Kinetic Analysis of Blood Levels and Urinary Excretion in the Absorptive Phase after Single Doses of Drug

Wagner, John G.; Nelson, Eino

doi:10.1002/jps.2600531126

Cited by 375 publications

(126 citation statements)

References 5 publications

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“…The percent drug absorbed was calculated with the Wagner and Nelson method (34) followed by in vitro-in vivo correlation (R 2 ) determination, which turned out to be 0.7293 for the test tablet (see Fig. 5).…”

Section: Discussionmentioning

confidence: 99%

“…Percent relative bioavailability of the test tablet was calculated with the following equation (33) Percent risperidone absorbed (P a ) was plotted against percent risperidone released to determine in vivo-in vitro correlation. Percent risperidone absorbed was determined by the Wagner-Nelson method (34), while percent risperidone released values were taken from the in vitro drug release data.…”

Section: In Vivo Evaluationsmentioning

confidence: 99%

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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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Section: Discussionmentioning

confidence: 99%

Section: In Vivo Evaluationsmentioning

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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“…Standard known methods. [14], [15] were used for the estimation of various pharmacokinetic parameters.…”

Section: Estimation Of Pharmacokinetic Parametersmentioning

confidence: 99%

Preclinical Pharmacokinetic Evaluation of Valsartan Floating Tablets Formualted Using Cross Linked Starch Urea - A New Modified Starch

Chowdary¹

2017

WJPPS

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The objective of the present study is optimization of valsartan floating tablet formulation by 2 3 factorial design and to evaluate the optimized valsartan floating tablets for in vitro drug release, preclinical pharmacokinetics and also for in vitro -in vivo correlation (IVIVC).Valsartan is an orally active anti-hypertensive drug, majorly absorbed from stomach and upper small intestine. Formulation of sustained release floating tablets of valsartan is needed because of its poor oral bioavailability and short biological half-life. Valsartan floating tablets were formulated as per 2 3 factorial design and were evaluated.Valsartan floating tablets prepared as per 2 3 factorial design were nondisintegrating in water and aqueous acidic (pH 1.2) and alkaline (pH7.4) fluids and were of good quality with regard to drug content, hardness, friability and suitable for controlled

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“…The in vitro release profiles of labelled Oros dosage forms were determined prior to the study using a flow cell dissolution method [DISSOTEST dissolution apparatus (volume unlimited) Since the time-course of plasma CBZ concentrations after i.v. administration can be adequately described by a mono-exponential function, drug release from the Oros was estimated by the Wagner-Nelson method (Wagner & Nelson, 1964 …”

Section: Labelling Of the Oros And Scintigraphic Proceduresmentioning

confidence: 99%

Relationship between systemic drug absorption and gastrointestinal transit after the simultaneous oral administration of carbamazepine as a controlled‐release system and as a suspension of 15N‐labelled drug to healthy volunteers.

Wilding

Davis

Hardy

et al. 1991

Brit J Clinical Pharma

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1. Plasma drug concentrations after a single oral administration of a suspension of carbamazepine (CBZ) and a 20/200 CBZ Oros osmotic pump system were measured in eight healthy male volunteers. The oral suspension contained 100 mg CBZ labelled with the stable isotope nitrogen‐15, whilst the Oros contained 200 mg unlabelled CBZ. Plasma concentrations of [15N]‐CBZ and CBZ were measured simultaneously by gas chromatography‐mass spectrometry. 2. The position of the CBZ Oros (labelled with indium‐111) in the gastrointestinal tract was followed by gamma scintigraphy. Plasma drug concentrations after the two treatments were used to relate pharmacokinetic with transit data. 3. The Oros was taken after breakfast and gastric emptying occurred between 1.1‐ greater than h post‐dosing (median, 5.3 h). Small intestinal transit times ranged from 1.5‐ greater than 3.6 h, with a median of 2.2 h. There were wide individual variations in colonic transit, and the total transit time ranged from 10‐60 h (median, 22 h). 4. Relative systemic bioavailability of CBZ from the Oros was reduced compared with that from the suspension (mean dose normalised AUC ratio = 0.69 +/‐ 0.17; mean dose‐normalised AUC ratio = 0.85 +/‐ 0.13, allowing for actual release from the Oros system). 5. The in vivo absorption of drug into the systemic circulation from the Oros was estimated using the Wagner‐Nelson method. This showed that absorption of CBZ was rapid when the Oros was present in the stomach and small intestine, the rate being determined by the release of drug from the system.(ABSTRACT TRUNCATED AT 250 WORDS)

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Kinetic Analysis of Blood Levels and Urinary Excretion in the Absorptive Phase after Single Doses of Drug

Cited by 375 publications

References 5 publications

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

Preclinical Pharmacokinetic Evaluation of Valsartan Floating Tablets Formualted Using Cross Linked Starch Urea - A New Modified Starch

Relationship between systemic drug absorption and gastrointestinal transit after the simultaneous oral administration of carbamazepine as a controlled‐release system and as a suspension of 15N‐labelled drug to healthy volunteers.

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