Orally Disintegrating Systems: Innovations in Formulation and Technology

Abstract

Orally disintegrating systems have carved a niche amongst the oral drug delivery systems due to the highest component of compliance they enjoy in patients especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to with stand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. Therefore, research in developing orally disintegrating systems has been aimed at investigating different excipients as well as techniques to meet these challenges. A variety of dosage forms like tablets, films, wafers, chewing gums, microparticles, nanoparticles etc. have been developed for enhancing the performance attributes in the orally disintegrating systems. Advancements in the technology arena for manufacturing these systems include the use of freeze drying, cotton candy, melt extrusion, sublimation, direct compression besides the classical wet granulation processes. Taste masking of active ingredients becomes essential in these systems because the drug is entirely released in the mouth. Fluid bed coating, agglomeration, pelletization and infusion methods have proven useful for this purpose. It is important to note that although, freeze dried and effervescent disintegrating systems rapidly disintegrate in contact with fluids, they do not generally exhibit the required mechanical strength. Similarly, the candy process cannot be used for thermolabile drugs. In the light of the paradoxical nature of the attributes desired in orally disintegrating systems (high mechanical strength and rapid disintegration), it becomes essential to study the innovations in this field and understand the intricacies of the different processes used for manufacturing these systems. This article attempts at discussing the patents relating to orally disintegrating systems with respect to the use of different formulation ingredients and technologies.

Formulation of an anti-inflammatory drug as fast dissolving tablets

“…Micromeretic properties of the prepared physical mixtures of ketorolac tromethamine showed good compressibility and flowability behavior as indicated from their compressibility index, angle of repose and Hausner's ratio. These results were in agreement with standard requirements of USP as shown in table (2). Also, uniformity of particle size of the drug-excipient blends signified good homogeneity and uniformity during mixing and granulation processes as shown in figure (1).…”

“…All the prepared tablets had acceptable hardness in the range from (3.133 ± 0.404 Kp) to (5.967 ± 0.764 Kp) as graphically represented in figure (2). All the prepared tablets are with acceptable friability less than 1% as shown in figure (3).…”

“…Different approaches are used for development of fast dissolving tablets such as using superdisintegrants namely croscarmellose sodium,crospovidone and sodium starch glycolate. Another approach, maximaizes the porous structure of tablet by sublimation method .Vacuum drying has been used to form porous structure of tablets (2)(3) .Ketorolac tromethamine is a non steroidal anti-inflammatory drug commonly used to decrease post operative pain associated with surgical treatment (4) Ketorolac tromethamine is found to be as effective as morphine for postoperative pain in children with fewer side effects (5) .…”

An Electronic Tongue: Evaluation of the Masking Efficacy of Sweetening and/or Flavoring Agents on the Bitter Taste of Epinephrine

“…ASP, a first-generation artificial sweetener, enhances flavor systems and can be used to mask some unpleasant taste characteristics. It is widely used in medications including Feldene Melt (piroxicam), Maxalt-MLT (rizatriptan), Pepcid RPD (famotidine), Zyprexa Zydis (olanzapine), Zofran ODT (ondansetron), and Nulev (hyoscyamine) (22). ASK, a second-or new-generation artificial sweetener, is widely used as a sugar substitute in compounded formulations and as a toothpaste sweetener (21).…”

“…CA is widely used in a number of FDA approved products available in the market like Remeron Soltab (mirtazepine) and Zoming ZMT (zolmitriptan) (22).…”