A REVIEW: FORMULATION OF FAST DISSOLVING TABLET

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ABOUT AUTHORS:
Patel Zinkal K.*, Patel Rahul R, Dr Kanu R Patel, Dr Mukesh R Patel
Department of Pharmaceutics,
Shri B.M. Shah College of Pharmaceutical Education and Research
Dhansura Road College campus Modasa, Dist:- Arvali. Pin code:- 383315 Gujarat, (india)
*zinkal.pharm27@yahoo.in, rahulrpatel21089@yahoo.com

ABSTRACT
As pharmaceutical scientists are attaining a better understanding of biochemical and physicochemical properties related to the drug action, the drug delivery systems are becoming simple. Recent advances in Novel Drug Delivery Systems (NDDS) aim for designing dosage forms, convenient to be manufactured and administered, free of side effects, offering immediate release and enhanced bioavailability, so as to achieve better patient compliance Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the safest, most convenient and most economical method of drug delivery. Fast dissolving tablet is designed to allow administration of an oral solid dose form in the absence of water or fluid intake. Such tablets when put on the tongue. it readily dissolve or disintegrate in the saliva without chewing or water within <60 seconds. Fast- or mouth dissolving tablets have been formulated for pediatric, geriatric, and bedridden patients and for active patients who are busy and traveling and may not have access to water. This review includes requirements for fast disintegrating tablets, sailent features, advantages, limitations, challenges in formulation, various technologies developed for fast disintegrating tablets, patented technologies, evaluation methods and various marketed products.

REFERENCE ID: PHARMATUTOR-ART-2126

PharmaTutor (ISSN: 2347 - 7881)

Volume 2, Issue 3

Received On: 30/01/2014; Accepted On: 06/02/2014; Published On: 05/03/2014

How to cite this article: ZK Patel, RR Patel, KR Patel, MR Patel, A Review: Formulation of Fast Dissolving Tablet, PharmaTutor, 2014, 2(3), 30-46

INTRODUCTION OF THE DOSAGE FORM
Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the safest, most convenient and most economical method of drug delivery. Oral route of drug administration become popular route for systemic effects due to ease of ingestion, accurate dosage, self-medication, pain avoidance. Fast dissolving drug delivery system are Novel Drug Delivery techniques aim for designing dosage forms, convenient to be manufacture and administer without water, free of side effects, offering immediate release and enhanced bioavailability, so as to achieve better patient compliance.1 This segment of formulation is especially designed for  pediatric, geriatric,  bedridden, psychotic  patients who are unable to swallow or refuse to swallow conventional oral formulation and  also for active patients who are busy and traveling and may not have access to water.United states Food And DrugAdministration (FDA) defined fast dissolving tablet (FDT) as “a solid dosage form containing medicinal substance or active ingredient which disintegrate or dissolve rapidly  within seconds when placed upon the tongue.” Fast dissolving tablets are also known as mouth-dissolving tablets, rapid dissolving, melt-in mouth tablets, Orodispersible tablets, rapimelts, porous tablets, quick dissolving, quick melt, quick disintegrating tablets.2

Figure: 1.1 Timely comparisons between Conventional & Fast dissolving tablet

CRITERIA FOR FAST DISSOLVING DRUG DELIVERY SYSTEM3
The tablets should:

  • Not require water to swallow, but it should dissolve or disintegrate in the mouth within a seconds.
  • Be competible with taste masking.
  • Have a pleasant mouth feel.
  • Leave minimum or no residue in the mouth after oral administration.
  • Exhibit low sensitive to environmental condition as temperature and humidity.4
  • Allow the manufacture of the tablet using conventional processing and packaging equipments at low cost.
  • Allow high drug loading.

ADVANTAGES  OF FDT 5

  • Ease of Administration to the patient who cannot swallow and therefore Improved patient compliance
  • No water needed. which is useful for patients who are traveling and do not have immediate access to water.
  • Rapid dissolution, absorption  of the drug and hence increase bioavailability
  • Pregastric absorption of drug can increase oral bioavailability of drug, and as a result of reduces dose administration.
  • The risk of chocking or suffocation during oral administration of conventional formulation due to physical obstruction is avoided, thus providing improved safety.
  • Good chemical stability as conventional oral solid dosage form.
  • Convenience of administration  and accurate dosing as compared to liquid formulation.
  • Cost effective
  • Have sufficient strength to withstand the rigors of the manufacturing process and post manufacturing handling.
  • Advantageous over liquid formulation in terms of administration as well as transportation.6
  • Reduced first pass metabolism.

LIMITATIONS OF FDT7

  • The tablets usually have insufficient mechanical strength. Hence, careful handling is required.
  • The tablets may leave unpleasant taste and/or grittiness in mouth if not formulated  properly
  • Drugs with larger doses are difficult to formulateinto FDT e.g. rifampin (600 mg), ethambutol (1000mg) etc.

DRUG SELECTION CRITERIA8

  • Able to permeate the oral mucosa.
  • At least partially non-ionized at oral cavity PH.
  • Have the ability to diffuse and partition into the epithelium of upper GIT.
  • Small to moderate molecular weight.
  • Low dose drugs mostly less than 50 mg.
  • Drug should have good stability in saliva and water.
  • Drugs which have lower bioavailability,  are good candidates for FDT.
  • Short half life and frequent dosing drugs are unsuitable for FDT.
  • Very bitter taste and unacceptable  odor drugs are unsuitable for FDT.

Pharmaceutical Companies have formulated FDT for various categories of drugs such as neuroleptics, cardiovascular agents, analgesics, antiallergic, antiepileptics, anxiolytics, sedatives, hypnotics, diuretics, anti-parkinsonism agents, anti-bacterial agents and drugs used for erectile dysfunction.

THE NEED FOR DEVELOPMENT OF FDT9
* Patient factors
FDT  are suitable for those patients (particularly pediatric andgeriatric patients) who are unable to swallow traditional tablets and capsules. These include the following:

  • Patients who have difficulty in swallowing oral tablet
  • Patients incompliance due to fear of chocking
  • A middle-aged patient undergoing radiation therapy  may be too nauseous to swallow  H2- blocker
  • A psychotic patient who may try to hide a conventional tablet under his or her tongue to avoid their daily dose of an atypical antipsychotic
  • A patient with persistent nausea, who may be journey, or has little or no access to water.10

* Effectiveness factor
Dispersion of drug  in oral cavity causes pre-gastric absorption  which avoids first pass hepatic metabolism which increase the bioavailability. Furthermore, safety profiles may be improved for drugs.

* Manufacturing and marketing factors
As a drug nears the end of its patent life, it is possible for pharmaceutical manufacturers to develop a given drug entity in a new and improved dosage form. A new dosage form allows a manufacturer to extend market exclusivity, unique product differentiation, value-added product line extension, and extend patent protection, while offering its patient population a more convenient dosage form.

CHALLENGES IN FORMULATING FDT11
* Palatability
As  most drugs are unpalatable, orally disintegrating drug delivery systems usually contain the medicament in a taste-masked form. FDT disintegrate or dissolve in patient’s oral cavity, thus releasing API comes in contact with taste buds, so taste-masking become a critical to patient compliance   

* Mechanical strength
Order to allow FDTs to disintegrate in oral cavity, they are either vary porous or compressed into tablets with very low compression force, which makes tablets friable, difficult to handle and requiring specialized packing. This tablets have very poor mechanical strength

* Hygroscopicity
Several fast dissolving dosage form are hygroscopic in nature and not able to maintain physical integrity under normal conditions of temperature and humidity. So, require special packaging

* Amount of drug      
The application of technologies used for ODTs is limited by the amount of drug that can be incorporated into each unit dose. For lyophilized dosage forms, the drug dose must be lower than 400 mg for insoluble drugs and less than 60 mg for soluble drugs. This parameter is particularly challenging when formulating a fast-dissolving oral films or wafers

* Aqueous solubility
Water-soluble drugs pose various formulation challenges because they form eutectic mixtures, which result in freezing-point depression and the formation of a glassy solid that may collapse upon drying because of loss of supporting structure during the sublimation process. Such collapse sometimes can be prevented by using various matrix-forming excipients such as mannitol than can induce crystallinity and hence, impart rigidity to the amorphous composite.

* Size of tablet
The degree of ease when taking a tablet depends on its size. It has been reported that the easiest size of tablet to swallow is 7-8 mm while the easiest size to handle was one larger than 8 mm. Therefore, the tablet size that is both easy to take and easy to handle is difficult to achieve

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