parenteral, Sterilization, Tonicity

scholarly journals FORMULATION AND EVALUATION OF COLON TARGETED PELLETS OF BUMADIZONE CALCIUM

2019 ◽  
Vol 7 (3) ◽  
Author(s):  
Mr. Shah Akashkumar Nareshkumar ◽  
Mr. Anil G. Raval
Keyword(s):  
Drug Release ◽  
Phosphate Buffer ◽  
Compatibility Study ◽  
Enteric Coating ◽  
Eudragit S100 ◽  
Ph Dependent ◽  
Enteric Coated ◽  
Full Factorial ◽  
Extrusion Spheronization ◽  
Pvp K30

Aim: The aim of this study was to Formulation and Evaluation of colon targeted pellets of Bumadizone Calcium Objective: Bumadizone Calcium is an acetic acid derivative, having irritation in stomach. Bumadizone Calcium has short half-life (4hrs) and undergoes first pass metabolism. It is pH-dependent. This research work was carried out to improve the bioavailability, patient compliance on oral colon targeted drug delivery. Bumadizone Calcium sustained release enteric coated pellets were prepared, which minimize the release of drug in stomach for treatment of IBD formulated by Extrusion Spheronization process. Experimental work done: Enteric coated pellets prepared by Extrusion Spheronization technique. Eudragit S100, HPMC, PVP K30, and Ethyl Cellulose were used as rate controlling polymers. In this study, a pH dependent colon targeted enteric coated pellets was established using 32 full factorial design by giving enteric coating with Eudragit S100. Different Concentration of Eudragit S100 as an enteric coating material (4%, 5%, & %6) and PVP K30 as a Binder (0.5%, 1% & 1.5%) are taken for the measurements of % Drug Release that are performed by using USP dissolution 1 (Basket type) at 50 rpm. The test is performed with gastric fluid (pH 1.2) at 37±0.5 for first 2 hours & then in phosphate buffer 6.8 for 4 hrs & finally in phosphate buffer pH 7.4 for 6 hrs. The prepared formulations were evaluated for drug-excipient compatibility study, flow property, drug content, and coating process efficiency. Results and Discussion: Optimized batch shown that less than 0.50% of the drug released at the end of 2 hrs in pH 1.2, less than 20% of drug released after end of 4 hrs in pH 6.8 and more than 85% at the end of 12 hrs in pH 7.4. Conclusion: Bumadizone Calcium Enteric Coated pellets can be successfully formulated by addition of PVP K-30 as a binder and Eudragit S100 as Coating polymer. It was also concluded that prepared formulation minimizes drug release in stomach and avoid side effect of the drug. Keywords: Bumadizone calcium, Eudragit S100, Enteric coating, extrusion spheronization technique, 32 full factorial designs.

Pharmacokinetic peculiarities of drugs used in the form of rapidly dispersible tablets (oral delivery system)

2020 ◽  
pp. 7-24
Author(s):  
Zhanna Kozlova ◽  
Ivan Krasnyuk ◽  
Yuliya Lebedeva ◽  
Ekaterina Odintsova
Keyword(s):  
Oral Mucosa ◽  
Oral Delivery ◽  
Chemical Properties ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Mucosal Drug Delivery ◽  
Physical And Chemical ◽  
Pass Metabolism

Oral mucosal drug delivery is an alternative method of systemic delivery with several advantages over both injectable and enteral methods. Drugs that are absorbed through the oral mucosa directly enter the systemic circulation, passing through the gastrointestinal tract and first-pass metabolism in the liver due to oral mucosa being highly vascularised. This results in rapid onset of action for some drugs because of a more comfortable and convenient way of delivery than the intravenous one. But not all drugs can be administered through the oral mucosa due to characteristics of the oral mucosa and physical and chemical properties of the drug.

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