racterizes moisture sorption pro

2021/05/21

Characterizes moisture sorption properties and physical stability of lyophilized formulation in humidity, Characterization of hydrates and polymorphs, X-ray powder diffraction (XRPD)

This pre-gastric absorption can reduce side effects caused by metabolites formed by liver enzymes. Floss-based tablet technology (e.g., FlashDose, Biovail, Mississauga, ON, Canada) also is used to produce fast-dissolving tablets using a floss known as the shearform matrix (16, 21). DeRoche et al., "Consumer Preference for Orally Disintegrating Tablets Over Conventional Forms of Medication: Evolving Methodology for Medication Intake in Dysphagia," lecture presented at the 12th Annual Meeting of the Dysphagia Research Society, San Francisco, CA, Oct. 24, 2003. S.V. The formed matrix structure is very porous in nature and rapidly dissolves or disintegrates upon contact with saliva (16).

The saccharides are converted into floss by the simultaneous action of flash-melting and centrifugal force in a heat-processing machine similar to that used to make cotton candy (3743).

Initially, the polymer particles are deposited in a discrete polymer layer around the outside of the API particles, but the combination of the vibration and the impact of collision with the milling media cause these closepacked coating particles to deform into a continuous polymer layer.

Furthermore, if the drug is absorbed within the oral cavity rather than being digested, it avoids the first pass of the liver.

E.L. Hamilton and E.M. Luts, "Advanced Orally Disintegrating Tablets Bring Significant Benefits to Patients and Product Life Cycles," Drug Deliv.

Technol. The area under the curve for the low-dose ODT is equivalent to that of 10mg formulated conventionally. No liquid is required when taking the medication either, which is a significant advantage when on the go. V. Agarwal, "Fast Dispersing Dosage Forms: Opportunities and Challenges in Packaging," paper presented at the annual meeting of the AAPS, Salt Lake City, UT, Oct. 29, 2003. To make the tablets, the excipients are first dissolved or suspended in purified water, and the API added. As previously mentioned, fragile products require special unit-dose packaging, which may add to the cost.

Examples are cited in the literature in which the pharmacokinetic profiles and bioavailabilities of the same dose of drug in an ODT are not bioequivalent to the conventional oral dosage form.

40. Tablets made with this process have higher mechanical strength and are sufficiently robust to be packaged in blister packs or bottles (5, 15). 24. Cherukuri and R. Fuisz, "Process and Apparatus for Making Tablets and Tablets Made Therefrom," US Patent 5,654,003 (1997). The technology involves the direct compression of active ingredients, effervescent excipients, and taste-masking agents (27). Ghosh, "Quick Dissolving Oral Dosage Forms: Clinical Pharmacology, Biopharmaceutical, and Regulatory Considerations," paper presented at the annual meeting of the American Association of Pharmaceutical Scientists (AAPS), Salt Lake City, UT, Oct. 29, 2003. Several clinical pharmacological and biopharmaceutical aspects of ODT development also must be considered. S.V.

Ghosh and W.R. Pfister, Eds. Body weight loss, which is an indicator of the extent of the disease, was greatest for the unvaccinated and infected control group, which is demonstrated by the results shown on the lowest set of data points on the graph and shows rapid weight loss after day 2 of the study. There are many patients for whom traditional tablets and capsules are not ideal dosage forms. R.P. Myers et al.,"Delivery of Controlled-Release Systems," US Patent 5,567,439 (1996).

Scherer (now Cardinal Health), personal communication, (2005). Both ibuprofen and acetaminophen have been successfully formulated in this way to date.

Within the freeze dryer, the shelves are heated gently under a very low pressure, causing the ice crystals present in the blister pockets to sublime.

10. Particles as small as 100m can be coated, significantly smaller than the 200400 m particles that conventional coating is successful for. The future potential for ODTs is promising because of the availability of new technologies combined with strong market acceptance and patient demand. All rights reserved.

In contrast to normal coating methods, no solvent is required, and the API retains 7085% potency w/w. 3 (6), 5861 (2001). 17. This vibrates, causing the particles to move and accelerate by as much as 100 times the force of gravity. In general, an ODT is formulated as a bioequivalent line extension of an existing oral dosage form.

Chemical analysis of API in support of preformulation studies (e.g., solubility determinations, compatibility testing).

(CRC Press, New York, NY, 2005), pp.

Many APIs have an unpleasant taste or create other unappealing sensations as they are solubilized. In the graph in Figure 6, the vaccine was administered sublingually to mice before they were challenged with influenza virus. The trays are stored in a freezer until a sufficient quantity has been prepared to fill the freeze dryer, and then they are transferred into the dryer. However, if the API is suitable, then careful ODT formulation can be used to ensure the drug is absorbed in the oral cavity rather than in the gastrointestinal tract. Several alternative ODT technologies are available, as can be seen in Table 1. Wong, "Method for Making Freeze-Dried Drug Dosage Form," US Patent 5,631,023 (1997). With this new process, tablets are made by combining noncompressible fillers with a taste-masking excipient and active ingredient into a dry blend. Development work has been carried out using influenza as a model vaccine antigen. 31. *To whom all correspondence should be addressed. The frozen units are then transferred to large-scale freeze dryers for the lyophilization process.

337356. The Bio ODT also holds out promise for oral vaccines.

(CRC Press, New York, NY, 2005), pp. It is possible that these differences may, in part, be attributed to the drug molecule, formulation, or a combination of both. The coating process is initiated by the addition of a reaction initiator, which is purified water in this case.

In addition, the matrix may contain taste-masking agents such as sweeteners, flavorants, pH-adjusting agents such as citric acid, and preservatives to ensure the aqueous stability of the suspended drug in media before sublimation. W.R. Pfister and T.K.

Ghosh and W.R. Pfister, Eds. The target population has expanded to those who want convenient dosing anywhere, anytime, without water.

Additional technologies for manufacturing and packaging ODT dosage forms have been highlighted elsewhere (18, 19). The US Food and Drug Administration Center for Drug Evaluation and Research (CDER) defines in the Orange Book an ODT as "A solid dosage form containing medicinal substances, which disintegrates rapidly, usually within a matter of seconds, when placed upon the tongue" (1). As an example, the drug selegeline is a monoamine oxidase B inhibitor used to treat Parkinsons disease and depression, but its active metabolites include methamphetamine, which leads to side-effects. 9. 19. As can be seen in Figure 3, the area under curve (AUC) over time is the same for the ODT taken both with and without water, and the standard capsule formulation. This review article discusses orally disintegrating tablets and their manufacturing technologies, development issues, and future trends.

Through expert analysis and interpretation of data, our Zydisfast dissolve technology team will fully characterize your API and associated Zydisformulations throughout the development process to provide a robust data package in support of regulatory filings.

A structure former, usually mannitol chosen for its high compatibility and its well-known documented properties - is also added.

In a taste evaluation study of an ODT formulation incorporating beta-cyclodextrin, more than 80% of a group of 30 subjects judged the taste profile to be acceptable.

Prescription ODT products initially were developed to overcome the difficulty in swallowing conventional tablets with water among pediatric, geriatric, and psychiatric patients with dysphagia.

The filled trays are passed through a liquid nitrogen freeze channel, causing the API solution or suspension to freeze very rapidly. 41.

The convenience of the dosing, and the lack of requirement for cold chain storage, could permit faster distribution in pandemic and emergency situations, and would permit administration by less qualified healthcare professionals. The bulk API is formulated into a liquid solution or suspension.

The overall preclinical, clinical, and biopharmaceutical development programs necessary to support successful ANDA and NDA marketing applications for ODTs were recently reviewed (44) and presented in detail in a symposium on this topic (13, 45).

Pre-gastric absorption can have significant advantages in terms of both a faster onset of action and the reduction of side-effects. P. Kearney and S.K. The freeze-drying process involves the removal of water (by sublimation upon freeze drying) from the liquid mixture of drug, matrix former, and other excipients filled into preformed blister pockets. 27 (10 Suppl), 1013 (2003). Drug coatings also can be used to mask bitter drugs and to protect the drug from stomach acidinduced metabolism. 61 , 3637 (1990). In the most effective vaccine formulation, there was very little change in body weight across the period of monitoring. QuickSolv disintegrates very rapidly but is limited to low drug content and can be used only with active ingredients that are insoluble in the extraction solvent (36).

Careful taste-masking can greatly improve compliance by making the ODT more palatable.

S.R. Today, ODTs are more widely available as over-the-counter products for the treatment of allergies and cold and flu symptoms. K. Cremer, "Orally Disintegrating Dosage Forms Provide Drug Life Cycle Management Opportunities," Pharm.

Wilkosz, and C.T. Technol.

Iles et al., "Freeze-Dried Dosage Forms and Methods for Preparing the Same," US Patent 5,188,825 (1993).

In yet another modification, a solution of soluble drug can be sprayed onto a preformed matrix, following which the solvent is evaporated (8, 32). 261290.

Possible benefits of orally disintegrating tablet drugs. Copyright 2022 CompareNetworks, Inc. All rights reserved. 13.

Conventional tablet process. ODTs release drug in the mouth for absorption through local oromucosal tissues and through pregastric (e.g., oral cavity, pharynx, and esophagus), gastric (i.e., stomach), and postgastric (e.g., small and large intestines) segments of the gastrointestinal tract (GIT). N. Sharma et al., "Manufacturing Technology Choices for Mouth Dissolving Tablets," Pharm. As with all ODTs, products made with this process disintegrate in the mouth in 545 seconds and can be formulated to be bioequivalent to conventional tablet dosage forms (5).