Mahesh Babasaheb Kolap, Pratiksha Kisan Omase, Abhijeet Vijay Dashwant, Rutuja Shrikant Namde
Dr. Bapuji Salunkhe Institute of Pharmacy, Miraj
*Corresponding Author E-mail: kolapmb@gmail.com
ABSTRACT:
Lozenges are one of the widely used solid, unit dosage form of medicament which are meant to be dissolved in mouth or pharynx. The benefits of the medicated lozenges is they increase the retention time of the dosage form in oral cavity which increases bioavailability, reduces gastric irritation and bypasses first pass metabolism. This dosage form can be adopted for local as well as systemic therapy and a wide range of active ingredient can be incorporated in them. The present review covers more or less all aspects associated with lozenge such as its manufacturing, classification, evaluation and its application Lozenges are one of the widely used solid, unit dosage form of medicament which are meant to be dissolved in mouth or pharynx. The benefits of the medicated lozenges is they increase the retention time of the dosage form in oral cavity which increases bioavailability, reduces gastric irritation and bypasses first pass metabolism. This dosage form can be adopted for local as well as systemic therapy and a wide range of active ingredient can be incorporated in them. The present review covers more or less all aspects associated with lozenge such as its manufacturing, classification, evaluation and its application.
KEYWORDS: Lozenges
INTRODUCTION:
Lozenges are the flavourized medicated dosage form intended to be sucked and held in the mouth or pharynx containing one or more medicaments usually in the sweetened base. Lozenges are intended to relieve oropharyngeal symptoms, which are commonly caused by local infections and also it provides systemic effect, the drug is well absorbed through the buccal linings or when it is swallowed. They are usually used for throat pain as well as irritation into throat extensively used to deliver the drug having topical anesthetic effect and also antibacterial effect[1].
Lozenges slowly releases the drug into buccal cavity for the purpose of yielding the required quantity of drug. Multiple number of drugs or ingredients can be incorporate into lozenges. These are OTC as well as prescription drug which totally depending on its content, it maximizes the local activity of drug and its absorption too, Widely they are used for treating the various conditions regarding to the mouth, tongue, throat.[1]
Definition:
“Lozenges are solid dosage form containing the flavoring and sweetening agents that are intended to dissolve or disintegrate slowly in the mouth or oral cavity”. They are most often used for localized effect into oral cavity and can also show systemic effect if it is well absorbed in the buccal lining and pharynx. [2]
Types of lozenges:
· Medicated lozenges.
· Non-medicated lozenges.
Classification of lozenges:
I. According to its site of action:
a. Local Effect-
e.g Antiseptics, Decongestant.
b. Systemic Effect-
e.g Vitamins, Nicotine.
II. According to its texture and composition:
a. Chewable-
e.g Vitamins.
b. Hard-
e.g Lollipops.
c. Soft-
e.g Bentasil.
d. Compressed-
e.g Troches.
A. CHEWABLE LOZENGES: [3]
The medicaments in chewable lozenges are incorporated into caramel base, hence instead of dissolving it into mouth it is chewed. These lozenges are prepared or formulated by using Glycerin, Gelatin, and Water. They are highly flavourized by fruits and also having somewhat acidic taste which is intentionally provided to mask the acrid taste of glycerin. These kinds of lozenges are especially for the pediatric use so that the medication meant for GIT absorption and systemic effect can be acquired. The Glycerin base used for chewable lozenges are totally similar with base used in glycerin suppositories or glycerin gelatinized suppositories. Which consists of 70% glycerin, 20% gelatin and 10% purified water.
B. HARD LOZENGES:
These types of lozenges are the mixture of sugar and carbohydrates. They are in noncrystalline forms usually in amorphous or glassy state. They are also called as “syrups of sugar”. The weight of hard candy lozenges are between 1.5-4.5gm. Moisture content of those are 0.5-1.5% these lozenges must undergo directly into dissolution instead of disintegration, but these lozenges preparation requires high temperature hence heat liable substance or ingredient cannot be formulated. Hard lozenges are widely used to treat the sore throat pain or to treat the various throat infection and also to get the relief from irritation by delivering the drug having the category of topical anesthetic or antibiotic activity.
C. SOFT LOZENGES:
Soft lozenges are meant for slow release of drug into mouth, and are prepared by using ingredients like PEG (polyethylene glycol), chocolate or acacia base some of soft lozenges contain silica gel also in its base acacia is the hero ingredient into these lozenges to achieve the smoothness and texture. PEG based lozenges get soften at high temperature and are also hygroscopic hence must be advised to store in a cool and dry place.
D.COMPRESSED LOZENGES:
The heat liable ingredients i.e heat sensitive ingredients are not possible to formulate by procedure same as that of soft lozenges, hard lozenges. Simply the compression method is applicable for such type of ingredients, same as like compressed tablet. The only difference between them is non-disintegrating and slower dissolution profile. The granulation method is used in compressed lozenges.
Table no-1:Formulation of lozenges
|
Ingredients |
Examples |
|
Candy base a. Sugar. b. Sugar free vehicle. c. Fillers.
|
Lactose, Maltose, Sucrose, Dextrose. Mannitol, Sorbitol, Polyethylene glycol. Di-calcium phosphate, Calcium sulphate, Calcium carbonate, Microcrystalline cellulose. |
|
Lubricants
|
Magnesium stearate, Calcium stearate, Stearic acid, PEG, Vegetable oils, Fats. |
|
Binders |
Acacia, Corn syrup, Sugar syrup, Gelatin, Polyvinyl pyrrolidone, Tragacanth, Methyl cellulose. |
|
Coloring agent |
Water soluble and lakolene dyes, Colors, Orange color paste, Red color cubes etc. |
|
Flavoring agent |
Menthol, Eucalyptus oil, Spearmint, Cherry flavor, etc. |
|
Whipping agent |
Milk protein, Egg albumin, gelatin, Xanthan gum, Starch, Pectin, Algin, Carrageenan. |
|
Humectant |
Glycerin, Propylene glycol, Sorbitol. |
Criteria for preparation of lozenges:
· Selection of proper drug for manufacturing of lozenges.
· Selection of appropriate drug carrier.
Method of preparation of lozenges:[4]
Technique used in Manufacturing-
Manufacturing of some lozenges are complicated it requires the conditions regarding to temperature and pressure and also some kind of special storage conditions. Hard lozenges are hygroscopic in nature, that they usually absorb the moisture from atmosphere. Chewable lozenges also dry and it becomes difficult for chewing, those lozenges are packed in blisters type packing or air tight plastic packets. These must label properly along with the exact storage condition.
Candy base- These is used to check the various parameters such as- corn syrup, sugar delivery gear, temperature, steam pressure, vaccum of cookers used for candy base.
Moisture analysis-
1. Gravimetric method- 1gm of testing sample is to be placed in vaccum oven at 60-70° for 12- 16 hrs. After specific given period of time, the sample is to be weighed and moisture content is calculated as follows-
Moisture content = Initial weight – Final weight
2. Karl fisher titration- A sample calculated so that to contain 10-250 mg water, is taken in titration flask and Karl fisher reagent is used and titrated.
3. Determination of sugar and corn syrup ratio- These can be done by using “Dextrose equivalent method” which is also termed as “Lane eyvon titration method”.
4. Percentage of reducing sugar- 3gm of anhydrous dextrose is dissolved in 500 ml of water and 2 drops of methylene Blue is added which is then boiled for 2 min and titrated against 25 ml of fehling solution and the end is yellowish red.
Percentage reducing sugar = (Reducing sugar factors × 100) ÷ (Sample weight / 250
× Volume of sample solution consumed by Fehling’s solution)
Diameter and thickness- Uniformity of lozenges is depending upon it’s diameter. It can be determined by vernier caliper. The extent limit for the diameter of lozenges is deviated from +-5 % of the standard value.
Hardness- The resistance of lozenges to shipping, storage conditions breakage, Transportation and handling, depending upon the hardness. hence it becomes necessary to measure hardness for checking it’s threshold capacity which can be measured by using Monsanto hardness tester in terms of kg/cmsq.
Weight variation- The USP weight variation test is done by weighing 20 lozenges individually and then by taking average comparing it as follows:
Weight variation = (average weight – initial weight) ÷ average weight
Friability- These is carried out for same as hardness testing. Friability testing is carried out by using Roche Friabilator operated at specific speed for specific time such 25 rpm for 4 min.
In-vitro drug release- This test is also termed as dissolution test and carried out in USP-II paddle type dissolution apparatus.
Drug content- Specific numbers of lozenges are crushed and dissolved in specified solvent and absorbance is determined by spectrophotometrically. Some of the example are as follows:
1. Anesthetics – Lidocaine, Benzocaine.
2. Analgesic – Fentanyl, codeine.
3. Antifungal – Clotrimazole, Miconazole.
4. Smoking cessation – Nicotine.
5. Nausea relief – Ondansetron, Promethazine.
These can be used to recognized or checkout the presence of any bacteria, mold, spores in the raw materials, finished products, machinaries, tunnels, environment of production or storage etc. Laboratories microbial test include the following counts :
Total plate
Total coliform
Yeast and mold
E.coli
Staphylococcus
Salmonella
1. Stability Testing of lozenges before packaging-
Lozenges are carried for stability testing under following conditions-
1-2 months at 60°C.
3-6 months at 45°C.
9-12 months at 37°C.
36-60 months at 25°C and 4°C.
2. Stability testing of lozenges after packaging-
Lozenges after final packing is carried for stability testing under following conditions-
25°C at 80%RH for 6-12 months.
37°C at 80%RH for 3 months.
25°C at 70%RH for 6-12 months.
Lozenges are the formulation which is easy and time saving process, And also it is the formulation which is more ever accepted and preferable for pediatric patients. Medicated lozenges such as used for treatment of throat infection, sore throat etc, are ideal dosage form for children’s and additional advantage of this include patient compliance, comfortable and effective treatment including fast onset of action, it requires low dose, dose regimen is also reduced, and the main thing is it is economic. Lozenges plays an very important role in pharmacy and also acquired a great position in this field and will remain it’s position at the same in future.
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10. Esimone CO, Okoye FBC, Odimegwu DC, Nworu CS, Oleghe PO, Ejogha PW. In vitro Antimicrobial Evaluation of Lozenges Containing Extract of Garlic and Ginger. Int J Health Res. 2010; 3(2): 105-110.
Received on 05.03.2021 Modified on 16.03.2021
Accepted on 16.04.2021 ©AandV Publications All right reserved
Res. J. Pharmacology and Pharmacodynamics.2021; 13(2):75-78.
DOI: 10.52711/2321-5836.2021.00016