Design and Optimization of Hydrophilic Matrix-based Sustained Release Felodipine Tablets

2018 ◽  
Vol 11 (3) ◽  
pp. 4136-4144
Author(s):  
Duyen Nguyen Thi Thanh ◽  
Duc Hoang Van ◽  
Minh Vo Xuan ◽  
Xuan Dam Thanh Thanh ◽  
Tung Bui Thanh
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Release Profile ◽  
Therapeutic Effects ◽  
Hydrophilic Matrix ◽  
Design And Optimization ◽  
Dependent Variables ◽  
Kinetics Of

Felodipine is a calcium channel blocker used for hypertensive and unstable angina treatments. The sustained release formulations of felodipine have advantages of achieving good therapeutic effects, increasing the bioavailability, decreasing dosing times per day and reducing side effects.The aim of our study was to study the formulation screening, then use an experiment design for formulating a hydrophilic matrix sustained release tablet of felodipine. Methods: The optimization process had the influences of the chosen excipients (including HPMC E4M, HPMC  E15LV) on the drug release. Three dependent variables were percentages of released felodipine at the sampling times 2h, 6h, 10h (Y2, Y6, Y10, respectively). Results: The release profile from the optimized formula almost met the predicted release profile and was similar to reference tablets. The kinetics of drug release the optimized tablets and reference tablets were also followed the Korsmeyer – Peppas model.Conclusion: The optimized formula was obtained, and the in vitro release profile was similar to the predicted profile and reference tablets.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED-RELEASE PELLETS OF LORNOXICAM

2021 ◽  
pp. 221-227
Author(s):  
MILIND J. AMIN ◽  
KEYUR S. PATEL ◽  
DEEPA R. PATEL ◽  
ZIL P. PATEL ◽  
JAYANTI V. BAJAG
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
Dependent Variables ◽  
Full Factorial ◽  
Eudragit Rlpo

Objective: The aim of the study was to develop sustained release pellets of lornoxicam using Eudragit RLPO and Eudragit RSPO to reduce the dosing frequency. Methods: The sustained release pellets of lornoxicam were prepared by extrusion–spheronization technique using Eudragit RLPO and Eudragit RSPO as release retardant polymers and microcrystalline cellulose as spheronizing agent. A 32 Full factorial design was applied to investigate the combined effect of the two independent variables i.e. concentration of Eudragit RLPO (X1) and concentration of Eudragit RSPO (X2) on the dependent variables, In vitro drug release at 1h (Y1), In vitro drug release at 4 h (Y2) and In vitro drug release at 12 h. (Y3). Results: The optimized formulation (F0) show in vitro drug release 11.24±1.21 %, 43.69±1.28 %, 82.69±1.74 % and 100.24±1.56 % at 1 h, 4 h, 12 h and 24 h respectively. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients. Eudragit RLPO and Eudragit RSPO had a significant effect on in vitro drug release. Conclusion: From all parameters and experimental design evaluation, it was concluded that the drug release rate decreased with an increase the concentration of Eudragit RLPO and Eudragit RSPO. SEM Photomicrograph of pellets revealed that the surface was rough and the pellets were spherical shaped in nature. The in vitro release kinetics revealed higuchi model is followed and drug release is by anamolous diffusion.

scholarly journals Formulation and Evaluation of Bi-Layer Tablets of Ketorolac Tromethamine

2021 ◽  
Vol 11 (1) ◽  
pp. 36-41
Author(s):  
Dhaval M. Patel ◽  
Riddhi Trivedi ◽  
Hardik Patel
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Immediate Release ◽  
Release Profile ◽  
Hydrophilic Polymers ◽  
Ketorolac Tromethamine ◽  
Vitro Release ◽  
Gastro Retentive

The objective of the present study was to develop and evaluate bi-layer tablets of Ketorolac tromethamine, a nonsteroidal antiinflammatory drug with short half-life, that are characterized by initial burst drug release in the stomach and comply with the release requirements of sustained-release products. Each of the proposed bi-layer tablets is composed of an immediate-release layer and a sustained-release layer, anticipating rapid drug release that starts in the stomach to rapidly alleviate the symptoms and continues in the intestine to maintain protracted analgesic effect. Gastro retentive Bi-Layer tablets of Ketorolac Tromethamine were prepared by using hydrophilic polymers with direct compression on floating – matrix technology and evaluated. Ketorolac tromethamine is freely soluble in water, so it is suitable to develop it as gastro retentive bi-layer tablets using hydrophilic polymers. The developed formulation is equivalent to calculated theoretical drug profile in view of its in vitro release. Immediate release layer was prepared by using dry granulation method in which ac-di sol used as a disintigrant for immediate release of drug. Sustained release layer formulated by using HPMC as release retardant, two grades of HPMC that are HPMC K4M and HPMC K100M used to get sustained release profile for 24 hr. Various trial batches are taken to get desired release profile. Ketorolac tromethamine release from the developed floating formulation followed Higuchi model and nonFickian diffusion is found to be the main mechanism of drug release. The manufacturing procedure was found to be reproducible and formulations were stable after one month of stability studies. Keywords: FTIR; Gastro retentive bilayer; ketorolac tromethamine; in vitro release; stability; higuchi.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

Fabrication and Release Kinetics of Liposomes Containing Leuprolide Acetate

2021 ◽  
Vol 7 (1) ◽  
pp. 35-38
Author(s):  
Sudipta Das ◽  
Arnab Samanta ◽  
Koushik Bankura ◽  
Debatri Roy ◽  
Amit Nayak
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Zero Order ◽  
Leuprolide Acetate ◽  
Lipid Film ◽  
In Vitro Drug Release ◽  
Liposomal Formulations ◽  
Kinetics Of

The present work is focused on the preparation and in vitro release kinetics of liposomal formulation of Leuprolide Acetate. In this work, “Thin Lipid Film Hydration Method” was used for preparation of Leuprolide Acetate loaded liposomes. Prepared liposomal formulations of Leuprolide acetate was evaluated by drug entrapment study, in-vitro drug release kinetics and stability studies. The percentage drug entrapment of Leuprolide acetate for F1 and F2 formulations were found to be 78.14 ± 0.67 and 66.70 ± 0.81% respectively. In-vitro drug release study of liposomal formulations had shown zero order release pattern. Regression co-efficient (R2) value of Zero order kinetics for F1 and F2 formulations were 0.9912 and 0.9676 respectively. After storing formulations for 1 month, stability testing was done at 40C.It was found that all batches were stable. These liposomal formulations of Leuprolide acetate can be formulated for parenteral application to treat prostate cancer and in women, to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals DESIGN AND STATISTICAL OPTIMIZATION OF A BILAYERED TABLET OF METOPROLOL SUCCINATE SUSTAINED RELEASE AND ATORVASTATIN CALCIUM IMMEDIATE RELEASE: ONCE A DAY FORMULATION IN THE MANAGEMENT OF HYPERTENSION

2018 ◽  
Vol 11 (3) ◽  
pp. 293
Author(s):  
Pearl Pires Dighe ◽  
Tank Hm
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Blood Cholesterol ◽  
Fixed Dose ◽  
Content Uniformity ◽  
Metoprolol Succinate ◽  
Atorvastatin Calcium ◽  
Vitro Release

 Objective: The current study involves the fabrication of oral bilayer matrix designs of a combination of two drugs, metoprolol succinate and atorvastatin calcium, the optimization of their in vitro release and characterization using the design expert software. Metoprolol succinate, a β1- selective adrenergic receptor blocking agent, is used in the management of hypertension has a half-life of approximately 4–5 h; thus, there is the need to use extended-release formulation for prolonged action. Atorvastatin is a hydroxymethylglutaryl-coenzyme A reductase inhibitor, an antilipidemic, used to lower blood cholesterol. The rationale for this fixed-dose combination is to coadminister two drugs acting by different mechanisms of action together, reduce dosing frequency, and increase patient compliance.Methods: A 32 factorial design was selected to analyze the effect of critical factors, polymer concentration of Kollidon sustained release (SR), and Eudragit RS and their interaction on the in vitro release of the SR part containing metoprolol succinate. The drug release at 2 h (Q2), 8 h (Q8), and 20 h (Q20) was taken as responses. The blends of both layers were prepared, evaluated for precompression characteristics, and compressed by direct compression. The compressed bilayer tablets were evaluated for their hardness, weight variation, friability, content uniformity, diameter, and in vitro release.Result and Conclusion: The release profile indicates Higuchi’s kinetics. Contour and surface response plots show significant interaction among the formulation variables. Formulation MS06 containing 70 mg Kollidon SR and 10 mg Eurdragit RS was found to be the optimized formulation, controlling the drug release for a 24 h period.

scholarly journals In vitro Studies on Sustained Release Suppository Formulations of Tiaprofenic Acid with Sucrose Fattv Acid Ester

2003 ◽  
Vol 71 (4) ◽  
pp. 357-364
Author(s):  
Sevgi Gūngör ◽  
Mine Orlu ◽  
Yildiz Özsoy ◽  
Ahmet Araman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Tiaprofenic Acid ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Sugar Ester ◽  
Disintegration Time ◽  
Suppository Base ◽  
Vitro Release

The objective of this study was to evaluate the performance of Sucro Ester 7 (sucrose distearate) as additive for preparing sustained release suppositories of tiaprofenic acid. Suppocire AIM (semi-synthetic glycerides) was used as suppository base and formulations were prepared containing different ratios of sugar ester: Suppocire AIM. Content uniformity, disintegration time and in vitro release characteristics of suppositories were investigated. Significant decrease in the extent of drug release was observed with the increase in the content of sugar ester, which was due to the longer disintegration time of suppositories.

scholarly journals FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE COATED MATRIX GRANULES OF METFORMIN HYDROCHLORIDE

2018 ◽  
Vol 11 (7) ◽  
pp. 387
Author(s):  
Radha Rani Earle ◽  
Kiran Kumar Bandaru ◽  
Lakshmi Usha A
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Diabetes Mellitus Type Ii ◽  
Drug Content ◽  
Percentage Yield

Objective: Metformin hydrochloride is a biguanide antihyperglycemic agent which is a generally recommended first-line drug for the treatment of diabetes mellitus (Type II). The purpose of this investigation is to prepare sustained release matrix granules of metformin hydrochloride which are coated to extend the drug release over a longer time period.Methods: Metformin hydrochloride granules were prepared by mixing all the dry powders in a V-cone blender and wetting the powder mix with aqueous solution of hydroxypropyl methyl cellulose K100. The prepared granules (MG1-MG5) were investigated for drug release. The batch of granules which exhibited extended release for up to 4 h was coated in a standard coating pan with blends of Eudragit RS and RL to further enhance release period. These were marked as coated metformin granules (CMG3) and CMG4 which were later filled into empty capsules. The granules were characterized for micromeritic properties, percentage yield, particle size distribution, percentage of drug content, and in vitro release of the drug.Results: All the formulations showed percentage yield in the range of 77.66–82.86% and drug content in the range of 78.23–96.62%. CMG3 showed drug release of 97.02% for 12 h. Fourier-transform infrared spectroscopy and differential scanning calorimetry studies indicated that no possible interaction existed between the drug and the polymers used. Scanning electron microscopy images revealed that the granules were spherical in shape with smooth surface and completely covered with a coating of polymer. Kinetic analysis of drug release confirmed that drug release followed zero-order kinetics where it is independent of the concentration.Conclusion: From the results, it was analyzed that design of coated granules employing the polymers used in the present work can produce a sustained release of the drug over a period of 12 h.

scholarly journals Application of Mathematical Models in Drug Release Kinetics of Cyanocobalamine Fast Dissolving Sublingual Film

2021 ◽  
pp. 72-81
Author(s):  
Adil Patel ◽  
Ami Kalsariya ◽  
Srushti Patel ◽  
Chandni Patel ◽  
Shreya Patel
Keyword(s):  
Drug Release ◽  
Mathematical Models ◽  
Release Kinetics ◽  
Release Profile ◽  
Suitable Model ◽  
Order Model ◽  
Drug Release Profile ◽  
Casting Technique ◽  
Kinetics Of

The aim of present work is to determine and analyse the kinetics of drug release from the fast dissolving sublingual by employing various mathematical models. A study was done with Cyanocobalamine fast dissolving sublingual films, 1.5 mg/film by employing solvent casting technique using dehydrated banana starch and Gelatin. The in-vitro drug release profile was carried out in pH 6.8 phosphate buffer (900 mL) using USP dissolution apparatus I (Basket) at 50 rpm for 20 mins. The drug release data was obtained, quantitatively correlated and interpreted with various mathematical models viz. Zero order model, first order model, Higuchi model, Hixson-Crowell model and Korsmeyer-Peppas model and evaluated to understand the kinetics of drug release. The criterion for the most suitable model was based on the high degree of coefficient of correlation of drug release profile of Cyanocobalamine fast dissolving sublingual films.

Sign in / Sign up

Export Citation Format

Share Document