scholarly journals An Account of Modified Release of Melatonin from Compression-coated, Uncoated and Bilayer Tablets

2016 ◽  
Vol 1 (4) ◽  
pp. 10-14 ◽  
Author(s):  
Marilena Vlachou
2019 ◽  
Vol 16 (10) ◽  
pp. 931-939
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Yannis Dotsikas

Background: The loop diuretic drug furosemide is widely used for the treatment of edema in various conditions, such as pulmonary, cardiac and hepatic edema, as well as cardiac infarction. Furosemide, due to its poor water solubility and low bioavailability after oral administration of conventional dosage form, is categorized as class IV in the biopharmaceutical classification system. Objective: In the case of furosemide, this release profile is responsible for various physiological problems, acute diuresis being the most serious. This adverse effect can be circumvented by the modified release of furosemide from tablet formulations compared to those forms designed for immediate release. Method: In this report, a D-optimal combined experimental design was applied for the development of furosemide containing bilayer and compression coated tablets, aiming at lowering the drug’s burst release in the acidic environment of the stomach. A D-optimal combined design was selected in order to include all requirements in one design with many levels for the factors examined. The following responses were selected as the ones reflecting better criteria for the desired drug release: dissolution at 120 min (30-40%), 300 min (60-70%) and 480 min >95%. The new formulations, suggested by the Doptimal combined design, incorporated different grades of Eudragit ® polymers (Eudragit® E100 and Eudragit® L100-55), lactose monohydrate and HPMC K15M. The dissolution profile of furosemide from these systems was probed via in vitro dissolution experiments in buffer solutions simulating the pH of the gastrointestinal tract. Results: The results indicate that the use of Eudragit® E100 in conjunction with lactose monohydrate led to 21.32-40.85 % drug release, in the gastric medium, in both compression-coated and bilayer tablets. This is lower than the release of the mainstream drug Lasix® (t=120 min, 44.5% drug release), implying longer gastric retention and drug waste minimization. Conclusion: Furosemide’s release in the intestinal environment, from compression coated tablets incorporating Eudragit® L100-55 and HPMC K15M in the inner core or one of the two layers of the bilayer tablets, was delayed, compared to Lasix®


2016 ◽  
Vol 46 (1) ◽  
pp. 5-15 ◽  
Author(s):  
Neha Dhiman ◽  
RAJENDRA AWASTHI ◽  
Shammy Jindal ◽  
Smriti Khatri ◽  
Kamal Dua

2001 ◽  
Vol 120 (5) ◽  
pp. A749-A749
Author(s):  
A CORTOT ◽  
J COLOMBEL ◽  
P RUTGEERTS ◽  
K LAURITSEN ◽  
H MALCHOW ◽  
...  

2015 ◽  
Author(s):  
Marianne Weigel ◽  
Stefanie Hahner ◽  
Daniela Beier ◽  
Kathrin Zopf ◽  
Marcus Quinkler

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

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.


Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  


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