Discover everything about Tablet Lozenges lozenges, their types, medicinal uses, preparation methods, ingredients, and benefits for sore throat and cough relief.
INTRODUCTION OF LOZENGES:
Lozenge are pharmaceutical oral dosage form which is intended to dissolve within the oral cavity to treat disease condition and suppress cough. First pass metabolism, reduce gastric irritation and increase the retention time of the dosage form in mouth which increase their bioavailability due to the medicated Lozenge This dosage form show the effects as local as well as systemic therapy.
Patient who have difficulty in swallowing solid dosage form so the lozenges are recommended. Lozenges composed of one or more active substances also addition of inert vehicle, flavoring agent, carrier (sucrose, dextrose) or diluent. A throat lozenge like cough drop, troche, cachou or cough sweet which is medicated tablet but small taken to be dissolved slowly in mouth to temporarily arrest coughs, to lubricate and to soothe the irritated tissues of the throat infections (sore throat) caused due to common cold and influenza.
Lozenges are set in oral cavity. Since the sublingual lozenges may be unreasonable due to their size, buccal lozenges are defined and have been extensively used and are aiming to be set between the cheek and the gum. In spite of the fact that the lozenge disintegration time is approximately 30 minutes, this effect on the patient; as the patient controls the rate of disintegration and retention by sucking on lozenge until dissolves. Sucking and the ensuing generation of saliva may also lead to expanded dilution of the medicated and accidental swallowing. .
LOZENGES INCORPORATED WITH OTHER MEDICATIONS:
Any of the medications which are ordinarily joined into lozenges may be utilized within the present invention the single medication can be consolidated into the lozenge or different medications can be consolidated into the lozenge like Antimicrobial agents are typically consolidated into lozenges to treat throat infections. The amount of antimicrobial agent that will be joined into the lozenge will vary depending upon the specific agent utilized. Typically from about 1 to about 20 mg of antimicrobial agent will be utilized per lozenge.
Local anesthetics are also consolidated into lozenges which is used to treat sore throats. Anti-fungal agents are consolidated into lozenges which is used to treat fungal infections. Medications to control coughs can also be incorporated into these lozenges. Breath fresheners are also routinely incorporated into lozenges in order to minimize halitosis.
TYPES OF LOZENGES:
According to Site of Action:
- Local effect. Ex. Antiseptic, Decongestants
- Systemic effect. Ex. Vitamins, Nicotine
According to texture and Composition:
- Chewy or caramel based medicated lozenges
- Compressed tablet lozenges
- Soft lozenges
- Hard candy lozenges
DISADVANTAGE OF LOZENGES:
- Some drug may not be suitable with aldehyde candy bases e.g. Benzocaine.
- Possible draining of drug from oral cavity to stomach along with saliva.
- By mistakenly the lozenges dosage form could be used as candy by children.
- A hard candy lozenges required high temperature for their preparation
DOSING:
Patients to use the lozenge on the following pattern:
- Weeks 1-6: Use 1 lozenge every 1 to 2 hours (use at least 9 lozenges per day for the first 6 weeks)
- Weeks 7-9: Use 1 lozenge every 2 to 4 hours
- Weeks 10-12: Use 1 lozenge every 4 to 8 hours
Do not use more than 20 lozenges per day
TYPES OF LOZENGES:
There are so many different types of lozenges, some are medicated and some are non-medicated that are based on their action and also based on their texture. Some of the herbal types of lozenges are also present.
According to the site of action;
(a) Local effect
Example: Antiseptics, Decongestants.
(b) Systemic effect
Example: Vitamins, Nicotine.
According To Texture And Composition;
- Hard candy lozenges
- Soft lozenges
- Compressed tablet lozenges
- Chewy or caramel based medicated lozenges
HARD CANDY LOZENGES:
Hard candy lozenges is prepared by mixing sugar and other carbohydrates that are kept in an amorphous or glassy condition. In this hard candy lozenges the content of moisture should be 0.5 to 1.5%. Lozenges traditionally were used for the relief of youngster sore throat ache and inflammation and had been used drastically to deliver topical anesthetics and antibiotics.
Lozenges are diverse-shaped, solid dosage forms normally containing a medicinal agent and a flavoring substance, supposed to be dissolved slowly within the oral cavity for localized or systemic outcomes.
SOFT LOZENGES:
Soft lozenges have turn out to be famous due to the fact of the ease of extemporaneous training and applicability to a vast range of drugs. The bases normally consist of a combination of quite a number polyethylene glycols, acacia or comparable materials. One shape of these smooth lozenges is the pastille, which is described as a gentle range of lozenge, commonly transparent, consisting of a medicine in a gelatin, glycerogelatin or acacia: sucrose base.Soft lozenges are comparable to a historic structure of medicinal drug that is making a comeback the “confection”.
COMPRESSED TABLET LOZENGES:
When the API is temp sensitive, it may additionally be organized via compression. The granulation technique is comparable to that used for any compressed tablet. These lozenges range are differ from other by following factor:
- Organoleptic property
- Non disintegrating traits
- Slower dissolution profiles
The lozenge is made the usage of heavy compression tools to supply a pill that is more difficult than usual, as it is ideal for the troche to dissolve slowly in mouth. Commercially, these lozenges are less important.
CHEWY OR CARAMEL BASED MEDICATED LOZENGES:
Soft, chewable sweets have been on the market for a range of years. They are very highly flavored and many frequently include a barely acidic taste. They are an splendid way of administering drug product as the flavour of the drug regularly can be masked very efficiently with fruit-flavored products. They are pretty handy to prepare extemporaneously. These are the dosage structure in which medicament is included into a caramel base which is chewed as a substitute of being dissolved in mouth
STABILITY OF LOZENGES:
The steadiness research have been carried out to investigate bodily as well as the chemical balance of the drug, which may also perhaps have an effect on the organoleptic houses of the lozenges. Accelerated steadiness learn about was once carried out as per ICH pointers (zone IV) at 45°C and 75% relative humidity over a length of seven weeks. Sufficient quantity of optimized formulations have been packed in amber colored screw capped bottles and saved in incubator maintained at 37°C. Samples had been taken at intervals of 15 days to estimate the drug content material and to consider organoleptic properties.
For each hard sweet lozenges and compressed tablet lozenges, steadiness concerns lengthen to areas no longer typically of difficulty with different kinds of tablets.
STORAGE OF LOZENGES:
These preparations ought to be saved away from heat and should be out of the reach of children. They need to be covered from extremes of humidity. Depending on the storage condition of both the drug and base, either room temperature or refrigerated temperature is typically indicated.
PACKAGING OF LOZENGES: Hard lozenges are hygroscopic and commonly susceptible to absorption of atmospheric moisture. Considerations need to consist of the hygroscopic nature of the sweet base, storage requirement of the lozenges, size of time they are saved and the conceivable for drug interactions. These product have to be kept in tight containers to stop drying. This is mainly actual of the chewable lozenges that may additionally dry out excessively and come to be challenging to chew. If a disposable mould with a cardboard sleeve is used, it is first-class to slip this unit into a desirable labelled, sealable plastic bag.
1. List Of Type Of Ingredients:
MATERIAL AND METHODOLOGY:
| S.no | Type of ingredients | Ingredients used |
| 1. | APIs | · Liquorice· Ginger· Black pepper |
| 2. | Binders | Gelatin |
| 3. | Flavouring agent | · Menthol· Orange essence |
| 4. | Colouring agent | Red colour |
| 5. | Sugar | Honey |
ABOUT THE INGREDIENTS:
Liquorice:
Liquorice is the popular name for Glycyrrhiza glabra, a flowering plant in the bean family Fabaceae from which a sweet, fragrant flavouring may be obtained.
Liquorice is a plant that grows throughout Europe and Asia. Glycyrrhizin, found in liquorice root, can induce negative effects if consumed in sufficient quantities. Liquorice’s compounds are supposed to reduce edoema, cough, and enhance the chemicals in our bodies that heal ulcers.
It is also recognized as mulethi and is frequently used in Ayurvedic medicine for a variety of respiratory ailments. It has expectorant and demulcent properties and, Glycyrrhenic acid is responsible for these qualities.
Ginger:
Ginger (Zingiber officinale) is a herbaceous perennial plant of the Zingiberaceae family, most likely native to Southeast Asia. Its strong fragrant rhizome used as a spice, flavouring, food, and medicinal.
Ginger contains roughly 2% essential oil; the main component is zingiberene, while the spice’s pungent principle is zingerone. The oil is extracted from rhizomes and used in the culinary and fragrance industries.
Black pepper:
Black pepper (Piper nigrum) is a flowering plant in the Piperaceae family that is grown for its fruit, known as a peppercorn, which is often dried and consumed as a spice and condiment.
Black pepper is one of the most widely used spices in the world. Peppercorns, which are dried berries from the plant Piper nigrum, are ground to make it. It has a crisp and gently spicy taste that complements a variety of foods. However, black pepper is much more than a culinary essential. Because of its high concentration of strong, beneficial plant chemicals, it has been dubbed the “King of Spices” and has been utilised in traditional Ayurvedic medicine for thousands of years.
Gelatin:
Gelatin, also known as gelatine, is a transparent, colourless, and flavourless culinary component manufactured mostly from collagen extracted from animal body parts. When dry, it is brittle, and when wet, it becomes rubbery. After hydrolysis, it is also known as hydrolyzed collagen, collagen hydrolysate, gelatine hydrolysate, hydrolyzed gelatine, and collagen peptides. It is extensively used in food, drinks, pharmaceuticals, drug and vitamin capsules, photographic films and papers, and cosmetics as a gelling agent, thickening agent and binding agent.
Colouring Agent:
Colorants are mostly employed to enhance the look of pharmacological dosage forms. Tablets, tablet coatings, capsules (hard gelatin, soft gelatin), liquid orals, dental pastes, ointments and salves, and other medicinal preparations must all be coloured.. Colorings may be necessary to improve the visual appearance, extend the stability, provide standard preparations, or identify a specific formulation.
According to colour psychology, the colour of a product can impact the efficacy of therapy. As a result, the primary goal of colourants is to improve the aesthetic look of the product, and we may refer to colourants as cosmetics for medicinal formulations.
Flavouring Agents:
Flavoring agents are substances that give drug a different taste or flavor while improving the quality of their taste. This is especially crucial in the case of children, as it can have a considerable influence on their ability to take a formulation as well as their medicine adherence. A formulation’s flavour is frequently matched with its colour, which increases patient acceptance.
Flavoring agents should be avoided in procedures requiring high temperatures due to their great sensitivity to heat.
Honey:
Honey is a sweet, viscous food material produced by honey bees and other bee species. Honey is harvested from wild bee colonies or domesticated bee hives, a process known as beekeeping or apiculture.
Honey is sweetened by the monosaccharides fructose and glucose and has a similar relative sweetness to sucrose. When used as a sweetener, it possesses appealing chemical qualities for baking and a particular taste. Because most germs do not develop in honey, preserved honey will not deteriorate for thousands of years.
3. USE OF INGREDIENTS USED IN LOZENGES:
| S.no | Ingredients | Use |
| 1. | Liquorice | It is added to treat and prevent the sore throat and cough. |
| 2. | Ginger | It is added to treat pain and inflammation as it has antibacterial properties. |
| 3. | Black pepper | Due to its expectorant properties, it is added to suppress cough. |
| 4. | Menthol | It is used as a flavouring agent to mask the unpleasant taste of the formulation. |
| 5. | Orange essence | It is also used as a flavouring agent that helps in masking the unpleasant taste of the preparation. |
| 6. | Gelatin | Gelatin is added to thicken the formulation. It acts as a binder. |
| 7. | Red colour | It is used as a colouring agent to enhance the appearance of the preparation. |
| 8. | Honey | It is used as a sugar base. |
4. METHOD OF PREPARATION:
i. Weighing and heating to prepare the formulation:
· Weighed all the ingredients accurately on weighing balance.
· Sieved the ingredients with sieve no 150 to achieve better uniformity.
· In a beaker, the sugar base was made by heating the necessary amount of honey on a hot plate.
· The temperature was kept constant at 105-110 °C until the consistency of the mixture thickened.
· After that liquorice, ginger and black pepper powders were added and mixed for 15 minutes with continuous stirring.
· Menthol and orange essence were manually introduced in a mixture containing base and drugs to mask the unpleasant taste of the drugs.
· Red food colour is added to enhance the look of the preparation.
· Then lastly, gelatin is added to thickening the formulation.
ii. Molding the mixture:
· Then the mixture was poured into the desired shaped container to form a candy.
· Cooled down the mixture for 15-20 minutes.
· Kept the mould in refrigerator to harden the lozenges.
· Lozenges were taken out from the mould for physical evaluation.
5. PHYSICAL EVALUATION OF LOZENGES
By pharmaceutical standard techniques, the manufactured lozenges were assessed for criteria such as drug content uniformity, hardness, thickness and diameter, weight fluctuation, friability and in vitro dissolving test, drug content, moisture content analysis, and stability tests.
i. Diameter test
Vernier callipers were used to measure the thickness and diameter of the lozenges. Three lozenges from each batch were used to calculate mean values.
ii. Variation in weight
The weight variation was carried out by weighing 20 lozenges separately, computing the usual weight, and comparing the weight of each lozenge to the typical value. Variation in weight can be determined by a formula i.e;
Weight variation = average weight – initial weight x average weight
iii. Hardness test
The Monsanto Hardness tester was used to determine the hardness of the lozenges, and the force necessary to interrupt the lozenges was recorded. The hardness was measured in kg/cm.
iv. Flexibility
The Roche Friabilator was used to determine the friability of the lozenges. Lozenges were weighed and placed into the friability for 4 minutes at 25 rpm.
v. Analysis of moisture content
The Helium moisture balance equipment is used to determine the moisture content of the finished confectionery. The sample was weighed and crushed in a mortar, and the moisture content was determined using the moisture balance device based on one gramme of the sample.
vi. Drug dissolution studies in vitro
The effectiveness of the tablet lozenge is considered to be determined by the rate of dissolving. The dissolving research was performed in 800 cc of pH 6.8 phosphate buffer at 150 rpm using the USP II paddle system. Every 5 minutes, a sample was obtained and promptly replaced with an equivalent amount of fresh buffer before being examined using a UV spectrophotometer.
vii. Drug content
A suitable number of lozenges are crushed and dissolved in a suitable solvent, and the absorbance of the solution is determined spectrophotometrically.
viii. Lozenge Microbiological Test
The presence of bacteria, mould, or spores in the formed lozenges is monitored using raw materials, completed goods, machinery, cooling tunnels, ambient conditions, and storage drums, among other things. Counts on a total plate, total coliform, yeast and mould, E.coli, staphylococcus species, and salmonella are all examples of laboratory microbiological testing.
ix. Stability tests
Over a seven-week period, an accelerated stability study was carried out in accordance with ICH recommendations (zone IV) at 45°C and 75 percent ratio. A sufficient number of optimal formulations were packed in amber-colored screw-capped bottles and stored in a 37°C incubator. Samples were obtained at 15-day intervals to evaluate drug concentration and organoleptic characteristics.
x. Storage techniques
Keep these preparations away from heat and out of the reach of minors. They should be kept away from severe humidity. Depending on the medication and base storage requirements, either room temperature or refrigerated temperature is commonly advised.
xi. Packaging techniques
Hard candies are hygroscopic, meaning they absorb ambient moisture. The candy base’s hygroscopic design, the storage circumstances of the lozenges, the amount of time they are produced, and the risk for medication reactions must all be considered. Store these goods in sealed containers to avoid drying. This is especially true with chewable lozenges, which can become difficult to chew if they become too dry. When using a disposable mould with a cardboard sleeve, store it in a clearly labelled, sealable plastic container.
REERENCE:
http://www.jddtonline.info/index.php/jddt/article/view/2300/1632
https://www.researchgate.net/profile/Renuka-Pothu/publication/305748457_LOZENGES_FORMULATION_AND_EVALUATION_A_REVIEW/links/579f0b9d08ae802facbdff94/LOZENGhttps://www.webmd.com/drugs/2/drug-3867/throat-lozenges-mucous-membrane/details
| Pundir, Suchitra, and Abhay Murari Lal Verma. “Review on lozenges.” Journal der pharmazie Forschung 2.1 (2014): 1-10. | |
| APA | |
Dawes, C. and Macpherson, L.M.D., 1992. Effects of nine different chewing-gums and lozenges on salivary flow rate and pH. Caries research, 26(3), pp.176-182.
| Peters, David. “Medicated lozenges.” Pharmaceutical Dosage Forms: Tablets, 2nd Ed.; Lieberman, HA, Lachman, L., Schwartz, JB, Eds (1989): 419-463. | |
