Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.8
Anjali Kushwaha
The bioavailability of drug is affected by various excipients present in the formulation. In case of tablets, the role of binders is very important for release of drug and bioavailability. In the present study, starch was extracted from the cashew nuts and used as binding agentat a concentration of 2% w/v, 4% w/v, 6% w/v and 8% w/v. The tablets were formulated by using famotidine drug and they were further evaluated for various parameters like weight variation, hardness, friability, disintegration time, in vitro and in vivo drug release. The results show that all parameters were found within the given Indian Pharmacopeial limits. The in vitro release studies were performed in 0.1 N HCl using dialysis methods. This shows that tablets containing 2 % of cashew starch showed maximum drug release (89%) then other formulations. Then optimized formulation was further used for in vivo study and results shows better bioavailability as compared to marketed products.
{"title":"Cashew Nut Starch as Natural Excipient for Improved Bioavailability of Drugs","authors":"Anjali Kushwaha","doi":"10.37285/ijpsn.2019.12.4.8","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.8","url":null,"abstract":"The bioavailability of drug is affected by various excipients present in the formulation. In case of tablets, the role of binders is very important for release of drug and bioavailability. In the present study, starch was extracted from the cashew nuts and used as binding agentat a concentration of 2% w/v, 4% w/v, 6% w/v and 8% w/v. The tablets were formulated by using famotidine drug and they were further evaluated for various parameters like weight variation, hardness, friability, disintegration time, in vitro and in vivo drug release. The results show that all parameters were found within the given Indian Pharmacopeial limits. The in vitro release studies were performed in 0.1 N HCl using dialysis methods. This shows that tablets containing 2 % of cashew starch showed maximum drug release (89%) then other formulations. Then optimized formulation was further used for in vivo study and results shows better bioavailability as compared to marketed products.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86786579","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.4
H. Mohammadi, H. V, R. S, B. D. V. R. N.
Lornoxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies, and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 33 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plantago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24 (99.21±1.87%) within 10 minutes and was found to superior over Marketed formulation i.e., 87.27±0.27 %. From in vivo bioavailability studies the best formulation has shown Tmax of 1.0 h which was highly significant (P < 0.05) when compared with marketed formulation 2.5 h. The statistical significance was assessed by one-way analysis of variance. Therefore, the solid dispersions incorporated fast disintegrating tablets of Lornoxicam can be successfully used for improvement of dissolution, resulted in faster onset of action as indicated by in vivo studies. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance with immediate action in the effective management of pain and inflammation.
{"title":"Development and Evaluation of Fast Disintegrating Tablets of Lornoxicam Solid Dispersions","authors":"H. Mohammadi, H. V, R. S, B. D. V. R. N.","doi":"10.37285/ijpsn.2019.12.4.4","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.4","url":null,"abstract":"\u0000Lornoxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies, and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 33 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plantago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24 (99.21±1.87%) within 10 minutes and was found to superior over Marketed formulation i.e., 87.27±0.27 %. From in vivo bioavailability studies the best formulation has shown Tmax of 1.0 h which was highly significant (P < 0.05) when compared with marketed formulation 2.5 h. The statistical significance was assessed by one-way analysis of variance. Therefore, the solid dispersions incorporated fast disintegrating tablets of Lornoxicam can be successfully used for improvement of dissolution, resulted in faster onset of action as indicated by in vivo studies. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance with immediate action in the effective management of pain and inflammation.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73227007","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.7
Noura Berakda, A. Radwan
Fungal infections with candida species are an important cause of morbidity and mortality. Situation is further worsened by increasing resistance to antifungal drugs. In this study, we sought to investigate the antifungal activity of peppermint oil against candida albicans of urinary tract candidiasis in females from Syria. An in vitro study was carried out using the following Candida albicans strains involved in urinary tract candidiasis using well diffusion (WD) testing: Candida albicans (ATCC 90028) and 15 strains were compiled from Aleppo university Hospital. It was taken from women having urinary tract candidiasis. The antifungal activity of peppermint oil was determined in the form of inhibition zone using antifungal assay agar WD testing. In all experiments, the obtained results indicated that peppermint oil has inhibitory effects on Candida albicans (ATCC 90028) and some 15 strains. This study showed that peppermint oil was active against the tested Candida albicans strains. Peppermint oil was more effective against Candida albicans compared to fluconazole. Peppermint oil may have potential for use in the development of clinically useful antifungal preparations. Therefore, peppermint oil might be highly effective in the natural prevention treatment of urinary tract candidiasis.
{"title":"Antifungal Activity of Peppermint Oil against Candida Albicans Isolated from Urine Samples","authors":"Noura Berakda, A. Radwan","doi":"10.37285/ijpsn.2019.12.4.7","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.7","url":null,"abstract":"\u0000Fungal infections with candida species are an important cause of morbidity and mortality. Situation is further worsened by increasing resistance to antifungal drugs. In this study, we sought to investigate the antifungal activity of peppermint oil against candida albicans of urinary tract candidiasis in females from Syria. An in vitro study was carried out using the following Candida albicans strains involved in urinary tract candidiasis using well diffusion (WD) testing: Candida albicans (ATCC 90028) and 15 strains were compiled from Aleppo university Hospital. It was taken from women having urinary tract candidiasis. The antifungal activity of peppermint oil was determined in the form of inhibition zone using antifungal assay agar WD testing. In all experiments, the obtained results indicated that peppermint oil has inhibitory effects on Candida albicans (ATCC 90028) and some 15 strains. This study showed that peppermint oil was active against the tested Candida albicans strains. Peppermint oil was more effective against Candida albicans compared to fluconazole. Peppermint oil may have potential for use in the development of clinically useful antifungal preparations. Therefore, peppermint oil might be highly effective in the natural prevention treatment of urinary tract candidiasis.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78457371","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.5
A. P., Mancy S.P., M. K, S. V. Kulkarni, Jagadeesh R
Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.
{"title":"Formulation and Evaluation of Fluvoxamine Maleate Loaded Lipid Nanoparticle","authors":"A. P., Mancy S.P., M. K, S. V. Kulkarni, Jagadeesh R","doi":"10.37285/ijpsn.2019.12.4.5","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.5","url":null,"abstract":"Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"33 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76221097","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.6
B. Wakure, N. Bhatia
We explored the nanoneedles− a novel nanostructured material (NSM) fabricated by nanofabrication techniques and assessed their suitability as a carrier for delivery of silver drug cargo. We achieved individual nanoneedles with tip diameter of 220-250 nm, desired micro-scale length, high Young’s modulus (~100 GPa), and large external surfaces. Owing to large external surfaces of nanoneedles compared to micro-carriers utilized to deliver cargo of drug substances for topical drug delivery. Drug molecules were conjugated on nanoneedle surface and then released by means of predesigned surface chemistry. SEM, TEM, FTIR, XRD and TGA confirmed surface morphologies, structure of nanoneedles. SQUID magneto-meter was used to ascertain the magnetic behavior of nanoneedles. In vivo methods were carried out to assess wound healing potential of Silver Chitosan nanoneedle, wherein it shows the better results for wound healing. Thus, it could provide better scaffold for wound healing in near future.
{"title":"Nanoneedle Mediated Delivery of Silver for Topical Therapies","authors":"B. Wakure, N. Bhatia","doi":"10.37285/ijpsn.2019.12.4.6","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.6","url":null,"abstract":"We explored the nanoneedles− a novel nanostructured material (NSM) fabricated by nanofabrication techniques and assessed their suitability as a carrier for delivery of silver drug cargo. We achieved individual nanoneedles with tip diameter of 220-250 nm, desired micro-scale length, high Young’s modulus (~100 GPa), and large external surfaces. Owing to large external surfaces of nanoneedles compared to micro-carriers utilized to deliver cargo of drug substances for topical drug delivery. Drug molecules were conjugated on nanoneedle surface and then released by means of predesigned surface chemistry. SEM, TEM, FTIR, XRD and TGA confirmed surface morphologies, structure of nanoneedles. SQUID magneto-meter was used to ascertain the magnetic behavior of nanoneedles. In vivo methods were carried out to assess wound healing potential of Silver Chitosan nanoneedle, wherein it shows the better results for wound healing. Thus, it could provide better scaffold for wound healing in near future.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86493862","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.2
Raja Sekharan Thenrajan
Nanocapsules are submicroscopic colloidal drug carrier systems consist of a liquid/solid core in which the drug, gene, protein, and other substances are incorporated into the interior cavity that is surrounded by a distinctive polymeric membrane. Polymers like collagen, albumin, and gelatin are mainly using polymers in nanocapsule formulations. Nanocapsules can serve as nano-sized drug carriers to achieve controlled release as well as efficient drug targeting. The process is used to improve the poor aqueous drug solubility, taste, stabilizing drugs by protecting the molecule from the environment, providing the desired pharmacokinetic profile, allowing controlled release, as well as facilitating oral administration. Capsules are generally prepared between the range of 100 and 1000 nm. Their release and degradation properties largely depend on the composition and the structure of the capsule walls. The dispersion stability of nanocapsules determined by the surfactant, nature of the outer coating. This review describes various facts of nanocapsule drug delivery systems in relation to the method of formulation, characterization, potential benefits and risks, and pharmaceutical applications in drug delivery.
{"title":"Recent Advances in Nanocapsule: Types, Preparation Methods and Characterizatio","authors":"Raja Sekharan Thenrajan","doi":"10.37285/ijpsn.2019.12.4.2","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.2","url":null,"abstract":"Nanocapsules are submicroscopic colloidal drug carrier systems consist of a liquid/solid core in which the drug, gene, protein, and other substances are incorporated into the interior cavity that is surrounded by a distinctive polymeric membrane. Polymers like collagen, albumin, and gelatin are mainly using polymers in nanocapsule formulations. Nanocapsules can serve as nano-sized drug carriers to achieve controlled release as well as efficient drug targeting. The process is used to improve the poor aqueous drug solubility, taste, stabilizing drugs by protecting the molecule from the environment, providing the desired pharmacokinetic profile, allowing controlled release, as well as facilitating oral administration. Capsules are generally prepared between the range of 100 and 1000 nm. Their release and degradation properties largely depend on the composition and the structure of the capsule walls. The dispersion stability of nanocapsules determined by the surfactant, nature of the outer coating. This review describes various facts of nanocapsule drug delivery systems in relation to the method of formulation, characterization, potential benefits and risks, and pharmaceutical applications in drug delivery.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"3346 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86617847","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-31DOI: 10.37285/ijpsn.2019.12.4.3
Abrham Temesgen, Yohannis Eshetu, M. Nigatu
The impact of counterfeit and substandard medicines has been increasing and becoming a public health problem as it significantly increases mortality and morbidity in low income countries. Loratadine is among the drug classes which are most falsified worldwide and is a frequently prescribed anti-allergy medication. As Ethiopia is one of the low-income countries and depends mostly on imported pharmaceutical products, it is necessary to evaluate the quality of drug products being marketed. This study was conducted with the objective of evaluating and comparing the quality of different brands of loratadine 10 mg tablets collected from pharmacy outlets in Addis Ababa city. Tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time and in vitro drug release. All products complied with the pharmacopeial specifications for weight variation and friability. With regard to disintegration time, all sample products disintegrate in less than 15 min as per the pharmacopeial requirement except one product (product E) which is out of the pharmacopeial specification. Dissolution test showed that all the tested products released more than 80% of drug content within 60 min which is in agreement with the pharmacopeial specification.
{"title":"Comparative Evaluation of Different Brands of Loratadine Tablets Marketed in Addis Ababa, Ethiopia","authors":"Abrham Temesgen, Yohannis Eshetu, M. Nigatu","doi":"10.37285/ijpsn.2019.12.4.3","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.4.3","url":null,"abstract":"The impact of counterfeit and substandard medicines has been increasing and becoming a public health problem as it significantly increases mortality and morbidity in low income countries. Loratadine is among the drug classes which are most falsified worldwide and is a frequently prescribed anti-allergy medication. As Ethiopia is one of the low-income countries and depends mostly on imported pharmaceutical products, it is necessary to evaluate the quality of drug products being marketed. This study was conducted with the objective of evaluating and comparing the quality of different brands of loratadine 10 mg tablets collected from pharmacy outlets in Addis Ababa city. Tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time and in vitro drug release. All products complied with the pharmacopeial specifications for weight variation and friability. With regard to disintegration time, all sample products disintegrate in less than 15 min as per the pharmacopeial requirement except one product (product E) which is out of the pharmacopeial specification. Dissolution test showed that all the tested products released more than 80% of drug content within 60 min which is in agreement with the pharmacopeial specification. \u0000 ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"141 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81773459","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.4
Ramarao Ajmeera, R. Gollapudi
Rebamipide is an amino acid analog of 2-(1H)-quinolinone used in the treatment of peptic ulcer. Here we sought to formulate and evaluate gastroretentive floating-bioadhesive tablets of rebamipide to increase the gastric residence time and further compare their pharmacokinetics with conventional immediate release tablets. Floating-bioadhesive tablets of rebamipide were prepared with combination of Polyox WSR 303 and CP 971P/HPMC K4M and Sodium CMC by direct compression method. The prepared formulations were evaluated for hardness, thickness, weight variation, friability, drug content, in vitro buoyancy and drug release. The optimized formulation (RBF12) floated with a lag time of 28.3 ± 3.2 sec, duration of floating 12 h and released about 99.91 ± 1.84% of drug in 12 h, and then followed non-Fickian diffusion release mechanism with n value of 0.635. The RBF12 tablets with BaSO4 remained in stomach for 5.13 ± 0.64 h (n=3) in radiological studies. The formulation, RBF12 exhibited maximum bioadhesive strength (1.346 ± 0.110 N) than other formulations. The bioavailability studies were carried out for the optimized formulation (RBF12) and compared with that of reference IR tablets “Rebagen” in nine healthy human volunteers. Based on in vivo performance significant difference was observed between Cmax, tmax, t1/2, AUC0–∞, and MRT of RBF12 and IR tablets. The increase in relative bioavailability of RBF12 was 1.7-fold when compared to reference IR tablets. The increased relative oral bioavailability may be due to the floating-bioadhesive mechanism of dosage form, which is desirable for drugs absorbed from the upper part of gastrointestinal tract.
{"title":"Gastroretentive Floating-Bioadhesive Drug Delivery System for Rebamipide: Design, In vitro and In vivo Evaluation","authors":"Ramarao Ajmeera, R. Gollapudi","doi":"10.37285/ijpsn.2019.12.3.4","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.3.4","url":null,"abstract":"Rebamipide is an amino acid analog of 2-(1H)-quinolinone used in the treatment of peptic ulcer. Here we sought to formulate and evaluate gastroretentive floating-bioadhesive tablets of rebamipide to increase the gastric residence time and further compare their pharmacokinetics with conventional immediate release tablets. Floating-bioadhesive tablets of rebamipide were prepared with combination of Polyox WSR 303 and CP 971P/HPMC K4M and Sodium CMC by direct compression method. The prepared formulations were evaluated for hardness, thickness, weight variation, friability, drug content, in vitro buoyancy and drug release. The optimized formulation (RBF12) floated with a lag time of 28.3 ± 3.2 sec, duration of floating 12 h and released about 99.91 ± 1.84% of drug in 12 h, and then followed non-Fickian diffusion release mechanism with n value of 0.635. The RBF12 tablets with BaSO4 remained in stomach for 5.13 ± 0.64 h (n=3) in radiological studies. The formulation, RBF12 exhibited maximum bioadhesive strength (1.346 ± 0.110 N) than other formulations. The bioavailability studies were carried out for the optimized formulation (RBF12) and compared with that of reference IR tablets “Rebagen” in nine healthy human volunteers. Based on in vivo performance significant difference was observed between Cmax, tmax, t1/2, AUC0–∞, and MRT of RBF12 and IR tablets. The increase in relative bioavailability of RBF12 was 1.7-fold when compared to reference IR tablets. The increased relative oral bioavailability may be due to the floating-bioadhesive mechanism of dosage form, which is desirable for drugs absorbed from the upper part of gastrointestinal tract.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85568299","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.7
Shweta Agarwal, Pallavi Tempta, Poonam Kaushik, K. Kaushik
Niosomes are lamellar vesicles formed by self-association of non-ionic surfactants and cholesterol having good compatibility with the biological system and low toxicity. Their ability to encapsulate both hydrophilic and hydrophobic drugs, their potential use in protection of drugs, controlled release and targeted drug delivery makes them a promising drug delivery system. Various factors like nature of drug, amount and type of surfactant used, method of preparation, amount and charge of cholesterol used, type and volume of hydrating medium, speed of agitation, time and temperature of hydration medium affect the type and characteristics of niosomes formed. Therefore, a study was conducted to determine the effect of hydration temperature on the size of niosomes formed by ether injection method. Aceclofenac was used as the model drug as it is lipophilic and shows good encapsulation in niosomes. Span 20 was used as the non-ionic surfactant. The study was conducted at three temperatures of hydration and all the other variables were kept constant. The niosomes formed at the different hydration temperatures were evaluated for shape and size by optical microscopy and mean vesicle size determined at each temperature. The data obtained for size was statistically analysed by the software Graphpad prism version 7 using ordinary one-way ANOVA. The p value obtained (at 95% confidence interval: p< 0.05) was used to determine significant difference between the mean vesicle sizes at the three temperatures. The study showed that hydration temperature played a major role in the size of niosomes formed by ether injection method.
乳小体是由非离子表面活性剂与胆固醇自结合形成的层状囊泡，与生物系统相容性好，毒性低。它们包封亲水和疏水药物的能力，以及在药物保护、控释和靶向给药方面的潜在应用，使其成为一种很有前途的给药系统。药物的性质、表面活性剂的用量和种类、制备方法、胆固醇的用量和电荷、水化介质的种类和体积、搅拌速度、水化介质的时间和温度等因素影响所形成的纳米粒的种类和特性。因此，我们研究了水化温度对乙醚注射法形成的纳米体大小的影响。采用乙酰氯芬酸作为模型药物，因为它具有亲脂性，在囊体中具有良好的包被性。采用Span 20作为非离子表面活性剂。本研究在三种水化温度下进行，所有其他变量保持不变。通过光学显微镜观察不同水化温度下形成的乳质体的形状和大小，并测定每个温度下的平均囊泡大小。尺寸数据采用Graphpad prism version 7软件进行统计分析，采用普通单因素方差分析。用得到的p值(95%置信区间:p< 0.05)来确定三种温度下平均囊泡大小之间的显著差异。研究表明，水化温度对乙醚注射法形成的乳质体的大小起主要作用。
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Pub Date : 2019-05-31DOI: 10.37285/ijpsn.2019.12.3.6
R. Md, Rajnarayana K, A. M
The main objective of the present study was to develop colon-targeted tablets of mesalazine by wet granulation method using 33 Response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16 % of mesalazine after 24 h, whereas marketed product drug release was 92.02 ± 2.15 after 24 h. From in vivo bioavailability studies, after oral administration of colon targeted tablet containing 400 mg mesalazine, the Cmax, Tmax, and AUC0–∞ of optimized formulation and marketed product was found to be 683.21 ± 0.03 ng/mL, 6.01 ± 0.04 h, 4150.12 ± 5.12 ng*h/mL and 445.34 ± 3.22 ng/mL, 4.00 ± 0.01 h, 3457.18 ± 5.32 ng*h/mL respectively. Cmax, Tmax and AUC values of optimized formulation were found to be significantly higher than of marketed product. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of mesalazine for the treatment of disease at colon region.
采用33响应面法，设计实验软件，以HPMC K4M、Eudragit RL100、乙基纤维素和PVP K-30为pH依赖聚合物，采用湿造粒法制备美沙嗪大肠靶向片。对各制剂(F1 ~ F27)进行理化参数评价，并进行体外释药研究。采用紫外分光光度法测定不同时间间隔美沙拉嗪片的释放量。制定F26释放98.16%的mesalazine后24 h,而销售产品药物释放为92.02±2.15 24 h后,从体内生物利用度研究,在口服结肠靶向平板含有400毫克mesalazine Cmax,达峰时间,和AUC0 -∞优化配方和销售产品被发现是683.21±0.03 ng / mL, 6.01±0.04,4150.12±5.12 ng * h /毫升和445.34±3.22 ng / mL, 4.00±0.01 h, h * 3457.18±5.32 ng / mL。优化配方的Cmax、Tmax和AUC值均显著高于市售产品。pH依赖片剂系统是一种很有前途的载体，可以防止美沙拉嗪在胃环境中快速水解，提高口服生物利用度，用于治疗结肠区域疾病。
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