Utilization of natural superdisintegrants in mouth dissolving tablet: A simplified review
Many drugs belong to BCS class-2 having poor solubility in water requires enhancement in solubility and dissolution rate for increasing its oral bioavailability; however, in many cases, immediate onset of action is required than conventional therapy. Tablet is the most popular among all dosage forms existing today because of its convenience of self-administration, compactness, and easy manufacturing, because of physiological changes associated with, especially elderly and pediatrics, are quite unable to swallow (dysphagia), rather this common problem of all age group patients. Solid dosage forms that can be disintegrated, dissolved, or suspended by saliva in the mouth resulting in easy swallowing, can provide significant benefits to the pediatric and geriatric population, as well as other patients who prefer the convenience of easily swallow able dosage forms. Mouth dissolving tablets (MDT) disintegrate instantaneously when placed on the tongue, releasing the drug that dissolves or disperses in the saliva. In MDT, superdisintegrants are incorporated in the right amount for quick disintegration with improved bioavailability. Based on the source, various types of superdisintegrants are available. They are synthetic, semi-synthetic, natural, and co-processed. In this review, the main emphasis is given on different types of natural superdisintegrants used in MDT, their mechanisms, and applications.
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Bhatti S, Kaushik M. Utilization of natural superdisintegrant in mouth dissolving tablet: A simplified review. Innov Pharm Pharmacother 2020;8(2):32-38. 2020 Innovations in Pharmaceuticals and Pharmacotherapy | Published by Innovational Publishers
Within this review you can find the following very interesting listing of natural polymers, advantages thereof and a comparison to synthetic superdisintegrants. For easier access we list it here as well and thank the auditors Bhatti S and Kaushik M. of “Utilization of natural superdisintegrant in mouth dissolving tablet: A simplified review” for this extensive overview.
Natural polymers used in fast dissolving tablets
Chitin and chitosan
Chitin (β-(1→4)-N-acetyl-D-glucosamine) is a natural polysaccharide obtained from crab and shrimp shells. It possesses an amino group covalently linked to the acetyl group as compared to the liberate amino group in chitosan. The DT in the oral cavity, as well as wetting time, could be analyzed by surface free energy. Chitosan is the best kenned natural polysaccharide utilized for its multifarious applications in the pharmaceutical industry.
Guar gum
Guar gum is mainly consisting of the high molecular weight (approximately 50,000–8,000,000) polysaccharides composed of galactomannans. It is utilized as a thickener, stabilizer, and emulsifier and approved in most areas of the world (e.g., EU, USA, Japan, and Australia). It is naturally occurring gum. It is free flowing, consummately soluble, a neutral polymer composed of sugar units and is approved for use in food. It is not sensitive to pH, moisture contents, or solubility of the tablet matrix. It is not always pristine white and sometimes varies in color from off-white to tan and inclines to discolor with time in alkaline tablets.
Gum karaya
Gum karaya is a vegetable gum produced as an exudate by trees of the genus Sterculia. The high viscosity nature of gum limits its uses as binder and disintegrant in the development of conventional dosage form. Gum karaya has been investigated for its potential as a tablet disintegrant. Different results showed that modified gum karaya produces rapid disintegration of tablets. Gum karaya can be utilized as an alternative superdisintegrant to commonly available synthetic and semisynthetic superdisintegrants due to its low cost, biocompatibility as well as facile availability.
Agar and treated agar
It is the dried gelatinous substance obtained from Gelidium amansii (Gelidanceae) and several other species of red algae such as Gracilaria (Gracilariaceae) and Pterocladia (Gelidaceae). Agar is yellowish-gray or white to proximately colorless, inodorate with mucilaginous taste, and is available in the form of divests, sheet flakes, or coarse powder. Agar consists of two polysaccharides, agarose, and agar pectin. High gel vigor of agar makes it a potential candidate as a disintegrants.
Fenugreek seed mucilage
Trigonella foenum-graceum commonly kenned as fenugreek is an herbaceous plant of the leguminous family. Fenugreek seeds contain a high percentage of mucilage (a natural gummy substance present in the coatings of many seeds). Albeit it does not dissolve in water, mucilage forms a viscous tacky mass when exposed to fluids. Like other mucilage-containing substances, fenugreek seeds swell up and become slick when they are exposed to fluids. Hence, the study revealed that this natural disintegrant (fenugreek mucilage) showed more preponderant disintegrating property than the most widely used synthetic superdisintegrants like Ac-di-sol in the formulations of FDTs. Studies betokened that the extracted mucilage is a good pharmaceutical adjuvant and concretely a disintegrating agent.
Soy polysaccharide
It is a natural superdisintegrants that does not contain any starch or sugar so can be utilized in nutritional products. Halakatti et al. 2010 evaluated soy polysaccharide (a group of high molecular weight polysaccharides obtained from soybeans) as a disintegrant in tablets made by direct compression utilizing lactose and dicalcium phosphate dihydrate as fillers. Soy polysaccharide performs well as a disintegrating agent in direct compression formulations, with results paralleling those of cross-linked CMC.
Gellan gum
Gellan gum is a water-soluble polysaccharide produced by Pseudomonas elodea, a bacterium. Gellan gum is an anionic, high molecular weight, and deacetylated exocellular polysaccharide gum. Antony and Sanghavi 1997 studied the gellan gum as a disintegrant and the efficiency of gum was compared with other conventional disintegrants such as dried corn starch, Explotab, Avicel (pH 10.2), Ac-di-sol, and Kollidon CL. The disintegration of tablet might be due to the instantaneous swelling characteristics of gellan gum when it comes in contact with water and due to its high hydrophilic nature. The consummate disintegration of tablet was proved itself as superior disintegrant.
Mango peel pectin
Mango peel which constitutes 20–25% of the mango processing waste was found to be a good source for the extraction of pectin of good quality, felicitous for the preparation of film, and acceptable jelly. Malviya et al. (2011) investigated and found that mango peel pectin stands as a good candidate as superdisintegrant, though not as more strong than synthetic superdisintegrants, due to its good solubility and higher swelling index, it may be utilized in the formulation of fast dispersible tablets.
Lepidium sativum mucilage
L. sativum (family: Cruciferae) is kenned as Asaliyo and is widely utilized as herbal medicine in India. It is widely available in market and has a very low cost. Components used are leaves, root, oil, seeds, and so forth. Seeds contain a higher amount of mucilage, dimeric imidazole alkaloids lepidine B, C, D, E, and F, and two incipient monomeric imidazole alkaloids, semilepidinoside A and B. Mucilage of L. sativum has different characteristics such as binding, disintegrating, gelling, and so forth.
Plantago ovata seed mucilage
Psyllium or ispaghula is the prevalent name utilized for several members of the plant genus Plantago whose seeds are utilized commercially for the production of mucilage. Mucilage of Plantago ovate has different characteristics such as binding, disintegrating, and sustaining properties. In an investigation, fast disintegrating tablets of amlodipine besylate were yare by direct compression method utilizing different concentrations of Plantago ovate mucilage as natural superdisintegrants.
Aegle marmelos gum (AMG)
It is obtained from the fruits of A. marmelos belonging to the disintegrated faster and consistently than the croscarmellose sodium. The ripened fruit pulp is red in color with mucilaginous and astringent taste. The pulp contains carbohydrates, proteins, Vitamin C, Vitamin A, angelenine, marmeline, dictamine, O-methyl fordinol, and isopentenyl halfordinol. AMG is prepared by the heat treatment technique. It increases the solubility of poorly soluble drugs. Purified, bael gum polysaccharide contains D-galactose (71%), D-galacturonic acid (7%), L-Rhamnose (6.5%), and L-arabinose (12.5%).
Locust bean gum
It is known as carob bean gum. It is a galactomannan vegetable gum extracted from the seeds of carob tree (Ceratonia siliqua). Locust bean gum is utilized as a gelling and thickening agent in the food industry and utilized as a bioadhesive, and it enhances the solubility. The gum is a white to yellowish-white, odorless powder. It is insoluble in most organic solvents, including ethanol. It is partially soluble in water at ambient temperature and soluble in hot water and needs heating to above 850 for 10 min for complete solubility.
Ficus indica Fruit Mucilage
The mucilage of ficus indica fruit is utilized as superdisintegrant which is obtained from the pulp of fruit ficus indica. Ficus indica is an astronomically immense tree up to 3 m and very fast-growing with spread branches and aerial roots. The fruits of ficus indica are of the size of a cherry. It has nutritional as well as medicinal value. The dried and uncooked ficus indica fruit gives 230 kcal (963 KJ) of energy per 100 g or 3.5 oz. (ounce). It is utilized in assuaging fever, pain, inflammation, wound rejuvenating, blood quandaries, and urinary quandaries.
Mangifera indica gum
Mundane name of M. indica is mango and it belongs to Anacardiaceae family. It is non-toxic and utilized as a disintegrant, binder, suspending agent, and emulsifying agent in different formulations. The gum powder is white to off white in color, and the powder was soluble in water and virtually insoluble in acetone chloroform, ether, methanol, and ethanol.
Hibiscus rosa-sinensis mucilage and treated agar
It is withal called shoe flower plant, China rose, and Chinese hibiscus and belongs to the family Malvaceae. Mucilages are utilized as thickeners, suspending agent, water retention agent, and disintegrants. The plant is facilely available and its leaves contain mucilage and are present in mucilage L-rhamnose, D-galactose, D-galacturonic acid, and D-glucuronic acid. Treated agar is yare by treating it with water for 1 day.
Dehydrated banana powder (DBP)
Banana is additionally called plantain. DBP is yare from the variety of banana called Ethan and nenthran (nenthra vazha) and belongs to the family Musaceae. It contains Vitamin A, so it is utilized in the treatment of gastric ulcer and diarrhea. It withal contains Vitamin B6, which avails in reducing the stress and solicitousness. It is a very good source of energy due to high carbohydrate content, and it contains potassium, which is responsible for more preponderant brain functioning.
Advantages of natural polymers
The various advantages of natural plant-based materials include the following.
- Biodegradable: Biodegradable as they are naturally available, and they are produced by all living organisms.
- Biocompatible and non-toxic: Basically, all of these plant materials are reiterating sugar polysaccharides.
- Low cost: They are cheaper to utilize as natural sources. The production cost is less compared with synthetic material. India and many other developing countries are dependent on agriculture, and there are substantial amounts of money investment on agriculture.
- Environmental-friendly processing: There are many types of natural compounds obtained from different plant sources which are widely utilized in the pharmaceutical industry and collected in immensely large quantities due to the simple production processes involved.
- Local availability (especially in developing countries): In India and homogeneous developing countries, there is a promotion for the production of plants as pharmaceutical excipients being done by government, and it withal provides the facilities for bulk production such as gum and mucilage’s because of their wide applications in industries.
- Patient tolerance as well as public acceptance: There is less chance of side and adverse effects with natural materials compared with synthetic one.
Synthetic superdisintegrants
A group of superdisintegrants, including croscarmellose sodium (Ac-Di-Sol) sodium starch glycolate (Primojel and Explotab) and crospovidone (Polyplasdone XL), alleviate most of these problems. The use of the superdisintegrants in a fast dispersible tablet is possible as a tablet shows optimum physical properties.
Advantages of synthetic superdisintegrants
- Effective in lower concentrations than starch.
- Less effect on compressibility and flow ability.
- More effective intragranularly.
Examples of synthetic polymers
- Sodium Starch Glycolate.
- Cross-linked polyvinylpyrrolidone
- Modified cellulose (croscarmellose sodium, Ac-Di-Sol)
- Resins
Keywords: Bioavailability, dispersible, dysphagia, natural, superdisintegrant,