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131 INTERNATIONAL JOURNAL OF INNOVATION IN ENGINEERING RESEARCH & MANAGEMENT ISSN: 2348-4918
Peer Reviewed and Refereed Journal
VOLUME: 08, Issue 04, Paper id-IJIERM-VIII-IV, August 2021
ENHANCING THE ORAL BIOAVAILABILITY OF ALBENDAZOLE: DEVELOPMENT AND ASSESSMENT OF FAST-DISSOLVING TABLET FORMULATION
Dr. P.Raja Sridhar Rao
Assoc. Professor, Department of Pharmaceutics, Princeton College of Pharmacy, Hyderabad, Telangana, India
G Satheesh
Asst. Professor, Department of Pharmaceutics, Princeton College of Pharmacy, Hyderabad, Telangana, India
Abstract - Albendazole is a broad-spectrum anthelmintic that can be used to kill numerous helminths. Treatments for Tapeworm, Hookworm, and Threadworm are made with it. Due to its first-pass metabolism, it has a low bioavailability. In this study, a fast-dissolving Albendazole tablet was designed to provide a rapid onset of action. The study's primary objective was to develop Albendazole tablets with a faster dissolution rate in order to further enhance the drug's bioavailability. Tablets that are made to dissolve quickly, tested for the pre-compression parameters, and prepared through direct compression with various concentrations of super disintegrants. For the purpose of post-compressional evaluation, the prepared tablets were evaluated. The formulation F3 with 5% w/w superdisintegrant Crospovidone and 20% w/w microcrystalline cellulose was deemed to be the best of all, with a release rate of up to 99.097% in 40 minutes.
Keywords: Albendazole, superdisintegrants, in vitro disintegration time, in vitro dissolution test.
1 INTRODUCTION
By developing a dosage form that is intended for administration, recent advancements in novel drug delivery systems aim to enhance the drug molecule's safety and efficacy (Kuchekar et al., 2003). Patients such as children, geriatrics, bedridden, disabled, and mentally ill individuals experience difficulty swallowing (Seager et al., 1998). According to Shu et al., fast dissolving tablets are solid dosage forms containing medical substances that disintegrate rapidly upon being placed on the tongue, typically within a few seconds, requiring no additional water to facilitate swallowing. 2002; Bradoo and other, 2001). Albendazole (ABZ), also known as methyl [5-(propylthio)- 1-H-benzimidazol-2yl] carba-mate, is
a benzimidazol derivative that is effective against a variety of helminth parasites in both animals and humans (Cook et al., 1990).
Echinococcosis, neurocysticercosis, and hydrated cysts can all be effectively treated with ABZ (Wen et al., 1993).
One method, direct compression, necessitates the inclusion of superdisintegrants in the formulation or highly. Superdi- sintegrants like cross-linked Croscarmellose Sodium, Polyvinyl Pyrrolidone K30, Microcrystalline Cellulose, and Crospovidone, among others, were the fundamental method utilized in the creation of FDT. Which provide instantaneous tablet disintegration upon tongue
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132 INTERNATIONAL JOURNAL OF INNOVATION IN ENGINEERING RESEARCH & MANAGEMENT ISSN: 2348-4918
Peer Reviewed and Refereed Journal
VOLUME: 08, Issue 04, Paper id-IJIERM-VIII-IV, August 2021 placement, releasing the medication
into saliva.
2 MATERIAL AND METHODS
Brasica Pvt. provided a sample of albendazole as a gift. Ltd. Boisar (India). A sample of crospovidone, croscarmellose sodium, and microcrystalline cellulose were presented as a gift by Curex Pharma, Jalgaon. Emcure Pharma, Pune, provided Polyvinyl Pyrrolidone K30 as a gift sample, and Merck Ltd, Mumbai, India, provided Manni-tol, Aspartame as a gift sample. All of the reagents and chemicals used were of analytical quality.
2.1 Preparation of Fast Dissolving Tablets
Using the direct compression method and superdisintegrants Crospovidone (CP), Croscarmellose Sodium (CCS), and Polyvinyl Pyrrolidone K30 (PVPK30), fast-dissolving Albendazole tablets were prepared beforehand.
Using a pestle, the 200 mg of Albendazole, mannitol, and microcrystalline cellulose were thoroughly mixed in a glass mortar. In accordance with each tablet formulation, superdisintegrants were added to the powder mixture, and then Aspartame and magnesium stearate were added. Sieve No. 1 was used to process the entire mixture.
The rotary tablet machine [Jaguar (JMD4-8)]'s 12mm round flat-faced punch was used to make the tablets.
3 PRECOMPRESSION PARAMETERS 3.1 Angle of Repose
The fixed funnel method was used to determine the angle of repose. A funnel that can be raised vertically to a maximum cone height (h) was used
to pour the mixture through. The heap's radius (r) was measured, and a formula was used to determine the angle of repose (Rockville et al., 2007).
3.2 Bulk Density
Apparent bulk density (LBD) was determined by pouring blend into a graduated cylinder. The bulk volume (Vo) and weight of powder (M) was deter-mined.
3.3 Tapped Density
The measuring cylinder containing known mass of blend was tapped for a fixed time. The minimum volume (Vt) occupied in the cylinder and weight of powder blend (M) as measured.
3.4 Carr’s Compressibility Index The simplex way of measurement of the free flow of powder is compressibility, an indication of the ease with which a material can be induced to flow is given by compressibility index of the granules was determined by Carr’s compressibility index (C) which is calculated.
3.5 Post compression parameters All the batches of tablets were evaluated for various parameters like weight variation, friability, hardness, drug content, disintegration and dissolution and results.
3.6 Uniformity of weight
By randomly weighing 20 tablets and calculating their average weight, this test is carried out to maintain the uniform weight of each tablet within the prescribed range. The mean and standard deviation were calculated (Thahera et al.,) for no more than two of the individual weights that differ
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133 INTERNATIONAL JOURNAL OF INNOVATION IN ENGINEERING RESEARCH & MANAGEMENT ISSN: 2348-4918
Peer Reviewed and Refereed Journal
VOLUME: 08, Issue 04, Paper id-IJIERM-VIII-IV, August 2021 from the average weight by more than
the 2012).
3.7 Thickness
Using a Micrometer screw gauge, the tablets' thickness and diameter were determined. Average values were calculated using five tablets from each formulation. It is given in millimeters (Liberman et al., 1990).
3.8 Hardness Test
The hardness of the tablet was determined using Monsanto Hardness Tester (Rockville et al., 2007).
3.9 Friability Test
Using Roche Fribilator (Tropical Equip-ment Pvt.) and six tablets from each batch, the friability of the tablets was evaluated. Ltd. Mumbai, India), and the apparatus was turned on for four minutes at 25 RPM. The tablets were removed, dedusted, and reweighed, and the percentage of friability was determined (Rockville et al., 2007).
3.10 Water Absorption Ratio
A piece of tissue paper collapsed two times was kept in a Petri dish (inner breadth 5.5cm) containing 6ml of refined water. The tissue paper was placed over the tablet and allowed to completely absorb the liquid. The wet tablet was taken out and weighed again.
3.11 In Vitro Disintegration Time At first, the Pharmacopoeia's standard test for tablets was used to measure the disintegration time of fast- dissolving tablets. Tablets were put in the crumbling cylinders and time expected for complete breaking down without leaving any deposits on the
screen was recorded as deterioration time (EP, 1988).
4 CHARACTERIZATION OF ALBENDAZOLE TABLET FT-IR STUDIES
For the pure Albenda-zole, an infrared spectrum was taken. Computer- mediated Fourier transformed infrared spectroscopy (FTIR) (Shimadzu Model – IRAFFINITY-1, Serial No.) was used for the KBr disk method of FT-IR research. A21374600405 ).
Albendazole fast-dissolving tablets were prepared by direct compression using superdisintegrants like Crospovidone, Croscarmellose sodium, and Microcrystalline Cellulose in concentrations of 5 percent, 4 percent, and 15 percent, respectively. Position of repose:
between 24.68 and 28.62 degrees indicate good flow. Tapped density and bulk density: between 0.61 and 0.72 g/ml, or 0.38 and 0.47 g/ml, respectively. The Hausner ratio and compressibility index, on the other hand, range from 1.13 to 1.58. The tablets were kept for 0 days, 30 days, 60 days, and 90 days at 45°C 2°C/75%. The hardness increased over time, but it remained within the limit in all cases. Time to decomposition: at various storage conditions rises, but not more than 40 seconds, or less than one minute (IP specification). According to studies on the dissolution of formulations, there was no significant difference between the dissolution data at the beginning and after a specific storage period.
5 CONCLUSION
Albendazole tablets that dissolve quickly can be made using direct compression techniques and certain
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134 INTERNATIONAL JOURNAL OF INNOVATION IN ENGINEERING RESEARCH & MANAGEMENT ISSN: 2348-4918
Peer Reviewed and Refereed Journal
VOLUME: 08, Issue 04, Paper id-IJIERM-VIII-IV, August 2021 superdisintegrants for better patient
compliance and effective treatment.
Crospovidone was found to be superior to Croscarmellose sodium in terms of their ability to improve tablets' disintegration and dissolution rates.
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