Influence of Food on the Bioavailability of an Enteric-Coated Tablet Formulation of Omeprazole 20 mg Under Repeated Dose Conditions

The objective of this study was to investigate the influence of food on the bioavailability of omeprazole (20 mg) given as an enteric-coated tablet under repeated dose conditions. This open randomized crossover study consisted of three seven-day treatment periods, each separated by a drug-free period. During each treatment period an enteric-coated tablet of omeprazole was taken once daily either under fasting conditions, or immediately before or after a standardized breakfast. On the last day of each treatment period, blood samples for the determination of plasma omeprazole concentrations were collected at baseline and at predetermined intervals over the 24 h period following drug administration. Fifty-seven male and female subjects, aged 18 to 52 years, completed the study according to the protocol. No statistically significant differences were found when comparing either the before breakfast or after breakfast treatment regimens with the fasting regimen for the estimated mean area under the plasma concentration-time curve (AUC). The maximum plasma concentration was not found to differ significantly among any of the treatment regimens. However, the lower limit of the CI for the comparison of fasting/before breakfast was not contained within the limits of bioequivalence. The time to reach maximum plasma concentration was significantly different when fasting and after breakfast regimens were compared. Thus, under repeated dose conditions, food has no influence on the bioavailability (expressed as AUC) of omeprazole given as the enteric-coated tablet formulation.

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Pharmacokinetics and Pharmacodynamics during Treatment with the Omeprazole 20 mg Enteric-Coated Tablet and 20 mg Capsule in Asymptomatic Duodenal Ulcer Patients

Canadian Journal of Gastroenterology ◽

10.1155/1997/910471 ◽

1997 ◽

Vol 11 (8) ◽

pp. 657-660 ◽

Cited By ~ 7

Author(s):

ABR Thomson ◽

P Kirdeikis ◽

R Lastiwka ◽

K Rohss ◽

P Sinclair ◽

...

Keyword(s):

Duodenal Ulcer ◽

Plasma Concentration ◽

Plasma Concentrations ◽

Maximum Plasma ◽

Intragastric Ph ◽

Time Curve ◽

Enteric Coated Tablet ◽

Coated Tablet ◽

Enteric Coated ◽

Repeated Dosing

This study compared the 24 h intragastric pH profile and bioavailability at repeated dosing conditions of the omeprazole 20 mg enteric-coated tablet versus the 20 mg capsule. Forty duodenal ulcer patients in asymptomatic remission completed this randomized open two-way crossover study. Omeprazole 20 mg tablets or capsules were administered for seven days in each period. A 24 h pH recording was performed before the start of treatment and on day 7 of each treatment period. Plasma concentrations of omeprazole were determined 24 h after the dose. The treatment periods were separated by two to four weeks. The difference in percentage of time with pH of at least 3 was less than 16% in favour of the tablet (not significant). The estimated mean area under the plasma concentration-time curve as well as the maximum plasma concentration (Cmax) for omeprazole were 18% and 41% higher, respectively, for the tablet versus the capsule, with the latter percentage being statistically significant. The time to reach Cmax(tmax) with the tablet was, on average, about 0.5 h longer than to reach the tmaxof the capsule. This study indicates that the enteric-coated tablet formulation of omeprazole is biodynamically equivalent to the capsule regarding their effects on intragastric pH during repeated dosing.

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Granulation by Roller Compaction and Enteric Coated Tablet Formulation of the Extract of the Seeds of Glinus Lotoides Loaded on Aeroperl® 300 Pharma

AAPS PharmSciTech ◽

10.1208/s12249-007-9027-3 ◽

2008 ◽

Vol 9 (1) ◽

pp. 31-38 ◽

Cited By ~ 11

Author(s):

Abebe Endale ◽

Tsige Gebre-Mariam ◽

Peter C. Schmidt

Keyword(s):

Tablet Formulation ◽

Roller Compaction ◽

Enteric Coated Tablet ◽

Coated Tablet ◽

Enteric Coated

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Formulation and In-Vitro Evaluation of Enteric Coated Tablet Incorporating Rabeprazole

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i2-s.3953 ◽

2020 ◽

Vol 10 (2-s) ◽

pp. 50-57

Author(s):

Gautam D. Mehetre ◽

Rameshwar S. Cheke ◽

Vinayak N. Shrikhande

Keyword(s):

Drug Release ◽

Acid Resistance ◽

Tablet Formulation ◽

In Vitro Dissolution ◽

Content Uniformity ◽

In Vitro Evaluation ◽

Enteric Coated Tablet ◽

Coated Tablet ◽

Enteric Coated

The objective of the work is to try and assess the applicability and manufacturing possibilities to optimize an enteric coated tablet formulation containing Rabeprazole sodium as the drug aiming at the anti-acidity activity with desired drug release properties. Enteric coated tablet was chosen as dosage form being a cost-effective technology for pharmaceutical industry requiring fewer procedures. Before the implementation of the pharmaceutical technological aims, analysis of critical factors influencing the manufacture was carried out. Reproducible manufacturing processes are required to achieve suitability and tablets uniformity to achieve the uniform properties of tablets, which could influence experimental parameters. Rabeprazole in core content of tablet is blended with HPMC (different grades), xanthan gum, PVPK30, mannitol, crosspovidone, Sodium starch glycolate, Colloidal silicon dioxide to formulate the product. Prepared formulation was tested for weight and content uniformity, physical characteristics, in vitro dissolution behaviour, acid resistance and accelerated stability studies. All studies performed resulted and revealed for assurance of such enteric coated tablet formulation for drug Rabeprazole with optimum characteristics, concluding it as a promising approach to enhance drug release characteristics. Keywords: Rabeprazole, HPMC, enteric coated tablets, In Vitro evaluation.

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Determination of Eudragit® L100 in an Enteric-Coated Tablet Formulation Using Size-Exclusion Chromatography with Charged-Aerosol Detection

Scientia Pharmaceutica ◽

10.3390/scipharm86030038 ◽

2018 ◽

Vol 86 (3) ◽

pp. 38 ◽

Cited By ~ 1

Author(s):

Marsella Widjaja ◽

Jefri Gan ◽

Joseph Talpaneni ◽

Raymond Tjandrawinata

Keyword(s):

Coating Layer ◽

Tablet Formulation ◽

Drug Formulation ◽

Size Exclusion ◽

Charged Aerosol ◽

Enteric Coated Tablet ◽

Coated Tablet ◽

Exclusion Chromatography ◽

Enteric Coated

Eudragit® L100 is a commonly used polymer in a coating layer of modified-release drug formulation to prevent drug release in the stomach. The amount of Eudragit® L100 in the formula determines the dissolution profile of drug at its release medium. Hence, its quantification in reference product will facilitate the formulation of a bioequivalent drug product. Some analytical methods including size-exclusion chromatography (SEC) have been reported for characterization of Eudragit® L100 either as single component or its conjugate with the enzyme, but none for its quantification in drug formulation. In this work, an SEC method with charged-aerosol detection (CAD) was developed for determination of Eudragit® L100 in an enteric-coated tablet formulation using Waters Ultrahydrogel 1000 and Waters Ultrahydrogel 120 columns in series. The mobile phase was a mixture of 90:10 (v/v) 44.75 mM aqueous ammonium acetate buffer, pH 6.6 and acetonitrile pumped at a constant flow rate of 0.8 mL/min in isocratic mode. The method was validated for specificity, working range, limit of detection (LOD), limit of quantification (LOQ), accuracy and precision. The method was shown to be specific for Eudragit® L100 against the diluent (mobile phase) and placebo of a coating layer for the tablet. A good correlation coefficient (r = 0.9997) of CAD response against Eudragit® L100 concentration from 0.1–1.0 mg/mL was obtained using polynomial regression. LOD and LOQ concentrations were 0.0015 and 0.0040 mg/mL, respectively. The mean recovery of Eudragit® L100 was in the range of 88.0–91.1% at three levels of working concentration: 50%, 100% and 150%. Six replicated preparations of samples showed good precision of the peak area with % relative standard deviation (RSD) 2.7. In conclusion, the method was suitable for quantification of Eudragit® L100 in an enteric-coated tablet formulation.

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