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Medicated Chewing Gum: A Review
AIM AND OBJECTIVES
The aim of this review article is (1) to discuss the advantages and limitation of chewing as drug delivery system, (2) to describe the methods of preparation, evaluation, stability, release of drugs, factors affecting release, safety aspects and development with respect to the medicated chewing gums.
CHEWING GUM DOSAGE FORM FOR BUCCAL DELIVERY
Dosage forms such as mouthwashes, erodible/ chewable buccal tablets, and chewing gums allow release of drugs for only a short period and thus the reproducibility of drugs absorption is comparatively poor. Application of bioadhesive semisolid gels creates considerable technical problems in the buccal absorption. Although medicated chewing gums pose difficulties in regulating the dose administered, they still have some advantages as drug delivery devices, particularly in the treatment of diseases in the oral cavity and in nicotine replacement therapy. Some commercially available chewing gums are Caffeine chewing gum, (Stay Alert®,) and Nicotine chewing gums (e.g. Nicorette ® and Nicotinell®). The permeability of nicotine across the buccal mucosa is faster than across the skin. However, chewing gum slowly generates a steady plasma level of nicotine rather than a sharp peak as experienced when smoking. Possible swallowing of considerable amount of nicotine during chewing may lead to decreased effectiveness of the chewing gum due to first pass metabolism and gastrointestinal discomfort. It is a major challenge to optimize the dose-response relationship of nicotine administered in a chewing gum.
1. Convenient – promoting higher compliance
2. Discreet- less stigmatization
3. Administration without water can be taken anywhere
4. Excellent for acute medication
5. Advantageous for patients with difficulty in swallowing tablets
6. Pleasant taste
7. Dose not requires water to swallow. Hence can be take anywhere.
8. Counteracts dry mouth: Through stimulation of the salivary secretion thereby preventing
9. Candidacies and caries
10. Highly acceptable by children
11. Excellent for acute medication
12. The active compounds absorbed at oral level avoid the hepatic circulation and the associated metabolism.
13. Gum does not reach the stomach. Hence G.I.T. suffers less from the effects of excipients.
14. The product is rapidly released from the gum after a short period mastication; some absorption takes place by directly through the oral mucosa depending on the active ingredient. Importantly not being swallowed the gum does not reach the stomach. Moreover, the stomach does not suffer from direct contact with high concentrations of active principle, thus reducing the risk of intolerance of the gastric mucosa.
15. The fraction of product reaching the stomach is conveyed by the saliva and delivered Continuously and regularly. Active substances are released from medical chewing gum during chewing and are dissolved in saliva. The release rate can be carefully controlled through the formulation of the chewing gum allowing extendedexposure in the oral cavity. Active substances that are absorbed through the buccal mucosa pass via the jugular veins directly into the systemic circulation. Due to the rich vascular supply of the buccal mucosa, measurable concentrations of active substances may be in the blood after only a few minutes of chewing and fast onset of action is thus likely to be attained. Furthermore, bioavailability may be increased, as hepatic first pass metabolism and gastrointestinal tract degradation are tract degradation are avoided for buccal-absorbed substances.
16. Aspirin, Dimenhydrinate and Caffeine shows faster absorption through MCG than tablets.
17. Consequently, a lower dosage of substance may be therapeutically sufficient, possibly resulting in a fewer side effects, and promote fast absorption. Active substances released from chewing gum are dissolved in saliva when swallowed and are, therefore, readily accessible for absorption in the gastrointestinal tract.
1. Gum Base-Gum base is an inert and insoluble nonnutritive product used as a support for the edible and soluble of the chewing gum (sugar, glucose, poly oils and flavors) Other raw materials are generally grouped in the following classes:
2. Elastomers: including natural and synthetic rubbers. The gum base composition may contain conventional elastomer solvents to aid in softening the elastomer base component. Such elastomer solvents may comprise terpinene resins such as polymers of alpha-pinene or beta-pinene, methyl, glycerol or pentaerythritol esters of resins or modified resins and gums, such as hydrogenated, dimerized or polymerized resins or mixtures. The elastomer solvents may be employed in amounts from 5.0% to 75.0%, by weight of the gum base, and preferably from 45.0% to 70.0%, by weight of the gum base. Synthetic elastomers such as butadiene, styrene copolymers, polyisobutylene, isobutylene isoprene copolymers, polyethylene mixtures, and non-toxic vinyl polymer, such as polyvinyl alcohol are widely used bases. The molecular weight of the vinyl polymer may range from 3,000 to 94,000. The amount of gum base employed varies greatly depending upon various factors such as the type of base used, the consistency of the gum desired and the other components used in the composition to make the final chewing gum product. In general, the gum base will bepresent in amount from 5% to 94%, by weight of the final chewing gum composition. Preferably, the gum base is used in amounts from 15% to 45% and more preferably in amounts from 15% to 35% by weight of the final chewing gum composition.
3. Plasticizers: waxes, vegetable oils, glycerides. Plasticizers or softeners such as lanolin, palmitic acid, oleic acid, stearic acid, sodium stearate, potassium stearate, glyceryl triacetate, glyceryl lecithin, glyceryl monostearate, propylene glycol monostearate, acetylated monoglyceride, glycerine, natural and synthetic waxes, hydrogenated vegetable oils, polyurethane waxes, paraffin waxes, microcrystalline waxes, fatty waxes, sorbital monostearate, propylene glycol, may be incorporated into the gum base to obtain a variety of desirable textures and consistency properties.
4. Adjuvants: calcium carbonate, talc, or other charging agents are used. Mineral adjuvant such as calcium carbonate, magnesium carbonate, aluminum hydroxide, aluminum silicate, talc, tricalcium phosphate, dicalcium phosphate serve as fillers and textural agents.
5. Antioxidants: An anti- oxidant such as butylated hydroxytoluene, butylated hydroxyanisole, propyl gallate and mixtures there of, may be included as antioxidants.
6. Compression adjutants: Suitable compression adjuvant such as silicon dioxide, magnesium stearate, calcium stearate and talc can be used in medicated chewing gum for ease of compression. The alkaline earth metal phosphates and alkali metal phosphates prevent caking and balling of “High” i.e. 2 to 8% moisture- containing chewing gum compositions during grinding. Additionally, it has been discovered that maltodextrin enhances the grinding of “high” moisture-containing chewing gum compositions by absorbing moisture to allow lubrication in the gum as it separates into granules. If oil lubricants are used, it is preferred to be 0.4% to 1% by weight of the tableted chewing gum composition. The amount of glidant present in the tableted chewing gum composition is from 0.5% to 5% by weight of the tableted chewing gum composition. Those glidants useful are selected from the group consisting of alkali metal salts, talc, starch, polyhydric alcohols and mixtures. Antiadherents function to prevent tablet granulations from sticking to the faces of the punches and the die walls, but most importantly, prevent adherence of chewing gum granules from adhering to one another, a phenomenon known as blocking. Anti- adherents may be added to the chewing gum composition while the composition is in the hoppers, or subsequent to grinding and are selected from the group consisting of silicates, silicon dioxide, talc and mixtures thereof present in amount of 0.2% to 1% by weight of the tableted chewing gum composition and preferably about 0.3 to about 0.6% by weight. Generally anti-adherent is a finely divided low bulk density powder, which is preferably water insoluble. The preferred anti-adherents are fumed silica and talc. The term-fumed silica is meant to include pyrogenic silicas, micron sized silicas and hydrated silicas.
a) Water-soluble sweetening agents: xylose, ribulose, glucose, mannose, galactose, fructose, sucrose, maltose, invert sugar partially hydrolyzed starch, dihyrochalcones, monellin, steviosides, glycyrrhizin, and sugar alcohols such as sorbitol, mannitol, hydrogenated starch hydrolsates.
b) Water-soluble artificial sweeteners: soluble saccharin salts, i.e. sodium or calcium saccharin salts,cyclamate salts.
c) Dipeptide based sweeteners: L- aspartic acid derived sweeteners such as Aspartame, Alitame, methyl esters of L-aspartyl-L phyenyl-glycerine and Laspartyl- L 2,5-dihyrophenylglycine, L-aspartyl 2,5- dihydro-L phenylalanine – L aspartyl – L (1-cyclohexen) alanine.
d) Water-soluble sweeteners: derived from naturally occurring water-soluble sweeteners, chlorinated derivatives of ordinary sugar (sucrose, known as Sucralose)
e) Protein based sweeteners: such as thaumaoccous danielli (Thaumatin I and II) In general an effective amount of sweetener is utilized to provide the level of sweetness desired, and this amount will vary with the sweetener selected and are present in amounts from 0.0025% to 90% by weight of the gum composition.
8. Coloring Agents: The coloring agents include pigments, which may be incorporated in amounts up to about 6% by weight of the gum composition, titanium dioxide may be incorporated in amounts up to about 2%. The colorants may also include natural food colors and dyes suitable for food drug and cosmetic applications.
9. Flavoring Agents: Flavoring agents suitable for use are essential oils and synthetic flavors such as citrus oils, fruit essences, peppermint oil, spearmint oil, clove oil wintergreen oil, and anise oil.
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