scholarly journals Drivers of absolute systemic bioavailability after oral pulmonary inhalation in humans

2021 ◽  
Vol 164 ◽  
pp. 36-53
Author(s):  
Astrid Bacle ◽  
Guillaume Bouzillé ◽  
Arnaud Bruyère ◽  
Marc Cuggia ◽  
Olivier Fardel ◽  
...  
Keyword(s):  
Systemic Bioavailability

Skin Microdialysis-Based Estimation of Systemic Bioavailability Fraction

2012 ◽  
Vol 101 (1) ◽  
pp. 405-413 ◽  
Author(s):  
Ravi Juluru ◽  
Chinmay Shukla ◽  
Hongjun Yin ◽  
Grazia Stagni
Keyword(s):  
Systemic Bioavailability

scholarly journals Therapeutic potential of curcumin in medicinal chemistry

2013 ◽  
Vol 6 (1) ◽  
pp. 89-99 ◽  
Author(s):  
Daniela Košťálová ◽  
Lýdia Bezáková ◽  
Lucia Račkovác ◽  
Silvia Mošovská ◽  
Ernest Šturdík
Keyword(s):  
Clinical Trials ◽  
Therapeutic Potential ◽  
Chemical Reactivity ◽  
Curcuma Longa ◽  
Nucleophilic Attack ◽  
Drug Candidate ◽  
Systemic Bioavailability ◽  
Past Half Century ◽  
Multiple Cell ◽  
Cell Signaling Pathways

Abstract Extensive research over the past half century has shown that curcumin (diferuloylmethane), a polyphenolic compound of turmeric (Curcuma longa L.), can modulate multiple cell signaling pathways. Extensive clinical trials have addressed the pharmacokinetics, safety, and efficacy of this nutraceutical against numerous diseases in human. Curcumin, known for thousand years as a subject of Ayurvedic medicine, has undergone in recent times remarkable transformation into a drug candidate with prospective multipotent therapeutic application. Characterized by high chemical reactivity, resulting from an extended conjugated double bond system prone to nucleophilic attack, curcumin has been shown to interact with a plethora of molecular targets, in numerous experimental observations. In clinical trials, has been used either alone or in combination with other agent. However, its clinical advance has been limited by its short biological half-life, fast metabolism and poor systemic bioavailability after oral administration. To mitigate the above limitations, recently various formulation of curcumin, including nanoparticles, micelles, liposomes, phytosomes delivery system has been examined. The present review has been devoted towards better understanding of the phytonutraceutic properties of curcumin and turmeric based on their disease specific indications and enhancing their prophylactic and therapeutic nutraceutical qualities. The article deals with the biological activity, mode of action, toxicity and forthcoming application of these leads.

Analytical methods for estimation of Budesonide in bulk and in Pharmaceutical dosage forms: A Review

2021 ◽  
pp. 2873-2877
Author(s):  
Anuja Kolsure ◽  
Kratika Daniel ◽  
Mahesh Bhat
Keyword(s):  
Analytical Methods ◽  
Quantitative Estimation ◽  
Hplc Method ◽  
Chronic Obstructive ◽  
Obstructive Pulmonary Disease ◽  
Pharmaceutical Dosage Forms ◽  
Systemic Bioavailability ◽  
Term Management ◽  
Inflammatory Effect

Budesonide is a potent glucocorticoid with a high local anti-inflammatory effect and low systemic bioavailability. The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease. Several analytical methods including UV, HPLC, LC-MS techniques has been developed for Budesonide alone and in combination with others. Methods indicating HPLC bioanalytical method, stability indicating HPLC method, ion pairing chromatographic method and chemometrics assisted HPLC methods are also described for Budesonide. For qualitative and quantitative estimation of Budesonide these analytical methods can be used. The following study describes reported analytical methods of Budesonide.

scholarly journals Inhaled Drug Delivery: A Practical Guide to Prescribing Inhaler Devices

1998 ◽  
Vol 5 (3) ◽  
pp. 180-183 ◽  
Author(s):  
Pierre Ernst
Keyword(s):  
Drug Delivery ◽  
Inhaled Corticosteroids ◽  
High Ratio ◽  
Dose Inhaler ◽  
Breath Hold ◽  
Major Drawback ◽  
Inhalation Devices ◽  
Systemic Bioavailability ◽  
Metered Dose ◽  
Residual Capacity

Direct delivery of medication to the target organ results in a high ratio of local to systemic bioavailability and has made aerosol delivery of respiratory medication the route of choice for the treatment of obstructive lung diseases. The most commonly prescribed device is the pressurized metered dose inhaler (pMDI); its major drawback is the requirement that inspiration and actuation of the device be well coordinated. Other requirements for effective drug delivery include an optimal inspiratory flow, a full inspiration from functional residual capacity and a breath hold of at least 6 s. Available pMDIs are to be gradually phased out due to their use of atmospheric ozone-depleting chlorofluorocarbons (CFCs) as propellants. Newer pMDI devices using non-CFC propellants are available; preliminary experience suggests these devices greatly increase systemic bioavailability of inhaled corticosteroids. The newer multidose dry powder inhalation devices (DPIs) are breath actuated, thus facilitating coordination with inspiration, and contain fewer ingredients. Furthermore, drug delivery is adequate even at low inspired flows, making their use appropriate in almost all situations. Equivalence of dosing among different devices for inhaled corticosteroids will remain imprecise, requiring the physician to adjust the dose of medication to the lowest dose that provides adequate control of asthma. Asthma education will be needed to instruct patients on the effective use of the numerous inhalation devices available.

scholarly journals Interaction between Gut Microbiota and Curcumin: A New Key of Understanding for the Health Effects of Curcumin

Nutrients ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 2499 ◽  
Author(s):  
Beatrice Scazzocchio ◽  
Luisa Minghetti ◽  
Massimo D’Archivio
Keyword(s):  
Gut Microbiota ◽  
Neurological Diseases ◽  
Curcuma Longa ◽  
Pharmacological Activities ◽  
Systemic Bioavailability ◽  
Microbiome Profile ◽  
Regulatory Effects ◽  
High Concentrations

Curcumin, a lipophilic polyphenol contained in the rhizome of Curcuma longa (turmeric), has been used for centuries in traditional Asian medicine, and nowadays it is widely used in food as dietary spice worldwide. It has received considerable attention for its pharmacological activities, which appear to act primarily through anti-inflammatory and antioxidant mechanisms. For this reason, it has been proposed as a tool for the management of many diseases, among which are gastrointestinal and neurological diseases, diabetes, and several types of cancer. However, the pharmacology of curcumin remains to be elucidated; indeed, a discrepancy exists between the well-documented in vitro and in vivo activities of curcumin and its poor bioavailability and chemical instability that should limit any therapeutic effect. Recently, it has been hypothesized that curcumin could exert direct regulative effects primarily in the gastrointestinal tract, where high concentrations of this polyphenol have been detected after oral administration. Consequently, it might be hypothesized that curcumin directly exerts its regulatory effects on the gut microbiota, thus explaining the paradox between its low systemic bioavailability and its wide pharmacological activities. It is well known that the microbiota has several important roles in human physiology, and its composition can be influenced by a multitude of environmental and lifestyle factors. Accordingly, any perturbations in gut microbiome profile or dysbiosis can have a key role in human disease progression. Interestingly, curcumin and its metabolites have been shown to influence the microbiota. It is worth noting that from the interaction between curcumin and microbiota two different phenomena arise: the regulation of intestinal microflora by curcumin and the biotransformation of curcumin by gut microbiota, both of them potentially crucial for curcumin activity. This review summarizes the most recent studies on this topic, highlighting the strong connection between curcumin and gut microbiota, with the final aim of adding new insight into the potential mechanisms by which curcumin exerts its effects.

scholarly journals Human volunteer study of the decontamination of chemically contaminated hair and the consequences for systemic exposure

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Samuel Collins ◽  
Thomas James ◽  
Felicity Southworth ◽  
Louise Davidson ◽  
Natalie Williams ◽  
...  
Keyword(s):  
United Kingdom ◽  
Methyl Salicylate ◽  
Systemic Exposure ◽  
Mass Casualty ◽  
Human Studies ◽  
Human Volunteer ◽  
Toxic Chemicals ◽  
Systemic Bioavailability ◽  
Volunteer Study ◽  
Careful Management

AbstractThe decontamination of exposed persons is a priority following the release of toxic chemicals. Efficacious decontamination reduces the risk of harm to those directly affected and prevents the uncontrolled spread of contamination. Human studies examining the effectiveness of emergency decontamination procedures have primarily focused on decontaminating skin, with few examining the decontamination of hair and scalp. We report the outcome of two studies designed to evaluate the efficacy of current United Kingdom (UK) improvised, interim and specialist mass casualty decontamination protocols when conducted in sequence. Decontamination efficacy was evaluated using two chemical simulants, methyl salicylate (MeS) and benzyl salicylate (BeS) applied to and recovered from the hair of volunteers. Twenty-four-hour urinary MeS and BeS were measured as a surrogate for systemic bioavailability. Current UK decontamination methods performed in sequence were partially effective at removing MeS and BeS from hair and underlying scalp. BeS and MeS levels in urine indicated that decontamination had no significant effect on systemic exposure raising important considerations with respect to the speed of decontamination. The decontamination of hair may therefore be challenging for first responders, requiring careful management of exposed persons following decontamination. Further work to extend these studies is required with a broader range of chemical simulants, a larger group of volunteers and at different intervention times.

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