Time taken for the ODT to pass through the wire cloth considered as disintegration time, Charge coupled device (CCD) camera method, Disintegration of ODT placed on a grid placed over a stirring element contained in a dissolution medium. Time required by the ODT to pass through sinker screen, Water dropped at a rate of 4ml/min over the ODT placed in wire cloth No. The bioavailability of ODTs is mostly comparable with that of other oral dosage forms such as conventional tablets and capsules, and bioequivalence has already been demonstrated for selected formulations. This research received no specific grant from any funding agency in the public, commercial or not-for-profit sectors. Orally disintegrating tablets, fast-diss . : Issue Theme: Orally disintegrating tablets, fast-dissolving, buccal and sublingual formulations, comoglu@pharmacy.ankara.edu.tr tcomoglu@yahoo.com, Medicine, Dentistry, Nursing & Allied Health. defines them as uncoated tablets intended to be placed in the mouth where they disperse rapidly before being swallowed. He has worked within R&D for more than 15 years, primarily on Catalents Zydis ODT technology formulation and process development. He has worked within R&D for more than 15 years, primarily on Catalents Zydis, is Catalent Pharma Solutions Group Product Manager for Drug Delivery Solutions. US patent application 20010014340, Oxford University Press is a department of the University of Oxford. The taste-masking is provided by the presence of a coating around particles of the API, which can be as small as 100 m in size. Catalents Zydis Bio technology was developed as a way of achieving oral delivery of biologics. November 1-3 He is responsible for driving the global marketing strategy for the oral drug delivery solutions business unit, including patient-centric Solutions, Zydis.
And, importantly, the two are bioequivalent. Registered in England & Wales No. [6] The physiological conditions of the oral cavity should be considered for in-vivo testing, including the biopharmaceutical properties of the API at a salivary pH of 5.57,[7,8] salivary flow rate and chronobiological state of the target population. In a study commissioned by Hermes Pharma and conducted by Spiegel Institut Mannheim based on 2,000 individuals in Germany and North America (www.epmmagazine.com accessed Sep.23, 2016). But where it is feasible, if the ODT is designed correctly, then it is possible to ensure that the active will be absorbed buccally or sublingually, without being swallowed. [5] Agitation speeds as low as 25 rev/min using paddle and 50 rev/min for basket (USP I) apparatus have been recommended for certain ODT formulations. X-ray diffraction is used to determine the crystalline state of the API and relevant excipients; whether it is crystalline or amorphous will have a bearing on the structural integrity of the final dosage forms. Boston, MA, CPhI Worldwide In addition, ODTs provide clinical advantages such as improved safety and, in some cases, improved efficacy. Disintegration of the dosage form in the oral cavity followed by wetting is the primary requisite for ODTs to release the API. The orally disintegrating tablet, or ODT, offers an easy-to-take alternative form to consumers of over-the-counter (OTC) treatments who perhaps do not have access to water, and patients of prescribed drugs who cannot, or will not, swallow standard oral dosage forms, such as tablets and capsules. 1.
By avoiding the need for injection, there would be none of the pain, and potential for injection site reactions, that can engender reluctance to immunization among patients and parents. The ability to deliver pre-gastrically depends very much on the molecular weight, lipophilicity, and required dose level of the API.
[2] The United States Food and Drug Administration (FDA) Center for Drug Evaluation and Research (CDER) drafted a guidance which states ODTs as a solid dosage form containing medicinal substances, which disintegrates rapidly, usually within a matter of seconds, when placed upon the tongue. One way this can be achieved is via the Zydis Ultra formulation. The similarity factor (f2) value for product A at pH 6.8 was 66.19, and for product B at pH 1.2 was 79.42. Furthermore, they facilitate drug loading and are expected to remain unaffected by changes in humidity or temperature. However, these dosage forms require more than 1 min to disintegrate in the oral cavity[6] or do not disintegrate at all. Orally disintegrating tablets are generally characterized by their high porosity, low density and low tensile strength. The peptide drug calcitonin has been successfully formulated in this way, and vaccine ODTs could be particularly important in the future. When a drug is absorbed within the mouth, it enters the bloodstream directly, thus avoiding the first-pass metabolism by the liver, where side-effect-causing metabolites may be formed. The API still has 70%-85% potency w/w compared to uncoated particles. The mucosal response that can occur is a further benefit in immunizations against infections, such as human papillomavirus, influenza, and pneumonia. Due to the nature of the dosage form and the existing standardized equipment, conventional methods of dissolution testing[48] could be extended to ODTs. October 18-19 Orally disintegrating tablets or orodispersible tablets (ODTs) are solid oral dosage forms intended to disintegrate and disperse in the oral cavity prior to drug release, independent of the site of absorption.
Such physical properties of the dosage form necessitate stringent methods to ensure the quality of the end product. In-vitro dissolution test. These techniques are lyophilization, tablet moulding, sublimation, spray drying, flash heat process and films.
These include Catalents Zydis ODTs, which are made via freeze-drying technology, and others, such as loosely compressed tablets. All Rights Reserved.
Dissolution recommendations are also given in the FDA (CDER) dissolution database for ODTs. In order to test the applicability of the compendial USP disintegration method[47] for ODTs, two different commercially available ODT products containing a non-steroidal anti-inflammatory drug (product A) and a centrally acting drug (product B) were chosen. (b) Product A after a disintegration time of 60 s. (c) Product B before disintegration.
This is particularly important for biologic products, such as vaccines, that are destined for developing countries, where access to refrigeration cannot be relied upon, and in pandemic situations, where speed of distribution is key to success. Due to their very short disintegration time this is not an important factor in the resulting dissolution profile. October 24-25 It furthers the University's objective of excellence in research, scholarship, and education by publishing worldwide, This PDF is available to Subscribers Only.
There are several factors to be considered in formulating ODT products. Superdisintegrants, such as crosscarmellose sodium, starch glycolate and crospovidone, are responsible for rapid dissolution in the mouth.
Besides identity, purity and assay, additional product quality tests are used by manufacturers to reflect the quality of the dosage form. ODTs have become a standard dosage form for a number of medicines, where the fast onset of action or ease of dosing are important. The basket with the ODT was then placed for 60 s in a 30-ml beaker, containing 10 ml of buffer solution at pH 6.8. The choice of packaging materials is important, and each blister strip is sealed using specially designed, multi-layer foils that are resistant to moisture ingress. This delivery route extends numerous advantages over the other delivery routes such as oral, parenteral and dermal, due to its rich blood supply, rapid onset of action, avoidance of the first pass metabolism as well as enzymatic degradation, which results in enhanced bioavailability, increased patient compliance, and ease of self-medication. If a patient-friendly ODT is to be created, then more creative formulation methods will have to be applied. [4] The FDA's dissolution database[5] contains 23 dissolution/drug release methods for ODTs, which constitutes about 4% of all dissolution tests listed. Fax: (973) 299-7937.
As an example, a beta-cyclodextrin ODT formulation was created of the very bitter tasting antihistamine, cetirizine. [3] Thus, the results of the disintegration test allow a given product to be categorized as an ODT formulation. Another technique, dynamic vapor sorption, is used to determine the moisture sorption and desorption profiles. Given the very fast disintegration of ODTs, the relationship between disintegration and dissolution is worthy of closer scrutiny. Hygroscopicity of most formulations also leads to special packaging requirements for ODTs. ODTs are designed to disperse quickly within the oral cavity, removing the need to swallow a solid tablet or capsule. It may be waived on a product-by-product basis. More than three-quarters of a test group claimed its taste profile was acceptable and that the reformulated product incorporating Zydis technology was more pleasant tasting than the standard formulation. The FDA's perspective is to define ODTs based on the product characteristics, despite the fact that many other dosage forms possess a disintegration behaviour with or without the aid of mechanical stress or liquids. Hence, disintegration testing is usually insufficient to judge product performance of COSDFs. Chewable Oral Drug Products: What's New with In Vitro Drug Release? The ingredients are all dissolved or suspended in water, accurately dosed into blister trays, and then frozen in liquid nitrogen freeze tunnels before being placed in freeze dryers.
Copyright 2018-2022 Drug Development & Delivery. Acceptance for a waiver of dissolution by disintegration for ODTs could only be extended based on the procedure described in the ICH Harmonised Tripartite Guideline Q6A decision tree #7. Eur.) The prospect of formulating biologics as ODTs offers even more promise for the dose form. The objective of dissolution testing is to ensure the complete release of the drug into the medium within a reasonable amount of time. This has been proven with ibuprofen, which, if formulated as an ODT, could offer significant advantage to consumers in speed of onset. A summary of the investigation and the test results are given in Table 4. Recent market studies indicate that more than half of the patient population prefers orally disintegrating dosage forms and most consumers would ask their doctors for ODTs (70%), purchase ODTs (70%). (a) Product A before disintegration.
The similarity test (f2) statistic confirmed the similarity of the dissolution profiles at the respective pH values of 1.2 and 6.8. Zydis technology has been used to formulate a number of commercial products, particularly those for which a fast onset of action is beneficial. [27,28], Extra measures such as special blister packs are required to avoid breakage or damage of dosage forms before use. Non-compendial disintegration method. Also, in the case of ODTs, the active pharmaceutical ingredient (API) is intended to remain in the oral cavity after the disintegration, to be dissolved or dispersed in the saliva, and then absorbed via the oral mucosa for local or systemic therapy or subsequently swallowed and then absorbed through the gastrointestinal tract. A number of technologies are available to create ODTs.
10. 219 Changebridge Road Many new excipients have improved physical, mechanical and/or chemical properties to solve formulation challenges. Figure 4 shows that the lower-dose ODT produces the same area under curve (AUC) as a conventionally formulated selegeline tablet. When the vibrator is activated, the contents begin to accelerate rapidly, and the polymer is deposited around the API. There are regional variations in the thickness of the epithelium that can be exploited; the sublingual epithelium is typically 100-200 m, while the buccal membrane is thicker, at 500-800 m. By closing this message, you are consenting to our use of cookies. Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine. If they can be delivered through the mucous membranes in the mouth, they could enter the bloodstream undamaged as the acidity of saliva is normally close to neutral, and none of the protease enzymes that digest proteins are present. Johannes Kraemer, Jayachandar Gajendran, Alexis Guillot, Julian Schichtel, Akif Tuereli, Dissolution testing of orally disintegrating tablets, Journal of Pharmacy and Pharmacology, Volume 64, Issue 7, July 2012, Pages 911918, https://doi.org/10.1111/j.2042-7158.2012.01473.x. It is inferred from the results that for the test ODT formulations, prior disintegration has no influence on the release behaviour. The vibration and collisions within the mixer result in a continuous polymer layer being formed. Moreover, the presence of a large volume of medium and the mechanical agitation does not accurately reflect the disintegration environment in vivo. Small displacements of the piston and disintegration rate are measured, With prior disintegration, pH6.8, 500ml, With prior disintegration, pH1.2, 500ml, Copyright 2022 Royal Pharmaceutical Society. For example, fast disintegrating, fast melting and mouth dissolving tablets are all categorized as ODTs. When referring to ODTs, the differences to other oral dosage forms having similar product characteristics, for example with respect to the site and route of application, the release behaviour should be clearly understood. Intrabuccaly rapidly disintegrating tablet. Cyclodextrins are sugar-based, ring-shaped macromolecules with holes in the middle that can trap smaller molecules inside if they are the right size. Given the very short disintegration time of ODTs, the dissolution is independent of the disintegration time. Samples were withdrawn at the end of the disintegration and the amount of drug released into the medium was analysed. Several process techniques can be involved in production of ODTs.
No solvent is needed for this coating process.
This could be particularly beneficial if those ingredients were otherwise incompatible, whether it were two different APIs or an API and an excipient, for example, vitamins B and C; and the artificial sweetener, aspartame, which is unstable above pH 6.5 and so is incompatible with many basic excipients and APIs, such as calcium carbonate. Some APIs, even if these properties are favorable, are still not suitable for pre-gastric absorption.
It can be easier to give a medication to a child using an ODT and of course, in the animal health arena, it can be a significant challenge to get pets or livestock to swallow tablets. These points can be summarized[25,26] as follows: (1) do not require water to swallow and should dissolve or disintegrate in the mouth within a few seconds; (2) allow high drug loading and compatible with taste-masking and other excipients; (3) have a pleasant mouth feel and leave minimal or no residue in the mouth after oral administration; (4) avoid local irritations in particular if used for longterm treatment; (5) exhibit low sensitivity to humidity and temperature; (6) be adaptable and amenable to existing processing and packing machinery; and (7) have sufficient strength towithstand the rigors of the manufacturing process and post-manufacturing handling. The composition of saliva produced at varying rates of secretion by the same person with special reference to calcium and phosphorus, A New Method of Characterizing the Buccal Dissolution of Drugs, The composition of unstimulated whole saliva of healthy dental students. October 16-19 For product B, after the disintegration test, gel formation was observed due to the presence of gelatin in the matrix. He earned his BSc in Pharmaceutical Science from the University of Greenwich, London and his Masters in Industrial Pharmaceutical Science from the University of Manchester, UK. Time for the probe to penetrate into the ODT is measured, Application of very low force (10mN) to the ODT placed on holder followed by an addition of 5ml of aqueous medium. Many taste unpleasant, or can produce burning, numbing, or tingling sensations.
The procedure is based on the compendial disintegration test described by the USP, but other equivalent approaches providing similar results may be used. The drug release was complete for both products A and B within the tested time. For this reason, sublingual tablet formulations should be designed to disintegrate and dissolve rapidly in saliva, without the aid of water. If the taste of the active ingredient, or the sensation it generates on the tongue, is not too unpleasant, the simple strategy of including flavor ingredients and sweeteners in the formulation can be sufficient to make it acceptable to patients. Recently, higher doses of up to 200 mg have been launched, and peptide and protein products formulated in this way are also available.
We hope that the scientists will benefit from reading the recent advances in the field of oral mucosal delivery contained in this issue. In this issue, readers will have the opportunity to explore examples of the recent studies in this area. In the future, it is expected that new quality control methods for ODTs will be developed to accommodate more specifically the technological aspects of these pharmaceutical dosage forms. As an ODT is designed to reside in the mouth for only a number of seconds; it cannot avoid the taste buds. [711] Several initiatives are underway to standardize the test methods for these novel dosage forms. For full access to this pdf, sign in to an existing account, or purchase an annual subscription. [23], Since their introduction, ODTs have become widely accepted dosage forms, especially for paediatric and geriatric patients. [1215], The objective of ODTs is to provide a suspension of the dosage form after disintegration for further dissolution/drug release and absorption. Did you know that with a free Taylor & Francis Online account you can gain access to the following benefits? Orodispersible formulations have also been named as orally disintegrating, orodisperse, mouth-dissolving, quick-dissolve, fast-melt and rapid-disintegrating and freeze-dried formulations. This helps inform the choice of packaging and formulation characteristics, allowing the products to be marketed in all geographic regions, including those where high humidity is common.
And, importantly, the two are bioequivalent. Registered in England & Wales No. [6] The physiological conditions of the oral cavity should be considered for in-vivo testing, including the biopharmaceutical properties of the API at a salivary pH of 5.57,[7,8] salivary flow rate and chronobiological state of the target population. In a study commissioned by Hermes Pharma and conducted by Spiegel Institut Mannheim based on 2,000 individuals in Germany and North America (www.epmmagazine.com accessed Sep.23, 2016). But where it is feasible, if the ODT is designed correctly, then it is possible to ensure that the active will be absorbed buccally or sublingually, without being swallowed. [5] Agitation speeds as low as 25 rev/min using paddle and 50 rev/min for basket (USP I) apparatus have been recommended for certain ODT formulations. X-ray diffraction is used to determine the crystalline state of the API and relevant excipients; whether it is crystalline or amorphous will have a bearing on the structural integrity of the final dosage forms. Boston, MA, CPhI Worldwide In addition, ODTs provide clinical advantages such as improved safety and, in some cases, improved efficacy. Disintegration of the dosage form in the oral cavity followed by wetting is the primary requisite for ODTs to release the API. The orally disintegrating tablet, or ODT, offers an easy-to-take alternative form to consumers of over-the-counter (OTC) treatments who perhaps do not have access to water, and patients of prescribed drugs who cannot, or will not, swallow standard oral dosage forms, such as tablets and capsules. 1.
By avoiding the need for injection, there would be none of the pain, and potential for injection site reactions, that can engender reluctance to immunization among patients and parents. The ability to deliver pre-gastrically depends very much on the molecular weight, lipophilicity, and required dose level of the API.
[2] The United States Food and Drug Administration (FDA) Center for Drug Evaluation and Research (CDER) drafted a guidance which states ODTs as a solid dosage form containing medicinal substances, which disintegrates rapidly, usually within a matter of seconds, when placed upon the tongue. One way this can be achieved is via the Zydis Ultra formulation. The similarity factor (f2) value for product A at pH 6.8 was 66.19, and for product B at pH 1.2 was 79.42. Furthermore, they facilitate drug loading and are expected to remain unaffected by changes in humidity or temperature. However, these dosage forms require more than 1 min to disintegrate in the oral cavity[6] or do not disintegrate at all. Orally disintegrating tablets are generally characterized by their high porosity, low density and low tensile strength. The peptide drug calcitonin has been successfully formulated in this way, and vaccine ODTs could be particularly important in the future. When a drug is absorbed within the mouth, it enters the bloodstream directly, thus avoiding the first-pass metabolism by the liver, where side-effect-causing metabolites may be formed. The API still has 70%-85% potency w/w compared to uncoated particles. The mucosal response that can occur is a further benefit in immunizations against infections, such as human papillomavirus, influenza, and pneumonia. Due to the nature of the dosage form and the existing standardized equipment, conventional methods of dissolution testing[48] could be extended to ODTs. October 18-19 Orally disintegrating tablets or orodispersible tablets (ODTs) are solid oral dosage forms intended to disintegrate and disperse in the oral cavity prior to drug release, independent of the site of absorption.
Such physical properties of the dosage form necessitate stringent methods to ensure the quality of the end product. In-vitro dissolution test. These techniques are lyophilization, tablet moulding, sublimation, spray drying, flash heat process and films.
These include Catalents Zydis ODTs, which are made via freeze-drying technology, and others, such as loosely compressed tablets. All Rights Reserved.
Dissolution recommendations are also given in the FDA (CDER) dissolution database for ODTs. In order to test the applicability of the compendial USP disintegration method[47] for ODTs, two different commercially available ODT products containing a non-steroidal anti-inflammatory drug (product A) and a centrally acting drug (product B) were chosen. (b) Product A after a disintegration time of 60 s. (c) Product B before disintegration.
This is particularly important for biologic products, such as vaccines, that are destined for developing countries, where access to refrigeration cannot be relied upon, and in pandemic situations, where speed of distribution is key to success. Due to their very short disintegration time this is not an important factor in the resulting dissolution profile. October 24-25 It furthers the University's objective of excellence in research, scholarship, and education by publishing worldwide, This PDF is available to Subscribers Only.
There are several factors to be considered in formulating ODT products. Superdisintegrants, such as crosscarmellose sodium, starch glycolate and crospovidone, are responsible for rapid dissolution in the mouth.
Besides identity, purity and assay, additional product quality tests are used by manufacturers to reflect the quality of the dosage form. ODTs have become a standard dosage form for a number of medicines, where the fast onset of action or ease of dosing are important. The basket with the ODT was then placed for 60 s in a 30-ml beaker, containing 10 ml of buffer solution at pH 6.8. The choice of packaging materials is important, and each blister strip is sealed using specially designed, multi-layer foils that are resistant to moisture ingress. This delivery route extends numerous advantages over the other delivery routes such as oral, parenteral and dermal, due to its rich blood supply, rapid onset of action, avoidance of the first pass metabolism as well as enzymatic degradation, which results in enhanced bioavailability, increased patient compliance, and ease of self-medication. If a patient-friendly ODT is to be created, then more creative formulation methods will have to be applied. [4] The FDA's dissolution database[5] contains 23 dissolution/drug release methods for ODTs, which constitutes about 4% of all dissolution tests listed. Fax: (973) 299-7937.
As an example, a beta-cyclodextrin ODT formulation was created of the very bitter tasting antihistamine, cetirizine. [3] Thus, the results of the disintegration test allow a given product to be categorized as an ODT formulation. Another technique, dynamic vapor sorption, is used to determine the moisture sorption and desorption profiles. Given the very fast disintegration of ODTs, the relationship between disintegration and dissolution is worthy of closer scrutiny. Hygroscopicity of most formulations also leads to special packaging requirements for ODTs. ODTs are designed to disperse quickly within the oral cavity, removing the need to swallow a solid tablet or capsule. It may be waived on a product-by-product basis. More than three-quarters of a test group claimed its taste profile was acceptable and that the reformulated product incorporating Zydis technology was more pleasant tasting than the standard formulation. The FDA's perspective is to define ODTs based on the product characteristics, despite the fact that many other dosage forms possess a disintegration behaviour with or without the aid of mechanical stress or liquids. Hence, disintegration testing is usually insufficient to judge product performance of COSDFs. Chewable Oral Drug Products: What's New with In Vitro Drug Release? The ingredients are all dissolved or suspended in water, accurately dosed into blister trays, and then frozen in liquid nitrogen freeze tunnels before being placed in freeze dryers.
Copyright 2018-2022 Drug Development & Delivery. Acceptance for a waiver of dissolution by disintegration for ODTs could only be extended based on the procedure described in the ICH Harmonised Tripartite Guideline Q6A decision tree #7. Eur.) The prospect of formulating biologics as ODTs offers even more promise for the dose form. The objective of dissolution testing is to ensure the complete release of the drug into the medium within a reasonable amount of time. This has been proven with ibuprofen, which, if formulated as an ODT, could offer significant advantage to consumers in speed of onset. A summary of the investigation and the test results are given in Table 4. Recent market studies indicate that more than half of the patient population prefers orally disintegrating dosage forms and most consumers would ask their doctors for ODTs (70%), purchase ODTs (70%). (a) Product A before disintegration.
The similarity test (f2) statistic confirmed the similarity of the dissolution profiles at the respective pH values of 1.2 and 6.8. Zydis technology has been used to formulate a number of commercial products, particularly those for which a fast onset of action is beneficial. [27,28], Extra measures such as special blister packs are required to avoid breakage or damage of dosage forms before use. Non-compendial disintegration method. Also, in the case of ODTs, the active pharmaceutical ingredient (API) is intended to remain in the oral cavity after the disintegration, to be dissolved or dispersed in the saliva, and then absorbed via the oral mucosa for local or systemic therapy or subsequently swallowed and then absorbed through the gastrointestinal tract. A number of technologies are available to create ODTs.
10. 219 Changebridge Road Many new excipients have improved physical, mechanical and/or chemical properties to solve formulation challenges. Figure 4 shows that the lower-dose ODT produces the same area under curve (AUC) as a conventionally formulated selegeline tablet. When the vibrator is activated, the contents begin to accelerate rapidly, and the polymer is deposited around the API. There are regional variations in the thickness of the epithelium that can be exploited; the sublingual epithelium is typically 100-200 m, while the buccal membrane is thicker, at 500-800 m. By closing this message, you are consenting to our use of cookies. Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine. If they can be delivered through the mucous membranes in the mouth, they could enter the bloodstream undamaged as the acidity of saliva is normally close to neutral, and none of the protease enzymes that digest proteins are present. Johannes Kraemer, Jayachandar Gajendran, Alexis Guillot, Julian Schichtel, Akif Tuereli, Dissolution testing of orally disintegrating tablets, Journal of Pharmacy and Pharmacology, Volume 64, Issue 7, July 2012, Pages 911918, https://doi.org/10.1111/j.2042-7158.2012.01473.x. It is inferred from the results that for the test ODT formulations, prior disintegration has no influence on the release behaviour. The vibration and collisions within the mixer result in a continuous polymer layer being formed. Moreover, the presence of a large volume of medium and the mechanical agitation does not accurately reflect the disintegration environment in vivo. Small displacements of the piston and disintegration rate are measured, With prior disintegration, pH6.8, 500ml, With prior disintegration, pH1.2, 500ml, Copyright 2022 Royal Pharmaceutical Society. For example, fast disintegrating, fast melting and mouth dissolving tablets are all categorized as ODTs. When referring to ODTs, the differences to other oral dosage forms having similar product characteristics, for example with respect to the site and route of application, the release behaviour should be clearly understood. Intrabuccaly rapidly disintegrating tablet. Cyclodextrins are sugar-based, ring-shaped macromolecules with holes in the middle that can trap smaller molecules inside if they are the right size. Given the very short disintegration time of ODTs, the dissolution is independent of the disintegration time. Samples were withdrawn at the end of the disintegration and the amount of drug released into the medium was analysed. Several process techniques can be involved in production of ODTs.
No solvent is needed for this coating process.
This could be particularly beneficial if those ingredients were otherwise incompatible, whether it were two different APIs or an API and an excipient, for example, vitamins B and C; and the artificial sweetener, aspartame, which is unstable above pH 6.5 and so is incompatible with many basic excipients and APIs, such as calcium carbonate. Some APIs, even if these properties are favorable, are still not suitable for pre-gastric absorption.
It can be easier to give a medication to a child using an ODT and of course, in the animal health arena, it can be a significant challenge to get pets or livestock to swallow tablets. These points can be summarized[25,26] as follows: (1) do not require water to swallow and should dissolve or disintegrate in the mouth within a few seconds; (2) allow high drug loading and compatible with taste-masking and other excipients; (3) have a pleasant mouth feel and leave minimal or no residue in the mouth after oral administration; (4) avoid local irritations in particular if used for longterm treatment; (5) exhibit low sensitivity to humidity and temperature; (6) be adaptable and amenable to existing processing and packing machinery; and (7) have sufficient strength towithstand the rigors of the manufacturing process and post-manufacturing handling. The composition of saliva produced at varying rates of secretion by the same person with special reference to calcium and phosphorus, A New Method of Characterizing the Buccal Dissolution of Drugs, The composition of unstimulated whole saliva of healthy dental students. October 16-19 For product B, after the disintegration test, gel formation was observed due to the presence of gelatin in the matrix. He earned his BSc in Pharmaceutical Science from the University of Greenwich, London and his Masters in Industrial Pharmaceutical Science from the University of Manchester, UK. Time for the probe to penetrate into the ODT is measured, Application of very low force (10mN) to the ODT placed on holder followed by an addition of 5ml of aqueous medium. Many taste unpleasant, or can produce burning, numbing, or tingling sensations.
The procedure is based on the compendial disintegration test described by the USP, but other equivalent approaches providing similar results may be used. The drug release was complete for both products A and B within the tested time. For this reason, sublingual tablet formulations should be designed to disintegrate and dissolve rapidly in saliva, without the aid of water. If the taste of the active ingredient, or the sensation it generates on the tongue, is not too unpleasant, the simple strategy of including flavor ingredients and sweeteners in the formulation can be sufficient to make it acceptable to patients. Recently, higher doses of up to 200 mg have been launched, and peptide and protein products formulated in this way are also available.
We hope that the scientists will benefit from reading the recent advances in the field of oral mucosal delivery contained in this issue. In this issue, readers will have the opportunity to explore examples of the recent studies in this area. In the future, it is expected that new quality control methods for ODTs will be developed to accommodate more specifically the technological aspects of these pharmaceutical dosage forms. As an ODT is designed to reside in the mouth for only a number of seconds; it cannot avoid the taste buds. [711] Several initiatives are underway to standardize the test methods for these novel dosage forms. For full access to this pdf, sign in to an existing account, or purchase an annual subscription. [23], Since their introduction, ODTs have become widely accepted dosage forms, especially for paediatric and geriatric patients. [1215], The objective of ODTs is to provide a suspension of the dosage form after disintegration for further dissolution/drug release and absorption. Did you know that with a free Taylor & Francis Online account you can gain access to the following benefits? Orodispersible formulations have also been named as orally disintegrating, orodisperse, mouth-dissolving, quick-dissolve, fast-melt and rapid-disintegrating and freeze-dried formulations. This helps inform the choice of packaging and formulation characteristics, allowing the products to be marketed in all geographic regions, including those where high humidity is common.