Bioavailability studies on para-aminosalicylic acid and its various salts in man. I. Absorption from solution and suspension

Wan, Suk Han; Pentikäinen, Pertti J.; Azarnoff, Daniel L.

doi:10.1007/bf01062142

Cited by 14 publications

(13 citation statements)

References 11 publications

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“…1) and the plasma half-life (Fig. 2) are comparable with reported values (Way et al, 1948;Lavigne and Marchand, 1973;Wan et al, 1974;Weinstein, 1975). The PAS concentrations ( Fig.…”

Section: Resultssupporting

confidence: 90%

“…First, the presence of cancer modifies the pharmacokinetics of many drugs, antineoplastic (Kato et al, 1968b;Bartosek et al, 1973;Benjamin, 1974;Bartosek et al, 1975;Lavigne et al, 1975;Donelli et al, 1976) as well as other (Kato, Takanaka and Oshima, 1968a;Rosso, Dolfini and Donelli, 1968;Franchi and Rosso, 1969;Rosso et al, 1971;Basu, Parke and -1-583 iiO Williams, 1974a;Sharma and Garb, 1974;Beck, Mandel and Fabro, 1975;Nadeau and Marchand, 1975;Marchand and Nadeau, 1976). Second, some metabolic properties of PAS (Way et al, 1948;Wan et al, 1974) such as short plasma half-life, predominantly renal excretion and the absence of side-effects at the dose used (Weinstein, 1975) make it an interesting model drug.…”

Section: Resultsmentioning

confidence: 99%

“…3) in Group III patients. N-acetyl-p-aminosalicylic acid (APAS) is the principal metabolite of PAS (Way et al, 1948;Wan et al, 1974) and this conjugation of PAS with acetyl radical leads to an inactive product, as happens in most Phase II drug reactions (Bousquet, 1970). The high percentage of APAS might therefore be correlated with the low plasma level of unchanged active PAS in the plasma of Group III (Fig.…”

Section: Resultsmentioning

confidence: 99%

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P-aminosalicylate metabolism in cancer patients sensitive and resistant to chemotherapy

Lavigne¹,

Barry²,

d'Auteuil³

et al. 1977

Br J Cancer

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Summary.-A reduced response of a tumour to chemotherapy may be due to the host's drug metabolism. To test this hypothesis, we measured the metabolism of a model drug, para-aminosalicylate (PAS). Volunteers and cancer patients ingested a single oral dose (2 g) of PAS and we measured the plasma disappearance curve of the drug and its metabolite. In 7 patients suffering from lymphosarcoma, acute or chronic leukaemia and resistant to cancer chemotherapy, we observed low plasma PAS concentrations, an increase in PAS acetylation and an increased number (and a higher frequency) of abnormal liver-function tests. In 14 patients with malignant blood disease, yet responding well to chemotherapy, the metabolism of PAS is similar to that of healthy controls of the same age and sex. The plasma half-life of PAS is similar in sensitive and resistant patients, but slightly longer than in volunteers. Finally, in urine collected 120 min after drug administration, we observed the same results as in plasma. In conclusion, cancer patients resistant to chemotherapy do not metabolize the model drug PAS as volunteers or sensitive patients do, and this might be relevant to the terminal stage of the disease.

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“…1) and the plasma half-life (Fig. 2) are comparable with reported values (Way et al, 1948;Lavigne and Marchand, 1973;Wan et al, 1974;Weinstein, 1975). The PAS concentrations ( Fig.…”

Section: Resultssupporting

confidence: 90%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

P-aminosalicylate metabolism in cancer patients sensitive and resistant to chemotherapy

Lavigne¹,

Barry²,

d'Auteuil³

et al. 1977

Br J Cancer

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“…The nonspecific colorimetric method used does not differentiate between unchanged PAS and the glycine conjugated, p-aminosalicyluric acid (PASU). However, on the basis of low concentrations of PASU found in plasma and the doseindependent formation of PASU, it is possible to analyze PAS in plasma by a nonspecific method which gives the same relative error of about 5% regardless of plasma concentration (Lauener et al, 1957;Wan et al, 1974).…”

Section: Discussionmentioning

confidence: 99%

“…The concentration of PAS in plasma and in the incubates was assayed for nonacetylated PAS and in urine for total PAS (nonacetylated + acetylated PAS + p-aminosalicyluric acid, PASU) using the Marshall colorimetric method as modified by Wan et al (1974).…”

Section: Assaymentioning

confidence: 99%

Effect of charcoal‐drug ratio on antidotal efficacy of oral activated charcoal in man.

Olkkola¹

1985

Brit J Clinical Pharma

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The effect of charcoal‐drug ratio on the antidotal efficacy of oral activated charcoal was studied in six healthy volunteers in a randomized cross‐over study and compared with the adsorption capacity of activated charcoal in vitro. Aminosalicylic acid (PAS) 1 g and 5 g were ingested on an empty stomach in 30 ml of water. Immediately afterwards the subjects ingested 50 g of activated charcoal in 300 ml of water or 300 ml of water only. PAS 10 g 20 g were only given with 50 g of activated charcoal administered immediately afterwards. The plasma concentrations and the cumulative excretion of PAS into urine were measured for 48 h. Increasing the dose of PAS from 1 g to 20 g reduced the antidotal efficacy of activated charcoal: at a charcoal‐drug ratio of 50:1 under 5% of the dose was absorbed but at a ratio of 2.5:1 about 37%. These data correlated well to the saturation of adsorption capacity of charcoal in vitro. To minimize the possibility of saturation of the adsorption capacity of charcoal in acute intoxications where the amount and type of drug taken is usually unknown, large doses (50‐100 g) of activated charcoal should be used.

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Calcium Coordination Solids for pH‐Triggered Release of Olsalazine

et al. 2017

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Calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H4olz), an anti‐inflammatory compound used for treatment of ulcerative colitis. The materials include one‐dimensional Ca(H2olz)⋅4 H2O chains, two‐dimensional Ca(H2olz)⋅2 H2O sheets, and a three‐dimensional metal‐organic framework Ca(H2olz)⋅2DMF (DMF=N,N‐dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H2olz) phase when exposed to aqueous HCl. The compounds Ca(H2olz)⋅x H2O (x=0, 2, 4) were each pressed into pellets and exposed to simulated gastrointestinal fluids to mimic the passage of a pill from the acidic stomach to the pH‐neutral intestines. All three calcium materials exhibited a delayed release of olsalazine relative to Na2(H2olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.

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Bioavailability studies on para-aminosalicylic acid and its various salts in man. I. Absorption from solution and suspension

Cited by 14 publications

References 11 publications

P-aminosalicylate metabolism in cancer patients sensitive and resistant to chemotherapy

P-aminosalicylate metabolism in cancer patients sensitive and resistant to chemotherapy

Effect of charcoal‐drug ratio on antidotal efficacy of oral activated charcoal in man.

Calcium Coordination Solids for pH‐Triggered Release of Olsalazine

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