pH-dependent, enteric acrylic, and cellulosic polymers were used either alone, in combination, or applied one over the other to impart delayed-release properties to the core drug pellets. plasticizer, wherein the said polymer possesses only enteric house and dissolves at pH 5.5. C Eudragit L30D55 and Eudragit NE30D (in ratio 90: 10) made up of triethyl citrate (20% w/w of dry polymer) as the plasticizer, wherein the former polymer, i.e., Eudragit L30D55 is the enteric polymer while Eudragit NE30D is usually pH-independent sustained-release polymer. In totality, the applied covering composition dissolves at pH 6.0. C Hypromellose phthalate HP55 alone with dibutyl sebacate (20% w/w of polymer) as the plasticizer, wherein the said polymer possesses only enteric house and dissolves at pH 5.5. C WYE-687 Eudragit L30D55 made up of triethyl citrate as the plasticizer (applied to a level of 15% w/w of seal-coated pellets) as the first enteric covering, followed by a second enteric covering of hypromellose phthalate HP55 made up of dibutyl sebacate as the plasticizer (applied to a level of 10% w/w of seal-coated pellets). The producing enteric-coated drug pellets dissolve at pH 5.5. The various enteric compositions utilized for preparing the four prototype drug pellets can be expressed in simple terms as given in Table 6. The actions involved in the preparation of all the four prototype enteric-coated drug pellets are enlisted below: Preparation of enteric-coating composition-the actions involved were: (a) Dissolution Studies on Delayed-Release Rabeprazole Sodium Pellets Dissolution in acid stage is done to determine acid resistance of formulations, an essential criterion which must be fulfilled by delayed-release drug products. Subsequent to test for acid resistance, the formulations are exposed to buffer media to assess the rapidity of drug dissolution in alkaline buffer, a feature that too is essential for all those enteric-coated formulations. Dissolution assessments were performed in accordance with pharmacopoeial method and using USP dissolution apparatus 2 (paddle). The selected dissolution conditions were in accordance with the US Food and Drug Administration CDERdissolution methods for drug products, and indicated for rabeprazole sodium delayed-release tablets. Dissolution test conditions as recommended by the US FDA are given in WYE-687 Table 8. Table 8 dissolution conditions for delayed-release rabeprazole sodium pellets as per USFDA-CDER Open in a separate window Pellets equivalent to 20 mg rabeprazole sodium (253 mg pellets) were subjected to dissolution screening. The dissolution test comprised of following two stages as per US FDA guidance: Drug Dissolution Studies on Delayed-release Rabeprazole Sodium Pellets Results of acid resistance of enteric-coated pellets are offered in Table 11. Table 11 Amount of rabeprazole sodium released from enteric-coated pellets in acid stage in 2 hours Open in a separate windows Dissolution profile of the product in buffer stage is usually presented in Table 12. Graphical representation of drug release at alkaline stage is usually depicted in Physique 3 (enteric-coated pellets). Table 12 Amount of rabeprazole sodium dissolved at numerous sampling time intervals from enteric-coated pellets after dissolution in buffer stage Open in a separate window Open in a separate window Physique 3 Comparative dissolution profile of rabeprazole sodium in buffer from numerous enteric-coated pellet formulations A direct influence of polymer type, composition, and manner WYE-687 of covering on the drug release properties of delayed-release rabeprazole sodium pellets was observed. All the tested enteric-coated formulationsA through D, exhibited comparable delayed-release properties owing to presence of solid polymeric covering on the surface of drug pellet. Dissolution of drug in simulated intestinal fluid for all those formulations was demonstrated to be dependent upon the following: Type of enteric-coating polymer Composition of enteric covering Number of covering polymer(s), and Manner of deposition of enteric covering. Application of acrylic enteric covering (Eudragit L30D555) that contained additional sustained-release polymer (Eudragit NE30D) resulted in a product (formulation B) that exhibited slowest drug release in buffer stage. The relative retarding effect on dissolution in buffer stage could be attributed to presence of sustained-release polymer that prevents the polymer from dissolving fast enough in the alkaline pH. This was followed by formulation A which was coated with a lone enteric acrylic polymer Eudragit L30D55. This was obvious since such a lone enteric polymer has good and quick solubility in alkaline pH compared with when it is mixed with a Rabbit Polyclonal to Catenin-alpha1 sustained-release polymer like Eudragit NE30D. In comparison with formulations A and B,.35C48. in more effectively producing a better rabeprazole sodium delayed-release pellet product. The pH-dependent, enteric acrylic, and cellulosic polymers were WYE-687 used either alone, in combination, or applied one over the other to impart delayed-release properties to the core drug pellets. It was exhibited that dual delayed-release covering with two different enteric polymersan inner acrylic covering followed by an outer cellulosic coatingyields the best product that provides all the desired physicochemical and drug dissolution characteristics. C Eudragit L30D55 alone with triethyl citrate (20% w/w of dry polymer) as plasticizer, wherein the said polymer possesses only enteric house and dissolves at pH 5.5. C Eudragit L30D55 and Eudragit NE30D (in ratio 90: 10) made up of triethyl citrate (20% w/w of dry polymer) as the plasticizer, wherein the former polymer, i.e., Eudragit L30D55 is the enteric polymer while Eudragit NE30D is usually pH-independent sustained-release polymer. In totality, the applied covering composition dissolves at pH 6.0. C Hypromellose phthalate HP55 alone with dibutyl sebacate (20% w/w of polymer) as the plasticizer, wherein the said polymer possesses only enteric house and dissolves at pH 5.5. C Eudragit L30D55 made up of triethyl citrate as the plasticizer (applied to a level of 15% w/w of seal-coated pellets) as the first enteric covering, followed by a second enteric covering of hypromellose phthalate HP55 made up of dibutyl sebacate as the plasticizer (applied to a level of 10% w/w of seal-coated pellets). The producing enteric-coated drug pellets dissolve at pH 5.5. The various enteric compositions utilized for preparing the four prototype drug pellets can be expressed in simple terms as given in Table 6. The actions involved in the preparation of all the four prototype enteric-coated drug pellets are enlisted below: Preparation of enteric-coating composition-the actions involved were: (a) Dissolution Studies on Delayed-Release Rabeprazole Sodium Pellets Dissolution in acid stage is done to determine acid resistance of formulations, an essential criterion which must be fulfilled by delayed-release drug products. Subsequent to test for acid resistance, the formulations are exposed to buffer media to assess the rapidity of drug dissolution in alkaline buffer, a feature that too is essential for all those enteric-coated formulations. Dissolution assessments were performed in accordance with pharmacopoeial method and using USP dissolution apparatus 2 (paddle). The selected dissolution conditions were in accordance with the US Food and Drug Administration CDERdissolution methods for drug products, and indicated for rabeprazole sodium delayed-release tablets. Dissolution test conditions as recommended by the US FDA are given in Table 8. Table 8 dissolution conditions for delayed-release rabeprazole sodium pellets as per USFDA-CDER Open in a separate window Pellets equivalent to 20 mg rabeprazole sodium (253 mg pellets) were subjected to dissolution screening. The dissolution test comprised of following two stages as per US FDA guidance: Drug Dissolution Studies on Delayed-release Rabeprazole Sodium Pellets Results of acid resistance of enteric-coated pellets are offered in Table 11. Table 11 Amount of rabeprazole sodium released from enteric-coated pellets in acid stage in 2 hours Open in another home window Dissolution profile of the merchandise in buffer stage can be presented in Desk 12. Graphical representation of medication launch at alkaline stage can be depicted in Shape 3 (enteric-coated pellets). Desk 12 Quantity of rabeprazole sodium dissolved at different sampling period intervals from enteric-coated pellets after dissolution in buffer stage Open up in another window Open up in another window Shape 3 Comparative dissolution profile of rabeprazole sodium in buffer from different enteric-coated pellet formulations A primary impact of polymer type, structure, and types of layer on the medication launch properties of delayed-release rabeprazole sodium pellets was noticed. All the examined enteric-coated formulationsA through D, proven similar delayed-release properties due to existence of heavy polymeric layer on the top of medication pellet. Dissolution of medication in simulated intestinal liquid for many formulations was proven to.