Formulation and Evaluation of Propranolol HCl Floating Tablets-A Gastro Retentive Drug Delivery

Gastro-retentive dosage forms enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal tract and improve the bioavailability of medications those are characterized by a narrow absorption window. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of terbinafine were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of terbinafine were evaluated tablet hardness, uniformity of weight, friability, uniformity of content, in vitro buoyancy test, swelling index, in vitro dissolution study and stability study. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of terbinafine shown that the formulation F5 was found to be the best formulation as it releases 96.22% terbinafine in a controlled manner for an extended period of time (up to 480 min). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of terbinafine may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.

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Formulation of Gastro-retentive Floating Tablets of Valsartan by 2 power 2 Factorial Designs: In vitro and In vivo Evaluations

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.7 ◽

2019 ◽

Vol 12 (2) ◽

pp. 4496-4505

Author(s):

Sandhya Pamu ◽

Subrahmanyam C. V. S ◽

Patnaik K. S. K. Rao

Keyword(s):

Drug Delivery ◽

Factorial Design ◽

Drug Delivery System ◽

Delivery System ◽

Hot Melt Extrusion ◽

Floating Tablets ◽

Hot Melt ◽

Gastro Retentive

An oral dosage form containing gastro-retentive floating tablets forms a stomach-specific drug delivery system for the treatment of hypertension. Valsartan belongs to the BCS class II (poo Classification System). It is desirable to improve the extent of bioavailability (23%). The objective of the present study was to apply design of experiment to optimize floating drug delivery of valsartan by employing 22 factorial design. Improvement of the aqueous solubility of valsartan was done by solid dispersions using hot melt extrusion technique. Plasdone S630 copovidone is a variable carrier and drug to carrier ratio of 1:2 was optimized. Valsartan floating tablets were prepared by employing factorial design (22), where HPMC K15M (X1) and pregelatinized starch (X2) were independent variables and drug dissolution was the dependent parameter (Y1) to prepare matrix tablets. The factorial analysis, steepest ascent method was utilized for obtaining optimized formulation. In vitro evaluation, In vivo radiographic study and biopharmaceutical analysis in rabbits for valsartan optimized formulation (FT-5). Floating lag time (FLT) for valsartan optimized formulation (FT-5) was 15 s and total floating time (TFT) of the tablets was about 33 h, which was satisfactory. A four-point (1 h, 4 h, 8 h and 16 h) dissolution analysis gave satisfactory dissolution profile up to 24 h. The release kinetics of valsartan optimized formulation (FT-5) followed zero order and the release mechanism was found to be Korsemeyer Peppas model, i.e. swelling type. The dissolution efficiency for valsartan floating tablets was 1190.89% against the marketed formulation of 39.77%. The accelerated stability profile of valsartan optimized formulation (FT-5) was evaluated in terms of drug content and percent cumulative dissolution of valsartan in 24 h, in a 6 months study. In vivo X-ray image study for valsartan optimized formulation (FT-5) indicated the presence of intact tablet up to 12 h in gastric region of rabbit. The biopharmaceutical analysis in rabbits was conducted for valsartan optimized formulation (FT-5). The HPLC method was established and validated for the in vivo analysis. The Cmax was 453.2 ng/mL compared to that of the marketed tablets (522.4 ng/mL). The mean residence time (MRT) for the valsartan optimized formulation (FT-5) was 14.82 h as against 4 h for marketed tablet. The relative bioavailability of valsartan optimized formulation (FT-5) was 650% higher than the marketed tablet. To overcome the poor bioavailability of valsartan, it was suitably modified using hot-melt extrusion for improving therapeutic outcome. In conclusion, gastro-retentive drug delivery system is an excellent approach for improving the bioavailability of valsartan.

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Gastro retentive Drug Delivery of Cyclobenzaprine Hydrochloride

Gastroenterology Pancreatology and Hepatobilary Disorders ◽

10.31579/2641-5194/006 ◽

2018 ◽

Vol 2 (1) ◽

pp. 01-03

Author(s):

Swathi chilukala

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

In Vitro Release ◽

Wet Granulation ◽

Floating Tablets ◽

Compression Properties ◽

Weight Variation ◽

Vitro Release ◽

Gastro Retentive

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.

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FORMULATION AND EVALUATION OF GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF ZANAMIVIR USING DIFFERENT POLYMERS

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v8i4.641 ◽

2019 ◽

Vol 8 (4) ◽

Author(s):

V. Vijaya Kumar ◽

B. Deekshi Gladiola ◽

C. Madhusudhana Chetty ◽

R. E. Ugandar

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Guar Gum ◽

Release Kinetics ◽

Methyl Cellulose ◽

Floating Tablets ◽

Floating Tablet ◽

Gastro Retentive

The objective of the present study is to develop gastro retentive drug delivery system of Zanamivir .Floating tablets of Zanamivir were developed with a gas generating agent NaHCO3 and in combination of different hydrophobic and hydrophilic polymers like xanthan gum, guar gum, HPMC and methyl cellulose .In the present work attempts have been made to prepare six formulations of Zanamivir in different ratios of drug and polymer to get a desired release profile by direct compression method .All the prepared tablets were evaluated in terms of pre compression and post compression parameters. FTIR studies revealed the absence of drug polymer interactions .Among all the formulations F5 Showed 97.4% of in vitro drug release for 10 hours and hence formulation F5 is selected as an optimized formulation. The optimized formulation F5 was found to follow Higuchi release kinetics and zero order. Further formulation F5 was subjected to accelerated stability studies for 3 months. It showed that the optimized formulation was intact without any interactions. Finally the optimized formulation F5 complying with all properties of floating tablets was found to be satisfactory Keywords: Zanamivir, floating tablet, natural gums, sodium bicarbonate, gastro retentive drug delivery systems

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Formulation and Evaluation of directly compressed Floating Tablets of Candesartan Cilexetil for Gastro Retentive Drug Delivery

Research Journal of Pharmacy and Technology ◽

10.5958/0974-360x.2018.00517.6 ◽

2018 ◽

Vol 11 (7) ◽

pp. 2804

Author(s):

Palak Agrawal ◽

Ajazuddin ◽

Tripti Banjare ◽

Swapnil Gupta ◽

Akansha Bhandarkar ◽

...

Keyword(s):

Drug Delivery ◽

Candesartan Cilexetil ◽

Floating Tablets ◽

Gastro Retentive

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Formulation Development and Evaluation of Sustain Release Gastroretentive Floating Tablets of Prochlorperazine Dimaleate

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i4-s.3353 ◽

2019 ◽

Vol 9 (4-s) ◽

pp. 445-450

Author(s):

Bharti Patle ◽

Vivek Jain ◽

Shradha Shende ◽

Prabhat Kumar Jain

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Extended Period ◽

Lag Time ◽

In Vitro Dissolution ◽

Compression Method ◽

In Vitro Drug Release ◽

Floating Tablets ◽

Gastro Retentive

Floating drug delivery systems are the gastroretentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of Prochlorperazine dimaleate (PCZ) were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of PCZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of PCZ shown that the formulation F9 was found to be the best formulation as it releases 98.89% in a controlled manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. The optimized formulation (F9) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Prepared floating tablets of PCZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Prochlorperazine dimaleate, Floating tablet, Gastro retentive, Total floating time.

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