Buccal tablet: Difference between revisions
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#REDIRECT [[Buccal administration#Tablets]] |
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{{Merge to|Buccal administration|discuss=Talk:Buccal administration#Proposed merge of Buccal tablets into Buccal administration|date=May 2022}} |
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'''Buccal tablets''' are a type of solid [[dosage form]] administered orally in between the gums and the inner linings of the cheek.<ref name=":0">{{cite journal | vauthors = Targhotra M, Chauhan MK | title = An Overview on Various Approaches and Recent Patents on Buccal Drug Delivery Systems | journal = Current Pharmaceutical Design | volume = 26 | issue = 39 | pages = 5030–5039 | date = 2020 | pmid = 32534560 | doi = 10.2174/1381612826666200614182013 | s2cid = 219705731 }}</ref> These [[Tablet (pharmacy)|tablets]], held within the buccal pouch, either act on the [[oral mucosa]] or are rapidly absorbed through the buccal mucosal membrane.<ref>{{cite book | veditors = Taylor JB, Triggle DJ |title=Comprehensive Medicinal Chemistry II |date=2007 |publisher=Elsevier |location=Amsterdam |isbn=978-0-08-045044-5}}</ref> Since drugs "absorbed through the buccal mucosa bypass gastrointestinal [[Enzyme|enzymatic]] degradation and hepatic [[First pass effect|first-pass effect]]",<ref name=":1">{{cite journal | vauthors = Hua S | title = Advances in Nanoparticulate Drug Delivery Approaches for Sublingual and Buccal Administration | journal = Frontiers in Pharmacology | volume = 10 | pages = 1328 | date = 2019 | pmid = 31827435 | pmc = 6848967 | doi = 10.3389/fphar.2019.01328 | doi-access = free }}</ref> prescribing buccal tablets is increasingly common among healthcare professionals. |
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Buccal tablets serve as an alternative drug delivery in patients where compliance is a known issue, including those who are [[Unconsciousness|unconscious]], [[Nausea|nauseous]], or having difficulty in swallowing (i.e. [[dysphagia]]).<ref name=":2">{{cite journal | vauthors = Chinna Reddy P, Chaitanya KS, Madhusudan Rao Y | title = A review on bioadhesive buccal drug delivery systems: current status of formulation and evaluation methods | journal = Daru | volume = 19 | issue = 6 | pages = 385–403 | date = 2011 | pmid = 23008684 | pmc = 3436075 }}</ref> A wide variety of these drugs are available on the market to be prescribed in hospitals and other healthcare settings, including common examples like Corlan®, Fentora®, and Buccastem®. |
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The most common route for drug transport through the buccal mucosa is the [[Paracellular transport|paracellular]] pathway. Most [[Hydrophile|hydrophilic]] drugs permeate the cheek linings via the paracellular pathway through the mechanism of [[passive diffusion]], and [[Hydrophobe|hydrophobic]] drugs are transported through the [[Transcellular transport|transcellular]] pathway.<ref name=":2" /> This route of administration is beneficial for [[Mucous membrane|mucosal]] administration and [[Route of administration|transmucosal]] administration.<ref name=":6"/> Buccal tablets are typically formulated through the direct compression of drug, powder mixture, swollen polymer, and other agents that assist in processing.<ref name=":6">{{cite journal | vauthors = Fonseca-Santos B, Chorilli M | title = An overview of polymeric dosage forms in buccal drug delivery: State of art, design of formulations and their in vivo performance evaluation | journal = Materials Science & Engineering. C, Materials for Biological Applications | volume = 86 | pages = 129–143 | date = May 2018 | pmid = 29525088 | doi = 10.1016/j.msec.2017.12.022 | hdl = 11449/179480 | hdl-access = free }}</ref> |
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Buccal tablets offer many advantages in terms of accessibility, ease of administration and withdrawal, and hence may improve [[patient compliance]].<ref name=":4">{{Cite journal | vauthors = Li KL, Castillo AL |date=2020-06-21 |title=Formulation and evaluation of a mucoadhesive buccal tablet of mefenamic acid |url=http://www.scielo.br/j/bjps/a/Py55RXWjYktHgNvgwQcYmvp/ |journal=Brazilian Journal of Pharmaceutical Sciences |language=en |volume=56 |doi=10.1590/s2175-97902019000418575 |s2cid=238068377 |issn=2175-9790|doi-access=free }}</ref> Notable drawbacks of buccal tablets include the hazard of choking by involuntarily swallowing the tablet and irritation of the gums.<ref name=":2" /> Caution should be exercised along with counselling from medical practitioners before use of these tablets. |
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== Clinical uses and common drug examples == |
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With recent advances on buccal tablets and in conditions where the conventional oral route (i.e. swallowing of tablet) cannot be delivered effectively, some commonly prescribed buccal tablets available in healthcare settings are listed below as examples. |
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=== Hydrocortisone === |
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[[Hydrocortisone]] is a [[corticosteroid]] that is clinically used to relieve the pain and discomfort of [[mouth ulcer]]s and functions to speed the healing of mouth ulcers.{{citation needed|date=May 2022}} Common side effects include: [[Oral candidiasis|oral thrush]], visual disturbances (e.g. [[Blurred vision|blurry vision]]), worsening of [[diabetes]], worsening of mouth [[infection]]s, and [[allergic reactions]] (e.g. skin rash). Hydrocortisone is contraindicated in patients [[Hypersensitivity|hypersensitive]] to hydrocortisone and those with mouth ulcers caused by [[dentures]] or infection as it can worsen the severity of mouth ulcers. |
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Some cautions and remarks include needing to gargle and spit water once tablet is fully dissolved to minimise risk of oral thrush, prolonged use may lead to withdrawal symptoms, chewing and swallowing of the tablet may limit its efficacy and give rise to additional side effects, and caution with [[CYP3A4]] [[Enzyme inhibitor|inhibitors]]. |
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=== Fentanyl === |
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[[Fentanyl]] is an [[opioid analgesic]] used for the treatment of [[breakthrough pain]] in [[cancer]] patients who are already receiving and/or are tolerant to maintenance opioid therapy for chronic cancer pain<ref>{{cite journal | vauthors = Blick SK, Wagstaff AJ | title = Fentanyl buccal tablet: in breakthrough pain in opioid-tolerant patients with cancer | journal = Drugs | volume = 66 | issue = 18 | pages = 2387–2393 | date = 2006-12-01 | pmid = 17181383 | doi = 10.2165/00003495-200666180-00013 | s2cid = 46963854 }}</ref><ref>{{cite journal | vauthors = Darwish M, Hamed E, Messina J | title = Fentanyl buccal tablet for the treatment of breakthrough pain: pharmacokinetics of buccal mucosa delivery and clinical efficacy | journal = Perspectives in Medicinal Chemistry | volume = 4 | pages = 11–21 | date = June 2010 | pmid = 20634985 | pmc = 2901636 | doi = 10.4137/pmc.s3928 }}</ref><ref>{{cite journal | vauthors = Kaplan S, Bergamasco A, Sergerie M, Castilloux AM, Moride Y | title = Effectiveness of Risk Minimization Measures for Fentanyl Buccal Tablet (FENTORA) in Canada: A Mixed-Methods Evaluation Using Surveys, Medical Chart Records and Web Surveillance | journal = Drug Safety | volume = 43 | issue = 2 | pages = 163–177 | date = February 2020 | pmid = 31691255 | doi = 10.1007/s40264-019-00882-7 | s2cid = 207890267 }}</ref> Common side effects include: [[nausea]], [[vomiting]], [[headache]], [[constipation]] and [[Somnolence|drowsiness]]. Fentanyl is contraindicated in patients hypersensitive to fentanyl, opioid non-tolerant patients, management of acute or [[postoperative]] pain, and those with severe [[hypotension]] or severe obstructive airway diseases (e.g. [[Chronic obstructive pulmonary disease|COPD]]) |
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Some cautions include needing to keep tablets out of the sight and reach of children, and must not be sucked, chewed or swallowed. Other remarks include caution when administered in patients with [[Hepatic impairment|hepatic or renal impairment]], having drug interactions with CYP3A4 inducers and inhibitors and co-administration with CNS [[sedative]] agents (e.g. [[antihistamine]]s) will increase CNS side effects. |
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=== Prochlorperazine maleate === |
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[[Prochlorperazine maleate]] is under the class of [[antiemetic]]s and [[antipsychotic]]s. These buccal tablets are administered for the treatment of severe nausea and vomiting associated with [[migraine]],<ref>{{cite book | vauthors = Abdul Rasool BK, Shahiwala A | chapter = Buccal and Intraoral Drug Delivery: Potential Alternative to Conventional Therapy |date=2019 | title =Novel Drug Delivery Technologies: Innovative Strategies for Drug Re-positioning |pages=29–71 | veditors = Misra A, Shahiwala A |place=Singapore |publisher=Springer |language=en |doi=10.1007/978-981-13-3642-3_3 |isbn=978-981-13-3642-3 | s2cid = 214482342 }}</ref><ref>{{Cite journal | vauthors = Gupta S, Das S, Singh A, Ghosh S |date=2021-08-15 |title=A Brief Review on Bucco-adhesive Drug Delivery System |journal=Journal of Drug Delivery and Therapeutics |language=en |volume=11 |issue=4–S |pages=231–235 |doi=10.22270/jddt.v11i4-S.4934 |s2cid=238653353 |issn=2250-1177|doi-access=free }}</ref> as well as managed in symptoms of [[schizophrenia]]. Side effects typically seen in patients using prochlorperazine maleate tablets include drowsiness, blurred vision, [[dry mouth]], and headache. In rare cases, these tablets may cause serious allergic reactions (i.e. [[anaphylaxis]]). Prochlorperazine maleate is contraindicated in certain patient groups, including hypersensitivity to prochlorperazine maleate, certain diseases like [[glaucoma]], [[epilepsy]] and [[Parkinson's disease]]. They are also avoided in those with hepatic and [[prostate gland]] problems. |
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Special caution is taken in patients with high risk of [[Thrombus|blood clot]] and [[stroke]], along with associated risk factors (e.g. [[Hypertension|high blood pressure]] and [[Hyperlipidemia|high cholesterol]] levels). Those taking prochlorperazine maleate should avoid exposure to direct sunlight due to [[photosensitivity]] and taken certain drugs that are either sedative and give dry mouth (e.g. [[anticholinergic]]s) or target the heart (e.g. [[Antihypertensive drug|antihypertensives]] and [[anticoagulant]]s). Other remarks include being most effective when taken after food and possible withdrawal symptoms if they are abruptly stopped. |
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== Mechanism of action == |
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[[File:Buccal Mucosa.png|thumb|285x285px|A figure illustrating the cross-sectional area of the buccal mucosa.]] |
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The buccal mucosa, along with the gingival and sublingual mucosa, is part of the [[oral mucosa]].<ref>{{cite journal | vauthors = Wanasathop A, Patel PB, Choi HA, Li SK | title = Permeability of Buccal Mucosa | journal = Pharmaceutics | volume = 13 | issue = 11 | pages = 1814 | date = October 2021 | pmid = 34834229 | pmc = 8624797 | doi = 10.3390/pharmaceutics13111814 | doi-access = free }}</ref> It is composed of non-keratinised tissue. Unlike intestinal and nasal mucosae, it lacks tight junctions and is instead equipped with loose intercellular links of [[desmosome]]s, [[gap junction]]s and [[hemidesmosome]]s.<ref name=":2" /> While it has a less [[Vascular permeability|permeable]] effect than [[sublingual administration]], [[buccal administration]] is still capable of creating local or [[systemic effect]]s following drug administration.<ref name=":2" /> In the oral cavity, buccal tablets potentiate their effect by entering the bloodstream direction through the [[internal jugular vein]] into the [[superior vena cava]],<ref name=":6"/> avoiding acidic [[hydrolysis]] to take place in the [[gastrointestinal tract]].<ref>{{cite journal | vauthors = Hua S | title = Advances in Nanoparticulate Drug Delivery Approaches for Sublingual and Buccal Administration | journal = Frontiers in Pharmacology | volume = 10 | pages = 1328 | date = 2019-11-05 | pmid = 31827435 | pmc = 6848967 | doi = 10.3389/fphar.2019.01328 | doi-access = free }}</ref> |
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There are two major routes for drug transportation through the buccal mucosa: transcellular and paracellular pathways.<ref name=":6"/> |
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[[File:Zoobies.png|thumb|A schematic diagram illustrating the penetration pathway for buccal drug delivery.]] |
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Small hydrophobic molecules and other lipophilic compounds mostly move across the buccal mucosa via the transcellular pathway. Drugs are transferred via the transcellular pathway through either [[facilitated diffusion]] for polar or [[ionic compound]]s, [[diffusion]] for low molecular weight molecules, or [[transcytosis]] and [[endocytosis]] for macromolecules.<ref name=":6"/> The physicochemical properties of the drug, for example, its oil/water [[partition coefficient]], [[Molecular-weight|molecular weight]], structural conformation, determines whether the molecules are transported through the transcellular pathway.<ref name=":6"/> |
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As the [[cell membrane]] is [[Lipophilicity|lipophilic]], it is more difficult for drugs that are hydrophilic to [[Permeation|permeate]] the membrane. Hence, the [[excipient]]s of the formulation and the phospholipid bilayer assist in enhancing the diffusion of hydrophilic compounds (i.e. peptides, proteins, macromolecules).<ref name=":6"/> |
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Generally, small low-molecular-weight hydrophilic compounds diffuse across the buccal epithelium through the paracellular pathway via passive diffusion. The extracellular [[Amphiphile|amphiphilic]] lipid matrix proves to be a major barrier for [[Macromolecule|macromolecular]] hydrophilic compounds.<ref name=":6" /> After the administration of the buccal tablet, it must transport either through the epithelial layers to achieve its effect on the systemic circulation (systemic effect) or remain at a target site to elicit a local effect.<ref name=":6"/> |
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== Benefits and limitations == |
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=== Benefits === |
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Buccal tablets offer many advantages over other solid dosage forms also intended for oral administration (e.g. [[Enteric coating|enteric-coated]] tablets, [[Chewable tablet|chewable]] tablets, and capsules). |
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Buccal tablets can be considered in patients who experience difficulty in swallowing, since these tablets are absorbed into the blood stream between the gum and cheek.<ref name=":5">{{cite journal | vauthors = Hua S | title = Advances in Nanoparticulate Drug Delivery Approaches for Sublingual and Buccal Administration | journal = Frontiers in Pharmacology | volume = 10 | pages = 1328 | date = 2019 | pmid = 31827435 | doi = 10.3389/fphar.2019.01328 | pmc = 6848967 | doi-access = free }}</ref><ref name=":0" /> Difficulty in swallowing can occur in all age groups, especially in young infants and the elderly community.<ref>{{cite journal | vauthors = Lau ET, Steadman KJ, Cichero JA, Nissen LM | title = Dosage form modification and oral drug delivery in older people | journal = Advanced Drug Delivery Reviews | volume = 135 | pages = 75–84 | date = October 2018 | pmid = 29660383 | doi = 10.1016/j.addr.2018.04.012 | series = Drug delivery in older people – unique challenges and important opportunities | s2cid = 4955999 | url = https://espace.library.uq.edu.au/view/UQ:727335/UQ727335_OA.pdf }}</ref> Buccal tablets are also used in unconscious patients.{{citation needed|date=June 2022}} Additionally, in the case of accidental swallowing of a buccal tablet, adverse effects are minimal as most buccal drugs cannot survive hepatic first-pass metabolism. |
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Compared to orally ingested capsules and tablets, buccal tablets provide a more rapid [[onset of action]] because the oral mucosa is highly vascularised.<ref name=":5" /><ref name=":4" /> Buccal tablets are also used in emergency situations because they can exert their effects quickly. |
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Buccal tablets directly enter the systemic circulation, bypassing the gastrointestinal tract and first-pass metabolism in the liver.<ref name=":1" /> As such, patients can take a reduced overall dose to minimise symptoms. In addition, buccal tablets can be removed if adverse reactions appear. |
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=== Limitations === |
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In general, many drugs are not suitable to be delivered via the buccal mucosa due to the small dose criteria. Buccal tablets are rarely used in healthcare settings due to unwanted properties that may limit patient compliance, for example, unpleasant taste and irritation of the oral mucosa.<ref>{{Cite journal | vauthors = Hoogstraate JA, Wertz PW |date=1998-10-01 |title=Drug delivery via the buccal mucosa |journal=Pharmaceutical Science & Technology Today |language=en |volume=1 |issue=7 |pages=309–316 |doi=10.1016/S1461-5347(98)00076-5 |issn=1461-5347}}</ref> These undesired characteristics may lead to accidental swallowing or involuntary expulsion of the buccal tablet. Buccal tablets are also not preferred for drugs that require [[Extended release|extended-release]].<ref name=":5" /> |
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Absorption of drugs via the buccal membrane may not be suitable for all patients. Due to possible undesirable side effects and loss of drug effectiveness, buccal tablets must not be crushed, chewed, or swallowed under any circumstances. As such, buccal tablets are not always appropriate for patients (e.g. individuals on [[Feeding tube|enteral tube feeding]]). It is also noted that eating, drinking or smoking should be avoided until the buccal tablet is fully dissolved to prevent drug efficacy changes and concerns of choking.<ref>{{cite journal | vauthors = Macedo AS, Castro PM, Roque L, Thomé NG, Reis CP, Pintado ME, Fonte P | title = Novel and revisited approaches in nanoparticle systems for buccal drug delivery | journal = Journal of Controlled Release | volume = 320 | pages = 125–141 | date = April 2020 | pmid = 31917295 | doi = 10.1016/j.jconrel.2020.01.006 | hdl = 10400.14/29233 | s2cid = 210120570 | hdl-access = free }}</ref> |
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== Formulation and manufacturing == |
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Buccal tablets are dry formulations that attain bioadhesion through dehydrating local mucosal surfaces.<ref name=":2" /> Many bioadhesive buccal tablet formulations are created through the direct compression method with a release retardant and swollen [[polymer]],<ref name=":6"/> and are designed to either release the drug in a unidirectional or multidirectional manner into the saliva.<ref name=":2" /> |
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Conventional dosage forms are unable to ensure therapeutic drug levels in the circulation and the mucosa for mucosal and transmucosal administration because of the washing effect of saliva, and the mechanical stress of the oral cavity.<ref name=":2" /> These two mechanisms act as a physiological removal system that removes the formulation from the mucosa, resulting in a decreased exposure time and unpredictable pharmacological profile of the drug's distribution.<ref name=":2" /> |
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This effect can be countered by prolonging the contact between the [[Active ingredient|active substance]] from the buccal tablet and the mucosa, the tablet should contain: mucoadhesive agents, penetration enhancers, [[enzyme inhibitor]]s and solubility modifiers.<ref name=":2" /> |
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The mucoadhesive agents assist in the maintenance of prolonged contact between the drug with the absorption site.<ref name=":2" /> Penetration enhancers improve the ability of the drug to permeate the mucosa for transmucosal delivery or penetrate into the layers of the epithelium for mucosal delivery. Enzyme inhibitors partake in the protection of the drug from mucosal enzyme degradation, and solubility modifiers increase the [[solubility]] of drugs that are poorly absorbed.<ref name=":2" /> |
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== References == |
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{{Reflist}} |
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[[Category:Drugs]] |
[[Category:Drugs]] |
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Latest revision as of 12:38, 1 March 2023
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