Asian Journal of Pharmaceutical Research and Health Care

Ranabir Chanda , Amitava Ghosh , Santonu Biswas , Santanu Roy Chowdhury

Abstract

Mucoadhesive polymers that bind to the gastric mucin or epithelial cell surface are useful in drug delivery for the purpose of increasing the intimacy and duration of contact of drug with the absorbing membrane. Several synthetic polymers are in use for this purpose. Since the biodegradability of the synthetic polymers are questionable, in this investigation an oral mucoadhesive controlled delivery system has been developed for terbutaline sulphate (TS) using natural mucoadhesive materials extracted from the edible fruits like Zizyphus mauritiana (ZM) and Aegle marmelos (Linn.) Cor. (AM) that have better mucoadhesive property than synthetic polymer hydroxypropylmethylcellulose K4M (HPMC K4M). The in vitro adhesive and mucoadhesive strength of mucoadhesive materials extracted from the fruits of ZM and AM were evaluated and compared with HPMCK4M using both Share Stress and Wilhelmy Plate. Different formulations of oral mucoadhesive coated TS tablets were prepared using these natural materials and compared with tablets prepared with HPMCK4M and hardness, thickness, friability, weight variation and drug content of tablets were tested. The in vitro release of TS was studied in buffer pH 7.2 at 37°C ± 0.5°C. Tablets were orally administered to rabbits and blood plasma concentration of TS was determined using HPLC. It was found that mucoadhesive materials extracted from the fruits of ZM and AM exhibited better adhesiveness and mucoadhesiveness as compared with the HPMC- K4M. The in vitro study of TS exhibited showed greater drug release profile for tablets prepared with natural materials than synthetic polymers and confirmed with in vivo study. In vitro and in vivo correlation showed the same release profile.

Keywords

Terbutaline Sulphate, Natural Mucoadhesive Materials, HPMC - K4M.

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Amitava Ghosh , Koushik Sen Gupta

Abstract

The objective of the present study was to develop salbutamol sulphate matrix tablets, sustained release dosage form, for the treatment of Chronic Obstructive Pulmonary Disease (COPD). Simultaneous equations were formed to calculate the concentration values of Salbutamol sulphate and drug compatibility study was performed through Infrared spectroscopy. The matrix tablets were prepared by wet granulation method using two hydrophobic polymers such as Ethyl cellulose and Acrycoat S-100 in varying ratios. The granules exhibited satisfactory rheological demeanor. All the seven tablet formulations showed acceptable pharmacotechnical properties and complied with the in-house specifications for tested parameters. The results of formulation F-4 (Ethyl cellulose and Acrycoat in 2:1 ratio) could extend the release of Salbutamol sulphate up to 12 hr and was found comparable to marketed sustained release products. Model fitting analysis (Zero order, Higuchi and Korsmeyer-Peppas model) for all the formulations were performed and it was seen that all the formulations predominantly follow the Higuchi model. While comparing with the 'n' values of all the formulations of Korsmeyer-Peppas model, Fickian/Diffusion controlled release was observed in case of F-4 and F-5, whereas for the other formulations non-Fickian transport was observed.

Keywords

Salbutamol Sulphate, Matrix Tablet, Ethyl Cellulose, Acrycoat, Higuchi Model, Fickian/Diffusion, Korsmeyer - Peppas Model.

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