Release modulating hydrophilic matrix systems of losartan potassium: Optimization of formulation using statistical experimental design

Chopra, Shruti; Patil, Gayathri V.; Motwani, Sanjay K.

doi:10.1016/j.ejpb.2006.09.001

Cited by 144 publications

(58 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Drug release rate curves (Fig. 1, inset) of all the formulations portray an initial burst release of the drug, characteristic of most hydrophilic matrices (3,14,22). Summary of the drug release parameters (Table III) shows that the value of n varies from 0.4653 to 0.6618, distinctly delineating the non-Fickian release behaviour of all formulations.…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 92%

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

Singh¹,

Pahuja²,

Kapil³

et al. 2009

Acta Pharmaceutica

View full text Add to dashboard Cite

Oral controlled release (CR) systems constitute the most »sought after« route of drug administration since they obviate the need of frequent dosage administration and fluctuating blood levels characterized by saw-tooth kinetics, and hence improve the patient compliance (1). The success of CR devices is invariably hindered by their inability to localize in the selected region(s) of the gastrointestinal (GI) tract (2). Mucoadhesive drug delivery systems (DDS) offer a promising approach for controlled and site-specific delivery to the GI tract by attaching the devices to the mucus and mucosa of the tract via the process of bioadhesion. These mucoadhesive systems are also known to provide intimate contact between the dosage form and the absorptive mucosa, resulting in high drug flux through the absorbing tissue with improved bioavailability (3).Hydralazine (HZ), a directly acting vasodilator, is widely prescribed in the treatment of hypertension and congestive heart failure. Albeit the drug is readily absorbed following oral administration, it is subjected to significant first-pass metabolism (4). Oral bio- The current study involves development of oral bioadhesive hydrophilic matrices of hydralazine hydrochloride, and optimization of their in vitro drug release profile and ex vivo bioadhesion against porcine gastric mucosa. A 3 2 central composite design was employed to systematically optimize the drug delivery formulations containing two polymers, viz., carbomer and hydroxypropyl methyl cellulose. Response surface plots were drawn and optimum formulations were selected by brute force searches. Validation of the formulation optimization study indicated a very high degree of prognostic ability. The study successfully undertook the development of an optimized once-a--day formulation of hydralazine with excellent bioadhesive and controlled release characteristics.

show abstract

Section: In Vitro Drug Release Studiesmentioning

confidence: 92%

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

Singh¹,

Pahuja²,

Kapil³

et al. 2009

Acta Pharmaceutica

View full text Add to dashboard Cite

show abstract

“…Among various ER/CR dosage systems, the most famous one is the hydrophilic matrix tablet (3)(4)(5). Hydrophilic matrix tablets are usually assembled by hydrophilic polymer and/or other excipients with homogeneous dispersion of drug.…”

Section: Introductionmentioning

confidence: 99%

Design and Evaluation of Hydrophilic Matrix System Containing Polyethylene Oxides for the Zero-Order Controlled Delivery of Water-Insoluble Drugs

et al. 2016

View full text Add to dashboard Cite

Abstract. The aim of this study was to design a polyethylene oxide (PEO) binary hydrophilic matrix controlled system and investigate the most important influence(s) on the in vitro water-insoluble drug release behavior of this controlled system. Direct-compressed PEO binary matrix tablets were obtained from a variety of low viscosity hydrophilic materials as a sustained agent, using anhydrous drugs as a model drug. Water uptake rate, swelling rate, and erosion rate of matrices were investigated for the evaluation of the PEO hydrophilic matrix systems. The effect of the dose, the solubility of water-insoluble drug, and the rheology of polymers on in vitro release were also discussed. Based on the in vitro release kinetics study, three optimized PEO binary matrices were selected for further research. And, these PEO binary matrices had shown the similar release behavior that had been evaluated by the similarity factor f 2 . Further study indicated that they had identical hydration, swelling, and erosion rate. Moreover, rheology study exhibited the similar rheological equation of Herschel-Bulkley and their viscosity was also within the same magnitude. Therefore, viscosity plays the most important role to control drug release compared to other factors in PEO binary matrix system. This research provides fundamental understanding of in vitro drug release of PEO binary hydrophilic matrix tablets and helps pharmaceutical workers to develop a hydrophilic controlled system, which will effectively shorten the process of formulation development by reducing trial-and-error.

show abstract

“…The reasons behind the popularity of hydrophilic matrixes are that they offer precise drug release modulation as a result of hydration of non-ionic cellulose ethers, cost effectiveness, and the capacity to provide a prolonged and constant therapeutic effect (4,5). Although developing a hydroxypropyl methylcellulose (HPMC) matrix formulation may seem simple, a large number of variables need to be considered for a valid formulation with the desired release kinetics.…”

mentioning

confidence: 99%

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

et al. 2017

View full text Add to dashboard Cite

The main objective of the present study was to apply QbD methodology in the development of once-a-day sustained release quetiapine tablets. The quality target product profile (QTPP) was defined after the pharmaceutical properties and kinetic release of the innovator product, Seroquel XR 200 mg. For the D-optimal experimental design, the level and ratio of matrix forming agents and the type of extragranular diluent were chosen as independent inputs, which represented critical formulation factors. The critical quality attributes (CQAs) studied were the cumulative percentages of quetiapine released after certain time intervals. After the analysis of the experimental design, optimal formulas and the design space were defined. Optimal formulas demonstrated zero-order release kinetics and a dissolution profile similar to the innovator product, with f 2 values of 74.53 and 83.74. It was concluded that the QbD approach allowed fast development of sustained release tablets with similar dissolution behavior as the innovator product.Keywords: quality by design, design of experiments, sustained release, hydrophilic matrix, quetiapineIn the past years, the main goal of antipsychotic drug development has been to develop molecules with higher efficacy and fewer side effects usually associated with the classic antipsychotic medications. The newly developed agents, called atypical antipsychotics, are successfully used in the treatment of both positive and negative symptoms of schizophrenia and are associated with fewer neurological and endocrine side effects compared to older medications (1). Quetiapine is a recently introduced atypical antipsychotic, which has an excellent risk/benefit ratio and is indicated as the first-line option for the treatment of psychotic disorder manifestations and schizophrenia (2). Quetiapine is available as fumarate salt in immediate as well as in sustained released formulations, the innovative product being Seroquel. The sustained release formulation was introduced several years ago and its primary objective is to release the drug slowly over an extended ALEXANDRU GAVAN

show abstract

Release modulating hydrophilic matrix systems of losartan potassium: Optimization of formulation using statistical experimental design

Cited by 144 publications

References 26 publications

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

Design and Evaluation of Hydrophilic Matrix System Containing Polyethylene Oxides for the Zero-Order Controlled Delivery of Water-Insoluble Drugs

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

Contact Info

Product

Resources

About