Polymer particle erosion controlling drug release. I. Factors influencing drug release and characterization of the release mechanism

Zuleger, Susanne; Lippold, B.

doi:10.1016/s0378-5173(01)00596-8

Cited by 128 publications

(78 citation statements)

References 22 publications

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“…When the drug diffusion rate is slower than the relaxation rate of the polymeric chains, the diffusion is Fickian; whereas when the relaxation process is slow compared to diffusion, zero-order release kinetics occurs. When the drug diffusion rate and the polymeric relaxation rate are of the same order of magnitude, anomalous diffusion is observed and the value of n falls between 0.5 and 1.0 (40,45,46). As can be seen from the data listed in Table II (line 1), the THP release presented zero-order release kinetics.…”

Section: In Vitro Release Of Thpmentioning

confidence: 88%

Correlation Between Rheological Properties, In Vitro Release, and Percutaneous Permeation of Tetrahydropalmatine

Liu

et al. 2011

AAPS PharmSciTech

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Abstract. The aim of the present work was to investigate the influence of formulation factors including different grades of Carbopol® matrices and penetration enhancers on the percutaneous permeation of tetrahydropalmatine (THP), rheological properties, and in vitro release; and the correlation behind rheological properties, in vitro release, and percutaneous permeation. Transdermal penetration of THP through excised rabbit skin and in vitro release of THP across transparent Cellophane® were performed by vertical Franz diffusion cell. Rheological analyses were proceeded in terms of "steady flow tests", "oscillation stress sweep", and "creep recovery". The result of percutaneous penetration of THP indicated that, the emulgel prepared with Carbopol® 971P (Cp 971P) as the matrix and N-methyl-2-pyrrolidone (NMP) as the penetration enhancer had the highest cumulative permeation amount (118.19 μg/cm 2 ). All the experimental data showed a good fit to the Casson model in viscosimetric studies no matter what the types of matrices or the kinds of penetration enhancers were. The release profile fitted the zero-order release kinetics model with Cp 971P as the matrix without any penetration enhancers. However, when adding penetration enhancers, in vitro release of THP presented anomalous (non-Fickian) release kinetics. Clarifying the relationship behind percutaneous permeation of THP, rheological properties, and in vitro release will provide us with profound insights and facilitate the design of specific emulgel.

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Section: In Vitro Release Of Thpmentioning

confidence: 88%

Correlation Between Rheological Properties, In Vitro Release, and Percutaneous Permeation of Tetrahydropalmatine

Liu

et al. 2011

AAPS PharmSciTech

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“…The maximum correlation coefficient has been considered statistical parameter to designate the function with the best fit to the data [21]. The inspection of correlation coefficient values showed that the drug release followed the diffusion control mechanism from the patches [22][23]. The study of Jadhav SB [19] et al, (2014) showed that the stability studies were carried out at 25 °C/60% RH for the selected formulation up to 30 d. in the duration of stability study time interval, the tablets were analyzed for drug hardness, in vitro disintegration time, % drug release up to 30 d. These formulations show not much difference in any parameter.…”

Section: Discussionmentioning

confidence: 99%

Design, Formulation and in Vitro Drug Release From Transdermal Patches Containing Imipramine Hydrochloride as Model Drug

Hardainiyan

Kumar

Nandy

et al. 2017

Int J Pharm Pharm Sci

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Objective: The aim of the present investigation was to form matrix type transdermal patches containing imipramine hydrochloride were prepared using two polymers by solvent evaporation technique to minimise the dose of the drug for lesser side effect and increase the bioavailability of a drug. Methods:In the present study, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) was used as penetration enhancer. Drug-polymer interactions determine by FTIR and a standard calibration curve of imipramine hydrochloride was determined by using UV estimation. Results:The formulated transdermal patch by using PVP K-30, HPMC K100M showed good physical properties. All prepared formulations indicated good physical stability. The formulation F-1 gave the most suitable transdermal film with all desirable physicochemical properties. The thickness of the patches was varied from 0.263±0.67 mm to 0.301±0.61 mm, uniformity of patches showed that patches prepared by solvent evaporation while low standard deviation values ensued by thickness measurements of the film, and weights ranged between 50.5±0.75 mg and 52.15±2.15 mg, which indicates that different batches patch weights, were comparatively similar. Folding endurance was found to be>200 that is satisfactory for the patches, drug content was found to be 5.33±0.14 mg to 5.57±0.095 mg. In vitro, drug permeation studies of formulations were performed by using K-C diffusion cells using abdomen skin of the albino rat. The results were best in in-vitro skin permeation through rat skin as compared to all other formulations prepared with a hydrophilic polymer containing permeation enhancer. The formulation, F1 is considered as the best formulation, since it shows maximum in vitro drug release as 84.71±3.07 % at 24 h. The drug release kinetics studies showed that the majority of formulations were governed by Higuchi model and mechanism of release was non-Fickian mediated. Conclusion:In conclusion, controlled release transdermal drug delivery system (TDDS) patches of imipramine hydrochloride can be prepared using the polymer combinations, with plasticizer and enhancer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased. However, the mechanism of drug release of all formulations was non-Fickian. The properties of a film did not change during the period of study.

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“…In this model, certain neighbors might contain solid particles of drug or excipient, or polymer. We impose zero flux conditions on the boundaries to these solid neighbors, so that only terms involving neighboring cells in the ''wet'' (W) state are counted in the expression in equation (2). This gives the diffusion update rule described above.…”

Section: Author Biographiesmentioning

confidence: 99%

“…The most common systems include coated systems, matrix tablets, eroding tablets and oral osmotic therapeutic systems. [1][2][3] The present work focuses on the development of a mathematical model and simulation tool that describes the sustained drug release observed in matrix tablets. Matrix tablets are devices that deliver a drug in a controlled manner over an extended period of time.…”

Section: Introductionmentioning

confidence: 99%

Swallowing a cellular automaton pill: Predicting drug release from a matrix tablet

Buchla¹,

Hinow

Najera

et al. 2014

SIMULATION

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Matrix tablets are drug delivery devices designed to release a drug in a controlled manner over an extended period of time. We develop a cellular automaton (CA) model for the dissolution and release of a water-soluble drug and excipient from a matrix tablet of water-insoluble polymer. Cells of the CA are occupied by drug, excipient, water or polymer and the CA updating rules simulate the dissolution of drug and excipient and the subsequent diffusion of the dissolved substances. In addition we simulate the possible fracture of brittle drug and excipient powders during the tablet compression and the melting of the polymer during a possible thermal curing process. Different stirring mechanisms that facilitate the transport of dissolved drug in the fluid in which the tablet is immersed are modeled in the water cells adjacent to the boundary of the tablet. We find that our simulations can reproduce experimental drug release profiles. Our simulation tool can be used to streamline the formulation and production of sustained release tablets.

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Polymer particle erosion controlling drug release. I. Factors influencing drug release and characterization of the release mechanism

Cited by 128 publications

References 22 publications

Correlation Between Rheological Properties, In Vitro Release, and Percutaneous Permeation of Tetrahydropalmatine

Correlation Between Rheological Properties, In Vitro Release, and Percutaneous Permeation of Tetrahydropalmatine

Design, Formulation and in Vitro Drug Release From Transdermal Patches Containing Imipramine Hydrochloride as Model Drug

Swallowing a cellular automaton pill: Predicting drug release from a matrix tablet

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