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) 95 ENHANCING DISSOLUTION RATE OF PARACETAMOL THROUGH SOLID DISPERSION
AND POLYMER COATING TECHNIQUES FOR RAPID DISPERSIBLE TABLET FORMULATION
Dr. Kadasi Sundeep
Assoc. Professor, Department of Pharmaceutical Chemistry, Princeton College of Pharmacy, Hyderabad, Telangana, India
Hariprasad Kadiyam
Assoc. Professor, Department of Pharmaceutical Chemistry, Princeton College of Pharmacy, Hyderabad, Telangana, India
Abstract - The fundamental requirement for achieving a rapid onset of action is the concept of dosage forms that are rapid dispersible or fast dissolving. Paracetamol is a common over- the-counter pain reliever and antipyretic that doesn't cause gastric irritation or ulcers. Due to its low solubility, the rate-limiting step in paracetamol absorption is its dissolution. In the case of pediatrics, developing a high-quality formulation is further complicated by the active's bitter taste. The goal of the current study was to develop rapid dispersible paracetamol tablets by coating them in polymer and using solid dispersion to improve solubility and flavor masking. Different carriers in solid dispersion were used to make different paracetamol formulations, and a thin layer of polymer coating was used to hide the taste. The detailing was than assessed for different physical and logical properties of fast dispersible tablets. Results got showed that there was a critical effect of transporters utilized during definition of Strong scattering of paracetamol. Using Mannitol and Betacyclodextrin as carriers in the solid dispersion phase of paracetamol, a rapid release was observed. The organoleptic properties of formulations A-5 and A-6 were also found to be superior to those of other formulations and acceptable.
Keywords: Tablets with Rapid Dispersibility, Solubility Enhancement, Solid Dispersion, Taste Masking, and a Dissolution Profile.
1 INTRODUCTION
The novel drug delivery system concept known as a rapid disintegrating drug delivery system was developed to address the fundamental flaws of conventional tablets. Based on recent advancements, dispersible tablets can be distinguished into two categories: one that dissolves or dissolves directly in the mouth without the need to drink water; the other, on the other hand, needs water to form a dispersion in a matter of seconds and is simple for the patient to take. In both the cases, bioavailability of medication is fundamentally more noteworthy because of moment scattering and solvency than those saw from ordinary dose form.
Paracetamol (4'- hydroxyacetanilide, N- acetyl p-aminophenol, acetaminophen, Standard) is a broadly utilized over-the- counter pain relieving and antipyretic
medication with practically no gastric disturbance and ulcerative effects.
Paracetamol is white glasslike powder having unpleasant in taste. As per Biopharmaceutical Grouping framework, Paracetamol is a class IV, a low solvent and low porous drug. A medication with poor fluid dissolvability will commonly show disintegration rate restricted retention, and a medication with unfortunate layer porousness will regularly display saturation rate restricted absorption. Consequently, 'Definition researcher' centers around two regions for working on the oral bioavailability of medications include: (The Hydrotropy methods, the solid dispersion method, the use of carrier as co solvent, and the uses of surfactants, superdisintegrants, and polymers are some commonly used
ACCENT JOURNAL OF ECONOMICS ECOLOGY & ENGINEERING Peer Reviewed and Refereed Journal, ISSN NO. 2456-1037
Available Online: www.ajeee.co.in/index.php/AJEEE
Vol. 07, Issue 02,February 2022 IMPACT FACTOR: 7.98 (INTERNATIONAL JOURNAL) 96 approaches for enhancement of aqueous
solubility of formulations that have been reported in literature. However, all these formulation concepts were focusing on the enhancement of solubility and release profile of active, and the organoleptic prosperities such as taste and patient compliance is still required to be developed with an effective release profile of formulation. The ebb and flow research work is plan to figure out a quick dispersible Tablets of Paracetamol with further developed disintegration qualities of medication with joined approach of strong scattering solvency upgrade and polymer covering on strong scattering granules of paracetamol to work on the organoleptic properties for definition. The two technologies work together to make paracetamol more soluble and better at masking the bitter taste. The study's intended release profile called for at least 85 percent of release to occur within 15 minutes. The formulation is primarily intended for use by children and the elderly.
2 MATERIALS AND METHODS
Elder Pharmaceuticals Ltd., Navi Mumbai, India, provided a sample of Paracetamol, Urea, and Eudragit-EPO. Cadila Pharmaceuticals Limited, based in Ahmadabad, India, provided a complimentary sample of Aspartame and Flavor Vanilla. From commercial sources, sodium starch glycolate, polyethylene glycol, lactose monohydrate, cyclodextrin, mannitol, methanol, hypromellose, talc, magnesium stearate, and ac-di-sol were obtained.
2.1 Solubility Enhancement of Paracetamol
Mayersohn and Gibaldi used the solid dispersion, also known as the solid-state dispersions, for the first time while researching various dispersion techniques. One of the most common methods for increasing the bioavailability and solubility of water-insoluble drugs is
solid dispersion. The choice of the carrier ultimately has an impact on the dissolution characteristics of the dispersed drug because the second component mixture has an effect on the rate at which a component dissolves from a surface. Consequently a water solvent transporter brings about a quick arrival of medication from the blend.
3 EVALUATION OF SOLID DISPERSION By Fourier Transform Infrared (FTIR) Spectrum Studies
In order to evaluate the impact of solid dispersion of Paracetamol with other excipients, the solid dispersion of Paracetamol with various carriers was placed using FTIR (Shimadzu). Using the KBR disc method, the FTIR spectra of each and every sample were recorded on Perkin Elmer instruments. The solid paracetamol dispersion was mixed with potassium bromide (KBr), triturated in a glass mortar, and finally placed in the sample holder for sample preparation.
The sample was scanned in the range of 4000 to 400 cm-1 in frequency.
3.1 Drug content of Solid Dispersion of Paracetamol
The examination for drug content of definition was created in view of monograph of Paracetamol in English pharmacopeia. 1.0 grams of solid dispersion paracetamol were used to evaluate each formulation's assay. In a 200 ml volumetric flask, accurately weigh a quantity of powder equivalent to 150 mg of paracetamol. Add 50 milliliters of 0.1 M sodium hydroxide to 100 milliliters of water, shake for 15 minutes, and then dilute with water up to the limit. Mix, filter, and add 100 milliliters of water to 10 milliliters of the filtrate. Add 10 ml of 0.1M sodium hydroxide diluted to volume with water to the remaining 10 ml of the solution in a 100 ml volumetric flask, and then measure the maximum absorbance of the solution at 257 nm.
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Vol. 07, Issue 02,February 2022 IMPACT FACTOR: 7.98 (INTERNATIONAL JOURNAL) 97 3.2 Dissolution Procedure
Disintegration of tablets was started by putting one tablet in every one of six vessels containing 900 ml disintegration medium, involving paddle at 50 rpm for an hour. Filter after removing 10 milliliters of the sample solution from each dissolution vessel at predetermined intervals. By adding dissolution media to the dissolution vessel, the same volume of the sample that was taken out is used to replace it. Dilute the filtrate to the mark with 0.1 M sodium hydroxide solution by transferring 5ml of it to a 100ml volumetric flask. Utilizing a UV Spectrophotometer (Shimadzu) at a wavelength of approximately 257nm and 0.1M Sodium Hydroxide as the blank solution, measure the absorbance of the sample solution.
3.3 Fourier Transform Infrared (FTIR) Spectrum Studies FTIR studies were utilized to clarify the drug-carrier interaction. The drug's presence in the formulation was confirmed by comparing the IR spectra of solid dispersions and pure drug. Unsaturation absorbance bands at 1653 and 1610 cm-1, and aromatic absorbance bands at 1565 and 1502 cm-1. These bands shifted in a variety of solid dispersion formulations as a result of complexation between the drug and the carrier. This indicates that a complex was formed during solvent evaporation and that the drug was not degraded as a result of using solvent evaporation techniques for solid dispersion with various carriers. However, there was no additional peak observed in the paracetamol solid dispersion spectrum, indicating that there was no chemical interaction or degradation.
3.4 Drug content of Solid Dispersion of Paracetamol
In the observation, the drug contents of various solid dispersion paracetamol formulations were analyzed and tabulated. The assay values for
paracetamol in various solid dispersion samples ranged from 97.50 percent to 101.2%. The process loss of the drug during the solid dispersion stage could be the cause of the lower Paracetamol assay.
The evaluation revealed a range of the mean value between 3.5 and 5. In terms of taste, the formulation with SSG, PEG, and lactose as a carrier was found to be less popular than the formulation with betacyclodextrin, urea, and mannitol.
Among all of the taste mask formulations for rapid dispersible paracetamol tablets, it was observed that the formulation with betacyclodextrin and mannitol displayed the most pleasant flavor.
4 CONCLUSION
Based on a variety of physical and analytical evaluations of the formulation, the combination of solid dispersion technology and taste masking with a polymer coating of Paracetamol can easily achieve a rapid dispersion and prompt release profile with improved organoleptic properties. With better bioavailability of the active due to the active's rapid absorption into the systemic circulation, the combined approach demonstrated a promising effect in the formulation's acceptance by a targeted group of pediatrics and geriatric patients. The evaluation of formulations A-5 and A-6 in comparison to other formulations revealed a more favorable release profile and acceptable organoleptic properties, demonstrating the advantages of combined technology for formulation over single technologies.
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