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Pharmacology of Opioids
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
Buprenorphine can be administered intravenously and sublingually for the management of acute pain. However, it should be noted that the time to peak effect is much slower than that for the conventional IR opioids. The times to peak effect after IV and sublingual administration may be more than one hour and three hours, respectively (Macintyre & Huxtable, 2017). Buprenorphine also has a long terminal half-life of around 24 hours. These factors mean that the dose intervals prescribed for “as needed” administration of sublingual buprenorphine need to be longer than those often used for IR opioids such as morphine, fentanyl, and oxycodone in order to minimize the potential risk of “dose stacking.”
Spray Drying and Pharmaceutical Applications
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Metin Çelik, Pavan Muttil, Gülşilan Binzet, Susan C. Wendell
Despite the availability of numerous crystal engineering techniques, generating drug-rich microparticles with a predetermined size, morphology and crystallinity still represent a challenge. Among many techniques, spray drying, due to its ability to control the size, shape, and other properties of the resulting particles, has become a versatile technology for the preparation of microparticles and more importantly, nanoparticles for the pharmaceutical/biotech applications. For example, in a study, it was shown that the adsorption of excipients onto micron size drug substrates using a spray drying process was found to be an attractive approach to engineer drug-rich microparticles with characteristics suitable for drug delivery [106]. In another recent study, a fast-dissolving mucoadhesive microparticulate delivery system was developed using a spray drying method for piroxicam, which is a drug with low water solubility and high membrane permeability [107]. It is known that such delivery systems intended for sublingual administration could be a suitable alternative to fast-dissolving tablets because the sublingual adsorption can be improved as a consequence of prolonging residence time on the mucosa and reducing the amount of swallowed drug [108].
Emerging Oral Treatments: Oral Minoxidil for Androgenetic Alopecia
Published in Rubina Alves, Ramon Grimalt, Techniques in the Evaluation and Management of Hair Diseases, 2021
Jared Marc John, Rodney Sinclair
Oral minoxidil undergoes extensive first-pass glucuronidation before it reaches systemic circulation [18]. Sublingual administration bypasses hepatic metabolism, thereby increasing bioavailability compared to oral administration. A case series evaluating the efficacy and safety of low-dose sublingual minoxidil (0.45–0.9 mg) in 64 MPHL and FPHL patients over 12 months reported an improvement in hair density and reduction in shedding with lower rates of adverse effects compared to previous studies of oral minoxidil [19].
Cationic nanocapsule suspension as an alternative to the sublingual delivery of nifedipine
Published in Pharmaceutical Development and Technology, 2023
Bárbara Felin Osmari, Giovana Aime Medeiros, Jéssica Brandão Reolon, Vinícius Costa Prado, Natália Brucker, Letícia Cruz
Over the years, nanotechnology has been gaining emphasis in the pharmaceutical field due to the ability of nanocarriers to increase drug physicochemical stability. In addition, nanostructured systems enable controlled drug release, improving effectiveness and reducing adverse effects (Apolinário et al. 2020; Deng et al. 2020). The literature has reported on the benefits of incorporation of NIFE in nanostructured systems due to its ability to improve bioavailability (Weerapol et al. 2015), control the release profile (Granada et al. 2013), increase half-life time (Bi et al. 2020), and improve the photostability of NIFE (Tagliari et al. 2015). Among such structures, polymeric nanocapsules are reservoir systems composed of an oily core wrapped in a polymeric wall (Mora-Huertas et al. 2010; Jain and Thareja 2019). Sublingual administration is attractive because the formulations have properties that increase contact time with the mucosa when considering that part of the drug may be swallowed due to salivary flow (Mazzarino et al. 2014; Parodi et al. 2017). In this study, Eudragit® RS100 was chosen as a polymer for the development of nanocapsules due to its mucoadhesive characteristics (Adibkia et al. 2011; Chaves et al. 2018).
Thrombophilia and hormonal therapy in transgender persons: A literature review and case series
Published in International Journal of Transgender Health, 2022
Marianne Kerrebrouck, Anna Vantilborgh, Sarah Collet, Guy T’Sjoen
There are limitations to our study, as the design is a case series, that is retrospective and subject to selection bias. Although there may have been trans persons lost to follow-up, the number of patients is substantial. As no intramuscular formulations are available in our country and sublingual use of oral estrogens is only rarely mentioned, these have not been studied. In our literature search, we could not find data concerning the VTE risk of sublingual or intramuscular estrogens. We speculate that, for sublingual administration because of no first pass metabolism, this risk is low. On the contrary, as intramuscular application may induce supraphysiological peak levels, the risk could be elevated. However no clinical data sets are currently available to confirm these assumptions. In the future, it would be interesting to investigate the incidence of VTE, (genetic) thrombophilia and other vascular events in transgender persons on hormonal therapy with our without anticoagulation in a larger European prospective cohort study. Also, the cohort was Caucasian, therefore the risk may not be generalizable to other cohorts.
Sublingual insulin administration: application of hydroxypropyl beta-cyclodextrin and poloxamer188 as permeation enhancers
Published in Pharmaceutical Development and Technology, 2021
Anuja Paprikar, Ankit Soni, Neeraj Kaushal, Senshang Lin
Diabetes mellitus is a medical condition wherein either the pancreas is unable to produce insulin and/or the available insulin cannot be used for effective utilization of glucose for automatic function. As per the National Diabetes Statistics Report, 2020 about 34.2 million people which constitutes of 13% of the US population has diabetes (National diabetes statistics report 2020). Currently, injection of insulin or its analogues is the only treatment for insulin-dependent diabetes which reduces patient compliance. As a result, approaches of non-invasive administration for insulin have been studied. Among various approaches, oral administration is the safest and most patient compliant. However, it involves major hurdles like extensive degradation through the gastrointestinal tract, lack of permeation through epithelial cells, and first-pass effect in the liver. To overcome these hurdles, sublingual administration can be considered as a valid alternative for insulin administration.