Investigating the Influence of Tablet Location Inside Dissolution Test Apparatus on Polymer Erosion and Drug Release of a Surface-Erodible Sustained-Release Tablet Using Computational Simulation Methods

2021 ◽  
Vol 22 (3) ◽  
Author(s):  
Hao Lou ◽  
Michael J. Hageman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Computational Simulation ◽  
Simulation Methods ◽  
Dissolution Test ◽  
Test Apparatus ◽  
Sustained Release Tablet ◽  
Polymer Erosion ◽  
Release Tablet

scholarly journals Optimized chronomodulated dual release bilayer tablets of fexofenadine and montelukast: quality by design, development, and in vitro evaluation

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Bhupendra Singh ◽  
Geetanjali Saini ◽  
Manish Vyas ◽  
Surajpal Verma ◽  
Sourav Thakur
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Quality By Design ◽  
Immediate Release ◽  
Oral Dosage ◽  
Nocturnal Asthma ◽  
Sustained Release Tablet ◽  
Bilayer Tablets ◽  
Dual Release ◽  
Release Tablet

Abstract Background The conventional oral dosage forms are not effective in dealing with chronopathological conditions, such as nocturnal asthma. Therefore, there is an unmet need to develop a delivery system that can deliver drug as per the chronopharmacology of the diseases. The purpose of the study is to use quality by design (QbD) technique and pulsatile principles for the development of Eudragit-coated dual release bilayer tablets. The dual layer consists of immediate release layer of fexofenadine HCl and sustained release layer of montelukast sodium. Results The quality target product profile of the formulation was developed, and the critical quality attributes were identified. Three-level, three-factor Box-Behnken design was used for the optimization of the bilayer tablets. Based on the design, a total of 13 formulation combinations (F1–F13 and M1–M13) were made having acceptable micromeritic properties. The developed immediate and sustained release layers were evaluated for physicochemical properties. Depending upon the value of the diffusion exponent, the Fickian diffusion mechanism is dominant among immediate and sustained release tablet layers. Response curve for immediate release layer showed that concentrations of sodium starch glycolate and sodium bicarbonate had a negative effect on disintegration time and a positive effect on drug release. For sustained release tablet layer, concentrations of HPMC E 5 LV and magnesium stearate had a significant effect on drug release. The ANOVA and diagnostic plots confirmed the significance and goodness of fit of the used model. Based on desirability plot values, optimized formulation was developed and coated with Eudragit coat. The coated bilayer tablet showed met the requirement of providing an immediate release during the first hour and a sustained release action for a period of more than 8 h after passing the gastric region. Conclusions The formulation can be fruitful in curbing the menace of nocturnal asthma and providing a high degree of patient compliance as the patient will not have to wake up at night to take the medication.

scholarly journals FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE TABLET USING MARDI GUM

2021 ◽  
pp. 52-55
Author(s):  
MANGESH M KUMARE ◽  
GIRIDHAR R SHENDARKAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Sustained Release Tablet ◽  
Weight Variation ◽  
Release Tablet

Objective: The present research work was to develop and evaluate alprazolam sustained release tablet using Mardi gum, a comparative study on binding properties of gum and hydroxypropyl methylcellulose (HPMC) was performed. Methods: Formulation of alprazolam tablets (f1–f6) was done by direct compression method using 15%, 30%, and 45% concentration of gum as a natural binder, and HPMC was used as synthetic matrix forming agent. Microcrystalline cellulose was used as diluents, talc, and magnesium stearate as a lubricant and PVP K30 as the binder. The formulated batches were evaluated for parameters such as tablet thickness, % friability, hardness, weight variation, and in vitro drug release characteristics. The release information was fitted into different dynamics models to decide the release mechanism of the drug. Results: The results showed that all the parameters of the developed tablets (f1–f6) were in fulfillment with pharmacopeia limits. In vitro, drug release studies showed that formulation f1 had most controlled and sustained manner releaser with maximum drug release of 97.89±0.52% in 18 h with comparison to f2–f4 and f6 drug release is 98.12±0.55%, 97.24±0.57%, 98.16±0.74%, and 97.26±0.35%, respectively, in 16 h and f5 giving 97.89±0.85% release in 14 h. Conclusion: On the basis of obtained result, it can be concluded that Mardi gum can be used to sustain the drug release as a natural polymer in tablet dosage form.

scholarly journals Formulation and in-vitro evaluation of theophylline sustained release tablet

2019 ◽  
Vol 9 (1-s) ◽  
pp. 48-51
Author(s):  
Ravi U Gaware ◽  
Sujit T Tambe ◽  
Shankar M Dhobale ◽  
Suresh L Jadhav
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Ethyl Cellulose ◽  
Trial And Error ◽  
In Vitro Evaluation ◽  
Sustained Release Tablet ◽  
Release Tablet

The aim of present study was to prepare sustained release tablet of Theophylline so as to prolong its elimination time and at the same time to keep cost of the formulation minimum. In this study ethyl cellulose and Eudragit are used in the formulation to sustain the release of Theophylline. Ethyl cellulose and Eudragit are added at the granulation step to form a sustained release coating around each granule. Different batches were designed one after another on trial and error basis to get the optimum drug release upto 12 hours. Keywords: Theophylline, ethyl cellulose, Eudragit, sustained release, coating, tablet.

Formulation and Development of Metoprolol Succinate Sustained Release Matrix tablet using Remusatia vivipara tubers mucilage

2021 ◽  
pp. 5405-5410
Author(s):  
Ganesh N. Sharma ◽  
Mayur R. Bhurat ◽  
Vijay M. Shastry ◽  
Birendra Shrivastava
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Tablet Formulation ◽  
Matrix Tablets ◽  
Release Kinetic ◽  
Order Kinetic ◽  
Reference Formulation ◽  
Metoprolol Succinate ◽  
Sustained Release Tablet ◽  
Release Tablet

The purpose of this research was to formulate and evaluate sustained release tablet by using novel polymer Remusatia vivipara tubers mucilage. Currently natural gums and mucilages are being used extensively comparable to synthetic drug release modifiers. Natural plant materials possess various advantages. These are very cheap, biocompatible, biodegradable and free from side effects. In present research Metoprolol succinate matrix tablets were prepared by using Remusatia vivipara tubers mucilage. For the formulation of sustained release matrix tablets, direct compression method was used. The formulated matrix tablets were then evaluated for thickness, diameter, hardness, weight variation, friability, drug content, swelling index, in-vitro drug release and stability studies. The formulated sustained release tablet passed all tests required. The dissolution profile of prepared tablets showed sustained release of drug up to 11 hours compared to the reference tablet formulation PROLOMET XI 100. Drug release data were then fitted in to release kinetic models such as zero order kinetic, first order kinetic, Higuchi model and Korsmeyer-Peppas model to study the release pattern of drug from each formulation. The prepared sustained release tablet formulation was compared with marketed formulation (reference formulation) for drug release study and factor f1 (difference factor) and f2 (similarity factor) were determined. From this study it can be concluded that as the concentration of Remusatia vivipara mucilage increases, there is decrease in the rate of drug release from the formulation. The best formulation was found to be F3 which consists of 20% Remusatia vivipara mucilage but did not give comparable drug release profile to the reference formulation with factor f1 69.4 % and f2 34.8%. But it can be said that Remusatia vivipara gum mucilage can be used in tablet formulation to give sustained release effect up to 10 hours or in combination with other natural gum mucilage it may enhance the release retardant effect of drug up to or more than 20 hrs. The release kinetic study showed that the prepared sustained release tablet formulation shows anomalous (non-fickian) diffusion pattern and follows both diffusion controlled and swelling controlled mechanisms for drug release.

FOMULATION OF SALBUTAMOL SUSTAINED RELEASE TABLET

2011 ◽  
pp. 42-47
Author(s):  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Potassium Chloride ◽  
Ethyl Cellulose ◽  
Methyl Cellulose ◽  
Duration Of Action ◽  
The Core ◽  
Sustained Release Tablet ◽  
Coated Tablet ◽  
Release Tablet

Background: Salbutamol, a highly selective beta 2 adrenoceptor agonist with bronchodilating property, is widely used for the management of chronic and acute asthma. The biological half life of drug is about 4.5 hour, hence salbutamol is given orally four times daily to maintain a therapeutic blood level. The aim of recent study was to formulate film coated sustained release tablet for 12-hour duration of action. Materials and methods: The core tablet containing salbutamol sulphate, potassium chloride and lactose were prepared using wet granulation process. The resultant tablets were coated with mixtures of ethyl cellulose and hydroxylpropyl methyl cellulose to control the release of salbutamol. Results: Three formulations of the core were chosen to fabricate salbutamol tablets and the core tablets were coated with polymer at various ratio to core weight to control the drug release. It was found that the core containing 68 mg of potassium chloride and 6 % (W/W) of polymer possessed the drug release similar to that of reference product (Ventolin CR). The drug release kinetic of the experimental product was best fit to zero order. Active ingredient was released out of the coated tablet through pores formed by disolving of hydrophyllic one in mixture of polymer in contact with medium. Conclusion: The mixture of ethyl cellulose and hydroxylpropyl methyl cellulose could be used as coating to control the release of salbutamol. The dissolution of resultant coated tablet was similar to that of Ventolin CR 4 mg. The products were ready to be assessed further by conducting stability testing and bioequivalence evaluation in human volunteers.

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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