scholarly journals Preparation and Evaluation of Sustained Release Matrix Tablets of Tolterodine Tartrate Using Guggul Resin

2018 ◽  
Vol 21 (1) ◽  
pp. 24-34
Author(s):  
K Latha ◽  
T Chinni Kranthi ◽  
Naseeb Basha Shaik
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
Matrix Tablets ◽  
Natural Polymers ◽  
Duration Of Action ◽  
Tolterodine Tartrate ◽  
Vitro Release

The present study is based on preparation of sustained release matrix tablets of tolterodine tartrate (for overactive bladder treatment) using guggul resin. Tolterodine tartrate is a highly soluble drug, to increase the duration of action the release of the drug has to be sustained. Natural resin is used as a polymer to sustain the release of drug, which was isolated from guggul gum by petroleum ether. Natural polymers are economical, biodegradable and can be chemically modified. Different ratios of drug and guggul resin were tried in the formulation of sustained release matrix tablets of tolterodine tartrate. Wet granulation technique was adopted for preparation of tolterodine tartrate granules, showed good flow properties and compressibility. The fabricated tablets were evaluated for various physicochemical characteristics and in vitro release studies like hardness, thickness, weight variation, friability, drug content and content uniformity were found to be within the limits. The drug release of optimized formulation (F6) was fitted to various kinetic models and the R2 value is 0.988 and the n value of drug release is 0.787. Therefore, the drug release follows zero order with non-fickian diffusion. The mechanism of drug release involves erosion and diffusion. Stability studies were performed for the optimized formulation as per ICH guidelines climatic zone III and were found to be stable with insignificant changes in physicochemical characteristics and in vitro release studies.Bangladesh Pharmaceutical Journal 21(1): 24-34, 2018

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 Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet

2015 ◽  
Vol 16 (2) ◽  
pp. 177-183
Author(s):  
Md Ziaur Rahman ◽  
Sayed Koushik Ahamed ◽  
Sujan Banik ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Matrix Tablet ◽  
Vitro Release

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 and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013

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.

scholarly journals A study on the influence of the formulation factors on in vitro release of ketoprofen from sustained release tablets

2021 ◽  
Vol 14 (1) ◽  
pp. 41-48
Author(s):  
Larisa Cimpoaie ◽  
◽  
Luca Liviu Rus ◽  
Rareș Iuliu Iovanov ◽  
◽  
...  
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Inert Matrix ◽  
Sustained Release Tablets ◽  
Formulation Factors ◽  
Release Data ◽  
Vitro Release ◽  
Inert Matrix Tablets

Objectives. The aim of this study was to investigate the influence of formulation factors on in vitro release of ketoprofen from sustained release inert matrix tablets. Materials and methods. Laboratory scale, Ketoprofen sustained release inert matrix tablets were manufactured using Kollidon® SR as matrix formator, by direct tableting of powder blends. The influence of the formulation factors (X1 – matrix formator excipient and X2 – diluent type) on in vitro release of ketoprofen from sustained release tablets was studied by using a full factorial 23 experimental plan. Outcomes. Pharmacotechnical characterization of manufactured laboratory scale batches was performed and all 12 batches fulfilled European Pharmacopeia requests. In vitro release showed a sustained release profile in all cases. Variance analysis (ANOVA) showed a good correlation between experimental conditions and answers. In vitro release testing was performed in phosphate buffer pH = 7.4. Percentage release was determined spectrophotometrically at 258 nm. A decrease in the rate of in vitro release was registered, up to 4 h and 6 h when lactose DC and mannitol DC were used as diluents, respectively. Isomalt DC has increased the rate of in vitro release up to 6 h. Conclusions. In vitro release data, corresponding to formulation N1 shoed a good fitting with Weitbull, Korshmeyer-Peppas and Higuchi models while in vitro release data corresponding to formulation N8 presented a good fitting with Weitbull and Korsmeyer-Peppas. In case of formulations N1 and N8 a non-Fickian diff usion mechanism seems to be involved in drug release from the matrix tablets.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

2017 ◽  
Vol 10 (5) ◽  
pp. 285
Author(s):  
S Shanmugam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Kinetic ◽  
Natural Polymers ◽  
In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 

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 Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

The Preparation and In Vitro Release Study of the Novel Changchun Amine Sustained-Release Capsules

2014 ◽  
Vol 651-653 ◽  
pp. 313-316
Author(s):  
Ping Liu ◽  
Jin Liang Zhang
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
The Novel ◽  
Determination Method ◽  
Preparation Methods ◽  
Reference Preparation ◽  
Time Test ◽  
Vitro Release

Objective: to prepare sustained-release capsules, changchun amine build release degree determination method, study its drug release characteristics and compared with the reference preparation. Methods: using ordinary dissolution apparatus and fiber stripping analyzer to determine the in vitro release of sustained-release capsules. The content determination method, drug to pH 1.5 sodium chloride for the release of the medium of hydrochloric acid solution, using ultraviolet spectrophotometry to release a quantity, at the same time by optical real-time test evaluation of homemade consistency and reference formulation of drug release. Results: the analysis method can be effectively used to build the release of sustained-release capsules to measure, two kinds of similarity factor is more than 50, drug release characteristics match each batch sample, quality and stability. Conclusion: the self-made samples and reference preparation have similar in vitro release characteristics of homemade capsule good slow release effect, drug release and stability.

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