Influence of water soluble fillers in hydroxypropylmethylcellulose matrices on in vitro and in vivo drug release

Sako, Kazuhiro; Sawada, Toyohiro; Nakashima, Hiroshi; Yokohama, Shigeharu; Sonobe, Takashi

doi:10.1016/s0168-3659(02)00067-6

Cited by 87 publications

(59 citation statements)

References 16 publications

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“…After this manipulation, the tablets were transferred back to baskets and the dissolution test continued. Sampling times were 1.5, 2, 4, 6, 8, 12, 16, and 20 h. A similar dissolution test was previously used by Sako et al to simulate situations in the gastrointestinal tract with elevated mechanical stress (15). For comparison, the dissolution test of formulation F4 was performed without the mechanical manipulation.…”

Section: In Vitro Dissolution Test Simulating Transition Through the mentioning

confidence: 99%

“…There are few examples, such as a rotation beaker apparatus (14), application of mechanical stress on swollen matrices with glass beads (15), or systems that simulate the pressure forces exerted by gut wall motility (16). These models were used to evaluate matrix tablet formulations and determine the robustness of the gel layer during dissolution testing by introducing the mechanical stress phase in the test.…”

Section: Introductionmentioning

confidence: 99%

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Correlating Cellulose Derivative Intrinsic Viscosity with Mechanical Susceptibility of Swollen Hydrophilic Matrix Tablets

Klančar¹,

Horvat²,

Baumgartner

2012

AAPS PharmSciTech

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Abstract. Hydrophilic matrix tablets are prone to mechanical stress while passing through the gastrointestinal tract, which may result in inappropriate drug-release characteristics. Intrinsic viscosity is a physical polymer property that can be directly compared across various types and grades of polymers and correlated with the mechanical susceptibility of swollen matrix tablets. Five tablet formulations containing different HPMC and HPC polymers were prepared and analyzed using an in vitro glass bead manipulation test. The dissolution rate results were modeled using the Korsmeyer-Peppas equation and a correlation was found between the fit constants k and n, goodness-of-fit measure parameters, and intrinsic viscosity. Moreover, the dissolution profiles were used to calculate the degree of mechanical susceptibility for each formulation, defined as the ratio of the average dissolution rate after manipulation and the initial dissolution rate before manipulation. It was confirmed that an increased intrinsic viscosity polymer value resulted in a decrease in mechanical susceptibility. Considering this, two simple rules were defined for designing robust matrix tablets with respect to mechanical stresses.

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Section: In Vitro Dissolution Test Simulating Transition Through the mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Correlating Cellulose Derivative Intrinsic Viscosity with Mechanical Susceptibility of Swollen Hydrophilic Matrix Tablets

Klančar¹,

Horvat²,

Baumgartner

2012

AAPS PharmSciTech

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“…Being a semi-synthetic hydrophilic matrix polymer, HPMC has been widely employed in the design of extended-release formulations due to its good compression, rapid hydration and gelling characteristics as well as its ease of use and very low toxicity. [13][14][15][16][17] The in vitro release of apremilast from the developed formulations were * To whom correspondence should be addressed. e-mail: ping.hu@cqu.edu.cn; yun.he@cqu.edu.cn studied and fitted to various mathematic models.…”

Section: )mentioning

confidence: 99%

Development of an Extended-Release Formulation for Apremilast and a Level A <i>in Vitro</i>–<i>in Vivo</i> Correlation Study in Beagle Dogs

Tang

Shigui

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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The primary objective of the present study was to develop extended-release matrix formulations of apremilast for the oral delivery and to study their in vitro and in vivo correlation. Five extended-release formulations containing hydroxypropylmethylcellulose (HPMC) as the retarding excipient with different release rate of apremilast were prepared. Dissolution tests of all the formulated tablets were performed in water, pH 4.0 and 6.8 buffer solutions. The in vitro release kinetics was studied and supported by Korsmeyer-Peppas's equation as it presented highest values of correlation coefficients (r 2 up to 0.966). Among all formulated tablets, F2 (HPMC 25%) and F4 (HPMC 35%) were selected to perform an in vivo study in beagle dogs to obtain various pharmacokinetic parameters, i.e., peak plasma concentration (C max ), time to peak plasma concentration (t max ), area under the plasma-concentration vs. time curve (AUC). Higher t max and t 1/2 , lower C max and elimination coefficient (K e ) were observed for both extended formulations compared to marketed immediate-release products (Otezla ® ). Level A in vitro-in vivo correlations were created with the help of Wagner-Nelson and numeric deconvolution methods. Both formulations showed good in vitro-in vivo correlations whose accuracies were further verified by an internal validation.

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“…During hydration of HPMC a gel layer is formed around the dry core of polymer and swelling of polymer occurs. Drug is then released via pure diffusion or a diffusion-erosion controlled mechanism, where the ratio and properties of the active drug, HPMC and other excipients as well as the composition of fluids and the hydrodynamics in the gastrointestinal tract will determine the detailed release profile [7][8][9][10] . Figure 4 shows the intragastric release behavior of two commercially available HPMC-based tablet formulations containing an anti-asthmatic drug.…”

Section: Cellulose Ethersmentioning

confidence: 99%

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

Klein

2009

Polysaccharide Materials: Performance by Design

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Influence of water soluble fillers in hydroxypropylmethylcellulose matrices on in vitro and in vivo drug release

Cited by 87 publications

References 16 publications

Correlating Cellulose Derivative Intrinsic Viscosity with Mechanical Susceptibility of Swollen Hydrophilic Matrix Tablets

Correlating Cellulose Derivative Intrinsic Viscosity with Mechanical Susceptibility of Swollen Hydrophilic Matrix Tablets

Development of an Extended-Release Formulation for Apremilast and a Level A <i>in Vitro</i>–<i>in Vivo</i> Correlation Study in Beagle Dogs

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

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