scholarly journals EFFECT OF NATURAL AND SYNTHETIC POLYMERS ON THE PROPERTIES OF CANDESARTAN CILEXETIL MATRIX TABLET PREPARED BY DRY GRANULATION

Author(s):  
Omar Saeb Salih ◽  
Roaa Abdalhameed Nief

ABSTRACTObjective: The objective of this study is to develop a controlled release matrix tablet of candesartan cilexetil to reduce the frequency of administration,enhance bioavailability and improve patient compliance; a once daily sustained release formulation of candesartan cilexetil is desirable.Methods: The prepared tablets from F1 to F24 were evaluated with different evaluation parameters like weight variation, drug content, friability,hardness, thickness and swelling ability. In vitro release for all formulas were studied depends on the type and amount of each polymer, i.e. (16 mg,32 mg and 48 mg) respectively beside to the combination effect of polymers on the release of the drug from the tablet.Results: In vitro release showed that formula 13 had the faster release (100% after 4 h) which contained acacia (1:1) and the lowest sustain releasewas showed for F7 (73% after 8 h) which contained HPMC K100M (1:1). Formula 1 was an 89 % release after 8 h which contain eudragit RS100; F4was a 100 % release after 5 h which contain Na CMC, F10 was a 100% after 8 h which contain xanthan gum and F16 was a 100 % release after 5 hwhich contain tragacanth polymer. Formula 9 had a lower release than F7 and F8 respectively. Formula 7 can be used for sustain oral drug delivery ofcandesartan cilexetil while Formula 13 can be used in contrary as fast release tablets for faster response.Conclusion: Controlled drug delivery system is promising for less dosing and higher patient compliance.Keywords: Angiotensin II receptor antagonist, Hypertension, Matrix system, Control release.

2003 ◽  
Vol 20 (1) ◽  
pp. 125-131 ◽  
Author(s):  
Marı́a Luisa González-Rodrı́guez ◽  
Francesca Maestrelli ◽  
Paola Mura ◽  
Antonio Marı́a Rabasco

2018 ◽  
Vol 2 (1) ◽  
pp. 01-03
Author(s):  
Swathi chilukala

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.


Author(s):  
Ranajit Nath ◽  
Ratul Bhowmik ◽  
Rajarshi Chakraborty ◽  
Sourav Datta ◽  
Apala Chakraborty

Diltiazem, a calcium ion cellular influx inhibitor is known for its limited and variable bioavailability. This study is intended to explore the benefits of microemulsion formulation as an oral drug delivery system for immediate release to improve the bioavailability and efficacy of Diltiazem. Methods: Oil in water microemulsion was prepared using the simple water titration method. The optimized formulation was evaluated for physicochemical parameters like viscosity, pH, conductivity, and accelerated stability studies. In vitro release, diltiazem microemulsion was investigated.


Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.


Author(s):  
C Suja ◽  
Sismy C

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.


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