FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEM OF PIOGLITAZONE HYDROCHLORIDE
*Thoriya J. G, Patel S. D, Tank H. M
Matushree V. B. Manvar College of Pharmacy- Dumiyani,
Pioglitazone HCl is used for the management of type-2 diabetes. It is an absorption window limited drug, whose solubility decreases with increase in the pH and has a short half life of 3-7 h. Here an attempt is made to developed the floating matrix tablets, which design in way that after oral administration the GI resistant time is prolonged and thus to give sustained action with increase in the bioavailability of the drug. Pioglitazone HCl showed maximum absorption at wavelength 269 nm in 0.1N HCl. various formulations were developed by using release rate controlling and gel forming polymers like HPMC, and Carbopol-934 in single and combinations by direct compression method with the incorporation of sodium bicarbonate as gas generating agent. The prepared tablets were characteristics by drug content, floating property, swelling and in vitro dissolution test using USP dissolution test apparatus Type – II (paddle method) in dissolution medium of 0.1 N HCl. The in vitro dissolution results of all tablets were computed by using dissolution software. The prepared tablets were found to be good hardness, diameter, weight variation, thickness, friability drug content, floating property and in vitro drug release. Drug-polymer compatibility studies by FTIR gave conformation about drug purity and showed no interaction between drug and selected polymers. All the formulations had floating lag time below 3 minutes and constantly floated on dissolution medium for more than 12 h. Swelling studies indicated significant water uptake and contributed in drug release. From among all the developed formulations, as F7 prolonged the drug release (95.45 %) for longer period of time (12 hrs.); they were selected as best formulations. The best formulations were found to be stable during stability studies for two months. Thus, selected formulations satisfied floating time, swelling index and in vitro drug release profile requirements for a floating drug delivery system.Tablets of Pioglitazone HCl prepared with HPMC K4M, HPMC K100M and Carbopol 934P were found to be acceptable floating property, water uptake and in vitro drug release.
Reference Id: PHARMATUTOR-ART-1376
Development of newer drugs and medicines will be the goal of scientists across the world. In order to achieve satisfying results, a drug has to be properly formulated in proper dosage form. It is an established fact that the conventional immediate release drug delivery systems when taken frequently in a day can maintain drug concentration levels in therapeutically effective range. However, this result in significant fluctuations in plasma drug levels recently, several technical advancements have led to the development of various Novel Drug Delivery Systems (NDDS) that could revolutionize method of drug delivery and hence could provide definite therapeutic benefits.1
Oral route of administration is the most important and convenient route for drug delivery. Due to differential absorption from various regions of GI, the benefits of long-term delivery technology have not been fully realized for dosage forms designed for oral administration. Only recently drug delivery systems have been designed to target drugs to differential regions of GIT. These include gastro retentive systems, delayed release systems and colon targeting. The real issue in the development of oral controlled release dosage form is not just to prolong the delivery of drugs for more than 12 h but also to prolong the presence of dosage forms in the stomach or somewhere in the upper small intestine. Dosage forms with prolonged gastric residence time (GRT), i.e. gastro remaining or GRDF will bring about new and important therapeutic options.2, 3
Various approaches have been developed for gastric retention which includes Low density systems or floating delivery, High density (sinking) systems or non floating delivery, Swelling and expandable systems and Mucoadhesive/bioadhesive systems.Floatingsystems are also known as hydro dynamically balanced systems. (HBS/FDDS) They have a bulk density lower than gastric fluid (i.e. < 1.004 gm/ml)the specific gravity of gastric fluid is approximately 1.004-1.010 g/cm3 according to the “Documenta Geigy” and thus the FDDS remains buoyant in the stomach without affecting the gastric emptying rate for a prolonged period of time. It is an oral dosage form that is designed to prolong the residence time of the dosage form within the GIT. Based on the mechanism of buoyancy, two distinctly different technologies have been utilized in development of FDDS that are: Effervescent System, and Non- Effervescent System.
The Non effervescent floating drug delivery system is based on mechanism of swelling of polymer or bioadhesion to mucosal layer in GIT. The most commonly used excipients in non-effervescent floating drug delivery system are gel forming or highly swellable cellulose type hydrocolloids, polysaccharides and matrix forming material such as polycarbonate, polyacrylate, polymethacrylate, polystyrene as well as bioadhesive polymer such as chitosan and carbopol.4, 5
2. MATERIALS AND METHODS
Pioglitazone HCl was received from Taj pharmaceutical, Hyderabad, Methocel® K4M, K15MandK100M which are commercially available grades of hydroxypropyl methylcellulose from SEVA Fine Chemicals, Ahmadabad, carbopol 934P and sodium bicarbonate from Oxford Lab. Reagent, Mumbai Microcrystalline Cellulose (MCC), magnesium stearate and talc from SEVA Fine Chemicals, Ahmadabad.
2.2.1 Preparation of floating tablets
Pioglitazone HCl, selected polymers, sodium bicarbonate and lactose were taken in required quantities and passed through 60 # separately. In dry state, the drug with other ingredients was mixed for the period of 10 min in mortar to get uniform mixture power. The mixture was blended with Magnesium Stearate for 2-3 min. to improve flow property. The powder was compressed into tablets using a Rotary tablet press.6, 7
2.2.2 Experimental design
The formulations were fabricated according to a 32 full factorial design, allowing a simultaneous evaluation of two formulation variables and their interactions. The experimental design with corresponding formulations was given in Table 1.8
X1: HPMC K4M: HPMC K100M (mg)
X2: Concentration of Carbopol (mg)
Y1: % cumulative drug release at 12 hr.
Y2: Floating lag time
Y3: % Swelling
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