Fast Dissolving Tablets: A Comprehensive Review

M Sohil M Shabbir*, Shaikh Imran Kalam, Aejaz Ahmad, G.J. Khan, Md Moiz, Aman Shaikh

JIIU’s Ali Allana College of Pharmacy Akkalkuwa, Nandurbar; Maharashtra, India

*Correspondence: mohammadsohil8668@gmail.com; Tel.: (+91 8668983622)

 INTRODUCTION

Dosage forms, also known as unit doses, are pharmaceutical drug products in the form in which they are marketed for use. They contain a specific combination of active ingredients and inactive components (excipients), are arranged in a specific way (for instance, in a capsule shell), and are divided into certain doses. Two goods, for instance, might both include amoxicillin, but one comes in 500 mg capsules and the other in 250 mg chewable pills. Non-reusable packaging can also occasionally be included in the term "unit dose" (particularly when each drug product is packaged separately [1]), though the FDA makes a distinction between it and "packaging" or "dispensing.[2] Various contexts may use the term "multi(plea) unit dose" to describe different drug products packaged together or to describe a single drug product that contains several drugs and/or doses. A drug product's pharmaceutical formulation of its constituent drug substance or substances and any mixes involved may alternatively be referred to as its "dosage form" without taking into account other factors (such as how it is finally configured as a consumable product such as a capsule, patch, etc.). When speaking with someone who might not be familiar with another person's use of the phrase, care is frequently advised due to the relatively hazy boundaries, confusing overlap, and specific variations and qualifications within the pharmaceutical sector. There are various sorts of dosage forms, depending on the route or method of administration. Various liquid, solid, and semisolid dose forms are among them. Among the numerous common dose forms are drink, syrup, tablet, capsule, and pill. A combination drug (also known as a fixed-dose combination, or FDC) is a drug product that contains multiple drugs (also known as multiple active ingredients), such as a tablet, capsule, or syrup. Doses in naturopathy can be made using the more traditional techniques described above, as well as decoctions and herbal teas. The dosage form of the chemical in question determines the medication delivery route of administration (ROA). A single medicine may be in different dose forms since some medical situations, including unconsciousness, can limit ROA. For instance, chronic nausea, particularly when accompanied by vomiting, may make it difficult to provide a dose form orally. It may be essential to utilize an alternate route, such as parenteral, suppository, buccal, sublingual, nasal, or inhalational. Additionally, because of potential problems with pharmacokinetics or chemical stability, some types of medications may require a particular dose form. For instance, insulin cannot be administered orally. Because it cannot adequately reach its therapeutic target destinations when delivered in this way since it undergoes considerable gastrointestinal tract (GIT) metabolism before entering the bloodstream. A medication like paracetamol will have different oral and intravenous dosages for the same purpose.[3]

Form of dosage for medications Excipients + API how drug molecules are transported to the body's locations of action, either in form or by methods. medication (active compounds in pharmaceuticals) A chemical compound that is used to diagnose, treat, and prevent diseases.

OR

The component of any medication that generates its effects is called the Active Pharmaceutical Ingredient (API). The therapeutic effect of the active component is not enhanced or impacted by excipients. Often known as excipients or inert components, inactive compounds typically don't have any pharmacological effects. Binding materials, dyes, preservatives, flavourings, sweeteners, colourings, and so forth are examples of inactive substances. When a chemical compound is used as a drug or medication, its physical form is known as the Dosage Form (DF), and it is meant to be administered or consumed. Typical dose forms include, but are not limited to, pills, tablets, capsules, drinks or syrups, liquid injections, aerosols or inhalers, pure powder or solid crystal (for example, by oral intake or freebase smoking), and natural or herbal forms like plants or foods. A drug's dose form determines the route of administration (ROA) for drug delivery.

NEED FOR DOSAGE FORMS

ü  Accurate dose

ü  Protection e.g. coated tablets, sealed ampules

ü  Protection from gastric juice

ü  Masking taste and odour

ü  Placement of drugs within body tissues

ü  Sustained release medication

ü  Controlled release medication

ü  Optimal drug action

ü  Insertion of drugs into body cavities (rectal & vaginal)

ü  Use of desired vehicle for insoluble drugs

Figure 1 (Classification of dosage forms)

There are numerous ways to categorize dosage forms according to their physical condition, method of administration, intended use, application place, etc. Solid, semisolid, liquid, or gaseous are the physical states. Administration routes include nasal, vaginal, urethral, parenteral, rectal, and oral. Application Sites: Nose, Hand, Foot, Eye, Tooth, and Skin. Use: external and internal. The most popular classification, nevertheless, is based on the physical condition and the method of administration.

Examples of Dosage Forms

1)      Physical State

ü  Solid – Powders, granules, tablets, capsules, pills, sachets etc.

ü  Semisolid – Ointments, cream, suppositories, paste etc.

ü  Liquid – Solutions, elixirs, emulsions, suspensions, syrup, spirits etc.

ü  Gaseous – inhalants, aerosols etc.

2)      Route Of Administration

ü  Oral – Powders, tablets, capsules, elixirs, solutions, emulsions, syrup

ü  Parenteral – Solutions, suspension, emulsions etc.

ü  Rectal – Suppositories, enemas, ointments etc.

ü  Transdermal – Ointments, creams, powders, pastes, lotions etc.

ü  Intranasal – Solutions, sprays, inhalations etc.

ü  Vaginal – Suppositories, tablets, ointments, creams etc.

ü  Urethral – Suppositories etc.

ü  Sublingual – Tablets, lozenges etc.

ü  Conjunctival – Ointments etc.

ü  Intraocular – Solutions, suspensions, ointments etc.

ü  Intrarespiratory – Aerosols etc.

3)      Site Of Application

ü  Skin – Lotions, liniments, creams, powder etc.

ü  Eye – Eye drops, Eye ointments etc.

ü  Tooth – Toothpastes, etc.

ü  Foot – Foot powder etc.

ü  Hair – Shampoos, Hair oils, etc.

ü  Nose – Nasal drops, etc.

4)      Uses

ü  Internal – Tablets, capsules, syrup etc.

ü  External – Lotions, liniments, cream, ointments, etc.

Table 1 (Advantages & Disadvantage of dosage forms)

TABLETS ^[1]

A tablet is a solid pharmaceutical dosage form that is made by moulding or compression and contains one or more medications, either with or without appropriate additional ingredients. 1.1.1

PERKS OF THE TABLET

Tablets may have the following potential benefits. 1. Of all the oral dosage forms, they are the one with the best capabilities in terms of dose accuracy and the least amount of content variability. 2. They are the least expensive of all the oral dose forms. They are the smallest and lightest of all the oral dose forms. 4. They are the most affordable and straightforward to package and ship. 5. Some specific release profiles, including enteric or delayed release products, are well suited for them. 6. Compared to other unit oral dosage forms, tablets work better for large-scale manufacturing. 7. Of all the oral dose forms, their chemical, mechanical, and microbiological stability are the best combined.

CLASSIFICATION OF TABLETS: -                                                        

The tablets are divided into the following categories according to their function or mode of administration. 1) Orally administered tablets. One compressed tablet; two compressed tablets; i) Compression-coated tablet ii) Layered tablet c) Repeat-action tablet d) Enteric and delayed action coated tablets e) coatings of sugar and chocolate f) coatings of film g) Chewable tablets. 2) Orally administered tablets. Dental cones, troches and lozenges, buccal tablets, and sublingual tablets. 3) Tablets given by alternative methods.  a) Tablet for Implantation b) Tablets for Vaginal Use. 4) Solution preparation tablets. Triturate tablets, effervescent tablets, dispensing tablets, hypodermic tablets, and tablets.

TABLETS MANUFACTURING METHODS: -

Table.2 Illustrates the three methods used to create tablets: wet granulation, dry granulation, and direct compression. Granulation in Wet Conditions The process of wet granulation involves adding a liquid to a powder in a vessel that has any kind of agitation that might result in granules or agglomeration. Tablets are created by compressing these granules after they have dried. [2] Granulation that is dry There is no usage of liquids in this method. Slugs form as a result of the procedure. To create granules, the slugs are further filtered or ground. Tablets are then created by compressing the granules. 3) Direct compression Tablets made from powder blends of active ingredients and appropriate excipients that will flow uniformly in the die cavity and form a hard compact are compressed directly; this procedure is known as "direct compression."

Table 2 (Processing steps commonly required in the various tablet granulation preparation techniques)

ADVANTAGES OF DIRECT COMPRESSION METHOD: -

It's a more cost-effective method. Because it necessitates fewer manufacturing stages and processing time, labour costs and process validation are reduced. 2) No heat, high compaction pressure, or moisture were needed for the processing stages. 3) The disintegration of tablets is optimized, allowing each primary drug particle to be released from the tablet mass and dissolve. 4) Direct compression works better than the wet granulation method for disintegrating substances like starch.

FAST DISSOLVING TABLETS:

Over the last 20 years, there has been a greater need for dose forms that are more patient-friendly. Consequently, the demand for the technology has tripled every year. Given the expensive expense of developing a new chemical entity, pharmaceutical companies are concentrating on creating novel drug delivery methods for their current medications that have better bioavailability and efficacy as well as lower dosage frequency to lessen adverse effects. About 35% of the general population is said to suffer from dysphagia, or difficulty swallowing. Numerous medical conditions are also linked to this illness, including. Radiation therapy to the head and neck, AIDS, stroke, Parkinson's disease, and other neurological conditions like cerebral palsy. Pharmaceutical preparations for older individuals have recently been studied to enhance treatment compliance and patients' quality of life. [2,3] By creating a comfortable dosage form for administration, recent developments in Novel therapeutic Delivery Systems (NDDS) seek to improve patient compliance while also enhancing the safety and efficacy of therapeutic molecules. A method like this is the "Mouth/Fast Dissolving Tablet." This is a cutting-edge tablet technology that gives the patient the most convenience by dissolving the dose form containing the active medicinal components quickly—typically in a couple of seconds—without the need for water. Various names have been given to these tablets by innovators and invention businesses, including mouth dissolving (MD), quick melting, fast dissolving, or disperse, and orally disintegrating tablets (ODT). [4, 5] The goal to give patients a traditional way to take their medications gave rise to the idea of the Fast-Dissolving Drug Delivery System. Because of the physiological changes that these patient groups experience, dysphagia, or difficulty swallowing, is a common issue in all age groups, but it is most prevalent in the elderly and paediatrics. [6, 7] Other groups who have trouble with traditional oral dosage forms include individuals who are mentally unwell, irritable, and nauseated; those who suffer from motion sickness; and those who cough or have abrupt episodes of an allergic reaction. Sometimes the lack of water can make it harder to swallow conventional items. [8, 9] A new kind of solid oral dose form known as "Fast Dissolving Tablets" was created as a result of these issues. When the fast-dissolving tablet was placed in the mouth, it dissolved quickly. The medication is absorbed normally once the pill swells when it comes into touch with water. Medications are readily absorbed in the stomach and can have a quick start to their effects. [10] The drug's bioavailability in these situations is noticeably higher than that of the typical tablet dosing form. [11,12] Recently, it was emphasized how important fast-dissolving tablets are becoming. A fast-dissolving pill is defined by the European Pharmacopoeia as one that dissolves in the oral cavity in ten to three minutes. [13]

SIGNIFICANCE OF FAST DISSOLVING TABLETS:

System of Drug Delivery
1) Simplicity of administration.
2) The medication dissolves and is absorbed quickly.
3) In certain specific situations, improved bioavailability.
4) The advantages of using liquid medication in solid form.
5) Suitable for elderly and pediatrics patients.
6) The patient's cooperation has improved.
7) Dosage precision.

FUNDAMENTALS OF FAST DISSOLVING TABLETS: -

In order for the dosage form to dissolve or disintegrate quickly, water must quickly permeate the tablet matrix, resulting in instantaneous and rapid tablet breakdown. To formulate a fast-dissolving tablet, a number of methods are employed to accomplish these fundamentals. A few of the methods are explained here.

TECHNIQUES FOR PREPARING MOUTH DISSOLVING TABLETS: -

1) The process of freeze drying
2) The process of moulding
3) Third, sublimation
4) The use of spray drying
5) Immediate compression Technology Patented

A) Technology from Zydis.
B) Technology from Durasolve.
C) Technology from Orasolve.
D) Technology known as flash dose.
E) Tab technology is amazing.
F) Flash Tab Technology.

1)      Zydis Method (Freeze Drying) [14]

It is possible to make mouth-dissolving tablets via lyophilization or freeze-drying; these tablets are highly porous and dissolve or disintegrate rapidly when they come into contact with saliva. When the zydis units are too weak to resist being forced through the lidding foil of a traditional blister, the drug is incorporated into a water-soluble matrix and then transferred to the preformed blister using peelable foil. Water is then removed by sublimation through freeze drying. Zydis technology was created by R.P. Scherer, who used the freeze-drying method to create mouth-dissolving tablets based on a patent granted to Gregory et al. [15]. Seager talked on the creation, technology, and bioavailability of fast-dissolving tablets made with Zydis technology.[16] Fragility is a fundamental drawback of freeze-dried fast-dissolving tablets, making them difficult to package conventionally and potentially unstable when stored. However, Blank et al. used a combination of mannitol and natural gum as a carrier material in the formulation of freeze-dried tablets to solve stability issues. They found that the tablets demonstrated enhanced stability in blister packs, even when stored under demanding conditions.

2)      Moulding [17]

When making moulded tablets, water-soluble chemicals are used to ensure that the tablet dissolves or disintegrates entirely and quickly. With the use of a hydroalcoholic solvent, the powder is wet before being moulded into tablets with less pressure than in a traditional dosage form. The air-drying process eliminates the solvents. The tablet dissolves easily because of its porous nature. Including PVP K-30, 22, sucrose, or acacia may improve the tablet's mechanical strength. With multimoded tablets, there is very little room for taste masking. In order to create taste-masked mouth-dissolving tablets, Van Scoik created a mixture of particle cotton seed oil, lecithin, polyethylene glycol, sodium bicarbonate, and the medication. The mixture was then combined with lactose to create a triturate form.

3)      Sublimation [18]

The fundamental idea behind making fast-dissolving tablets using the sublimation process is to add a volatile salt to the tableting ingredients, mix them until they are a fairly homogenous mixture, and then volatize the volatile salt. When volatile salts are eliminated, the tablet develops holes that facilitate quick disintegration when it comes into contact with saliva. It is possible to create porous tablets with strong mechanical strength using substances like camphor, naphthalene, urea, ammonium bicarbonate, etc. Koizumi et al. [19] developed porous compressed tablets using camphor as a volatile ingredient and mannitol as a diluent. The tablets were vacuumed at 800C for 30 minutes in order to remove the camphor and create the tablet's pores. Makino et al. [20] created porous tablets with superior mechanical strength and dissolving characteristics by using water as a pore-forming substance.

4)      Drying by spraying [21]

It is possible to create a tablet that dissolves quickly by spray drying. The foundation of this method is a particulate support matrix, which is made into a small, extremely porous powder by spray drying and combining several ingredients in an aqueous mixture. After mixing with the active component, this is compacted into a tablet. Within 20 seconds, the fast-dissolving tablet made using the spray-drying method broke apart.

5)      Addition of disintegrant (direct compression) [22]

One of the most widely used methods for creating mouth-dissolving tablets is the disintegrant addition approach, which is inexpensive and simple to utilize. Adding super disintegrants in the right concentration to provide fast disintegration and a pleasant mouthfeel is the fundamental idea behind creating mouth-dissolving tablets using the disintegrant addition approach. Microcrystalline cellulose and low substituted hydroxy propyl cellulose combined in an 8:2 to 9:1 ratio result in the quickest disintegration time. A blend of various super disintegrants was used to create a fast-dissolving tablet with analgesic effects. Efavirenz, an anti-HIV medication, was made into fast-dissolving tablets by combining sodium starch glycolate as a super disintegrant with microcrystalline cellulose [23]. Disintegrants can aid in the dissolve of drugs, which in turn can increase their bioavailability. Even though starch has a long and solid history as a disintegrant, there are drawbacks to using it in direct compression formulation. The structure of the tablet is often weakened by the relatively high levels needed and the lack of compressibility. Therefore, it is crucial to create new disintegrants that aid in quick disintegration and are effective at lower concentrations when used in formulations for direct compression. Crosslinked carboxymethyl cellulose (Ac-di-sol®), sodium starch glycolate (Explotab®), and other disintegrants are examples of super disintegrants. The disintegration of tablets is significantly improved by crospovidone (polyplasdone XL®), which swells the tablet and applies enough pressure to cause it to fragment into tiny pieces. The swelling index of these super disintegrants is strong at lower concentrations. So, they are utilized in the formulation of tablets that dissolve in the mouth or that are dispersible.

SUMMARY AND CONCLUSION

As a novel drug delivery method, fast dissolving tablets can be formulated and administered without the need for water, have minimal side effects, provide immediate release, and enhance bioavailability to improve patient convenience and compliance.

ACKNOWLEDGMENT

I am thankful to principal and management of Ali Allana College of Pharmacy Akkalkuwa for providing all necessary facilities during this study.

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