A novel bi-layer ascending release osmotic pump tablet: In vitro investigation and in vivo investigation in pharmacokinetic study and IVIVC evaluation

Xu, Heming; Zhao, Li; Pan, Hao; Zhang, Zhihong; Liu, Dandan; Tian, Baocheng; Shi-lin, MA; Song, Shilong; Pan, Wei-San

doi:10.1016/j.ijpharm.2013.09.031

Cited by 21 publications

(6 citation statements)

References 15 publications

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“…40 The US Food and Drug Administration demonstrated a simultaneous release similarity factor .50. 41 However, the similarity factor of PUE and SCU was 42.08. Therefore, the PUE-SCU CLNs demonstrated asynchronous release.…”

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confidence: 97%

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Wang¹,

Zhao²,

Li³

et al. 2017

IJN

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The purpose of this study was to prepare, optimize, and characterize a cationic lipid nanoparticle (CLN) system containing multicomponent drugs using a molecular dynamics model as a novel method of evaluating formulations. Puerarin (PUE) and scutellarin (SCU) were used as model drugs. CLNs were successfully prepared using melt-emulsion ultrasonication and low temperature-solidification technique. The properties of CLNs such as morphology, particle size, zeta potential, entrapment efficiency (EE), drug loading (DL), and drug release behavior were investigated. The CLNs were evaluated by corneal permeation, preocular retention time, and pharmacokinetics in the aqueous humor. Additionally, a molecular dynamics model was used to evaluate the formulation. Electron microscopy results showed that the nanoparticles were approximately spherical in shape. The EE (%) and DL (%) values of PUE and SCU in the optimal formulation were 56.60±3.73, 72.31±1.96 and 1.68±0.17, 2.44±1.14, respectively. The pharmacokinetic study in the aqueous humor showed that compared with the PUE and SCU solution, the area under the concentration–time curve (AUC) value of PUE was enhanced by 2.33-fold for PUE-SCU CLNs ( p <0.01), and the SCU AUC was enhanced by 2.32-fold ( p <0.01). In the molecular dynamics model, PUE and SCU passed through the POPC bilayer, with an obvious difference in the free energy well depth. It was found that the maximum free energy required for PUE and SCU transmembrane movement was ~15 and 88 kJ·mol −1 , respectively. These findings indicated that compared with SCU, PUE easily passed through the membrane. The diffusion coefficient for PUE and SCU were 4.1×10 −3 ±0.0027 and 1.0×10 −3 ±0.0006 e −5 cm 2 ·s −1 , respectively. Data from the molecular dynamics model were consistent with the experimental data. All data indicated that CLNs have a great potential for ocular administration and can be used as an ocular delivery system for multicomponent drugs. Moreover, the molecular dynamics model can also be used as a novel method for evaluating formulations.

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confidence: 97%

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Wang¹,

Zhao²,

Li³

et al. 2017

IJN

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“…In a literature search of journal articles in 2013 in which dissolution IVIVIC was performed, Wagner-Nelson was the most frequently applied method. Of the 27 articles identified in the search, 15 applied Wagner-Nelson (e.g., 13 – 15 ), while only 4 applied numerical deconvolution (e.g., 16 ). The remaining either applied a different method to obtain a level A IVIVC (e.g., a mechanistic model) or did not attempt a level A IVIVC at all.…”

Section: Discussionmentioning

confidence: 99%

Deconvolution and IVIVC: Exploring the Role of Rate-Limiting Conditions

Margolskee

Darwich

Galetin

et al. 2015

AAPS J

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In vitro-in vivo correlations (IVIVCs) play an important role in formulation development and drug approval. At the heart of IVIVC is deconvolution, the method of deriving an in vivo “dissolution profile” for comparison with in vitro dissolution data. IVIVCs are generally believed to be possible for highly permeable and highly soluble compounds with release/dissolution as the rate-limiting step. In this manuscript, we apply the traditional deconvolution methods, Wagner-Nelson and numerical deconvolution, to profiles simulated using a simplified small intestine absorption and transit model. Small intestinal transit, dissolution, and absorption rate constants are varied across a range of values approximately covering those observed in the literature. IVIVC plots and their corresponding correlation coefficients are analyzed for each combination of parameters to determine the applicability of the deconvolution methods under a range of rate-limiting conditions. For highly absorbed formulations, the correlation coefficients obtained during IVIVC are comparable for both methods and steadily decline with decreasing dissolution rate and increasing transit rate. The applicability of numerical deconvolution to IVIVC is not greatly affected by absorption rate, whereas the applicability of Wagner-Nelson falls when dissolution rate overcomes absorption rate and absorption becomes the rate-limiting step. The discrepancy between the expected and deconvolved input arises from the violation of a key assumption of deconvolution that the unknown input and unit impulse enter the system in the same location.

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“…PEOs with low Mw (100 kDa � Mw � 600 kDa) were usually used in the drug layers to obtain the zero-order release profiles [26]. It was reported that low Mw PEOs hydrated fast in the first 3-4 h and rarely absorbed water afterwards [27]. Therefore, these types of PEOs would imbibe water rapidly, and then formed the flowable drug suspensions in the drug layer.…”

Section: Plos Onementioning

confidence: 99%

“…As the weight gain of tablets decreased, the coating membranes would become thinner and resulted in weaker films. It should be noticed that, when the weight gain of tablet was too smaller, the pressure in the tablet might exceed the tensile strength of the membrane and cracked it during the period of drug release [27].…”

Section: Influence Of Weight Gain Of Tablet Corementioning

confidence: 99%

Preparation and evaluation of bilayer-core osmotic pump tablets contained topiramate

Lin

Shi

et al. 2022

PLoS ONE

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Topiramate (TPM) was an antiepileptic agent commonly used in clinical. Studies showed that an oral preparation of TPM with extended-release manner could bring some benefits for epileptics. In this paper, controlled release push-pull osmotic pump (PPOP) tablets of sparingly water-soluble TPM were successfully prepared. This bi-layer tablet core mainly consisted of sodium chloride as osmotic promoting agent and polyethylene oxide as suspending and pushing agents. The influences of osmotic agents, pushing agents and the compositions of coating membrane on TPM release profiles were evaluated. An optimal formulation of TPM-PPOP was obtained through single-factor experiments. In vitro release tests showed that the optimum formulation could release TPM at an approximate zero-order rate up to 8 h. Pharmacokinetic behaviors of TPM-PPOP tablets were evaluated and compared with the immediate release capsules after an oral single dose in beagle dogs. Pharmacokinetics results demonstrated that the TPM-PPOP tablet was able to provide a prolonged release of TPM with longer tmax and mean residence time. Lower fluctuations of drug plasma levels could also be achieved with TPM-PPOP tablets. These results suggested that sparely water-soluble drugs as TPM can be designed to PPOP for efficacy and safety use.

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A novel bi-layer ascending release osmotic pump tablet: In vitro investigation and in vivo investigation in pharmacokinetic study and IVIVC evaluation

Cited by 21 publications

References 15 publications

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Novel cationic lipid nanoparticles as an ophthalmic delivery system for multicomponent drugs: development, characterization, in vitro permeation, in vivo pharmacokinetic, and molecular dynamics studies

Deconvolution and IVIVC: Exploring the Role of Rate-Limiting Conditions

Preparation and evaluation of bilayer-core osmotic pump tablets contained topiramate

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