ACCENT JOURNAL OF ECONOMICS ECOLOGY & ENGINEERING Peer Reviewed and Refereed Journal, ISSN NO. 2456-1037
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Vol. 07, Issue 02,February 2022 IMPACT FACTOR: 7.98 (INTERNATIONAL JOURNAL) 104 EXPLORING CAMPHOR SUBLIMATION FOR RAPID RELEASE OF
ONDANSETRON IN FAST DISSOLVING TABLETS: A COMPREHENSIVE CHARACTERIZATION STUDY
Kasireddy Swetha Reddy
Asst. Professor, Department of Pharmacology, Princeton College of Pharmacy, Hyderabad, Telangana, India
Shireesha Bandirala
Asst. Professor, Department of Pharmacology, Princeton College of Pharmacy, Hyderabad, Telangana, India
Abstract - Ondansetron Hydrochloride (OSH) is a drug that is only slightly soluble in water. Ondansetron fast dissolving tablets (FDTs) were made in this study by sublimating a variety of superdisintegrants. In vitro dissolution and physicochemical properties of FDTs were examined. The formulation batch that contained crospovidone (F2) had the shortest wetting time (10.5 s) and the tablets disintegrated the quickest (3.2 s). The formulation batch containing crospovidone (F2) was found to have the highest drug release (98 percent drug release after 30 minutes), making it a promising formulation. The drug release from FDTs containing superdisintegrants was higher than that from FDTs without superdisintegrants.
1 INTRODUCTION
OSH is a well-tolerated and effective antiemetic that is used to prevent nausea and vomiting caused by both radiotherapy and chemotherapy.
Water soluble OSH is sporadic. The drug dissolves or disperses in the saliva when this fast-dissolving tablet is placed on the tongue and dissolves instantly. First-pass metabolism occurs and it is well absorbed from the gastrointestinal tract. Following oral administration of a single 8-mg tablet, the mean bioavailability in healthy subjects is approximately 56 percent.
Because it is convenient for self-administration, small, and simple to manufacture, the tablet form of administration is the most widely used among all dosage forms currently in use. However, poor patient compliance is frequently
caused by hand tremors, dysphasia in elderly patients, underdeveloped muscular and nervous systems in young people, and the difficulty swallowing in uncooperative patients.
The desire to provide patients with a conventional method of taking their medication led to the development of the concept of a fast dissolving drug delivery system as a means of overcoming these limitationas.
Patients with persistent nausea, sudden episodes of allergic attack, or coughing for those who lead an active lifestyle—such as children, geriatrics, bedridden, or mentally disabled patients—may have difficulty swallowing conventional tablets or capsules, resulting in ineffective treatment. Fast dissolving tablets are useful in these patients.
ACCENT JOURNAL OF ECONOMICS ECOLOGY & ENGINEERING Peer Reviewed and Refereed Journal, ISSN NO. 2456-1037
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Vol. 07, Issue 02,February 2022 IMPACT FACTOR: 7.98 (INTERNATIONAL JOURNAL) 105 Utilizing subliming agents like
camphor, menthol, or thymol, among others, to maximize the tablet's pore structure is another method taken in the production of such tablets. in the method of sublimation. A permeable hydrophilic grid is produced which may effortlessly get the crumbling medium, break rapidly and subsequently give momentary deterioration.
The proposed work aimed to develop and characterize fast- dissolving ondansetron tablets using a sublimation method for rapid drug dissolution and absorption, potentially leading to a rapid onset of action.
2 MATERIALS AND METHODS 2.1 Materials
Zydus Cadila Ltd., Ahmedabad, provided OSH, Mannitol, aspartame, Crospovidone (CP), Sodium starch glycolate (SSG), and Low substituted hydroxy propyl cellulose (L-HPC).
Relax Pharmaceuticals Ltd., Baroda, supplied the microcrystalline cellulose PH-101. Molychem Ltd., Samir Tech Chem Pvt., and Talc supplied the camphor, magnesium stearate, and talc. Ltd., Baroda respectively, and Allied Chemical Corporation Ltd.
Analytical-grade chemicals and reagents were also used.
2.2 Preparation of Fast Dissolving Tablets
The sublimation method was used to prepare ten batches of OSH FDTs according to composition. Before use, a fine sieve was used to filter out mannitol, camphor, aspartame, and microcrystalline cellulose PH101.
After that, the drug and excipients
were combined by tumbling for ten minutes. Talc and one percent magnesium stearate were used to lubricate the mixture. Using a rotary tablet machine, the resulting blend was directly compressed into tablets.
Rimek, India's RSB-4 mini press). The tablet weight was acclimated to ~150 mg. In a vacuum oven at 60 degrees Celsius for six hours, the sublimation process was performed on the compressed tablets.
3 EVALUATION OF FAST DISSOLVING TABLETS
3.1 Weight Variation
The average weight of twenty tablets was determined after they were each individually weighed. For weight variation, the percentage deviation was calculated and evaluated.
3.2 Hardness
The force required to break a tablet in a diametric compression of five tablets, or tablet hardness, was measured with a Monsanto hardness tester (Dolphin, Mumbai).
3.3 Friability
The Roche friabilator (Erection and Instrumentation Engineers, Ahmedabad) was used to spin a sample of ten tablets that had been pre-weighed. A soft muslin cloth was used to dedust the tablets, and they were reweighed. It is determined how much friability there is.
3.4 In vitro Disintegration Time A modified disintegration method was used to measure the disintegration time of five tablets. A petridish with a diameter of 10 cm was filled with 10 mL of distilled water for this purpose.
ACCENT JOURNAL OF ECONOMICS ECOLOGY & ENGINEERING Peer Reviewed and Refereed Journal, ISSN NO. 2456-1037
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Vol. 07, Issue 02,February 2022 IMPACT FACTOR: 7.98 (INTERNATIONAL JOURNAL) 106 The time it took for the tablet to
completely break up into fine particles was recorded as the disintegration time. The tablet was placed with care in the middle of the petridish.
4 EVALUATION OF FAST DISSOLVING TABLETS
The tablets' hardness ranged from 2.5 to 4.3kg/cm2 according to the evaluation parameters. The tablets' lower than one percent friability indicates their high mechanical resistance. The amount of drugs found was between 95.14 and 98.21%.
All formulations had disintegration times between 3.22 and 7.56 seconds, which was within FDA's official requirement of less than 30 seconds. In order to establish a correlation between oral cavity disintegration time and wetting time, Understanding the capacity of disintegrants to swell in the presence of little water is crucially dependent on this criterion. The measurement of wetting time can be used as an additional confirmative test for the evaluation of fast-dissolving tablets because the dissolution process of a tablet is dependent on the wetting and subsequent disintegration of the tablet. The results showed that FDTs containing CP as a superdisintegrant (F2) had the shortest wetting time (10.5 s) and the fastest disintegration (3.22 s) when compared to CCS, L- HPC, and SSG. The wetting time of the formulated tablets ranged from 10.5 to 14.12 s.
The results of the dissolution show that, in comparison to batch F1 without a superdisintegrant, more than 90% of the drug released within
30 minutes from all batches containing supedisintegrants (F2–F5).
According to the findings, the batch containing CP (F2) had a higher rate of dissolution (98 percent release after 30 minutes) than the batches containing CCS, L-HPC, and SSG (F3–
F5). The order in which the superdisintegrants increase the rate of dissolution could be CP> L-HPC>
SSG> CCS. The comparison profile of the release. Due to its faster disintegration time, lower wetting time, and higher drug release, the F2 batch was chosen as a promising formulation.
Cross-sectional and surface scan electron micrographs of the promising batch (F2). The micrograph shows the exceptionally permeable nature of the pre-arranged sublimed tablet, which show up in both surface and the inward construction. These results indicate that the addition of camphor followed by sublimation had a significant impact on the inner structure of the tablet, which in turn had an impact on the wetting, disintegration, and dissolution of the final tablet. The rapid penetration of water into the tablet is explained by the tablet's highly porous nature.
After six months of storage at 25°C 2°C/50% 5 percent relative humidity, the tested parameters of the promising formulation did not significantly differ from the initial results, according to the stability studies. The selected formulation was found to be stable, as demonstrated by the stability study's findings.
5 CONCLUSION
In conclusion, the formulation of fast- dissolving Ondansetron tablets
ACCENT JOURNAL OF ECONOMICS ECOLOGY & ENGINEERING Peer Reviewed and Refereed Journal, ISSN NO. 2456-1037
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Vol. 07, Issue 02,February 2022 IMPACT FACTOR: 7.98 (INTERNATIONAL JOURNAL) 107 prepared using crospovidone as a
superdisintegrant through the camphor sublimation method appears to be promising, and additional in- vivo research may be conducted.
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