Brazilian Journal of Pain
https://brjp.org.br/article/doi/10.5935/2595-0118.20240044-en
Brazilian Journal of Pain
Original Article

A simple approach to enhance dissolution of commercial paracetamol tablets for fast relief of pain

Uma abordagem simples para melhorar a dissolução de comprimidos comerciais de paracetamol para alívio rápido da dor

Alaa A. Abdulla; Murtada A. Oshi

http://dx.doi.org/10.5935/2595-0118.20240044-en BrJP, vol.7, e20240044, 2024
PDF English
PDF Português
SciELO
Downloads: 0
Views: 2

Abstract

BACKGROUND AND OBJECTIVES: Pain is considered a major clinical problem worldwide. Faster pain relief was reportedly achieved using a fast-dissolving paracetamol (APAP) tablet. Microcrystalline cellulose (MCC) is the most widely used excipient to produce fast-dissolving APAP tablet formulations, but it retards the dissolution of APAP. The present investigation reports incorporation of croscarmellose sodium (CCS) instead of MCC into APAP commercial tablet formulations to enhance the dissolution rate of APAP.

METHODS: A wet granulation method was used to prepare APAP tablets with various CCS concentrations, using a factorial design with 31 CCS concentrations as independent variables, while the dissolution percentage of the drug release at different time intervals was used as dependent variable. The disintegration time and dissolution rate of these APAP tablets were determined and compared with the dissolution rate of Amidol® and Panadol®, commercial APAP tablets available in Sudan.

RESULTS: The mean time to complete disintegration of the APAP tablets with CCS was faster than that for the commercial APAP tablets, both Amidol® (0.58 min vs. 2.43 min) and Panadol® (0.58 min vs. 1.32 min), and these differences were statistically significant for Amidol (p≤0.001) and Panadol® (p≤0.01). Moreover, the dissolution rate for the APAP tablets with CCS was significantly faster than those for Amidol® and Panadol®.

CONCLUSION: The dissolution of APAP from Amidol® and Panadol® can be successfully enhanced by incorporating CCS in their formulation and can be considered as a simple approach for fast-pain relieving using APAP.

Keywords

Croscarmellose sodium; Disintegration time; Factorial design; Fast-dissolving tablets; Microcrystalline cellulose; Pain; Paracetamol; Tablet dissolution rate

Resumo

JUSTIFICATIVA E OBJETIVOS: A dor é considerada um grande problema clínico em todo o mundo. O alívio mais rápido da dor foi obtido com o uso de um comprimido de paracetamol (APAP) de dissolução rápida. A celulose microcristalina (CMC) é o excipiente mais amplamente usado para produzir formulações de comprimidos de APAP de dissolução rápida, mas retarda a dissolução do APAP. A presente pesquisa relata a incorporação de croscarmelose sódica (CCS) em vez de CMC em formulações comerciais de comprimidos de APAP para aumentar a taxa de dissolução do APAP.

MÉTODOS: Um método de granulação úmida foi usado para preparar o APAP com várias concentrações de CCS, sendo usado um desenho fatorial de 31 concentrações de CCS como variáveis independentes, enquanto a porcentagem de dissolução da liberação do fármaco em diferentes intervalos de tempo foi usada como variável dependente. O tempo de desintegração e a taxa de dissolução desses comprimidos de APAP foram determinados e comparados com a taxa de dissolução de Amidol® e Panadol®, comprimidos comerciais de APAP disponíveis no Sudão.

RESULTADOS: O tempo médio para a desintegração completa dos comprimidos de APAP com CCS foi mais rápido do que o dos comprimidos comerciais de APAP, tanto Amidol® (0,58 min vs. 2,43 min) quanto Panadol® (0,58 min vs. 1,32 min), e essas diferenças foram estatisticamente significativas para o Amidol® (p≤0,001) e o Panadol® (p≤0,01). Além disso, a taxa de dissolução dos comprimidos de APAP com CCS foi significativamente mais rápida do que as taxas de Amidol® e Panadol®.

CONCLUSÃO: A dissolução do APAP para Amidol® e Panadol® pode ser aprimorada com sucesso pela incorporação da CCS em sua formulação e pode ser considerada uma abordagem simples para o alívio rápido da dor usando APAP.

Palavras-chave

Celulose microcristalina; Comprimidos de dissolução rápida; Croscarmelose sódica; Dor; Paracetamol; Projeto fatorial; Taxa de dissolução do comprimido; Tempo de desintegração

References

1 Gan TJ. Poorly controlled postoperative pain: prevalence, consequences, and prevention. J Pain Res. 2017;10:2287-98.

2 Britta M, Charly G, Olaf R, Tim P. Peter K, Ruth R, Andreas S. Headache impact and socioeconomic status: findings from a study of the German Migraine and Headache Society (DMKG). J Headache Pain. 2023;24(1):37.

3 Gallelli L, Tiziana A, Daniela F, Caterina P, Francesco P, Maria E. Effects of acetaminophen and ibuprofen in children with migraine receiving preventive treatment with magnesium. Headache. 2014;54(2):313.

4 Thunshuda S, Pornchai J. Single dose intravenous paracetamol versus placebo in postorthognathic surgery pain: a randomized clinical trial. Anesthesiol Res Pract. 2024;2024: 8898553.

5 Abbas Raza, Morton B, Kar C. Perspectives on using fast-dissolving paracetamol for mild-to-moderate pain management in elderly or diabetic patients with delayed gastric emptying rates: an exploratory study. J Pain Res. 2022;15:3675-88.

6 Raffa RB, Pergolizzi JV, Taylor R, Decker JF, Patrick JT. Acetaminophen (paracetamol) oral absorption and clinical influences. Pain PracYadav AK, Rai BK, Budhathoki SS, Ghimire A, Shrestha SR, Malla GB. Self-prescription of Paracetamol by Undergraduate Students in BP Koirala Institution of Health Sciences. JNMA J Nepal Med Assoc. 2016;55(203):11-5.

7 Awad AI, Idris Bl, Phillip AC. Self-medication practices in Khartoum State, Sudan. Eu J Clin Phar. 2006;62(4):317-24.

8 Srinivas NR. Acetaminophen absorption kinetics in altered gastric emptying: establishing a relevant pharmacokinetic surrogate using published data. J Pain Palliat Care Pharmacother. 2015;29(2):115-9.

9 Petra M, Sára K,Győző K, Melinda P, Attila A. Investigation of intestinal absorption and excretion of paracetamol in streptozotocin-induced hyperglycemia. Int J Mol Sci. 2022;23(19):11913.

10 JMurtada AO, Abdelkarim MA, Huyam M. The effect of sodium starch glycolate concentration on physical effectiveness of chlorpheniramine tablets. J Pharm Educ Res. 2013;4(1):1-5.

11 Oshi MA. Evaluation of antibacterial activities and formulation of black mahlab seeds aqueous extract. Res J Phar Dosage Forms Tech. 2014;5(3):131-8.

12 Aminoshariae A, Khan A. Acetaminophen: Old Drug, J Endod. 2015;41:588-93.

13 TiSharma C, Mehta V, Paracetamol: Mechanisms and updates. Contin Educ Anaest Crit Care Pain. 2014;14:153-8.

14 m GKanharam NP, Seema VB, Dhananjay P, Snehal SM, Rahul TR, Bhavesh PK. A comparative study of the in vitrodissolution rate and Acid-Neutralizing capacity of Aceproxyvon with other marketed drugs. Ind J Phar Pharmacol. 2023;10(3):183-9.

15 Benchawan C, Pornsak S. Novel disintegrating microcrystalline cellulose pellets with improved drug dissolution performance. Powder Technol. 2013;233:278-85.

16 Souto C, Rodriguez A, Parajes S, Martinez-Pacheco R. A comparative study of the utility of two superdisintegrants in microcrystalline cellulose pellets prepared by extrusion-spheronization Powder Technology. Eur J Pharm Biopharm. 2013;233:278-85.

17 Benchawan C, Pornsak S. Novel disintegrating microcrystalline cellulose pellets with improved drug dissolution performance. Powder Technol. 2013;233:278-85.

18 Barth KS, Guille C, McCauley J, Brady KT. Targeting practitioners: a review of guidelines, training, and policy in pain management. Drug Alcohol Depend. 2017;173:S22-30.

19 Enschke N, Kamper S, Maher C. The epidemiology and economic consequences of pain. Mayo Clin Proc. 2015;90(1):139-47.

20 Wilson CG, Clarke CP, Starkey YYL, Clarke GD. Comparison of a novel fast-dissolving Acetaminophen tablet formulation (FD-APAP) and standard Acetaminophen tablets using gamma scintigraphy and pharmacokinetic studies. Drug Dev Ind Pharm. 2011;37(7):747-53.

21 Catlin JR, Brass EP. The effectiveness of nonprescription drug labels in the United States: insights from recent research and opportunities for the future. Pharmacy (Basel). 2018;6(4):119.

22 Murtada AO, Abdelkarim MA, Huyam AM. The effect of sodium starch glycolate concentration on physical effectiveness of chlorpheniramine tablets. J Pharm Educ Res. 2013;4(1):47-53.

23 Oshi MA, Abdelkareem AM. Design and evaluation of cost-effective conventional tablets from monechma ciliatum seeds extract. Int J Pharm Sci Res 2013;4(2):631-40.

24 Murtada AO. Evaluation of antibacterial activities and formulation of black mahlab seeds aqueous extract. research j. Pharma. Dosage Forms Tech. 2013;5(2):104-11.
 

Submitted date:
04/09/2024

Accepted date:
06/25/2024

678e82f9a953957ee700aaa5 brjp Articles
2595-3192 (Electronic) 2595-0118 (Printed)
BrJP ©2025 All rights reserved.

BrJP

Share this page
Page Sections