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Equilibrium, 11th Science, CBSE, GSEB.
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ABSTRACT Oral controlled release dosage forms face several physiological restriction like inability to retain and position the controlled drug delivery system within the targeted region of the gastrointestinal tract (GIT) due to fluctuation in gastric emptying. This results in non uniform absorption pattern, inadequate medication release and shorter residence time of the dosage form in the stomach. As the fallout of this episode there is inadequate absorption of the drug having absorption window predominantly, in the upper area of GIT. These contemplations have provoked to the development of oral controlled release dosage forms with gastroretentive properties. Microballoons (Hollow microspheres) hold certification as one of the potential approaches for gastric retention. Microballoons are spherical empty particles without core and can remain in the gastric region for delayed periods. They significantly increase the gastric residence time of medication, thereby enhance bioavailability, improves patient compliance by reducing dosing frequency, lessen the medication waste, enhance retention of medication which solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH environment. The present review preparation methods, characterization, advantages, disadvantages, mechanism of drug release from microballoons, applications and list of the drugs formulated as microballoons are discussed. KEYWORDS: Microballoons, Gastro-retention, Floating drug delivery system (FDDS).
MICROBALLOONS: A NOVEL APPROACH IN GASTRO-RETENTION FLOATING DRUG DELIVERY SY...
MICROBALLOONS: A NOVEL APPROACH IN GASTRO-RETENTION FLOATING DRUG DELIVERY SY...
Snehal Patel
Oral controlled release dosage forms face several physiological restriction like inability to retain and position the controlled drug delivery system within the targeted region of the gastrointestinal tract (GIT) due to fluctuation in gastric emptying. This results in non‑uniform absorption pattern, inadequate medication release and shorter residence time of the dosage form in the stomach. As the fallout of this episode there is inadequate absorption of the drug having absorption window predominantly, in the upper area of GIT. These contemplations have provoked to the development of oral controlled release dosage forms with gastroretentive properties. Microsponge hold certification as one of the potential approaches for gastric retention. Microsponge are porous spherical empty particles without core and can remain in the gastric region for delayed periods. They significantly increase the gastric residence time of medication, thereby enhance bioavailability, improves patient compliance by reducing dosing frequency, lessen the medication waste, enhance retention of medication which solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH environment. In the present review method of preparation, characterization, advantages, disadvantages and applications of floating microsponge are discussed. Please cite
MICROSPONGE: A NOVEL APPROACH IN GASTRO-RETENTION DRUG DELIVERY SYSTEM (GRDDS)
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Snehal Patel
Abstract: In present study an attempt was made to prepare microballoons of Telmisartan by emulsion solvent diffusion technique for sustained delivery by using polymers like Ethyl cellulose to extend the drug release for about 12 hours in the upper GIT, which may result in enhanced absorption and there by improved bioavailability. Formulation optimization of Telmisartan loaded microballoons was carried out by using different concentration of Polyvinyl alcohol (PVA) and Ethyl cellulose. Total 9 batches were formulated. All 9 batches were evaluated for entrapment efficiency (EE) and buoyancy. Among all batches DP4 shows maximum entrapment efficiency (EE) and buoyancy and was considered as optimized formulation. DP4 batch was further used for process optimization. The process optimization was carried out at three different stirring speeds i.e. 1300, 1500 and 1700 rpm for three different stirring time period i.e. 1hr, 2hr and 3 hr and another 9 batches were formulated. Out of all the batches DP13 showed the spherical shape of microballoons without formation of flakes. Optimized batch DP13 was evaluated for Zeta Potential, Particle Size Distribution which show - 41.8mV and 1.344 μm particle size, SEM, XRD Analysis. Batch DP13 was charged for stability and were placed in glass vials container and stored at ICH storage condition (2°C - 4°C Refrigeration condition , 30 ± 2°C / 60% ± 5% RH , 40 ± 2°C / 75% ± 5% RH ) for a period of 30 days. The samples were analyzed for physical appearance, buoyancy and for the drug release after 30 days. After 1 months samples were withdrawn and microballoons showed no change in physical appearances, buoyancy and drug release, which indicate that the microballoons were stable. Keywords: Telmisartan, Microballoons, Emulsion solvent diffusion technique, Buoyancy, Entrapment Efficiency.
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ABSTRACT Oral controlled release dosage forms face several physiological restriction like inability to retain and position the controlled drug delivery system within the targeted region of the gastrointestinal tract (GIT) due to fluctuation in gastric emptying. This results in non uniform absorption pattern, inadequate medication release and shorter residence time of the dosage form in the stomach. As the fallout of this episode there is inadequate absorption of the drug having absorption window predominantly, in the upper area of GIT. These contemplations have provoked to the development of oral controlled release dosage forms with gastroretentive properties. Microballoons (Hollow microspheres) hold certification as one of the potential approaches for gastric retention. Microballoons are spherical empty particles without core and can remain in the gastric region for delayed periods. They significantly increase the gastric residence time of medication, thereby enhance bioavailability, improves patient compliance by reducing dosing frequency, lessen the medication waste, enhance retention of medication which solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH environment. The present review preparation methods, characterization, advantages, disadvantages, mechanism of drug release from microballoons, applications and list of the drugs formulated as microballoons are discussed. KEYWORDS: Microballoons, Gastro-retention, Floating drug delivery system (FDDS).
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Snehal Patel
Oral controlled release dosage forms face several physiological restriction like inability to retain and position the controlled drug delivery system within the targeted region of the gastrointestinal tract (GIT) due to fluctuation in gastric emptying. This results in non‑uniform absorption pattern, inadequate medication release and shorter residence time of the dosage form in the stomach. As the fallout of this episode there is inadequate absorption of the drug having absorption window predominantly, in the upper area of GIT. These contemplations have provoked to the development of oral controlled release dosage forms with gastroretentive properties. Microsponge hold certification as one of the potential approaches for gastric retention. Microsponge are porous spherical empty particles without core and can remain in the gastric region for delayed periods. They significantly increase the gastric residence time of medication, thereby enhance bioavailability, improves patient compliance by reducing dosing frequency, lessen the medication waste, enhance retention of medication which solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH environment. In the present review method of preparation, characterization, advantages, disadvantages and applications of floating microsponge are discussed. Please cite
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Abstract: In present study an attempt was made to prepare microballoons of Telmisartan by emulsion solvent diffusion technique for sustained delivery by using polymers like Ethyl cellulose to extend the drug release for about 12 hours in the upper GIT, which may result in enhanced absorption and there by improved bioavailability. Formulation optimization of Telmisartan loaded microballoons was carried out by using different concentration of Polyvinyl alcohol (PVA) and Ethyl cellulose. Total 9 batches were formulated. All 9 batches were evaluated for entrapment efficiency (EE) and buoyancy. Among all batches DP4 shows maximum entrapment efficiency (EE) and buoyancy and was considered as optimized formulation. DP4 batch was further used for process optimization. The process optimization was carried out at three different stirring speeds i.e. 1300, 1500 and 1700 rpm for three different stirring time period i.e. 1hr, 2hr and 3 hr and another 9 batches were formulated. Out of all the batches DP13 showed the spherical shape of microballoons without formation of flakes. Optimized batch DP13 was evaluated for Zeta Potential, Particle Size Distribution which show - 41.8mV and 1.344 μm particle size, SEM, XRD Analysis. Batch DP13 was charged for stability and were placed in glass vials container and stored at ICH storage condition (2°C - 4°C Refrigeration condition , 30 ± 2°C / 60% ± 5% RH , 40 ± 2°C / 75% ± 5% RH ) for a period of 30 days. The samples were analyzed for physical appearance, buoyancy and for the drug release after 30 days. After 1 months samples were withdrawn and microballoons showed no change in physical appearances, buoyancy and drug release, which indicate that the microballoons were stable. Keywords: Telmisartan, Microballoons, Emulsion solvent diffusion technique, Buoyancy, Entrapment Efficiency.
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Equilibrium
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Equilibrium
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• Depending on
the nature of reaction and experimental condition, the reaction may be fast or slow. • Equilibrium reaction can be divided into following three categories:
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