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

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.

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
John C. Morgan ◽  
Rohit Dhall ◽  
Robert Rubens ◽  
Sarita Khanna ◽  
Suneel Gupta

Background. IPX066 is an extended-release (ER) oral formulation of carbidopa-levodopa (CD-LD). Following an initial peak at about one hour, plasma LD concentrations are maintained for about 4-5 hours. Objective. To present dosing factors that may affect the successful conversion to ER CD-LD from other LD formulations. Methods. Two-phase 3 studies of ER CD-LD vs. immediate-release (IR) CD-LD (ADVANCE-PD) and vs. CD-LD + entacapone (CLE; ASCEND-PD) in subjects with advanced PD included a 6-week, open-label conversion to ER CD-LD prior to treatment randomization. The “converted” daily LD dose ratio and dose frequency for ER CD-LD were compared to the prior LD treatment regimens at study entry. Results. The average daily LD dose ratio at the end of dose conversion to ER CD-LD was approximately 2.1 for IR CD-LD and 2.8 for CLE. The final dose ratios tended to be slightly higher for participants taking lower LD doses at study entry but independent of dose frequency. ER CD-LD dose frequency increased with increasing LD dose and dose frequency at study entry. Participants on higher baseline LD doses ≥800 mg and dose frequencies ≥6 tended to have higher rates of discontinuation during conversion to ER CD-LD. Conclusions. Converting participants from other LD formulations to ER CD-LD is based on their current LD regimen. For the most common daily doses (≤1250 mg) and dose frequencies (<7) of LD, final mean dose ratios were within tight ranges of 2.1 to 2.4 for IR CD-LD (ADVANCE-PD) and 2.4 to 2.8 for CLE (ASCEND-PD) and were generally independent of the LD dosing frequency at study entry. These trials are registered with NCT00974974, NCT01130493.


2006 ◽  
Vol 40 (7-8) ◽  
pp. 1274-1279 ◽  
Author(s):  
Joanne LaFleur ◽  
Clinton J Thompson ◽  
Vijay N Joish ◽  
Scott L Charland ◽  
Gary M Oderda ◽  
...  

Author(s):  
P.Vamsikrishna ◽  
T.Malyadri ◽  
Ch.Saibabu

The present work aims to develop a stable and optimized bilayer dosage form containing immediate release &extended release drug Nicardapine as an extended-release dosage form. A potent calcium channel blocker with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardio depressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. It has a plasma half-life of about (8.6h) and bioavailability is 15-45% orally. For the formulation of Bilayered tablets polymers such as Ethylcellulose, Sodium CMC, CCS, SSG, Magnesium stearate, Talc, PVP-K30, and MCC. Fourier transform Infrared spectroscopy confirmed the absence of any drug/ polymers/ excipients interactions. Preformulation studies were carried out to optimize the ratios required for various Ethylcellulose, Sodium CMC, CCS, SSG, MCC, and PVP-K30. Based on various evaluation parameters formulation M6 (IR) & M6F3 (SR) were selected as optimized formulation. It was observed that Formulations M6 (IR) & M6F3 (SR) gave maximum drug release within time. All formulations were subjected for drug release kinetics studies viz. Zero-order, First order, Higuchi matrix, Peppasmodel equations, and the formulations of floating sustained-release formulations followed the zero-order release with non-fickian diffusion mechanism. Thus conclusion can be made that a stable dosage form can be developed for  Nicardapine as immediate release & sustained release by Bilayered tablets.


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.


2016 ◽  
Vol 60 (4) ◽  
pp. 2492-2498 ◽  
Author(s):  
Marcelo Gomes Davanço ◽  
Michel Leandro Campos ◽  
Talita Atanazio Rosa ◽  
Elias Carvalho Padilha ◽  
Alejandro Henao Alzate ◽  
...  

ABSTRACTBenznidazole (BNZ) is the first-line drug for the treatment of Chagas disease. The drug is available in the form of immediate-release tablets for 100-mg (adult) and 12.5-mg (pediatric) doses. The drug is administered two or three times daily for 60 days. The high frequency of daily administrations and the long period of treatment are factors that significantly contribute to the abandonment of therapy, affecting therapeutic success. Accordingly, this study aimed to evaluate the preclinical pharmacokinetics of BNZ administered as extended-release tablets (200-mg dose) formulated with different types of polymers (hydroxypropyl methylcellulose K4M and K100M), compared to the tablets currently available. The studies were conducted with rabbits, and BNZ quantification was performed in plasma and urine by ultraperformance liquid chromatography methods previously validated. The bioavailability of BNZ was adequate in the administration of extended-release tablets; however, with the administration of the pediatric tablet, the bioavailability was lower than with other tablets, which showed that the clinical use of this formulation should be monitored. The pharmacokinetic parameters demonstrated that the extended-release tablets prolonged drug release from the pharmaceutical matrix and provided an increase in the maintenance of the drug concentrationin vivo, which would allow the frequency of administration to be reduced. Thus, a relative bioavailability study in humans will be planned for implementation of a new product for the treatment of Chagas disease.


2010 ◽  
Vol 11 (4) ◽  
pp. S44
Author(s):  
K. Moore ◽  
D. St. Fleur ◽  
N. Marricco ◽  
T. Ariyawansa ◽  
V. Page ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document