International Journal of Pharmaceutical Sciences Review and Research, 2021
The Liquisolid process is a novel and effective approach to improving solubility. Bioavailability... more The Liquisolid process is a novel and effective approach to improving solubility. Bioavailability relies on drug solubility. With the evolution of modern pharmaceutical products, solubility is a big problem for the pharmaceutical industry. One of the most daunting aspects of drug production remains the enhancement of oral bioavailability of poorly water-soluble drugs. A newer methodology "powdered solution technology" or "Liquisolid technology", has been applied to prepare water-insoluble drugs into rapid-release solid dosage forms. This method is efficient, economic, viable for industrial production, also useful in control drug delivery system. Hence due to above reasons Liquisolid technique is most efficient and novel approach for solubility enhancement. To prepare waterinsoluble drugs into rapid-release solid dosage forms, 'powdered solution technology' or 'Liquisolid technology' has been applied. This approach is reliable, cost-effective, viable for industrial production, and also useful in the drug delivery control system. Therefore, Liquisolid technique is the most effective and novel method for enhancing solubility due to the above factors.
The objective of present study is to design a novel multiparticulate system for colon targeting d... more The objective of present study is to design a novel multiparticulate system for colon targeting drug delivery system of cyclophosphamide (CPM) using biodegradable Konjac glucomannan (KGM) as a carrier for colorectal cancer treatment. Glucomannan is a high-molecular weight, water-soluble, non-ionic polysaccharide extracted from the tuber or root of the elephant yam, also known as konjac (Amorphophallus konjac or Amorphophallus rivieri). cyclophosphamide (CPM) has been the only agent with clinically active against colorectal cancer. Different batches of CPM granules were prepared and coated with KGM. Optimized CPM granules (KGM-STMP) were evaluated for flow properties, granular parameters, weight variation and content uniformity. The prepared formulations were subjected for in-vitro drug release studies in simulated gastric and intestinal fluids. It was found that during 2 hr at pH 1.2 HCl (SGF), 3 hr at pH 7.4 phosphate buffer (SIF) only less than 20% of drug was released. The drug release studies was also carried out in simulated colonic fluid (SCF) of pH 6.8 containing β-mannanase in order to mimic the conditions from mouth to colon. Drug release from 5-FU granules coated with KGM-STMP followed diffusion dependent zero order kinetics. Further, report suggested that konjac glucomannan (KGM) was biodegradable and susceptible to the colonic microfloras under anaerobic environments. Spectroscopic, (FTIR), X-ray Diffraction (X-RD) and DSC studies concluded that no polymer-drug interaction was concluded. Accelerated stability studies indicated that no significant changes, in drug release and micrometric patterns for observed when stored at 40± 2ºC / 75±5% RH. Therefore, it was concluded that konjac glucomannan (KGM) is a promising potential carrier for targeting CPM in the vicinity of colon in order to treat colon cancer effectively.
To formulate and evaluate the mouth dissolving tablet dosage forms of favipiravir using various s... more To formulate and evaluate the mouth dissolving tablet dosage forms of favipiravir using various superdisintegrants by using wet granulation technique. Batches of favipiravir Mouth dissolving tablets were formulated by using the wet granulation technique. The formulated granules were evaluated for their flow properties as a pre-compression parameter and the friability, hardness, disintegration, wetting ratio, wetting time, dissolution, and drug release parameters were evaluated as post-compression parameters. The effect of the varying concentrations of superdisintegrants on the formulation for disintegration time was ascertained and the results were compared. The tablet had friability and hardness values ranging from 0.60 to 0.68 % and 3.9 to 4.3 (kg/cm 2 ). Tablet weights did not vary significantly but the disintegration time varied from Original Research Article Avinash et al.; JPRI, 33(6): 28-39, 2021; Article no.JPRI.65646 29 44.66 to 142.66±2.51 min and the wetting time varied f...
Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absor... more Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastroretentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Metoprolol tartrate is an antihypertensive drug, which has low elimination half life: 3-4 h. The floating tablets of metoprolol tartrate were prepared to increase the gastric retention and to improve the bioavailability of the drug. Metoprolol tartrate was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. The rapid gastro-intestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to poor bioavailability of the drug. The floating tablets were formulated using HPMC K4M and HPMC K100M as the release retardant polymers, and sodium bicarbonate as the gas generating agent to reduce the floating lag time. The tablets were prepared by direct compression. ...
International Journal of Research in Pharmaceutical Sciences and Technology, 2020
Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infec... more Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infections. However, it has low skin permeability. Hence, the basic idea behind the development of such a system, transfersomes is to maintain a sustain release of drug from the dosage form and for target delivery. Miconazole nitrate was formulated as transfersomes, half-life can be increased and the desired effect can be obtained. MIC transfersomes were prepared using a thin lipid film hydration technique. The prepared transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC transfersomes was incorporated into a Carbapol 934 gel base which was for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro activity. The prepared MIC transfersomes had a high EE% ranging from 65.45% to 80.11%, with small particle sizes ranging from 368 nm...
Indo American Journal of Pharmaceutical Research, 2015
Article history Benzothiozoles are an important class of heterocyclic compounds which possess wid... more Article history Benzothiozoles are an important class of heterocyclic compounds which possess wide spectrum of biological properties. In the present research work, a series of new 2-substituted benzothiozole derivatives are synthesized and evaluated as enhanced antioxidant and antimicrobial agents. The chemical structure of newly synthesized 2-substituted benzothiazole derivatives are characterized by the spectral studies (IR, Mass and CHN analysis). The compounds were evaluated for their in -vitro antioxidant activity by using five standard protocols namely diphenyl picryl hydrazyl (DPPH) scavenging activity, nitric oxide scavenging activity, reducing power ability study, hydroxyl radical scavenging activity and by lipid peroxidation. Ascorbic acid was used as standard for DPPH, nitric oxide, reducing power ability and hydroxyl radical scavenging assay. Antibacterial activity was evaluated against B. pumilis, A. niger, S. aureous, C. albican and S. dysentriae using Norfloxacin, Ampicillin and Griseofulvin were standard. It was observed that the 2-substituted benzothiazole derivatives confirmed the antioxidant and antimicrobial activities.
Introduction: Orodispersible films (ODF) is a thin strip that is mostly transparent, biodegradabl... more Introduction: Orodispersible films (ODF) is a thin strip that is mostly transparent, biodegradable and it has hydrophilic polymers that disintegrate and dissolves immediately when getting in contact with saliva. Different disintegrants play a crucial role in film properties such as organoleptic properties, film thickness, and in particular disintegration time of the film. The main reason for the development of oral films is for their prominent role in increased patient compliance among pediatrics and geriatrics by disintegrating faster, releasing the drug rapidly, without the need for water, and mostly decreasing the risk of choking. Aim: To formulate orodispersible films of favipiravir and to study the effect of different superdisintegrants on various film properties. Methods: The method used to prepare the film is the solvent casting method. In this method, the solution is prepared using polymer, drug, and superdisintegrants. This solution is casted on a filmforming apparatus usin...
International Journal of Pharmaceutical Sciences Review and Research, 2021
The Liquisolid process is a novel and effective approach to improving solubility. Bioavailability... more The Liquisolid process is a novel and effective approach to improving solubility. Bioavailability relies on drug solubility. With the evolution of modern pharmaceutical products, solubility is a big problem for the pharmaceutical industry. One of the most daunting aspects of drug production remains the enhancement of oral bioavailability of poorly water-soluble drugs. A newer methodology "powdered solution technology" or "Liquisolid technology", has been applied to prepare water-insoluble drugs into rapid-release solid dosage forms. This method is efficient, economic, viable for industrial production, also useful in control drug delivery system. Hence due to above reasons Liquisolid technique is most efficient and novel approach for solubility enhancement. To prepare waterinsoluble drugs into rapid-release solid dosage forms, 'powdered solution technology' or 'Liquisolid technology' has been applied. This approach is reliable, cost-effective, viable for industrial production, and also useful in the drug delivery control system. Therefore, Liquisolid technique is the most effective and novel method for enhancing solubility due to the above factors.
The objective of present study is to design a novel multiparticulate system for colon targeting d... more The objective of present study is to design a novel multiparticulate system for colon targeting drug delivery system of cyclophosphamide (CPM) using biodegradable Konjac glucomannan (KGM) as a carrier for colorectal cancer treatment. Glucomannan is a high-molecular weight, water-soluble, non-ionic polysaccharide extracted from the tuber or root of the elephant yam, also known as konjac (Amorphophallus konjac or Amorphophallus rivieri). cyclophosphamide (CPM) has been the only agent with clinically active against colorectal cancer. Different batches of CPM granules were prepared and coated with KGM. Optimized CPM granules (KGM-STMP) were evaluated for flow properties, granular parameters, weight variation and content uniformity. The prepared formulations were subjected for in-vitro drug release studies in simulated gastric and intestinal fluids. It was found that during 2 hr at pH 1.2 HCl (SGF), 3 hr at pH 7.4 phosphate buffer (SIF) only less than 20% of drug was released. The drug release studies was also carried out in simulated colonic fluid (SCF) of pH 6.8 containing β-mannanase in order to mimic the conditions from mouth to colon. Drug release from 5-FU granules coated with KGM-STMP followed diffusion dependent zero order kinetics. Further, report suggested that konjac glucomannan (KGM) was biodegradable and susceptible to the colonic microfloras under anaerobic environments. Spectroscopic, (FTIR), X-ray Diffraction (X-RD) and DSC studies concluded that no polymer-drug interaction was concluded. Accelerated stability studies indicated that no significant changes, in drug release and micrometric patterns for observed when stored at 40± 2ºC / 75±5% RH. Therefore, it was concluded that konjac glucomannan (KGM) is a promising potential carrier for targeting CPM in the vicinity of colon in order to treat colon cancer effectively.
To formulate and evaluate the mouth dissolving tablet dosage forms of favipiravir using various s... more To formulate and evaluate the mouth dissolving tablet dosage forms of favipiravir using various superdisintegrants by using wet granulation technique. Batches of favipiravir Mouth dissolving tablets were formulated by using the wet granulation technique. The formulated granules were evaluated for their flow properties as a pre-compression parameter and the friability, hardness, disintegration, wetting ratio, wetting time, dissolution, and drug release parameters were evaluated as post-compression parameters. The effect of the varying concentrations of superdisintegrants on the formulation for disintegration time was ascertained and the results were compared. The tablet had friability and hardness values ranging from 0.60 to 0.68 % and 3.9 to 4.3 (kg/cm 2 ). Tablet weights did not vary significantly but the disintegration time varied from Original Research Article Avinash et al.; JPRI, 33(6): 28-39, 2021; Article no.JPRI.65646 29 44.66 to 142.66±2.51 min and the wetting time varied f...
Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absor... more Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastroretentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Metoprolol tartrate is an antihypertensive drug, which has low elimination half life: 3-4 h. The floating tablets of metoprolol tartrate were prepared to increase the gastric retention and to improve the bioavailability of the drug. Metoprolol tartrate was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. The rapid gastro-intestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to poor bioavailability of the drug. The floating tablets were formulated using HPMC K4M and HPMC K100M as the release retardant polymers, and sodium bicarbonate as the gas generating agent to reduce the floating lag time. The tablets were prepared by direct compression. ...
International Journal of Research in Pharmaceutical Sciences and Technology, 2020
Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infec... more Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infections. However, it has low skin permeability. Hence, the basic idea behind the development of such a system, transfersomes is to maintain a sustain release of drug from the dosage form and for target delivery. Miconazole nitrate was formulated as transfersomes, half-life can be increased and the desired effect can be obtained. MIC transfersomes were prepared using a thin lipid film hydration technique. The prepared transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC transfersomes was incorporated into a Carbapol 934 gel base which was for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro activity. The prepared MIC transfersomes had a high EE% ranging from 65.45% to 80.11%, with small particle sizes ranging from 368 nm...
Indo American Journal of Pharmaceutical Research, 2015
Article history Benzothiozoles are an important class of heterocyclic compounds which possess wid... more Article history Benzothiozoles are an important class of heterocyclic compounds which possess wide spectrum of biological properties. In the present research work, a series of new 2-substituted benzothiozole derivatives are synthesized and evaluated as enhanced antioxidant and antimicrobial agents. The chemical structure of newly synthesized 2-substituted benzothiazole derivatives are characterized by the spectral studies (IR, Mass and CHN analysis). The compounds were evaluated for their in -vitro antioxidant activity by using five standard protocols namely diphenyl picryl hydrazyl (DPPH) scavenging activity, nitric oxide scavenging activity, reducing power ability study, hydroxyl radical scavenging activity and by lipid peroxidation. Ascorbic acid was used as standard for DPPH, nitric oxide, reducing power ability and hydroxyl radical scavenging assay. Antibacterial activity was evaluated against B. pumilis, A. niger, S. aureous, C. albican and S. dysentriae using Norfloxacin, Ampicillin and Griseofulvin were standard. It was observed that the 2-substituted benzothiazole derivatives confirmed the antioxidant and antimicrobial activities.
Introduction: Orodispersible films (ODF) is a thin strip that is mostly transparent, biodegradabl... more Introduction: Orodispersible films (ODF) is a thin strip that is mostly transparent, biodegradable and it has hydrophilic polymers that disintegrate and dissolves immediately when getting in contact with saliva. Different disintegrants play a crucial role in film properties such as organoleptic properties, film thickness, and in particular disintegration time of the film. The main reason for the development of oral films is for their prominent role in increased patient compliance among pediatrics and geriatrics by disintegrating faster, releasing the drug rapidly, without the need for water, and mostly decreasing the risk of choking. Aim: To formulate orodispersible films of favipiravir and to study the effect of different superdisintegrants on various film properties. Methods: The method used to prepare the film is the solvent casting method. In this method, the solution is prepared using polymer, drug, and superdisintegrants. This solution is casted on a filmforming apparatus usin...
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