<i>In vivo</i> performance evaluation and establishment of IVIVC for osmotic pump based extended release formulation of milnacipran HCl

Laxman, et al.: IVIVC of Topiramate Extended Release Capsule The purpose of this study was to build an in vitro-in vivo correlation model for topiramate extended release capsules. Three formulations with different release rates were developed by varying the percent content of the rate controlling polymer ethyl cellulose and pore former hypromellose. In vitro dissolution of all formulations was performed by United States Pharmacopeia type I apparatus using multimedia dissolution conditions such as 0.1 N hydrochloric acid pH 1.2 for initial 2 h followed by phosphate buffer pH 6.8 for the rest of 22 h. Total dissolution time was up to 24 h. In vivo pharmacokinetic profile of the immediate release suspension and different extended release formulations were investigated in a rabbit model after single oral administration of topiramate at a dose of 10.33 mg/kg. An in vitro-in vivo correlation model was established by using two-stage numerical deconvolution approaches. Unit impulse response was obtained from pharmacokinetic profile of immediate release suspension which was used as a reference formulation. A linear correlation model with a time scaling factor was found to be useful to build level A correlation. The developed in vitro-in vivo correlation model was validated as per Food and Drug Administration guideline and the % prediction error for maximum concentration observed (C max) and area under the concentration time curve was within acceptable limits of below 15%. The utility of the developed model was evaluated by testing the targeted formulations. The observed % prediction error was 2.61 and-0.43 for C max and area under the concentration time curve, respectively suggesting the usefulness of the present in vitro-in vivo correlation model.

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“…Levy plot of Fdiss vs. Fabs gives preliminary information about which correlation model should be considered for IVIVC [19,20] . Levy plot ( fig.…”

Section: Resultsmentioning

confidence: 99%

Development and Validation of an In Vitro and In Vivo Correlation Model in NZ Rabbit for Topiramate Extended Release Capsules

Laxman¹,

Durgaprasad²,

Tirgar³

et al. 2016

pharmaceutical-sciences

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“…A high value of correlation coefficient (0.995) substantiates the fact. 28 During the preparation of microspheres some amount of drug always remains on the surface of the microspheres. The authors hypothesize that this drug gets in equilibrium with the gel so when this gel is spread as a thin film for the ex vivo studies it becomes immediately available for permeation.…”

Section: Characeterization Of Pp Loaded Microspheres Containing Gel Ementioning

confidence: 99%

Development and Characterization of Thermosensitive intranasal Gel Containing Paliperidone Loaded Microspheres

Maniyar¹,

Patel²,

Shelat³

et al. 2016

JYP

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Purpose: The objective of the present investigation was to fabricate a thermosensitive gel containing paliperidone loaded microspheres for the treatment of schizophrenia for brain delivery through nasal route. Incorporation of drug in to microspheres and then in to gel should increase the duration of release and nasal duration time respectively. Material and Method: Ethyl cellulose microspheres containing paliperidone palmitate were prepared by emulsification of ethyl acetate dispersion containing polymer and drug with aqueous external phase containing polysorbate 80. Amount of ethyl cellulose and polysorbate 80 were identified as critical formulation variables influencing the drug release at critical time points, percentage yield and particle size. These factors were studied using 2 factors and 3 level face centered factorial design using Design Expert ® . Drug-excipient compatibility was ascertained using FTIR analysis. The paliperidone microspheres were then incorporated in to Pluronic F127 and HPMC gel having required thermo sensitive and muco adhesive properties. Gel containing microspheres was subjected to Ex vivo permeation study, irritation study using sheep nasal mucosa and pharmacodynamic study (spontaneous motor activity in mice). Results: Microspheres that could sustain the drug release up to 8 hours were developed. Thermoreversible gel having required thermo sensitive and muco adhesive properties was developed. The Ex vivo permeation study and pharm a codynamic study of the drug loaded microsphere containing gel confirmed the release up to 8 hours. The histopathology study showed absence of irritation on sheep nasal mucosa. Conclusion: Paliperidone palmitate loaded microspheres containing gel could prolong and target the drug release to brain and therefore give prolonged and intense action.

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“…These tests can effectively evaluate in vivo behavior and reduce the number of clinical trials needed to investigate efficacy of a new drug (16)(17)(18). The correlations between the in vitro dissolution data and the in vivo absorption data are categorized as levels A, B, and C according to the FDA (19).…”

Section: Introductionmentioning

confidence: 99%

Development of a Dissolution Test for Extended-Release Bromopride Pellets with In Vivo–In Vitro Correlation

Giovani¹,

Silva²,

Volpato³

et al. 2015

Dissolution Technol.

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The aim of this study was the development of a dissolution test with IVIVC for extended-release bromopride (BPD) pellets using bioavailability data. BPD is a Biopharmaceutics Classification System Class 2 drug, and its absorption is primarily limited by its dissolution rate. Despite this, there are no reports describing a dissolution test for BPD dosage forms. The dissolution medium was selected based upon the sink condition and the gastrointestinal pH. Furthermore, USP Apparatus 1 and 3 were tested, and the dissolution method was compared with that outlined by the manufacturer of the reference drug. Deconvolution by the Wagner-Nelson method was used to obtain the fraction of drug absorbed. The dissolution test that yielded IVIVC for both the fasted and fed states (R 2 > 0.97) and also the discriminative power used Apparatus 1 at 75 rpm in 900 mL of HCl. The dissolution medium (900 mL PBS pH 7.2) was changed after 1 h. Additionally, quantitative analysis was successfully validated by UV absorption (273 nm). Drug release is controlled by the pellet coating and by BPD solubility. The Higuchi release kinetics model best describes the dissolution of commercial BPD pellets batches.

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In vivo performance evaluation and establishment of IVIVC for osmotic pump based extended release formulation of milnacipran HCl

Cited by 6 publications

References 23 publications

Development and Validation of an In Vitro and In Vivo Correlation Model in NZ Rabbit for Topiramate Extended Release Capsules

Development and Validation of an In Vitro and In Vivo Correlation Model in NZ Rabbit for Topiramate Extended Release Capsules

Development and Characterization of Thermosensitive intranasal Gel Containing Paliperidone Loaded Microspheres

Development of a Dissolution Test for Extended-Release Bromopride Pellets with In Vivo–In Vitro Correlation

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