The Influence of Excipients on Drug Release from Hydroxypropyl Methylcellulose Matrices

Levina, Marina; Rajabi‐Siahboomi, Ali R.

doi:10.1002/jps.20181

Cited by 119 publications

(51 citation statements)

References 21 publications

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“…The results of dissolution studies showed that F-XII, F-XIII and F-XIV released 13.68, 13.62 and 13.64 % of Stavudine at the end of 1 hr; 56.16, 56.08 and 55.68 at the end of 12 hr; 94.89, 91.84 and 89.74 at the end of 24 hr ( Figure 6). The results indicated that by increasing the hardness the burst effect decreases but not significantly as supported by previous studies [13,14]. The release rate decreased which resulted into less release at the end of 24 hr.…”

Section: Theoretical ( ) F-vi ( ) F-vii( )F-vii (supporting

confidence: 66%

“…The tablets were compressed at hardness of 7 kg/cm 2 (with similar hardness as previous eight formulations). The result of dissolution studies showed that F-IX, F-X and F-XI released 14 In these formulations the release rate decreased but the burst effect continued and was more than the desired theoretical release. Hence the formulation had to be developed further to minimize the burst effect.…”

Section: Theoretical ( ) F-vi ( ) F-vii( )F-vii (mentioning

confidence: 91%

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Design and evaluation of sustained-release matrix once daily formulation of stavudine.

Kumar¹,

Dave²,

Lewis³

et al. 2010

Int j Drug delivery

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The aim of the present study was to formulate once daily sustained release matrix tablets of Stavudine to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance. The sustained release tablets were prepared by direct compression and formulated using different drug: polymer ratios, formulations such as F1to F15. Hydrophilic polymers like Hydroxy propyl methyl cellulose (HPMC), Carboxymethyl cellulose (CMC) and Starch 1500 were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with pharmacopoeial standards. Formulation containing Stavudine:HPMCK15: Na-CMC (1:2:0.5) with hardness 10-11kg/cm 2 showed the desired release profile which matched the theoretical release profile. SEM studies of the formulations were carried out for the confirmation of mechanism of drug release. The in vitro drug release characteristics were studied in both simulated gastric and intestinal fluids for a period of 24 hr using USP Type 2 dissolution apparatus. Mathematical analysis of the release kinetics indicated a coupling of diffusion and erosion mechanisms. The study proves that the developed sustained release tablet is capable of releasing the drug in a sustained manner for 24 hr.

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Section: Theoretical ( ) F-vi ( ) F-vii( )F-vii (supporting

confidence: 66%

Section: Theoretical ( ) F-vi ( ) F-vii( )F-vii (mentioning

confidence: 91%

Design and evaluation of sustained-release matrix once daily formulation of stavudine.

Kumar¹,

Dave²,

Lewis³

et al. 2010

Int j Drug delivery

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show abstract

“…Lactose will dissolve and will increase water availability within the gel structure of the hydrophilic matrix, favoring a diffusion mechanism besides the main erosion mechanism and in this way increasing drug release (28). On the other hand, microcrystalline cellulose will slow down the release of the active substance.…”

Section: The Influence Of Formulation Factors On the Most Relevant Rementioning

confidence: 99%

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

et al. 2017

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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

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“…[15][16][17] PEO has been proposed as an alternate to the cellulose and ethylene glycol derivatives in the production of controlled release drug delivery system. [16][17][18][19][20][21][22][23][24][25][26] Further it also has mucoadhesive properties which may assist in prolonging the gastric residence time. They are characterized with flocculent, thickening, sustainedrelease, lubrication, dispersing and a water-retention property which extends its application to various drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Sodium Alginate with PEG/PEO Blends as a Floating Drug Delivery Carrier – In vitro Evaluation

C¹,

Swamiappan²

2016

Adv Pharm Bull

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The Influence of Excipients on Drug Release from Hydroxypropyl Methylcellulose Matrices

Cited by 119 publications

References 21 publications

Design and evaluation of sustained-release matrix once daily formulation of stavudine.

Design and evaluation of sustained-release matrix once daily formulation of stavudine.

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

Sodium Alginate with PEG/PEO Blends as a Floating Drug Delivery Carrier – In vitro Evaluation

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