Intestinal Absorption of Drugs I: The Influence of Taurocholate on the Absorption of Dantrolene in the Small Intestine of the Rat

Poelma, F. G. J.; Tukker, Josef J.; Crommelin, Daan J.A.

doi:10.1002/jps.2600780405

Cited by 27 publications

(10 citation statements)

References 24 publications

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“…The effect of bile salts on the intestinal absorption of model hydrophilic (paracetamol and theophylline) and lipophilic drugs (griseofulvin, ketaconazole, and dantrolene) was studied by Poelma et al 96,97 using a rat in situ intestinal perfusion technique. Simple or mixed bile salt micelles had no effect on absorption of the hydrophilic drugs, leading to the conclusion that bile salt micelles had minimal effect on the intrinsic barrier function of either the UWL or the intestinal membrane.…”

Section: Absorption Permeability and The Postprandial Intestinementioning

confidence: 99%

Physicochemical and Physiological Mechanisms for the Effects of Food on Drug Absorption: The Role of Lipids and pH

Charman

Porter

Mithani

et al. 1997

Journal of Pharmaceutical Sciences

535

343

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Drugs are absorbed after oral administration as a consequence of a complex array of interactions between the drug, its formulation, and the gastrointestinal (GI) tract. The presence of food within the GI tract impacts significantly on transit profiles, pH, and its solubilization capacity. Consequently, food would be expected to affect the absorption of co-administered drugs when their physicochemical properties are sensitive to these changes. The physicochemical basis by which ingested food/lipids induce changes in the GI tract and influence drug absorption are reviewed. The process of lipid digestion is briefly reviewed and considered in the context of the absorption of poorly water-soluble drugs. The effect of food on GI pH is reviewed in terms of location (stomach, upper and lower small intestine) and the temporal relationship between pH and drug absorption. Case studies are presented in which postprandial changes in bioavailability are rationalized in terms of the sensitivity of the physicochemical properties of the administered drug to the altered GI environment.

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Section: Absorption Permeability and The Postprandial Intestinementioning

confidence: 99%

Physicochemical and Physiological Mechanisms for the Effects of Food on Drug Absorption: The Role of Lipids and pH

Charman

Porter

Mithani

et al. 1997

Journal of Pharmaceutical Sciences

535

343

View full text Add to dashboard Cite

show abstract

“…The time dependence of the luminal concentration C can be written as: where C o and C t are the luminal concentration of the model compound at time 0 and t, respectively, and k dis is the first‐order disappearance rate constant. The disappearance rate constant k dis was calculated from plots of ln(C t /C o ) versus time by linear regression 17…”

Section: Resultsmentioning

confidence: 99%

In-situ absorption, protein binding and pharmacokinetic studies of S002-853, a novel antidiabetic and antidyslipidaemic flavone derivative in rats

Gautam

Kushwaha

Pratap

et al. 2010

Journal of Pharmacy and Pharmacology

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“…The C max was 55% AE 14% after 4 h and lasted through the duration of the experiment. NaTDC has been found to reduce the viscosity and elasticity of bronchial mucus and presumably other types of mucus as well (22), while NaTC is shown to increase mucus secretion (23). The presence of mucous layers that coat all Figure 4.…”

Section: Effect Of Conjugated Bile Salts Alone or In Combination Withmentioning

confidence: 97%

Effect of Different Bile Salts on the Relative Hypoglycemia of Witepsol W35 Suppositories Containing Insulin in Diabetic Beagle Dogs

Hosny

Al-Shora

Elmazar

2001

Drug Development and Industrial Pharmacy

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Insulin suppositories were formulated using Witepsol W35 as a base to investigate the effect of various bile salts/acids on the plasma glucose concentration of diabetic beagle dogs. Comparison of the effect of these formulations was made with that produced by insulin subcutaneous injections. Of the bile salts/acids studied, incorporation of 100 mg of deoxycholic acid (DCA), sodium cholate (NaC), or sodium deoxycholate (NaDC) with insulin (10 U/Kg) showed that suppositories containing NaDC produced the highest area under the curve (AUC) and relative hypoglycemia (RH) of 290 +/- 83 mg%h and 28% +/- 8.1%, respectively. To study the optimum amount of NaDC in insulin suppositories to produce the highest RH, 50-200 mg/suppository were used, and we found that 150 mg NaDC produced 35% +/- 13% RH. We also studied the influence of different doses of insulin (5-20 U/kg) in the presence of NaDC (100 mg). It was found that increase of the insulin dose was accompanied by an increase in AUC and maximum reduction in plasma glucose level Cmax. A combination of NaDC (100 mg) and NaC (50 mg) produced an AUC of 252 +/- 13mg%h and an RH of 49% +/- 2.6%, which were higher than produced by either of its individual components (NaC 50 mg or NaDC 100 mg) when used alone or when compared with an equivalent amount of NaDC (150 mg). When the effect of sodium taurocholate (NaTC) and sodium taurodeoxycholate (NaTDC) was studied, it was found that an insulin suppository containing 100 mg of either NaTC or NaTDC produced an RH equivalent to that produced previouslY with a mixture of NaDC (100 mg) and NaC (50 mg). On the other hand, NaC (50 mg) did not improve the hypoglycemic effect of NaTC any further. In conclusion, a relative hYpoglycemia of about 50% can be reached using insulin suppositories containing Witepsol W35 as a base and NaDC plus NaC (100 mg plus 50 mg, respectively), NaTDC (100mg), or NaTC (100 mg) as rectal absorption enhancers of insulin. A desirable hypoglycemia, expressed as Cmax, and/or AUC can be reached by adjusting the insulin dose in the formulation according to the degree of hyperglycemia.

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Intestinal Absorption of Drugs I: The Influence of Taurocholate on the Absorption of Dantrolene in the Small Intestine of the Rat

Cited by 27 publications

References 24 publications

Physicochemical and Physiological Mechanisms for the Effects of Food on Drug Absorption: The Role of Lipids and pH

Physicochemical and Physiological Mechanisms for the Effects of Food on Drug Absorption: The Role of Lipids and pH

In-situ absorption, protein binding and pharmacokinetic studies of S002-853, a novel antidiabetic and antidyslipidaemic flavone derivative in rats

Effect of Different Bile Salts on the Relative Hypoglycemia of Witepsol W35 Suppositories Containing Insulin in Diabetic Beagle Dogs

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