Dialysis of Ephedrine and Pentobarbital from Whole Human Saliva and Simulated Saliva

Davis, Robert E.; Hartman, C.W.; Fincher, Julian H.

doi:10.1002/jps.2600600318

Cited by 34 publications

(11 citation statements)

References 15 publications

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“…Titration of 25 ml of the syn thetic saliva from pH 8.0 to 4.4 required 7.05 ml 0.1 N HC1, demonstrating a buffer capacity of 2.8 x 10'5 Eq/ml, the same as the salivary supernatant. The inorganic composition was similar to that reported in the literature for saliva [Davies, 1973;Zipkin, 1970;Jenkins, 1960;Davis et al, 1971]. When tested in the suspended saliv ary sediment system the synthetic saliva buffer solution gave a curve similar in magnitude and shape to salivary supernat ant ( fig.…”

Section: Resultssupporting

confidence: 69%

Factors Affecting pH Rise of Suspended Salivary Sediment

Tavss¹,

Eigen²

1986

Caries Res

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The effect of some salivary constituents on pH rise was studied. A solution simulating salivary supernatant in buffer capacity and inorganic composition was used. Mixing this solution with glucose and salivary sediment resulted in a pH rise similar in magnitude and shape to that of the salivary supernatant control, demonstrating a significant contribution of buffer capacity to in vitro pH rise of salivary supernatant. Arginine peptides also showed pH rise activity, but only at concentrations not found in saliva. The salivary buffers are therefore the major contributors to pH rise in saliva. Additional studies demonstrated that the activity of arginine was diminished by attaching groups to the α-amino or guanidino functional group, but was not affected by esterification. Within the limits of the molecules tested, arginine peptides increased in activity with increasing number of arginyl groups, but were unaffected by varying the size of the peptide. Little difference was seen between a C- and N-terminal peptide.

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Section: Resultssupporting

confidence: 69%

Factors Affecting pH Rise of Suspended Salivary Sediment

Tavss¹,

Eigen²

1986

Caries Res

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“…0.7. Indeed, saliva has a protein concentration of 2 g/liter, and binding has been established with respect to salicylate (15) and pentobarbitone, for example (6). Another hypothesis is that fluconazole is excreted in saliva not only by a process of passive diffusion but also by an active transport mechanism.…”

Section: Resultsmentioning

confidence: 99%

Influence of local radiotherapy on penetration of fluconazole into human saliva

Oliary

Tod

Louchahi

et al. 1993

Antimicrob Agents Chemother

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The pharmacokinetics of fluconazole (50 mg, single oral dose) in saliva and plasma were determined for five healthy subjects and five patients who underwent radiotherapy (dose, >45 Gy over a 6-week period) in the salivary gland area and suffered from oropharyngeal candidiasis. Saliva was collected after electrical stimulation. Fluconazole was measured by liquid chromatography. From healthy volunteers and patients, saliva and plasma were sampled from 0 to 24 h. Although fluconazole penetration kinetics were significantly slowed down in irradiated patients, saliva concentrations of fluconazole were higher than those in the plasma, except at 1 h. In the postdistribution phase, the saliva/plasma concentration ratio was in the range of 1.2 to 1.4, and there was no significant difference between healthy subjects and patients. The saliva concentration of fluconazole was over 1 mg/liter throughout the entire interval 2 to 24 h after drug intake. From these results, the clinical efficacy of fluconazole for oropharyngeal candidiasis is not expected to be less than that in subjects with normal salivary glands, provided that salivary secretion remains.Fluconazole is a broad-spectrum antifungal agent approved in several countries for the treatment of some superficial and deep mycoses. Comparative trials have shown fluconazole to be equal or superior to ketoconazole in the treatment of oropharyngeal candidiasis in patients with AIDS (7) or cancer (17). Fluconazole exhibits a high penetration into body tissues as demonstrated recently by positron emission tomography (9). The volume of distribution of fluconazole approximates that of total body water, the drug exhibits a low level of protein binding (12%) to plasma proteins, and concentrations in saliva, sputum, and vaginal and blister fluid equal those measured in plasma (4). Fluconazole also penetrates into the central nervous system, with levels in the cerebrospinal fluid between 50 and 90% of corresponding levels in plasma, even in the absence of meningitis (11). However, physiological or pathological events can affect tissue penetration and thus possibly clinical outcome. Among these events, irradiation of the salivary glands at a dose greater than 45 Gy results in stomatitis, opportunistic infections (especially candidiasis), increased viscosity of saliva, and qualitative and quantitative modifications of its composition (14,20,22). These modifications are able to decrease penetration of drugs into the salivary gland (13, 18). Although there is no clear relation between fluconazole levels in saliva and clinical outcome, very low levels in saliva or absence of saliva caused by irradiation would be a priori detrimental to efficacy. Indeed, the only clinical failure in the study by Dupont and Drouhet (8) was in an irradiated patient who had no salivary secretion. Thus, the pharmacokinetic parameters describing fluconazole assimilation into saliva were determined for a population of patients who underwent radiotherapy in the salivary gland area.* Corresponding author. MATERIA...

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“…Drugs absorbed here are not exposed to gastrointestinal secretions that may cause degradation. Moreover, they bypass the liver in the first circulatory pass and are not exposed to microsomal enzymes before entering the general circulation, as is usually the case in gastrointestinal absorption (25,26).…”

Section: Buccal and Sublingual Routementioning

confidence: 99%

“…Davis et al (25) used SS4 in a dynamic dialysis system to investigate the interactions that might occur between drug molecules and the constituents of salivary secretions. Such interactions, if they occur, might influence drug absorption through the oral mucosa.…”

Section: Buccal and Sublingual Routementioning

confidence: 99%

Simulated Biological Fluids with Possible Application in Dissolution Testing

Marques¹,

Löebenberg²,

Almukainzi³

2011

Dissolution Technol.

892

523

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This literature review is a compilation of the composition and, in most cases, the preparation instructions for simulated biological fluids that may be used as dissolution media in the evaluation of dissolution profiles and amount of drug released from pharmaceutical dosage forms. The use of simulated biological fluids can give a better understanding of the release mechanisms and possible in vivo behavior of a product and enhance the predictive capability of the dissolution testing. A summary of the major characteristics of the most used routes of administration that may affect dissolution and absorption of drug substances is presented. The routes and simulated biological fluids covered by this review are:• Parenteral: simulated body fluid and simulated synovial fluid.• Oral: fasted-state simulated gastric fluid, fed-state simulated gastric fluid, fasted-state simulated intestinal fluid, fed-state simulated intestinal fluid, simulated colonic fluid, fasted-state simulated colonic fluid, and fed-state simulated colonic fluid.• Buccal and sublingual: simulated saliva.• Pulmonary: simulated lung fluid.• Vaginal: simulated vaginal fluid and simulated semen.• Ophthalmic: simulated tears.Simulated sweat is also included. Some examples of how these simulated biological fluids are used to evaluate dosage forms are included in each route of administration.

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Dialysis of Ephedrine and Pentobarbital from Whole Human Saliva and Simulated Saliva

Cited by 34 publications

References 15 publications

Factors Affecting pH Rise of Suspended Salivary Sediment

Factors Affecting pH Rise of Suspended Salivary Sediment

Influence of local radiotherapy on penetration of fluconazole into human saliva

Simulated Biological Fluids with Possible Application in Dissolution Testing

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