Assessment of the pharmaceutical quality of marketed enteric coated pantoprazole sodium sesquihydrate products

Abstract

Pantoprazole sodium sesquihydrate (PSS) is a proton pump inhibitor, used in acid-related disorders, like peptic ulcer and gastroesophageal reflux. Increasing the number of pantoprazole containing products in the market, raises questions of its efficacy and generic substitution. The pharmaceutical quality of 6 generic PSS enteric coated tablets in 2 local markets was assessed relative to the innovator product (pantozol®). Uniformity of dosage unit, disintegration and in vitro drug release were determined using United States pharmacopeia for delayed release tablets. The similarity factor (f2) was assessed using the FDA recommended approach (f2 similarity factor). The content uniformity of the innovator product was 98.39% of the labeled claim with RSD value of 1.08%, while the content of generic products ranged from 96.98% to 98.80% with RSD values of 1.24-2.19%. All the products showed no disintegration, cracks or swelling in 0.1 N HCl, except product 1, which showed complete disintegration after 20 min. However, the disintegration of all the products in phosphate buffer met USP requirements. Dissolution of tablets in 0.1 N HCl showed no drug release after 2 h except product 1 in which one tablet showed a drug release more than 10% at acid stage level A1. In addition, three tablets of this product showed dissolution of 45%, 48% and 69% at acid stage level A2. The similarity factor f2 of the products was between 71 and 74 indicating the similarity in dissolution profiles of all the products in accordance to FDA requirements, except product 1 in which f2 value was 18.67.

Investigation of the Impact of Cellulose Acetate Coating on the Release Pattern of Freely Soluble Drug: Metoprolol Succinate

“…The leaching of PVP from the membrane leads to formation of pores, and thus the release of drug takes place. In a previous study with sorbitol as pore-former, the pore size in the CA coating membrane after dissolution was reported as 1 -15 µ, which is significantly higher than that of formulation developed in this study 4 . The lower pore-size occurred with PVP in current formulation due to the fact that PVP polymer due to its longer chain length intrigued into the cellulose polymer coating.…”

“…Dissolution parameters include, USP apparatus II, 500 mL of pH 6.8 phosphate buffer, paddle speed 50 RPM, medium temperature 37 ± 0.5°C. 10 mL of samples were removed from the dissolution apparatus (Disso 2000, Lab India, Thane, India) at regular time intervals up to 24 h (1,2,4,8,12,16,20, and 24 h) and replaced with the same volume of fresh dissolution medium. Samples were filtered through 0.45 µm membrane filter and analyzed by UV-Visible spectrophotometer (Cary C50, Varian Inc., Palo Alto, CA, USA) at 223 nm to determine the cumulative percent drug release.…”

“…In order the drug permeable, water-soluble materials/particles as a pore-former are usually added to CA coating layers. After administration of the dosage form, the pore-former dissolves in situ and forms pores or channels in the coating, making the polymer coating micro-porous, and inducing drug release [2][3][4][5][6] . Among various pore-formers studied so far, water-soluble hydrophilic polymers like hydroxyl propyl methyl cellulose and PVP are most commonly used due to their desirable compatibilities with polymeric coat materials 7,8 .…”

Post-marketing Assessment of Esomeprazole and Lansoprazole Enteric Coated Products Available in Saudi Arabia Based on Quality Control

“…The growing number of proton pump inhibitors containing marketed pharmaceutical products increases the questions about the enteric coating efficiency of generic substitution. In our previous work [18]. The pharmaceutical quality control of 6 generic pantoprazole (PPIs) enteric coated tablets in 2 local markets was assessed relative to the innovator product.…”

Formulation, Optimization, Characterization and in Vivo Anti-Ulcer Activity of Esomeprazole Magnesium Trihydrate Gastroresistant Microspheres

“…As per<711>USP for delayed release dosage forms, not more than 10% of the drug should be released in acidic media after 120 min. Hence, it was proved that the prepared microspheres were gastroresistant [37,38]. It was concluded that the developed microspheres would prevent drug release in the acidic medium of the stomach so that intestinal absorption of the drug would be improved, leading to increased bioavailability.…”