INTRODUCTION:

The focus of pharmaceutical analysis has been steadily shifted from the event of the latest chemical entities to the event of novel drug delivery systems for current drug molecules to maximize their effectiveness in terms of therapeutic action, reducing the frequency of dosing and wastage of medication, improving patient compliance, and reducing adverse effects. It is to scale back the breakdown and loss of medicines, avoid harmful side effects, and improve the bioavailability of medicines.

The real challenge in the advancement of a controlled drug delivery system is not only to keep the drug unhitch, but additionally to keep the quantity form at intervals the abdomen or upper gut until all the drug is completely free throughout the required quantity.

The digestive tube (GIT) is the major route of drug delivery to the circulation. Oral controlled unharness dose forms aren't applicable for numerous major medicines, characterized by a slim uptake window within the higher portion of the stinker. This can be described by the comparatively shorter transit time of the dose type into these anatomic segments. This suggests that once solely for a brief time of a half-dozen hours, the controlled unharness formulation has already departed the higher stinker and the drug is free in a brief, non-absorbent distal phase of the stinker. This results in a brief uptake section that is then followed by a period of lower bioavailability. These types of issues will be resolved by employing a floating medication delivery system.

GASTRO-RETENTIVE DRUG DELIVERY SYSTEM (GRDDS):

Systems for administering gastro-retentive medications are designed to hold on inside the abdomen for an extended period of time. Systems for administering gastro-retentive medications will function as systems for administering controlled-release medications. The employment of floating systems may be a methodology for getting extended internal organ residence times, providing the chance for native and general intervention. Thus, gastro-retention might facilitate the larger convenience of recent merchandise and thus improve therapeutic activity and provide important advantages for patients.

Conventional oral indefinite quantity forms have short dwell times and unpredictable internal organ drain times. The thought of internal organ retention comes from the requirement of locating medicines in an exceedingly specific region of the canal (GIT), like the abdomen, within the body. Several medicines are absorbed solely from the higher viscus tract. Consequently, the appearance of molecules like once-a-day formulations is distinctive to those molecules. This has crystal rectifier to the creation of GI retention platforms.

FLOATING DRUG DELIVERY SYSTEMS (FDDS):

FDDS were invented to retain the drug in the stomach and are applicable for drugs with poor solubility and low stability in intestinal fluids. The basis behind FDDS is making the dosage form less dense than the gastric fluids to make it float on them. The drug is discharged slowly at the expected level of the system, and once the drug is discharged, the residual system is empty in the abdomen. As a result, matches will increase and changes in plasma drug concentrations will also be better controlled.

Meanwhile, the system buoyancies over the abdomen and the drug are slowly released at the required rate by the system. Once the drug has been removed, the remaining system from the abdomen is empty. However, in addition to the minimum internal organ content required to attain the principle of buoyancy retention, a minimum floating force is needed to maintain a buoyant state on the surface of the meal. The figure 1 illustrated the FDDS types.

Gas Generating Systems:

In these systems, effervescent reactions occur between citric/tartaric acid and carbonate/bicarbonate salts to unharness carbon dioxide that is trapped within the jelly matrix of the systems. This reduces its density and causes it to float higher than the internal organ fluid.

METHODS FOR MAKING READY FLOATING INDEFINITE QUANTITY FORMS

Direct compression technique:

The purpose is to compress the tablets directly from the powder while not sterilising the physical nature of the fabric itself. Direct compression or supporting vehicles should have smart output and compressible properties. These properties are transmitted by the predisposition of those vehicles to flap, spray drying, or crystallization. The most used transporters are di-inorganic phosphate, tri-inorganic phosphate, etc.

Melt granulation technique:

This is a method within which pharmaceutical powders are clustered with a liquefied binder, and water or organic solvents are not required for pelleting. As there's no drying section, the method takes less time and consumes less energy The pellets were ready in an exceedingly laboratory high-shear mixer, employing a 60°C duct temperature and twenty,000 rev rotation speed.

The technique of soften hardening:

This method involves emulsifying the liquefied mass within the liquid section, followed by hardening by cooling. The carriers of this methodology are lipids, waxes, and synthetic resin glycols. The medicines are incorporated into these vectors to get a controlled unharness.

The wet granulation technique:

The wet granulation method involves the wet mass of powders, wet size, or edge, and drying. Wet granulation forms the pellets by powder binding with an associated adhesive instead of compacting them. Wet pelleting uses a suspension or suspension resolution containing a binder that's usually supplemental to the powder mixture. However, the binder is integrated into the dry powder mixture and the liquid is supplemental on its own. The strategy of presenting the binder depends on its solubility and on the weather of the mixture since, in general, the mass must be compelled to simply be damp rather than wet or pasty, and there is a limit to the quantity of solvent used. Once the granulating liquid has extra, mingling continues until an even dispersion is achieved and each of the binders must be activated. Then, by passing through a hammer mill or multi mill equipped with screens having big perforations, the wet mass is formed in contact with the wet screening. By either using a receptacle appliance or a fluidized bed appliance, the polished wet mass is dried. Once the drying methodology is completed, the lubrication materials are homogenised with the dried granules. These lubricated granules are units created in contact compression.

Effervescent technique:

Organic acid (citric acid) and carbonate salt undergo an effervescent reaction which liberates CO₂ and leads to the formation of a floating chamber in the drug delivery system.

Spray drying techniques:

The spray drying process involves the atomization of a solution, slurry, or emulsion containing one or more components of the desired product into droplets by spraying, followed by the rapid evaporation of the sprayed droplets into solid powder by hot air at a certain temperature and pressure.

Table 1: The drugs and polymers used in the preparation of gas generating floating tablets are mentioned in this table.

Drug name	Polymer used	Reference
Fenovirine	Xanthan gum (XG)	⁷Rashmitha et al., 2021
Nimodipine	Glyceryl di behenate	⁸Panda et al., 2020
Propranolol HCl	Hydroxy propyl cellulose	⁹Lavanya et al., 2020
Captopril	Zein	¹⁰Raza et al., 2019
Dipyridamole	Hydroxypropyl methyl cellulose (HPMC), K15 M and HPMC K 4 M	¹¹Li et al., 2018
Quinapril HCl	Carbopol 934P	¹²Mali et al., 2017
Quetiapine fumarate	HPMC K4M and HPMC K 15 M	¹³Narendar et al., 2016
Omeprazole	HPMC K4M and HPMC K 15 M	¹⁴Patel, 2015
Ascaridole	Polyethylene oxide and HPMC K15M	¹⁵Zhao et al., 2015
Atenolol	HPMC K100M and XG	¹⁶Ugurlu et al., 2014
Clopidogrel	Methylcellulose and HPMC	¹⁷Rao et al., 2014
Clarithromycin	HPMC K4M, K15M and K100M	¹⁸Timucin et al., 2014
Curcumin	HPMC	¹⁹ Raju et al., 2014
Metformin HCl	HPMC	²⁰Eisenächer et al., 2014
Clarithromycin	Glycerol monostearate	²¹Kriangkrai et al., 2014
Metronidazole	Carbopol 934	²²Emara et al., 2014
Atenolol	HPMC K4M, and Hydrogenated Cotton seed Oil	²³Pawar et al., 2013
Diltiazem	Ethyl cellulose and beeswax	²⁴Chowdary, 2013
Tetrahydro curcumin	HPMC and microcrystalline cellulose	²⁵Sermkaew et al., 2013
Losartan Potassium	Methocel	²⁶Tanwar et al., 2013
Simvastatin	Methocel K 4 M	²⁷Hussain et al.,2012
Diltiazem HCl	HPMC K14M and K15M	²⁸Bera et al., 2012
Tapentadol	XG	²⁹Jagdale et al., 2012
Metoprolol succinate	HPMC K15 M and HPMC K 4 M	³⁰Shubhrajit et al., 2012
Ranitidine HCl	HPMC and polyox WSR303	³¹Gharti et al. P2012
Ofloxacin	Methocel K15, MethocelK15M and HPMC K100M	³²Padmavathy et al., 2011
Metformin HCl	HPMCK100M and XG	³³ Salve et al., 2011
Aceclofenac	HPMC and K15M	³⁴Gopalakrishnan et al.,2011
Dextromethorphan HCl	HPMC K4M	³⁵Hu et al., 2011
Levofloxacin	HPMC K4 M, K15M and K100M	³⁶Doodipala et al., 2011
Nifedipine	HPMC K 100 M	³⁷Shaikh et al., 2011
Cephalexin	HPMC and K 100M	³⁸Shinde et al., 2010
Furosemide	HPMC and Carbopol	³⁹Karkhil et al., 2010
Liquorice Extract	HPMC K100 and Polyvinyl pyrrolidine (PVP)	⁴⁰Ram et al., 2010
Ranitidine	Carbopol-934	⁴¹Kumar et al., 2010
Theophylline	Methocel K 100 M	⁴²Khan et al., 2009
Silymarin	PVP K 30	⁴³Garg, 2009
Theophylline	Methocel K4M	⁴⁴Ferdous et al., 2008
Atorvastatin	HPMC K4M and Ethyl cellulose (EC)	⁴⁵Arun et al., 2008
Anhydrous theophylline	HPMC K4M and Carbopol 971P	⁴⁶Sungtho et al., 2008
Carbamazepine	HPMC and EC	⁴⁷Patel et al., 2007
Carbamazepine	Methocel K15 and Methocel K15M	⁴⁸Jaimini et al., 2007
Ciprofloxacin	HPMC	⁴⁹Basak et al., 2004
Curcumin and captopril	HPMC	⁵⁰Baumgartner et al., 2000
Amoxycillin trihydrate	HPMC and Carbopol 974P	⁵¹Hilton et al. ,1992

CONCLUSION:

The study concludes that gas generating floating systems not only increase gastric residence time but also provide a means for attaining local and systemic action. The gastro-retentive system gives controlled release, but when formulated along with the floating drug delivery system, they exhibit extended internal organ residence times. In the case of the lower bioavailability of gastro-retentive drugs, floating systems are implemented to increase bioavailability. Thus, Gas Generating Floating Systems not only provide sustained and controlled release but also improve therapeutic activity and have important advantages for patients.

ACKNOWLEDGMENTS:

The authors are thankful to the college management for the encouragement and support.

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Received on 22.01.2022 Modified on 11.02.2022

Asian J. Research Chem. 2022; 15(2):171-175.

DOI: 10.52711/0974-4150.2022.00029