Model drug release from matrix tablets composed of HPMC with different substituent heterogeneity

Viridén, Anna; Larsson, Anette; Schagerlöf, Herje; Wittgren, Bengt

doi:10.1016/j.ijpharm.2010.09.017

Cited by 26 publications

(15 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A similar observation was produced in H2 formulation, whose rate of drug release increased in this medium, producing a higher percentage of drug released at 8 h. However, this improvement in drug release rate could not be evidenced in H3, H4, H5 and H6 formulations. This behaviour suggests that the HPMC could be suffering a hydrolysis process by the hemicellulolytic activity of pectinase, in spite of the previous studies by Viriden and co-workers that showed only a specific HPMC hydrolysis by endoglucanases (25). Moreover, these results could be attributed to the modification in the dissolution method which ensured the complete immersion of the H1, H2 and H3 matrices within the dissolution medium.…”

Section: In Vitro Dissolution Testmentioning

confidence: 80%

“…So, in order to mimic the physiological human conditions, and contributes to establish in vitro-in vivo correlations (23), it has been described as dissolution medium nature, medium ionic strength or temperature of the medium can affect the hydration of hydrophilic polymers, and in consequence the drug release from matrix systems could be affected (24). In this sense, Ebube and Jones have reported the significant impact of the pH of the dissolution medium on the drug release rate (3) while recent efforts have been undertaken to show that HPMC matrices were hydrolysed by a selective endoglucanase from Trichoderma reesei (25), suggesting that the study of the enzymes activity over HPMC formulations could be crucial in order to know the effects of physiological conditions.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Matrix Tablets: The Effect of Hydroxypropyl Methylcellulose/Anhydrous Dibasic Calcium Phosphate Ratio on the Release Rate of a Water-Soluble Drug Through the Gastrointestinal Tract I. In Vitro Tests

2012

View full text Add to dashboard Cite

Different hydroxypropyl methylcellulose (HPMC)/anhydrous dibasic calcium phosphate (ADCP) matrix tablets have been developed aiming to evaluate the influence of both components ratio in the control release of a water-soluble drug (theophylline). In order to characterise the matrix tablets, swelling, buoyancy and dissolution studies have been carried out in different aqueous media (demineralised water, progressive pH medium, simulated gastric fluid, simulated intestinal fluid and simulated colonic fluid). The HPMC/ADCP ratio has turned out to be the determinant in the matrix behaviour: the HPMC characteristic swelling behaviour was modulated, in some cases, by the ADCP characteristic acidic dissolution. When the HPMC/ADCP ratio was ≥0.69, buoyancy, continuous swelling and low theophylline dissolution rate from the matrices (H1, H2 and H3) were observed in all dissolution media. Consequently, these formulations could be adequate as gastro-retentive drug delivery systems. Additionally, HPMC/ADCP ratio ≤0.11 (H5 and H6) induces a pH-dependent drug release which could be applied to design control drug release enteric formulations (with a suitable enteric coating). Finally, a HPMC/ADCP ratio between 0.11 and 0.69 (H4) yield a gastrointestinal controlled drug release, due to its time-dependent buoyancy (7 h) and a total drug delivery in 17 h in simulated colonic fluid.

show abstract

Section: In Vitro Dissolution Testmentioning

confidence: 80%

Section: Introductionmentioning

confidence: 99%

Matrix Tablets: The Effect of Hydroxypropyl Methylcellulose/Anhydrous Dibasic Calcium Phosphate Ratio on the Release Rate of a Water-Soluble Drug Through the Gastrointestinal Tract I. In Vitro Tests

2012

View full text Add to dashboard Cite

show abstract

“…These above techniques are helpful because they provide structural information on the cellulose segments that are broken down during the enzymatic treatments, thus can assist pinpointing structural characteristics of the original cellulosic backbones. The substitution heterogeneity of HPMC has recently been shown to impact important properties of HPMC such as cloud point, swelling, and drug release …”

Section: Resultsmentioning

confidence: 99%

“…The substitution heterogeneity of HPMC has recently been shown to impact important properties of HPMC such as cloud point, swelling, and drug release. [21][22][23]28,29 In summary, the chemical heterogeneity of HPMC is a very important aspect that may impact the key release-controlling properties of this polymer. However, characterization of the heterogeneity is analytically challenging, time-consuming, and at most qualitative in nature.…”

Section: Nmr Investigationmentioning

confidence: 99%

Understanding and Managing the Impact of HPMC Variability on Drug Release from Controlled Release Formulations

Zhou

Law

Reynolds

et al. 2014

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…For many model substances, the relationship has been examined between the release rate from matrix tablets and the viscosity and size of HPMC particles, the percentage in formulations and the production method of this form [2,23,24]. In tablets containing 400 mg of metronidazole, sustained release over 8h was obtained by including in the composition, HPMC in quantities between 10% -30% (w/w) of the active substance.…”

mentioning

confidence: 99%

Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study

Letmanski

Kodym

Weber

et al. 2015

Current Issues in Pharmacy and Medical Sciences

View full text Add to dashboard Cite

The aim of this study was to examine the usefulness of a pH-dependent copolymer - Eudragit FS - for employment in the technology of preparing modified release metronidazole matrix tablets. In addition, in our work, Eudragit RL and Eudragit RS were included in the composition of some formulations, as well as sodium lauryl sulfate and polysorbate 80. As part of the study of the dissolution test, the similarity coefficient (f2) for the obtained profiles was calculated, and mathematic models were used to estimate the kinetics and mechanism of active substance release. In our work, it was observed that the inclusion of polymer Eudragit FS alone in the tablet composition ensured a modified release of the active substance for 10 h. After this time period, the amount of metronidazole determined in the acceptor fluid was 71% - 81% of the declared dose. Modification of the composition by the addition of surfactants resulted in an increased release of the active substance of up to 98%. This effect was dependent on the type of surfactant and its quantitative ratio to the Eudragit FS. Similar release profiles were obtained for tablets containing Eudragit RS and sodium lauryl sulfate, as well as Eudragit RS and polysorbate 80. Depending on the composition of tablets, metronidazole release proceeded in accordance with either first or second-order kinetics. We calculated as well, that the differing masses of Eudragit FS in the studied formulations correlates with the order of release kinetics (p < 0.002). Such an effect was validated using the Weibull model, wherein, in all the studied formulations, the release rate was seen as a decreasing function of time. An analysis of data according to the Ritger-Peppas model and the Peppas-Sahlin model for some formulations, indicated that the mechanism of active substance release from matrix tablets is diffusion.

show abstract

Model drug release from matrix tablets composed of HPMC with different substituent heterogeneity

Cited by 26 publications

References 21 publications

Matrix Tablets: The Effect of Hydroxypropyl Methylcellulose/Anhydrous Dibasic Calcium Phosphate Ratio on the Release Rate of a Water-Soluble Drug Through the Gastrointestinal Tract I. In Vitro Tests

Matrix Tablets: The Effect of Hydroxypropyl Methylcellulose/Anhydrous Dibasic Calcium Phosphate Ratio on the Release Rate of a Water-Soluble Drug Through the Gastrointestinal Tract I. In Vitro Tests

Understanding and Managing the Impact of HPMC Variability on Drug Release from Controlled Release Formulations

Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study

Contact Info

Product

Resources

About