Colonic metabolism of ranitidine: implications for its delivery and absorption

Basit, Abdul W.; Lacey, Larry F.

doi:10.1016/s0378-5173(01)00794-3

Cited by 94 publications

(58 citation statements)

References 12 publications

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“…This method has the advantage of capturing a greater diversity of organisms and has been successfully applied to identify numerous drugs that are susceptible to microbial metabolism (Valerino et al, 1972;Caldwell and Hawksworth, 1973;Smith and Griffiths, 1974;Powis et al, 1979;Koch and Goldman, 1979;Koch et al, 1980;Lindenbaum et al, 1981;Elmer and Remmel, 1984;Harris et al, 1986;Strong et al, 1987;Shu et al, 1991;DH Kim et al, 1992;Lavrijsen et al, 1995;Watanabe et al, 1995;Kitamura et al, 1997;Sasaki et al, 1997;Basit and Lacey, 2001;Basit et al, 2002;Deng et al, 2011;Li et al, 2012;McCabe et al, 2015). However, when testing a community of microorganisms collectively, inter-strain antagonism may mask This article has not been copyedited and formatted.…”

Section: Mastering Microbial Metabolismmentioning

confidence: 99%

How to Determine the Role of the Microbiome in Drug Disposition

et al. 2018

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With a paradigm shift occurring in health care towards personalized and precision medicine, understanding the numerous environmental factors that impact drug disposition is of paramount importance. The highly diverse and variant nature of the human microbiome is now recognized as a factor driving inter-individual variation in therapeutic outcomes. The purpose of this review is to provide a practical guide on methodology that can be applied to study the effects of microbes on the absorption, distribution, metabolism, and excretion of drugs. We also highlight recent examples of how these methods have been successfully applied to help build the basis for researching the intersection of microbiome and pharmacology. While in vitro and in vivo preclinical models are highlighted, these methods are also relevant in late-phase drug development or even as a part of routine after-market surveillance. These approaches will aid in filling major knowledge gaps for both current and upcoming therapeutics with the long-term goal of achieving a new type of knowledge-based medicine that integrates data on the host and the microbiome.

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Section: Mastering Microbial Metabolismmentioning

confidence: 99%

How to Determine the Role of the Microbiome in Drug Disposition

et al. 2018

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“…Ranitidine hydrochloride (RHCL) is an anti-ulcer drug that has been extensively used as model drug in prophylaxis and treatment of gastric ulcer, duodenal ulceration, stomach ulcer, gastritis, gastroesophageal reflux, Zollinger-Ellison syndrome and elevated stomach hypersecretion in endocrine multiple adenoma [4][5][6][7][8]. It is a H2 receptor antagonist which competitively inhibits gastric acid secretion with interaction of histamine with its receptors.…”

Section: Introductionmentioning

confidence: 99%

Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

Yadav¹,

Prakash²,

Yadav³

et al. 2016

Janaki Med. Coll. J. Med. Sci.

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Background and Objectives: The prevention and treatment of peptic ulcers has become an important challenge in the current medicine world. Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time. Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials and Methods: Nine batches of the light liquid paraffin entrapped emulsion gel beads were prepared by a new emulsion gelation technique using sodium alginate and xanthan gum as polymers. The polymeric solution was extruded into Calcium chloride solution by the use of 21G needles. Morphology of beads, drug content, drug entrapment efficiency, floating lag time and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results: Mean surface diameter were between 1.220 ± 2.259% (F1) to 1.230 ± 2.316% (F9) and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric fluid at 37ºC. The drug content and drug entrapment efficiency among the formulations were between 17.48%~19.68% and 71.06% ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion: The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12

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“…The conventional dose (150 mg) inhibits acid secretion for 4-5 h, requiring frequent dosing that causes fluctuations in plasma levels of the drug. Colonic metabolism, intestinal degradation of RHCl (15), and absorption window in the proximal part of the gut makes it a suitable candidate for a gastroretentive drug delivery device.…”

Section: Introductionmentioning

confidence: 99%

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

2012

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Abstract. A nondisintegrating, floating asymmetric membrane capsule (FAMC) was developed to achieve site-specific osmotic flow of a highly water-soluble drug, ranitidine hydrochloride (RHCl), in a controlled manner. Solubility suppression of RHCl was achieved by the common ion effect, using optimized coated sodium chloride as a formulation component. The capsular wall of FAMC was prepared by the phase inversion process wherein the polymeric membrane was precipitated on glass pins by dipping them in a solution of cellulose acetate followed by quenching. Central composite design was utilized to investigate the influence of independent variables, namely, level(s) of membrane former, pore former, and osmogen, on percent cumulative drug release (response). The release mechanism of RHCl through FAMC was confirmed as osmotic pumping. The asymmetry of the membrane was characterized by scanning electron microscopy that revealed a dense nonporous outer region of membrane supported by an inner porous region. Differential scanning calorimetry indicated no incompatibility between the drug and excipients. In vitro drug release in three biorelevant media, pH 2.5 (low fed), pH 4.5 (intermediate fed), and pH 6.5 (high fed), demonstrated pH-independent release of RHCl (P>0.05). Floating ability for 12 h of the optimized FAMC9 was visually examined during the in vitro release studies that showed maximal drug release with zero-order kinetics (r 2 00.9991). Thus, a novel osmotically regulated floating capsular system was developed for site-specific delivery of RHCl.

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Colonic metabolism of ranitidine: implications for its delivery and absorption

Cited by 94 publications

References 12 publications

How to Determine the Role of the Microbiome in Drug Disposition

How to Determine the Role of the Microbiome in Drug Disposition

Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

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