In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet

Nagarwal, Ramesh C.; Ridhurkar, Devendra N.; Pandit, J. K.

doi:10.1208/s12249-010-9380-5

Cited by 58 publications

(30 citation statements)

References 27 publications

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“…Rabbits fasted for 24 h before the experiment and were divided into two groups, each having six animals. The selection of rabbits as animal model for the present study was based on previously published pharmacokinetic studies (31)(32)(33). The first group received orally the 10-mg reference tablets (Zyprexa® by Eli Lilly) and the second group received orally 10-mg CR test tablets of olanzapine.…”

Section: In Vivo Evaluationmentioning

confidence: 99%

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability

2010

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Abstract. Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel® K100 LV-CR and Ethocel® standard 7FP premium by the dry granulation slugging method. Drug release kinetics of CR tablet formulations F1, F2, and F3, each one suitably compressed for 9-, 12-, and 15-kg hardness, were determined in a dissolution media of 0.1 N HCl (pH 1.5) and phosphate buffer (pH 6.8) using type II dissolution apparatus with paddles run at 50 rpm. Ethocel® was found to be distinctly controlling drug release, whereas the hardness of tablets and pH of the dissolution media did not significantly affect release kinetics. The CR test tablets containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness exhibited pH-independent zero-order release kinetics for 24 h. In vivo performance of the CR test tablet and conventional reference tablet were determined in rabbit serum using high-performance liquid chromatography coupled with electrochemical detector. Bioavailability parameters including C max , T max , and AUC 0-48 h of both tablets were compared. The CR test tablets produced optimized C max and extended T max (P<0.05). A good correlation of drug absorption in vivo and drug release in vitro (R 2 =0.9082) was observed. Relative bioavailability of the test tablet was calculated as 94%. The manufacturing process employed was reproducible and the CR test tablets were stable for 6 months at 40±2°C/75±5% relative humidity. It was concluded that the CR test tablet formulation successfully developed may improve tolerability and patient adherence by reducing adverse effects.

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Section: In Vivo Evaluationmentioning

confidence: 99%

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability

2010

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“…Rabbits fasted for 24 h before trial and were divided into two groups, each one having six animals. Selection of rabbits as the animal model for the present study was based on some successfully conducted previously published pharmacokinetic studies (22,29,30). The first group received 4-mg reference conventional tablets and the second group received 4 mg controlled-release (CR) test tablets of risperidone.…”

Section: In Vivo Evaluationsmentioning

confidence: 99%

“…Hydroxypropyl methylcellulose (HPMC, hydrophilic) has been a popular release-retarding polymer in simple matrix tablets (19,20) and floating gastro-retentive tablets (21,22). Fine particle ethyl cellulose (FPEC) was successfully used in the formulation of extended-release tablets of some non-ionizable drugs (23).…”

Section: Introductionmentioning

confidence: 99%

Development of Controlled-Release Matrix Tablet of Risperidone: Influence of Methocel®- and Ethocel®-Based Novel Polymeric Blend on In Vitro Drug Release and Bioavailability

et al. 2011

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Abstract. Controlled-release (CR) matrix tablet of 4 mg risperidone was developed using flow bound dry granulation-slugging method to improve its safety profile and compliance. Model formulations F1, F2, and F3, consisting of distinct blends of Methocel® K100 LV-CR and Ethocel® standard 7FP premium, were slugged. Each batch of granules (250-1,000 μm), obtained by crushing the slugs, was divided into three portions after lubrication and then compressed to 9-, 12-, and 15-kg hard tablets. In vitro drug release studies were carried out in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8) using a paddle dissolution apparatus run at 50 rpm. The CR test tablet, containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness, exhibited pH-independent zero-order release kinetics for 24 h. The drug release rate was inversely proportional to the content of Ethocel®, while the gel layer formed of Methocel® helped in maintaining the integrity of the matrix. Changes in the hardness of tablet did not affect the release kinetics. The tablets were reproducible and stable for 6 months at 40±2°C/75±5% relative humidity. Risperidone and its active metabolite, 9-hydroxyrisperidone, present in the pooled rabbit's serum, were analyzed with HPLC-UV at λ max 280 nm. The CR test tablet exhibited bioequivalence to reference conventional tablet in addition to the significantly (p<0.05) optimized peak concentration, C max , and extended peak time, T max , of the active moiety. There was a good association between drug absorption in vivo and drug release in vitro (R 2 =0.7293). The successfully developed CR test tablet may be used for better therapeutic outcomes of risperidone.

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“…The time for which the tablet remained floating on the surface of medium was determined as floating time. [25][26] …”

Section: Floating Timementioning

confidence: 99%

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2016

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In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet

Cited by 58 publications

References 27 publications

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability

Development of Controlled-Release Matrix Tablet of Risperidone: Influence of Methocel®- and Ethocel®-Based Novel Polymeric Blend on In Vitro Drug Release and Bioavailability

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