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The administration of medicines to children
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Buccal administration of small volume liquid medicines (e.g. midazolam for seizures) or solid dose fast-dissolving tablets or wafers (ibuprofen, ondansetron, paracetamol, piroxicam) can be useful for young and older children. ‘Melt’ technology uses freeze-dried active drug with flavours, which dissolve in the saliva and are difficult to spit out. Orodispersible tablets may dissolve in the mouth or be dissolved in a small amount of liquid before administration. Taste of these preparations and of chewable tablets should be acceptable [42]. Melting wafers may be difficult to divide to provide a dose appropriate to age or weight. Chewable tablets are considered safe to administer to young children [43]. Depending on their physicochemical properties, drugs administered by the buccal route may be absorbed locally (fentanyl) or swallowed and absorbed in the stomach and intestine (ondansetron, piroxicam).
Gastrointestinal Function and Toxicology in Minipigs
Published in Shayne C. Gad, Toxicology of the Gastrointestinal Tract, 2018
Maria R. Jones, Alain Stricker-Krongrad
A concern in drug absorption and bioavailability for oral compounds is first-pass metabolism through the liver, which can substantially reduce bioavailability. In order to enhance bioavailability, formulations are being developed for buccal administration. This allows for direct systemic absorption into the bloodstream through the oral mucosa. In fact, in vitro and ex vivo studies have used minipig and pig oral mucosa to assess permeability (Liu et al. 2002, Adhikari et al. 2010, Kumria et al. 2016). Furthermore, in vivo evidence suggests buccal administration and formulations have the potential to greatly enhance bioavailability in minipigs, where buccal administration of diazepam increased bioavailability up to 76%, whereas standard oral administration of similar dose levels resulted in bioavailability being 30% (Meng-Lund et al. 2016). Taken together, this suggests buccal formulations could be a useful to increase system exposure and avoid first-pass metabolism by the liver.
Oral formulations
Published in Karen Anne Gunnell, Rebecca Hayley Venables, A Practical Guide to Medicines Administration, 2018
Karen Anne Gunnell, Rebecca Hayley Venables
Buccal administration allows the drug to pass directly into the bloodstream via the oral mucosa in the buccal cavity, avoiding first-pass metabolism. This can improve the bioavailability of some drugs and allows for a faster onset of action.
Metoclopramide loaded buccal films for potential treatment of migraine symptoms: in vitro and in vivo study
Published in Pharmaceutical Development and Technology, 2023
Omar Mady, Sara Hussien, Dalia H. Abdelkader, Enas El-Dahaby
Mucoadhesive Buccal film containing an antihypertensive drug (candesartan cilexetil) was suggested to solve the drug’s two main biopharmaceutic and pharmacokinetic problems which are solubility and first bypass metabolism after oral ingestion. The results showed clear bioavailability enhancement of the drug from mucoadhesive buccal film comparing to oral administration (Mady et al. 2021). Therefore, the well-known advantage of the buccal as a route of administration, concerning the hindering first bypass metabolism, directed to use the same way for formulation of metoclopramide as a buccal dosage form. In the case of the patient suffering from vomiting, the loss of all or a part of the drug after oral or buccal administration could be expected. Consequently, the selection of a buccal bioadhesion film as a dosage form could solve this kind of problem. In addition, the rapid onset of action, which is also essential in this case, could be also anticipated (Gilhotra et al. 2014). The use of mucoadhesive buccal film showed a significant enhancement (p< 0.05) of Cmax and Tmax of MCP loaded film compared to the oral administration of the conventional Tablet.
Sublingual dexmedetomidine: repurposing an anesthetic as an anti-agitation agent
Published in Expert Review of Neurotherapeutics, 2023
Justin Faden, Meghan Musselman, Leslie Citrome
Sublingual dexmedetomidine is available in 120 mcg and 180 mcg films, each of which contain two ‘dots’ separated by a space so that the film may be cut in half, resulting in two doses of half the original strength (Table 2). The recommended dosage is dependent on the level of agitation (mild-moderate versus severe), age (≥65 years old versus <65 years old), presence and degree of hepatic impairment, and if additional doses are used within 24 hours (a second or third ‘half-dose’ can be given if at least 2 hours apart). Sublingual dexmedetomidine is self-administered under the supervision of a healthcare provider. A healthcare provider should monitor vital signs and alertness after administration to prevent falls and syncope. Patients should not eat or drink for 15 min following sublingual administration or an hour following buccal administration[26]. Additional doses are not recommended in individuals with systolic blood pressure less than 90 mmHg, diastolic blood pressure less than 60 mmHg, heart rate less than 60 beats per minute, or a postural decrease in systolic blood pressure of 20 mmHg or greater or in diastolic blood pressure of 10 mmHg of greater[26].
A critical evaluation of midazolam nasal spray for the treatment of patients with seizure clusters
Published in Expert Review of Neurotherapeutics, 2021
The FDA approved MDZ-NS, NAYZILAM® (MDZ) nasal spray, C-IV, on 17 May 2019 [68,69]. NAYZILAM® is marketed by UCB Pharma and there is currently no licensing filed to the European Medicines Agency for Europe. MDZ-NS is indicated for acute treatment of intermittent, stereotypic episodes of frequent seizure activity (i.e. SCs, acute repetitive seizures) that are distinct from a patient’s usual seizure pattern in patients with epilepsy who are 12 years of age and older [44]. MDZ-NS is the first FDA-approved nasal option for treating SCs [68]. In the US, it is the first new medication in over 20 years to be approved to treat SCs. It offers the benefits of intranasal administration, which allows for outpatient treatment by caregivers and other non-healthcare professionals, and may particularly be meaningful to patients who have limited treatment options [68]: for example, hypersalivation, jerking movements of the jaw, or general restlessness may rule out buccal administration of clonazepam and MDZ, and rectal diazepam may not be suitable because of the physical and social constraints to rectal administration [35].