Abstract
Drugs that are easily absorbed from the GI tract and have a short half-life are eliminated quickly from the blood circulation, require frequent dosing. To avoid this problem, the oral controlled release formulations are being developed. Gastro-retentive dosage forms have the potential from use as controlled release systems. The purpose of this research is to develop the gastro retentive drug delivery system of centrally acting alpha adrenergic agonist cyclobenzaprine Hydrochloride (cyclobenzaprine HCl). It is well absorbed from the upper part of the GIT, due to short gastric residence time the bioavailability is low and hence it is need to develop a dosage form that releases the drug in stomach using gastro retentive system. Different formulations of cyclobenzaprine HCl gastro-retentive floating tablets were prepared by wet granulation method using various concentrations of HPMC K4M / HPMC K100M and combination of Psyllium husk and HPMC K100M as matrix forming agent. Sodium bicarbonate and citric acid were used as a gas generating agent that helps in maintaining the buoyancy. The prepared cyclobenzaprine HCl gastro-retentive floating granules were subjected to pre-compression properties to comply with pharmacopoeial limits and the prepared gastro-retentive floating tablets were characterized for weight variation, hardness, thickness and friability drug content, swelling studies. The floating lag time of all formulation is good and the Total floating time of all the formulations was >12 hours. The tablets were evaluated for in vitro release characteristics for 12hrs in 0.1N HCl at 37 oC and from this in vitro release studies the formulations F-5, F-9 and F-15 exhibited good controlled release profile of about 96.0%, 94.5% and 95.0% when compared with other formulations while floating on the dissolution medium.
Highlights
Many of the drug delivery systems, available in the market are oral drug delivery systems
Standard graph of cyclobenzaprine Hydrochloride was plotted as per the procedure in experimental method and its linearity is shown in table 7 and graph 15
The granules prepared by wet granulation, direct compression had shown good flow properties with angle of repose values ranging from 25 to 30
Summary
Many of the drug delivery systems, available in the market are oral drug delivery systems. Oral drug delivery systems have progressed from immediate release to site-specific delivery over a period of time. Every patient would always like to have an ideal drug delivery system possessing the two main properties that are single dose or less frequent dosing for the whole duration of treatment and the dosage form must release active drug directly at the site of action[1]. An orally administered controlled drug delivery system encounters a wide range of highly variable conditions, such as pH, agitation intensity, and composition of the gastrointestinal fluids as it passes down the G.I tract. Considerable efforts have been made to design oral controlled drug delivery systems that produce more predictable and increased bioavailability of drugs. One of the important determinants of G.I transit is the residence time in the stomach 2
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