Tablet Evolution:
Exploring Cutting-edge Technologies in Formulation and Development
Anshika Garg*, Muskan Rathor
1Department of Pharmaceutics, Sanskar College of Pharmacy and Research, Ghaziabad, 201302, Uttar Pradesh.
*Corresponding Author E-mail: anshikacreations03@gmail.com
ABSTRACT:
Pharmaceutical sciences contain a wide number of territories including drug disclosure, plan improvement, testing, wellbeing and regulatory affairs. In this period of development and progression, in drug conveyance for better clinical impacts regular dosage forms have still a solid hold and are generally well known taking all things together sorts of medicinal preparation for oral use. In the last several years, the writing in drug advancement has been expanded in an amazing way. There is a consistent improvement of the assortment of details which are planned by the patient consistency, actual similarity, and therapeutic efficacy to overcome the deficiencies or antagonistic impacts of the previous formulations. In the current review, authors have tried to sum up various sorts of progression associated with solid dosage form i.e. 3D tablets, digital pills, inlay tablets, quick-dissolving tablets, mouth-dissolving tablets, or dispersive tablets, etc. The advances in innovations associated with them have additionally been examined in brief.
KEYWORDS: Pharmaceutical Science, Dosage Forms, Formulations, Dispersive tablets.
INTRODUCTION:
The pharmaceutical industry has seen tremendous advancements in the past few decades. Advancements in the conventional dosage forms have introduced viable dosage choices from the oral route for pediatrics, geriatric, confined to bed, sick or resistant patients. Conventional dosage forms encounter several problems, therefore, new trends and advancements have been continuously adopted to tackle and resolve those issues1.
The pharmaceutical drug research has been directed to develop new dosage forms with an objective to improve well-being and to accomplish better patient compliance.
Oral route of drug administration is the most generally used route of administration among all the routes for the systemic drug delivery system. The principle objective of drug delivery system is to give the therapeutic amount of the drug at the site of activity as a viable all throughout the treatment and afterward maintaining the desired drug concentration. The traditional dosage forms do not manage the drug concentration in the circulation system and body tissues effectively which leads to decrease in the effectiveness of drug or increased frequency of side effects along with undesirable harmfulness and poor efficiency. The new headways in tablet definitions incorporate prompt delivery The recent trends in tablet formulations contain rapid release tablets, for example, orally dispersible, minitablets, mouth dissolving/quick dissolving tablets, effervescent tablets, uncoated and film coated tablets and so on. Extended or sustained release tablet formulations contain layered tablets, for example, in-lay tablets, tablet in tablet, bilayered tablet, medicated chewing tablet, tablet tarts, pastilles, candy, tablet inserts, clinicaps, caplets and child encage tablets2,3.
Figure 1: Recent advancements in tablet technology
The fast-dissolving tablets have quick disintegration time, however along with its advantages, various disadvantages are also associated including physical solid form and hard to store and handle. Fast dissolving oral films are there to improve adequacy by dissolving within minute. Dissolution of the medicament or drug in the mouth is the best effective method, rather it is the new drug delivery system. This delivery system comprises of an extremely thin oral strip, which when put on the tongue, quickly hydrates by saliva present in oral cavity and follows onto the site of application. Fast dissolving tablets consist of liophylisates4. The epic kinds of tablets that deteriorate/ dissolve/disperse in saliva within few seconds. As per European Pharmacopeia, the Orodispersible tablets (ODT) ought to disperse/deteriorate within three minutes. The essential methodology utilized in the advancement of MDT is the utilization of superdisintegrants like Cross-linked carboxymethyl cellulose (Croscarmellose), Sodium starch glycolate (Primogel, Explotab), Polyvinylpyrrolidone (Polyplasdone) and so on. Additionally, the quantity of drug that is liable to first pass metabolism is diminished in contrast to the conventional tablets. Another methodology utilized in creating MD tablets is boosting pore structure of the tablets5.
1. Mass extrusion:- This method includes relaxing of the active blend utilizing the dissolvable combination of water dissolvable polyethylene glycol and methanol. This process can be used to cover granules of bitter medicament to mask their taste.
2. Sublimation:- It is the technique for sublimising material like camphor. High porosity is accomplished using this technique.
3. Melt granulation:- It is the method by which powders are effectively agglomerated by meltable binder. There is no need of water and natural dissolvable solvents that there is no progression of drying. It is a helpful method to improve the disintegration rate of inadequately water-dissolvable medications. Example: griseofulvin
4. Superdisintegrants:- In direct pressure, the expansion of superdisintegrants attaches the cycle of disintegration Examples include, Sodium starch glycolate, Crosspovidone etc.
5. Spraying drying:- Gelatin can be used as a supporting material and as a matrix, mannitol as a diluent and sodium starch glycolate or crosscarmellose or crosspovidone are utilized as superdisintegrants. Tablets manufactured from the spray dried powder have been accounted for to breakdown\ disintegration in under 20 seconds in aqueous medium6,7.
The fundamental objective of any drug delivery system is to give a required amount of medication to the targeted site in the body to accomplish and keep up the desired concentration of drug at that specific site. Conventional dosage form brings about wide scope of variance in drug concentration in the circulatory system and body tissues with subsequent unwanted poisonousness which brings about poor efficiency8. Because of various elements for example, repetitive dosing, unsure absorption and unfortunate toxicity lead to the idea of controlled drug delivery system. The fundamental point of planning controlled drug delivery system is to lessen the dosing frequency and to expand the adequacy of the drug by restriction at the particular site of activity in body.
Mini tablets are little tablets having measurement running between 1.0-3.0mm. They are commonly filled into a container or packed into bigger tablets and once in while in sachets for simple administration.
Drug |
Brand name |
Use |
Pancrelipase |
Ultresa |
Used in digestive disorders |
Olanzapine |
Olanex |
Used in schizophrenia |
Zafirlukast |
Zuvair |
Used in asthma |
Donepezil |
Donaz |
Used in alzheimer’s disease |
Prasugrel |
Effient |
Used in acute coronary syndrome |
Vorapaxar |
Zonitivity |
Prevent heart attack and stroke |
Bilayer tablet is another advancement of solid dosage form for controlled delivery formulations that have different highlights to give effective medication delivery.
In the recent time, interest in building up to incorporate at least two or more than two active pharmaceutical ingredients (API) in a single dosage form (Bi-layer tablet) has expanded in the pharmaceutical industries. Bi-layer tablets can be an essential choice to minimize the drug-drug and drug-excipients interactions, and to permit the improvement of various medication release profiles that are prompt delivered with broadened release9,10.
The essential target of sustained release drug delivery is to give security and to improve bioavailability of medications. Bi-layer tablet is appropriate for the successive delivery in mix of two medications, for partition two in congruent substances and furthermore for sustained release tablets having one layer that releases a fraction of drug immediately as initial dose and the second layer keeps the drug for sustained release.
Drug(s) |
Clinical Use |
Methods of preparation |
Atrovastatin And atenolol |
Treatment of hypertension And hypercholesterolemia |
Direct compression |
Diclofenac Sodium, Paracetamol |
Effective in reducing pain |
Wet Granulation |
Telmisartan and Hydrochlorthiazide |
To minimize contact between hydrochlorthiazide and basic component of Telmisartan |
Direct compression |
Amoxicillin and Potassium clavulanate |
Produce effect against microbial infections |
Dry Granulation |
Propranolol succinate and Amlodipine Besilate |
Bimodal drug release |
Wet Granulation |
Rifampicin and Isoniazid |
Treatment of Tuberculosis |
Wet Granulation |
Metformin Hydrochloride and Glipizide |
Treatment of Diabetes |
Direct compression |
Table 3: Bi-Layer Tablets Available in Market
Brand Name |
API (Active Pharmaceutical Ingredient) |
Volise-m |
Voglibose, Metformin hydrochloride |
Unistar |
Rosuvastatin, Aspirin |
Pioglu |
Pioglitazone, Metformin hydrochloride |
Glimeto-MP |
Glimepride, Pioglitazone |
Alpraxplus |
Sertraline, Alprazolam |
TRIOMUNE30 |
Nevirapine, Lamivudine, Stavudine |
Nanomaterials, for example, liposomes, micelles, polymeric and inorganic nanoparticles show a few points of interest most importantly related with their little size. Doxil (Doxorubicin) was the first promoted nanosystem for the treatment of cancer diseases11,12. It is a liposome that shows upgraded dissemination and improved half-time regard to the medication alone. Doxil can focus on the tumor by enhanced permeability effect. (EPR).
Oral Disintegrating Tablets (ODT) are characterized as "A solid dosage forms that contain medicinal substances which breakdown rapidly inside the oral cavity within seconds, when setup on the tongue. Oral route of administration is the most popular route for the systemic effect because of its simplicity of ingestion of exact dosage with pain avoidance, self-prescription, and most significant patient compliance. Fast disintegrating tablets are named as Fast dissolving tablets, Mouth-dissolving, Melt-in-mouth, quick dissolving, Rapid break down, Quick-deterioration, orally disintegrating, Fast-dissolve, Orodispersible, and Effervescent medication absorption system13.
Quick dissolving tablets can be prescribed to the patients who cannot swallow tablet/capsule, for example, old, stroke, casualty, out of commission patients and so forth. FDT can be administered without water, at any place, anytime. Beneficial in instances of motion sickness, coughing, cases of hypersensitive assault where quick beginning of activity is required.
Brand Name |
API |
Category |
Zofran ODT |
Piroxicam |
NSAIDs |
Felden fast melt |
Ondansetron |
Antiemetic |
Nulev |
Hyoscyamine Sulfate |
Antiulcer |
TorroxMT |
Rofecoxib |
NSAIDs |
Claritin Reditabs |
Loratadine |
Antihistamine |
Febrectol |
Paracetamol |
Antipyretic |
Olanex Instab |
Olanzapine |
Psychotropic |
DIFFERENT MUCILAGE/GUMS:
There are a portion of the normal gums and adhesive which are been utilized as drug excipients. It is essentially in view of the marine origin, green algae, plant, furthermore animal origin14,15.
Locust Bean Gum: It is acquired from carob tree Ceratonia siliqua. The gum contains D-galacto-D mannoglycan, pentane, proteins, and cellulose. Super disintegrant property of this gum was concentrated by oral dispersible tablets containing locust bean gum and assessing it against standard super disintegrant i.e. croscarmellose sodium.
This gum has moreover been explored for its controlled drug delivery property, and furthermore as a compression coat which when applied over core tablets act as carrier for colonic medication delivery, as it demonstrates skilled of ensuring the core tablet and subsequently is an potential carrier for drug focusing to the colon16.
Almond Gum:
It is acquired from the tree Prunus amygdalus. The medication release expanded with almond gum when compared with manufactured gum concentration and the delivery component was found to be non-Fickian dispersion. The almond gum was discovered to be helpful for the preparation of uncoated tablet dosage form.
Hibiscus Mucilage:
It is acquired from new fresh leaves of Hibiscus Rosasinensis. The utilization of its adhesiveness for the advancement of sustained delivery tablet has been accounted.
Neem Gum:
It is acquired from the tree Azadirachta indica (family: Meliaceae). Gum contains mannose, glucosamine, arabinose, galactose, fructose, xylose, and glucose. Various studies have been performed on neem gum for its coupling property and supported delivery property.
Albizia Gum:
It is acquired from incised trunk of the tree Albizia zygia. This gum was attempted as covering materials in compressed coating tablets, which corrupted, by the colonic micro flora, in this way delivers the medication.
Konjac Glucomannan:
It is acquired from the tubers of Amorphophallus konjac (family: Araceae). Konjac glucomannan contains D-glucose and D-mannose in the proportion 1:1.6. Studies have been done on konjac glucomannan for its gelling properties17,18.
Gum Copal:
It is a characteristic resinous material of plant Burserabip innata. Copal gum has been assessed as matrix forming material for supporting the medication delivery. In an autonomous investigation, copalpitch was utilized as a film forming agent. Films demonstrated great expanding property. It was reasoned that it tends to be utilized as a covering material for supported delivery and colon targeted drug delivery.
Terminalia Gum:
It is acquired from the incised trunk of the tree Terminalia randii. Gum exudates acquired from Terminalia randii have been assessed as binding agent. Studies have demonstrated that the crushing strength expands with increase in the polymer concentration while friability gets diminished.
Inlay tablets are kind of layered tablet in which the core of the tablet is being totally encircled by coating and the top surface is totally uncovered. While manufacturing, just the base segment of the die cavity is loaded with coating material and core is set upon it19. During the compression, a few coating material is dislodged to form sides and packs the entire tablet. The fundamental body part may comprise of uncoated granules which are compacted around the enteric coated inlay portion. In this alteration of tablet, the fundamental body is first delivered and acclimatized in the gastrointestinal tract while other the enteric coating ensures the in lay portion of tablet for a predetermination time frame in order to give time postponed or supported prescription.
Clinicaps capsules are the two-piece gelatin capsules which are uniquely intended for investigations of double blind during clinical preliminaries. After locking, caps are closed firmly on the body and keeping just the vault of the body visible. Subsequent to locking, it is hard to open the capsule that prevent altering and adequately covers up the sample. Clinicaps capsules are helpful to encapsulate the tablet or capsule dosage form in the body and provides covering to the encapsulated dosage form20,21. This will guarantee the uprightness of the visually impaired study of clinicaps and improves patient compliance. As wide is the diameter of clinicaps capsule that help to contain large width or in consistent molded tablets which serves to eliminate the need of split or grind tablets. These are filled by generally automatic, semi-automatic filling machines and manual capsules filling machine.
Dosage form of a medication is what enters the body, arrives at the site of activity and produces action. Dosage form of the drug is to be the most suitable form for each route of administration. It should be described by different angles as indicated by the need of covering unwonderful smell and awful taste. The caplets are oval in shape. Caplet is a tablet like some other tablet, however should be contrast just is being a smoothly coated tablet molded like a common capsule23,24,25.
· Calci-D film coated caplets, utilized for patients with calcium insufficiency. It is introduced as blisters of 10 caplets.
· Paracetamol (Acetaminophen) caplets, a notable NSAID and utilized as anti-inflammatory, antipyretic, pain relieving and mild to moderate pains with cold and influenza.
· Imodium caplets help to re-establish balance of our digestive system. The Imodium caplet controlling the side effects of diarrhea, including Traveler's Diarrhea.
· Nurofen caplets (ibuprofen), they are utilized for targeted relief or pain.
A pastille is a type of sweet or restorative pill comprised of set thick fluid that is intended to be devoured by light biting and permits it to breakup in the mouth. Pastilles are additionally used to characterize certain types of incense. Pastille is otherwise called Troche and cured capsule that break up quickly like treats26,27.
3,4-methylenedioxy-methamphetamine (MDMA) a psychoactive medication of the substituted methylenedioxyphenethylamine and amphetamine classes of medications that is consumed mostly for its euphoric and empathogenic impact. Pharmacologically, MDMA can act as a serotonin-norepinephrine-dopamine delivering agent and reuptake inhibitor28.
MDMA is generally known as Ecstasy ordinarily in its tablet form, despite the fact that this term may also hold the presence of possible adulterants, for example, mandyasnamed in the UK and mollyas named in the US. In many countries ownership of MDMA is unlawful. Some restricted exemptions exist for the logical and clinical examinations. MDMA may have wellbeing valuable impacts in certain psychological issues, yet additionally has potential adverse effect that incorporate neurotoxicity and cognitive impairment.
Vaginal tablets are utilized for some reasons, for example, infectious disease or their microbicide properties. One vaginal tablet has been explored as a microbicide dosage form. Praneem poly natural was initially figured with decontaminated ingredient from leaves of Neem (Azadirachta indica, fam.meliaceae), Sapindusmuker ossi (pericarp of organic product), and Mentha citrata oil into a pessary delivery gadget for spermicidal and contraceptive purposes29,30. The poly natural herbs were additionally formed into a vaginal tablet, in clinical preliminaries item was demonstrated to be safe for vaginal use for as long as a half year with minor unfavorable effects.
DIGITAL PILLS:
Digital pills are highly innovative class of pharmaceuticals comprised of digital sensors. These allows to combine traditional medicine with monitoring system that records data about patients’ medication adherence automatically. DP mainly comprises of three elements- an ingestible sensor, a wearble patch and a mobile application connected with external web server. These pills contain branded or generic drugs developed along with second generation artificial intelligence that overcome the problem of medication adherence. It includes mobile friendly app which can be downloaded easily in cell phones and can be used to follow the drug regimen. The ingestible sensor is basically a digital marker which upon ingestion gets activated by acid fluids and provides a signal that is recognized by the wearable patch. All information collected through the wearable patch on abdomen is transmitted to the mobile application31,32,33. This data gets automatically saved on the web server and can be accessed by the patient, healthcare providers and family members34,35.
3D PRINTED TABLETS:
3D printing is also referred to as additive manufacturing technology. It is based on sequential deposition of layers of materials that can help in production of small batches of medicinal products with tailored size, shapes, dosage regimen and release characteristics for individuals so that personalized therapy can be provided36,37. It allows to take in account the specific requirements of individuals for therapy such as age weight, pharmacokinetic characteristics and other comorbidities. This technology was first patented in 1986 but was not very popular at that time, tremendous progress has been made since last 5 years to advance and translate this technology into a more realistic concept.3D printing technology offers great advantages for drug development by reducing the time and expenditure on clinical trials38. Various orodispersible, sublingual and fast dissolving medications have been produced using 3D printing technology. Spritam® is the first 3D printed formulation approved by FDA in 201539,40.
There is a vast advancement in pharmaceutical drug development, drug delivery systems and technologies utilized has been observed in past decades and still is in progress. With developing drug market and needs of patients, new created tablets may fulfill the purchasers. Progression in tablet manufacturing or some novel tablet adjustment has made strong presence in the market by their critical commitment. A few of them has been outlined in this review. Although, these have provided so many beneficial effects, but still some problems are associated with these drug delivery systems. So, further advancements in technologies and adopted methodologies are the needs of the hour.
The authors are highly thankful to the management of Sanskar Educational Group for their constant support.
Received on 11.01.2024 Revised on 06.05.2024 Accepted on 16.07.2024 Published on 18.12.2024 Available online on December 21, 2024 Asian J. Pharm. Tech. 2024; 14(4):373-378. DOI: 10.52711/2231-5713.2024.00059 ©Asian Pharma Press All Right Reserved
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