Effects of Bile Salts on Gastrointestinal Absorption of Pravastatin

Chun, In‐Koo; Lee, Kyung Min; Lee, Jun Young; Gwak, Hye Sun

doi:10.1002/jps.23123

Cited by 13 publications

(6 citation statements)

References 20 publications

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“…The influence of surfactant on a solid dispersion of amorphous drug may also be beneficial in helping to understand whether bile salts, naturally occurring surfactants present in the gastrointestinal tract, can favourably influence the dissolution of amorphous drugs. In this context, it was recently found that bile salts incorporated into solid dispersions could improve dissolution of pravastatin in the gastrointestinal tract …”

Section: Introductionmentioning

confidence: 99%

Atypical effects of incorporated surfactants on stability and dissolution properties of amorphous polymeric dispersions

Al-Obaidi

Lawrence

Buckton

2016

Journal of Pharmacy and Pharmacology

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Section: Introductionmentioning

confidence: 99%

Atypical effects of incorporated surfactants on stability and dissolution properties of amorphous polymeric dispersions

Al-Obaidi

Lawrence

Buckton

2016

Journal of Pharmacy and Pharmacology

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“…40 Chun et al described a method for obtaining an amorphous form of the drug: they prepared crystalline pravastatin sodium solid dispersions using various bile salts and observed the complete conversion of the crystalline form into an amorphous form. 41 The permeation flux of amorphous pravastatin from the solid dispersion was much higher than that of the crystalline form from physical mixtures and commercial tablets, 41 which may improve the bioavailability of the compound in pharmaceutical formulations.…”

Section: Fluvastatinmentioning

confidence: 99%

The polymorphism of statins and its effect on their physicochemical properties

et al. 2018

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Polymorphism of pharmaceutical substances has a significant impact on their physicochemical properties, durability, bioavailability and consequently on their pharmacological activity. Solid dosage forms may exist in both crystalline and amorphous forms. Amorphous varieties are characterized by higher solubility and dissolution rates, while crystalline forms show greater purity and storage stability. The choice between the crystalline or amorphous form of a drug is extremely important to ensure effective and safe pharmacotherapy. Statins − the most commonly used group of drugs in the treatment of lipid disorders − are an example of drugs that occur in many crystalline and amorphous forms. Statins belong to class II in the biopharmaceutical classification system (BCS), which means that they are poorly soluble, but permeate biological membranes well. The bioavailability of statins shows considerable variation, which is associated with the first-pass effect in the liver and the accumulation of the drug in the hepatocytes. The improvement of bioavailability after oral administration of poorly soluble medicinal substances remains one of the most challenging aspects of the drug development process. A specific polymorphic form is obtained by applying appropriate conditions during the process of its preparation under industrial conditions, including the use of a suitable solvent, a specific temperature or rate of crystallization. The article provides a comprehensive update on the current knowledge of the influence of polymorphic form on statin solubility and bioavailability. Research is still being carried out to obtain new polymorphic varieties of statins that are characterized by better physicochemical and pharmacokinetic parameters.

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“…81 The formation of aminoclay complex with telmisartan led to improved AUC and C max , 82 while the potentials of bile salts to prevent API crystallization and enhance absorption have also been studied. 60,83 The use of inorganic salts as kosmotropic agents to disrupt gel strength and promote dissolution has been investigated, 84 while API complexation with weak acids led to increased solubility. 85…”

Section: Prodrugs For Increasing Permeability and Solubilitymentioning

confidence: 99%