scholarly journals Development of gastroretentiv floating tablets of losartan potassium by sublimation method

2021 ◽  
Vol 8 (2) ◽  
pp. 66-74
Author(s):  
Hiral S Bhusara ◽  
Ara T Patel ◽  
Mayuree D Patel
Keyword(s):  
Sustained Release ◽  
Polyethylene Oxide ◽  
Optimization Technique ◽  
Losartan Potassium ◽  
Gastric Residence Time ◽  
Sublimation Method ◽  
Speed Up ◽  
Floating Tablet ◽  
32 Factorial Design ◽  
Predicted Values

The purpose of present study was to formulate and Evaluate Sustained release floating tablet of losartan Potassium using Camphor and Polyethylene Oxide as Pore formation for floating and release retarding agent respectively to improve gastric residence time and patient compliance in management of hypertension. The tablet was prepared by direct compression by using HPMC K4 as dry binder. Camphor and PEO as floating and release retarding agent for sustained release floating tablet. Post compression was done to increase the hardness and floating time of tablet. Release modifier was used to speed up the release of drug from sustained release floating tablet. The effect of two independent variables like amount of Sublimating agent (camphor) and amount of Polyethylene oxide (PEO) on Q30min, Q360min, and Q720min was optimized using 32 factorial design and analyzed using the software design expert 10.0.3. The observed (actual values) responses were coincided well with the predicted values, given by the optimization technique. The floating tablet were characterized by FTIR for drug excipient compatibility.

FORMULATION AND STATISTICAL OPTIMIZATION OF MULTIPARTICULATE LAFUTIDINE-LOADED GASTRORETENTIVE DELIVERY SYSTEM USING 32- FACTORIAL DESIGN

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (10) ◽  
pp. 43-54
Author(s):  
K.A Sapate ◽  
◽  
P. V. Dangre ◽  
M. D. Godbole
Keyword(s):  
Drug Release ◽  
Interaction Analysis ◽  
Optimization Technique ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Fed State ◽  
32 Factorial Design ◽  
Predicted Values ◽  
Average Size

The purpose of this research was to develop and optimize buoyant beads containing lafutidine by ionic-gelation method for gastroretentive delivery. The effect of two independent process variables like NaHCO 3: Polymer, Drug: Polymer ratio on % drug entrapment, % swelling and % drug release of buoyant beads containing lafutidine was optimized using 32 factorial designs. The observed responses coincided well with the predicted values, given by the optimization technique. The optimized beads showed drug entrapment efficiency 78.76+0.27%, swelling 69.90+0.13%, cumulative drug release 69.00+0.36% after 8 h; the average size of all buoyant beads ranged from 1.35+0.01 to 1.56+0.05 mm. The buoyant beads were characterized by SEM, DSC and FTIR spectroscopy for surface morphology and excipient-drug interaction analysis, respectively. All these beads showed prolong release of lafutidine over 8 h in 0.1 N HCl (pH1.2) evaluation of buoyancy of the optimized formulation in vivo in human volunteers showed that the beads were buoyant in gastric fluid for 8 h both in fasted and fed state.

scholarly journals Development and evaluation of sustained release losartan potassium matrix tablet using kollidon SR as release retardant

2012 ◽  
Vol 48 (4) ◽  
pp. 621-628 ◽  
Author(s):  
Shahid Sarwar ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.

Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

2021 ◽  
pp. 5202-5206
Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Drug Bioavailability ◽  
Gastric Residence Time

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

scholarly journals Two-dimensional Placement Using Tabu Search

VLSI Design ◽  
2001 ◽  
Vol 12 (1) ◽  
pp. 13-23
Author(s):  
John M. Emmert ◽  
Dinesh K. Bhatia
Keyword(s):  
Simulated Annealing ◽  
Tabu Search ◽  
Optimization Technique ◽  
Vlsi Design ◽  
Two Dimensional ◽  
Search Technique ◽  
Quality Of Results ◽  
Circuit Performance ◽  
Speed Up

Search based placement of modules is an important problem in VLSI design. It is always desired that the search should converge quickly to a high quality solution. This paper presents a tabu search based optimization technique to place modules on a regular two-dimensional array. The goal of the technique is to speed up the placement process. The technique is based on a two-step placement strategy. The first step is targeted toward improving circuit routability and the second step addresses circuit performance. The technique is demonstrated through placement of several benchmark circuits on academic as well as commercial FPGAs. Results are compared to placements generated by commercial CAE tools and published simulated annealing based techniques. The tabu search technique compares favorably to published simulated annealing based techniques, and it demonstrates an average execution time speedup of 20 with no impact on quality of results when compared to commercial tools.

scholarly journals Formulation and Pharmacokinetic Evaluation of Ritonavir Floating Tablets in the Management of AIDS

2018 ◽  
Vol 10 (6) ◽  
Author(s):  
R. Shireesh Kiran ◽  
B. Chandra Shekar ◽  
B. Nagendra Babu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Controlled Drug Release ◽  
In Vitro Dissolution ◽  
Gastric Residence Time ◽  
Dissolution Studies ◽  
Floating Tablet ◽  
Gastro Retentive

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.

scholarly journals Development and Optimization of Floating Microspheres in Amethopterin

2021 ◽  
Vol 14 (4) ◽  
pp. 1538-1543
Author(s):  
Raghav Mishra
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Patient Compliance ◽  
Drug Loading ◽  
Practical Significance ◽  
In Vitro Dissolution ◽  
Minimal Risk ◽  
Gastric Residence Time

Due to the complexity of gastric emptying, as well as its considerable variability, the in vivo efficacy of drug delivery devices cannot be predicted. When it pertains to drugs with an absorption window in the upper small intestine, a controlled drug delivery system with a longer residence period in the stomach may be of considerable practical significance. Recent developments have shown that floating microspheres are particularly well suited for mixing sustained and delayed releases to achieve a variety of release models with a minimal risk of dumping. The aim of present investigation is to develop and analyze the floating microspheres of amethopterin, which after oral administration could increase the gastric residence time and enhance the bioavailability of the drug by sustained release and minimize the dose dependent side effects as well as improves patient compliance. Floating microspheres of ethyl cellulose, Polyvinyl alcohol and polyvinyl pyrrolidone-K90 were formulated by emulsification solvent evaporation technique. The various parameters of prepared microspheres were studied for SEM, flow properties, buoyancy, yield, percent drug loading, in vitro dissolution studies, stability in different pH and FTIR studies. Microspheres prepared with different concentrations of polymers were spherical in shape with smooth surface. The size of microspheres was in range of 256.02 µm and 362.84 µm. Good drug entrapment and buoyancy were observed for formulation F2. The in vitro drug release after 6h was found to be in range from 58.15% to 96.28%. It was established that the newly created floating microspheres of Amethopterin provide an appropriate and practical solution for the sustained release of medication over a longer period of time, resulting in increased oral bioavailability, effectiveness, as well as better patient compliance.

Development and evaluation of injection-molded sustained-release tablets containing ethylcellulose and polyethylene oxide

2010 ◽  
Vol 37 (2) ◽  
pp. 149-159 ◽  
Author(s):  
T. Quinten ◽  
T. De Beer ◽  
A. Almeida ◽  
J. Vlassenbroeck ◽  
L. Van Hoorebeke ◽  
...  
Keyword(s):  
Sustained Release ◽  
Polyethylene Oxide ◽  
Sustained Release Tablets ◽  
Injection Molded

Isolation and Characterization of Dillenia Fruit Mucilage: A Novel Polymer for Microspheric Delivery of Losartan Potassium

2020 ◽  
Vol 10 (4) ◽  
pp. 314-325
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Manami Dhibar ◽  
Shikha Yadav ◽  
Honey Kumari
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Rheological Behavior ◽  
Dosage Form ◽  
Functional Characteristic ◽  
Losartan Potassium ◽  
Modifying Agent ◽  
Isolation And Characterization ◽  
Polymeric Blend

Objective: The present investigation was aimed to isolate, characterize and establish a natural polymer obtained from partially ripe and fresh fruits of Dillenia indica and its utility to deliver losartan potassium in a sustained manner from microspheric macromolecular dosage form. Methods: All the microspheres were prepared by ionotropic gelation technique and investigated for various physico-chemical parameters along with in-vitro drug release studies to optimize the concentration of algino-Dillenia polymeric blend required to develop twice daily sustained release dosage form of losartan potassium. Results: The functional characteristic studies and rheological behavior analysis suggested that extracted polysaccharide can be used as a viscosity modifying agent as well as sustain release ingredient. All the microsphere formulations exhibited excellent mucoadhesion properties and site-specific drug release. In-vitro studies revealed that the optimum concentration of algino-Dillenia polymeric blend is suitable to deliver losartan potassium in a sustained manner for a prolonged period of time. SEM study revealed that the microspheres were spherical in shape with a smooth outer surface having small cracks. XRD and DSC studies revealed that losartan potassium is present as an amorphous form in the prepared optimized microsphere formulation. Conclusion: Thus, the present studies demonstrated that Dillenia fruit mucilage has an interesting rheological behavior which may be used as a viscosity modifying agent and exhibit promising properties of a sustained release dosage form to deliver losartan potassium from its microspheric dosage form.

scholarly journals Use of Response Surface Methodology in the Formulation and Optimization of Bisoprolol Fumarate Matrix Tablets for Sustained Drug Release

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Jadupati Malakar ◽  
Amit Kumar Nayak ◽  
Soumita Goswami
Keyword(s):  
Response Surface Methodology ◽  
Drug Release ◽  
Sustained Release ◽  
Response Surface ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Order Model ◽  
Sustained Drug Release ◽  
Predicted Values

The aim of this investigation was to develop and optimize bisoprolol fumarate matrix tablets for sustained release application by response surface methodology based on 23 factorial design. The effects of the amounts of calcium alginate, HPMC K4M, and Carbopol 943 in bisoprolol fumarate matrix tablets on the properties of bisoprolol fumarate sustained release matrix tablets like drug release and hardness were analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design. The optimized bisoprolol fumarate matrix tablets showed prolonged sustained release of bisoprolol fumarate over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism.

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