Development of Extended Zero-Order Release Gliclazide Tablets by Central Composite Design

Vijayalakshmi, P.; Devi, V. Kusum; Narendra, C; Srinagesh, Shailaja

doi:10.1080/03639040701386129

Cited by 18 publications

(9 citation statements)

References 29 publications

(25 reference statements)

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“…Design Expert software was also used to evaluate the statistical validity of the constructed polynomial equations by performing one-way analysis of variance (ANOVA), as shown in Tables VI, VII, and VIII for Y 1 , Y 2 , and Y 3 , respectively. Using a 1.414% significance level, a model is considered significant if the P-value (significance probability value) is less than 0.05 (Shah et al, 2009;Vijayalakshmi et al, 2008). The slowing effect of both independent variables X 1 (CP) and X 2 (SCMC) is depicted in Equation 6, which shows that both polymers have a negative effect on Y 1 , with a slightly more negative effect in the case of SCMC, confirming its release rate slowing ability.…”

Section: Mathematical Modelingmentioning

confidence: 87%

Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology

Khalid¹,

Ahmad²,

Minhas³

et al. 2014

Braz. J. Pharm. Sci.

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The objective of the current study was to formulate mucoadhesive controlled release matrix tablets of flurbiprofen and to optimize its drug release profile and bioadhesion using response surface methodology. Tablets were prepared via a direct compression technique and evaluated for in vitro dissolution parameters and bioadhesive strength. A central composite design for two factors at five levels each was employed for the study. Carbopol 934 and sodium carboxymethylcellulose were taken as independent variables. Fourier transform infrared (FTIR) spectroscopy studies were performed to observe the stability of the drug during direct compression and to check for a drug-polymer interaction. Various kinetic models were applied to evaluate drug release from the polymers. Contour and response surface plots were also drawn to portray the relationship between the independent and response variables. Mucoadhesive tablets of flurbiprofen exhibited non-Fickian drug release kinetics extending towards zero-order, with some formulations (F3, F8, and F9) reaching super case II transport, as the value of the release rate exponent (n) varied between 0.584 and 1.104. Polynomial mathematical models, generated for various response variables, were found to be statistically significant (P<0.05). The study also helped to find the drug's optimum formulation with excellent bioadhesive strength. Suitable combinations of two polymers provided adequate release profile, while carbopol 934 produced more bioadhesion.Uniterms: Flurbifrofen/mucoadhesive controlled release tablets/formulation. Flurbifrofen/mucoadhesive controlled release tablets/in vitro evaluation. Drugs/release profile. Drugs/bioadhesion. Tablets/direct compression.O objetivo do presente estudo foi formular comprimidos mucoadesivos de flurbiprofeno, de liberação controlada, e otimizar o perfil da liberação do fármaco e a bioadesão, utilizando a metodologia de superfície de resposta. Prepararam-se os comprimidos via técnica de compressão direta, que foram avaliados in vitro quanto aos parâmetros de dissolução e da força bioadesiva. Planejamento com componente central para dois fatores em cinco níveis cada foi empregado para esse estudo. Carbopol 934 e carboximetilcelulose sódica foram tomados como variáveis independentes. Efetuaram-se estudos de espectroscopia por transformada de Fourier (FTIR) para observar a estabilidade do fármaco durante a compressão direta e para avaliar a interação a fármaco-polímero. Aplicaram-se vários métodos cinéticos para avaliar a liberação do fármaco dos polímeros. Gráficos de superfície de contorno e de resposta foram efetuados para retratar a relação entre as variáveis dependentes e a resposta. Os comprimidos mucoadesivos de flurbiprofeno apresentaram cinética de liberação não-fickiana, estendendo para ordem zero, para algumas formulações (F3, F8 e F9), alcançando transporte super caso II, à medida que o valor do expoente (n) de taxa de liberação variou entre 0,584 e 1,104. Modelos matemáticos polinomiais, gerados por diversas variáveis de resposta, ...

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Section: Mathematical Modelingmentioning

confidence: 87%

Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology

Khalid¹,

Ahmad²,

Minhas³

et al. 2014

Braz. J. Pharm. Sci.

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“…A response surface type Central Composite Design was employed using Design-Expert Software (Version 7.0.0 Stat-Ease Inc., Minneapolis, USA). Independent factors are HPMC K100M (X1) and Eudragit RL100(X2) concentrations at three levels [13,14]. Weight Variation, Folding Endurance, Flatness, pH of patches, % Moisture Content, % Moisture uptake, % Elongation, % Drug Content & % Drug Release after 14 hours were kept as dependent variables [13,14].…”

Section: Experimental Designmentioning

confidence: 99%

“…Independent factors are HPMC K100M (X1) and Eudragit RL100(X2) concentrations at three levels [13,14]. Weight Variation, Folding Endurance, Flatness, pH of patches, % Moisture Content, % Moisture uptake, % Elongation, % Drug Content & % Drug Release after 14 hours were kept as dependent variables [13,14]. The different formulation of Nateglinide Transdermal Patches is as shown in Table-1.…”

Section: Experimental Designmentioning

confidence: 99%

Formulation and Evaluation of Nateglinide Patches for Transdermal Drug Delivery.

Solunke¹,

Chaudhari²

2017

JCPR

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Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. Nateglinide is an Anti-Diabetic drug with a shorter half life, low bioavailability up to 72 % undergoes extensive first pass metabolism are required to maintain the therapeutic level it has chosen as transdermal drug delivery system. The present study was to formulate and evaluate transdermal drug delivery system of Nateglinide using polymers such as HPMC & Eudragit RL100 by solvent casting technique. The prepared formulations were evaluated for different physicochemical characteristics like Weight Variation, Folding Endurance, Flatness, pH of patches, % Moisture Content, % Moisture uptake, % Elongation, % Drug Content & % Drug Release. The drug release characteristics of the formulation were studied in-vitro by using semi-permeable membrane. The in-vitro drug release plot has shown that the drug release followed zero order kinetics & Higuchi model, which was evidenced from the regression values. Based on the drug release and physicochemical values obtained from the formulation F 7 is considered as an optimized formulation which shows higher percentage of drug release (96.27±0.68 % at 14 hour) with diffusion mediated mechanism. Korsmeyer-Peppas exponential plots shows fairly linear & it is well supported by their regression coefficients values & slope value (n) were >1 which suggest that drug was released by Super Case-II transport.

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“…All the response variables are fitted to a quadratic model and regression analysis was preformed to obtain the quantitative relationships between the dependent (i.e., drug release rate) and independent variables such as amount of ingredient needed, tablet hardness, amount of coating, etc. [10]. With the cited advantages, D-optimal design with a polynomial quadratic statistical model instead of a quadratic model was used in this study.…”

Section: Introductionmentioning

confidence: 99%

“…In 2008, Vijayalakshmi et al [10] utilized a central composite design to develop an extended release tablet formulation of gliclazide with pH dependent matrix forming polymers like Keltone ® HVCR (sodium alginate) (X 1 ) and Eudragit ® EPO (X 2 ) as independent variables. Five dependent variables were considered: hardness, percent of drug release after 1 hour, percent of drug release after 6 hours, diffusion exponent and the time required for 50% drug release.…”

Section: Introductionmentioning

confidence: 99%

Application of D-Optimal Study Design with Contour Surface Response for Designing Sustained Release Gliclazide Matrix Tablets

Nguyen¹,

Christensen²,

Nguyen³

2014

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An optimized formulation of a sustained release tablet of Gliclazide was developed. The use of Doptimal design with a polynomial statistical model to analyze dissolution data reduced the number of laboratory tests required to obtain an optimal dosage form. The final formulation contained 22 mg of Methocel ® E15LV, 16.5 mg Methocel ® E15 and 10.0 mg of Dibasic Calcium Phosphate per 30 mg Gliclazide sustained release tablet. Dissolution studies performed on tablets from 5000 tablet test batches released greater than 90 percent of loaded drug in eight hours. Drug release from the optimized tablets followed a pattern more closely similar to zero-order than other mechanisms of drug release tested. Storage of tablets in accelerated and ambient conditions for 6 and 12 months respectively did not alter any of the physico-chemical properties, drug release or the drug release rate compared to initial observations and dissolution data of the prepared tablets. The addition of potassium phosphate and monosodium phosphate to the tablet reduced the effect pH has on Gliclazide dissolution compared to the commercially available product.

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Development of Extended Zero-Order Release Gliclazide Tablets by Central Composite Design

Cited by 18 publications

References 29 publications

Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology

Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology

Formulation and Evaluation of Nateglinide Patches for Transdermal Drug Delivery.

Application of D-Optimal Study Design with Contour Surface Response for Designing Sustained Release Gliclazide Matrix Tablets

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