Rao Khurram Ayoub1,
Ghulam Murtaza2 ,
Muhammad Imran1,
Shujaat Ali Khan2,
Sadullah Mir3,
Abida Kalsoom Khan3,
Saira Azhar2,
Zahid Mehmood3,
Ashif Sajjad3,
Syed Nisar Hussain Shah1
1Faculty of Pharmacy, Bahauddin Zakariya University, Multan;
2Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad;
3Institute of Biochemistry, University of Balochistan, Quetta, Pakistan.
For correspondence:- Ghulam Murtaza
Email: gmdogar356@gmail.com Tel:+23142082826
Received: 6 May 2014
Revised: 27 December 2014
Published: 28 February 2015
Citation:
Ayoub RK, Murtaza G, Imran M, Khan SA, Mir S, Khan AK, et al.
Formulation and permeation kinetic studies of flurbiprofen gel. Trop J Pharm Res 2015; 14(2):195-203
doi:
10.4314/tjpr.v14i2.2
© 2015 The authors.
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Abstract
Purpose: To investigate the in vitro permeation and drug release kinetics of flurbiprofen gel.
Methods: Thirteen batches (G1, G2 … G13) of flurbiprofen gels were prepared using different ratios of permeation enhancers, i.e., propylene glycol (PG) and polyethylene glycol (PEG), by response surface methodology (RSM). Viscosity, pH, spreadability, consistency and drug content of the flurbiprofen gels were measured. Permeation experiments were conducted using silicone membrane in a modified Franz diffusion cell. Permeation parameters determined include diffusion coefficient (D), Flux (J), lag time (tLag), permeation coefficient (Kp), input rate (IR) and enhancement ratio (ER). Primary skin irritation test was performed for the optimized gel, G3, using 11 human volunteers.
Results: Maximum solubility (72.15 ± 0.02 mg/mL) of flurbiprofen was observed in a mixture (2:1) of methanol and water. Partition coefficient (Ko/w) was determined as logP = 3.68 ± 0.11. The gels were stable under various storage conditions, and were homogenous, crystalline and transparent. Viscosity, pH, spreadability, consistency and drug content were in the range of 150 – 178 × 102 cps, 5.42 - 5.75, 5.0 - 7.0 g.cm/s, 3.0 - 9.0 mm, and 97.99 - 99.86 %, respectively. No irritation or lesions (erythma, redness and ulceration) occurred in human volunteers over a 30-day period. The optimized formulation, G3, showed maximum flux through silicone membrane.
Conclusion: PG and PEG are effective enhancers of flurbiprofen from various formulations when used in various ratios.
Keywords: Flurbiprofen, Gel, Diffusion, Permeation enhancers, Skin irritation, Silicone membrane