Pub Date : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49476
Phani Kumar Sunkara, Sreedhara Chaganty, K. Ramakrishna
Objective: The study was aimed to develop a precise and simple liquid chromatographic electrospray ionization tandem mass spectrometric (LC-ESI-MSMS) technique is essential for the quantification of Infigratinib in biological matrices. Methods: Chromatographic resolution was attained with PhenominexC18 (50 mm×2.6 mm, 3 µm) stationary column and a mobile solvent composition of 0.1% HCOOH, methyl alcohol and acetonitrile in the proportion of 10:10:80. Chromatograms were resolved by an isocratic separation with a flowing rate of 0.50 ml/min at 40 °C. Results: Quantitation was executed by monitoring the transitions of m/z. 560.19/189.13 for Infigratinib and 494.5→394.5 for Imatinib internal standard in multiple reaction monitoring. The standard curve regression line was y = 0.0016x+0.0062 and the correction coefficient (r2) was 0.9994. The % CV outcomes for matrix effect at Lower-QC and Higher-QC were 4.95% and 3.61% respectively. The percentage average recoveries for Infigratinib in Higher-QC (900ng/ml), MQC (600ng/ml) and Lower-QC (3ng/ml) were 93.27%, 94.69% and 97.24% respectively. The intra and interday precisions of analytical procedure was estimated by assessing the %CV outcomes and were in between 1.88 to 5.93% for the QC samples. Conclusion: The developed procedure can be useful for the assessment of Infigratinib in biological matrices in quality control, forensic and bioavailability studies.
{"title":"AN LC-ESI-MS/MS METHOD DEVELOPMENT AND VALIDATION FOR THE QUANTIFICATION OF INFIGRATINIB IN BIOLOGICAL MATRICES","authors":"Phani Kumar Sunkara, Sreedhara Chaganty, K. Ramakrishna","doi":"10.22159/ijap.2024v16i1.49476","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49476","url":null,"abstract":"Objective: The study was aimed to develop a precise and simple liquid chromatographic electrospray ionization tandem mass spectrometric (LC-ESI-MSMS) technique is essential for the quantification of Infigratinib in biological matrices.\u0000Methods: Chromatographic resolution was attained with PhenominexC18 (50 mm×2.6 mm, 3 µm) stationary column and a mobile solvent composition of 0.1% HCOOH, methyl alcohol and acetonitrile in the proportion of 10:10:80. Chromatograms were resolved by an isocratic separation with a flowing rate of 0.50 ml/min at 40 °C.\u0000Results: Quantitation was executed by monitoring the transitions of m/z. 560.19/189.13 for Infigratinib and 494.5→394.5 for Imatinib internal standard in multiple reaction monitoring. The standard curve regression line was y = 0.0016x+0.0062 and the correction coefficient (r2) was 0.9994. The % CV outcomes for matrix effect at Lower-QC and Higher-QC were 4.95% and 3.61% respectively. The percentage average recoveries for Infigratinib in Higher-QC (900ng/ml), MQC (600ng/ml) and Lower-QC (3ng/ml) were 93.27%, 94.69% and 97.24% respectively. The intra and interday precisions of analytical procedure was estimated by assessing the %CV outcomes and were in between 1.88 to 5.93% for the QC samples.\u0000Conclusion: The developed procedure can be useful for the assessment of Infigratinib in biological matrices in quality control, forensic and bioavailability studies.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"18 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448550","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49344
Chandana Narasimha Rao, M. Sujatha
Objective: The discharge of these synthetic food dyes, such as sunset yellow and tartrazine, into industrial wastewater can lead to significant environmental and health issues. Its removal through effective adsorption presents an economical and efficient solution. Hence this study proposed to fabricate metal nanoparticles for the adsorption of carcinogenic dyes. Methods: The fabrication of iron and zinc nanoparticles employed the green synthesis methodology, utilizing an aqueous extract of Diospyros chloroxylon (Roxb.) as a reducing agent. The fabricated nanoparticles were characterized using TEM (Transmission Electron Microscopy), EDX (Energy-Dispersive X-ray Spectroscopy), SEM (Scanning Electron Microscopy), FTIR (Fourier-Transform Infrared Spectroscopy), and UV-Visible Spectroscopy. The nanoparticles were studied for its efficiency for the adsorption of carcinogenic dyes such as tartrazine and Sunset Yellow. Results: The iron nanoparticles were noticed to be uniformly distributed rod-shaped particles having smooth surfaces with 23-51 nm size range and an average particle size of 34 nm. Whereas the iron nanoparticles were noticed to be uniformly distributed spherical to oval shape with 35 nm to 68 nm size range and an average particle size 53 nm. The XRD results confirm that the iron nanoparticles were rhombohedral phase structure with 71.91 % of elemental iron whereas the zinc nanoparticles were noticed to be hexagonal Wurtzite phase structure having 69.4 % of metallic zinc. These synthesized nanoparticles were applied for the removal of sunset yellow and tartrazine dyes were investigated and found more than 90 % was removed. Adsorption isotherm study was best fitted with Langmuir model, and the maximal adsorption capacity was found to be 52.18 and 75.04 mg/g for sunset yellow using iron and zinc nanoparticles, whereas tartrazine maximum adsorption capacity was noticed to be 69.96 and 84.24 mg/g for iron and zinc nanoparticles. The adsorption reaction follows pseudo-first-order kinetics with high correlation coefficient. Repeated cycles of regeneration, reuse and stability showed very high removal efficiency and stability. Conclusion: The biosynthesis of metal nanoparticles demonstrates substantial promise for applications in environmental protection.
{"title":"FABRICATION OF NANOSTRUCTURED IRON AND ZINC PARTICLES BY DIOSPYROS CHLOROXYLON (ROXB.) LEAF EXTRACT: CHARACTERIZATION, ADSORPTION MODELING AND CARCINOGENIC DYE ADSORPTION APPLICATIONS","authors":"Chandana Narasimha Rao, M. Sujatha","doi":"10.22159/ijap.2024v16i1.49344","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49344","url":null,"abstract":"Objective: The discharge of these synthetic food dyes, such as sunset yellow and tartrazine, into industrial wastewater can lead to significant environmental and health issues. Its removal through effective adsorption presents an economical and efficient solution. Hence this study proposed to fabricate metal nanoparticles for the adsorption of carcinogenic dyes.\u0000Methods: The fabrication of iron and zinc nanoparticles employed the green synthesis methodology, utilizing an aqueous extract of Diospyros chloroxylon (Roxb.) as a reducing agent. The fabricated nanoparticles were characterized using TEM (Transmission Electron Microscopy), EDX (Energy-Dispersive X-ray Spectroscopy), SEM (Scanning Electron Microscopy), FTIR (Fourier-Transform Infrared Spectroscopy), and UV-Visible Spectroscopy. The nanoparticles were studied for its efficiency for the adsorption of carcinogenic dyes such as tartrazine and Sunset Yellow.\u0000Results: The iron nanoparticles were noticed to be uniformly distributed rod-shaped particles having smooth surfaces with 23-51 nm size range and an average particle size of 34 nm. Whereas the iron nanoparticles were noticed to be uniformly distributed spherical to oval shape with 35 nm to 68 nm size range and an average particle size 53 nm. The XRD results confirm that the iron nanoparticles were rhombohedral phase structure with 71.91 % of elemental iron whereas the zinc nanoparticles were noticed to be hexagonal Wurtzite phase structure having 69.4 % of metallic zinc. These synthesized nanoparticles were applied for the removal of sunset yellow and tartrazine dyes were investigated and found more than 90 % was removed. Adsorption isotherm study was best fitted with Langmuir model, and the maximal adsorption capacity was found to be 52.18 and 75.04 mg/g for sunset yellow using iron and zinc nanoparticles, whereas tartrazine maximum adsorption capacity was noticed to be 69.96 and 84.24 mg/g for iron and zinc nanoparticles. The adsorption reaction follows pseudo-first-order kinetics with high correlation coefficient. Repeated cycles of regeneration, reuse and stability showed very high removal efficiency and stability.\u0000Conclusion: The biosynthesis of metal nanoparticles demonstrates substantial promise for applications in environmental protection.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"28 24","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448746","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}
Objective: The research aims to enhance poorly water-soluble drug Simvastatin (SMV) solubility and bioavailability by solid dispersion (SD) using various sugar carriers like lactulose, xylitol, Sorbitol, and soluplus. Methods: First, the drug was subjected to determine bulk density, carr’s index, Hausner’s ratio, angle of repose, solubility analysis in various solvents like 0.1 N HCl, 6.8pH, 7.2pH phosphate buffers, methanol, and ethanol and preformulation studies. via various carrier concentrations (1:0.5, 1:1, 1:1.5, 1:2, and 1:3), SMV solid dispersions (SD s) were made by solvent evaporation and fusion. The various physiochemical parameters of each formulation were tested. Results: For various physicochemical criteria, all of the formulations were found to be within the allowed pharmacopoeial limits. Preformulation studies such as FT-IR demonstrated the lack of interactions between drugs and excipients. In comparison to the other solvents, 0.1N HCl showed SMV to be more soluble. The SDs underwent yield, entrapment, and in vitro drug release study evaluations. 88 to 100.68% recovery rates and 92 to 101% capture efficiency were observed. While SDs containing Sorbitol released 74-98% of the medicine, formulations utilizing Sorbitol demonstrated 80-99% drug release, and formulations using xylitol as a carrier released 83-99% of the drug. For more than 60 min, the formulation, including lactulose, delivered 91-100% of the Simvastatin dose. Conclusion: Lactulose-containing SMV SDs demonstrated superior release characteristics, and an optimized formulation with a 1:1.5 drug-to-carrier ratio has been chosen.
{"title":"ENHANCEMENT OF DISSOLUTION AND BIOAVAILABILITY OF SIMVASTATIN BY SOLID DISPERSION TECHNIQUE USING SUGAR-BASED CARRIERS","authors":"Venkata Naga JYOTHI NAKKA, Kumar Shiva Gubbiyappa, Nagesh Nagaraju","doi":"10.22159/ijap.2024v16i1.49442","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49442","url":null,"abstract":"Objective: The research aims to enhance poorly water-soluble drug Simvastatin (SMV) solubility and bioavailability by solid dispersion (SD) using various sugar carriers like lactulose, xylitol, Sorbitol, and soluplus.\u0000Methods: First, the drug was subjected to determine bulk density, carr’s index, Hausner’s ratio, angle of repose, solubility analysis in various solvents like 0.1 N HCl, 6.8pH, 7.2pH phosphate buffers, methanol, and ethanol and preformulation studies. via various carrier concentrations (1:0.5, 1:1, 1:1.5, 1:2, and 1:3), SMV solid dispersions (SD s) were made by solvent evaporation and fusion. The various physiochemical parameters of each formulation were tested.\u0000Results: For various physicochemical criteria, all of the formulations were found to be within the allowed pharmacopoeial limits. Preformulation studies such as FT-IR demonstrated the lack of interactions between drugs and excipients. In comparison to the other solvents, 0.1N HCl showed SMV to be more soluble. The SDs underwent yield, entrapment, and in vitro drug release study evaluations. 88 to 100.68% recovery rates and 92 to 101% capture efficiency were observed. While SDs containing Sorbitol released 74-98% of the medicine, formulations utilizing Sorbitol demonstrated 80-99% drug release, and formulations using xylitol as a carrier released 83-99% of the drug. For more than 60 min, the formulation, including lactulose, delivered 91-100% of the Simvastatin dose.\u0000Conclusion: Lactulose-containing SMV SDs demonstrated superior release characteristics, and an optimized formulation with a 1:1.5 drug-to-carrier ratio has been chosen.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"24 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448668","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49245
Nurul Arfiyanti Yusuf, M. Abdassah, I. Sopyan, R. Mauludin, I. Joni, A. Chaerunisaa
Objective: Transethosome as a vesicular system offers high skin permeation; therefore, it is expected to improve the solubility and permeability of the poorly soluble drug glibenclamide. The study aimed to optimize the effect of lipid and surfactant concentration as well as sonication time on the physical characteristics of glibenclamide-loaded transethosomes. Methods: The transethosomes were prepared by solvent evaporation method. An experimental Box-Behnken design optimized the formula by assessing particle size, polydispersity index, zeta potential, and entrapment efficiency as response parameters. Further characterizations were conducted by determining the morphology by TEM, chemical interaction by FTIR, thermal behavior by DSC, as well as solubility improvement by using in vitro drug release and permeation study. Results: The result showed that the optimal formula was that with the lipid composition of 75 mg of soya lecithin, 5 mg of tween 80 as surfactant at a sonication time of 18.79 min. The responses were particle size of 166.8±5.3 nm, polydispersity index of 0.463±0.1, zeta potential of-44.7±2.2 mV, and entrapment efficiency as much as 87.18±3.8%. Glibenclamide-loaded transethosomes exhibited a spherical morphology with no visible aggregation. FTIR study revealed no chemical interactions between Glibenclamide and the excipients. Solubility and in vitro drug release tests showed a significant increase of Glibenclamide from transethosome (p<0.05) compared with that as a bulk powder. Conclusion: Overall, the optimized glibenclamide-loaded transethosomes designed with Box Behnken resulted in improved physicochemical characteristics and increased solubility and drug release compared with that from ethosomes and bulk powder comparison, which will be promising for Glibenclamide to be formulated as transdermal drug delivery.
{"title":"IMPROVED CHARACTERISTICS OF GLIBENCLAMIDE AS TRANSETHOSOME VESICULAR SYSTEM: PHYSICOCHEMICAL, SOLUBILITY AND IN VITRO PERMEATION STUDY","authors":"Nurul Arfiyanti Yusuf, M. Abdassah, I. Sopyan, R. Mauludin, I. Joni, A. Chaerunisaa","doi":"10.22159/ijap.2024v16i1.49245","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49245","url":null,"abstract":"Objective: Transethosome as a vesicular system offers high skin permeation; therefore, it is expected to improve the solubility and permeability of the poorly soluble drug glibenclamide. The study aimed to optimize the effect of lipid and surfactant concentration as well as sonication time on the physical characteristics of glibenclamide-loaded transethosomes.\u0000Methods: The transethosomes were prepared by solvent evaporation method. An experimental Box-Behnken design optimized the formula by assessing particle size, polydispersity index, zeta potential, and entrapment efficiency as response parameters. Further characterizations were conducted by determining the morphology by TEM, chemical interaction by FTIR, thermal behavior by DSC, as well as solubility improvement by using in vitro drug release and permeation study.\u0000Results: The result showed that the optimal formula was that with the lipid composition of 75 mg of soya lecithin, 5 mg of tween 80 as surfactant at a sonication time of 18.79 min. The responses were particle size of 166.8±5.3 nm, polydispersity index of 0.463±0.1, zeta potential of-44.7±2.2 mV, and entrapment efficiency as much as 87.18±3.8%. Glibenclamide-loaded transethosomes exhibited a spherical morphology with no visible aggregation. FTIR study revealed no chemical interactions between Glibenclamide and the excipients. Solubility and in vitro drug release tests showed a significant increase of Glibenclamide from transethosome (p<0.05) compared with that as a bulk powder.\u0000Conclusion: Overall, the optimized glibenclamide-loaded transethosomes designed with Box Behnken resulted in improved physicochemical characteristics and increased solubility and drug release compared with that from ethosomes and bulk powder comparison, which will be promising for Glibenclamide to be formulated as transdermal drug delivery.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"14 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448680","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49218
R. E. Tarigan, Muhammad Andry, Annisa Tifany ZULMI MARPAUNG, Muhammad Amin Nasution, Muhammad Fauzan Lubis
Objective: This study aims to develop a spectrophotometric method with the Ratio Difference method using ethanol pro analysis solvent to obtain the results of Dextromethorphan Hydrobromide (HBr) levels of Guaifenesin and Diphenhydramine Hydrochloride (HCl) in tablets. Methods: The Ratio Difference Sprctrophotography method involves dividing the mixture spectrum by the standard spectrum of each analyte and reducing the ratio to obtain a spectrum that does not depend on the concentration of the analyte used as a divider and can directly determine the levels of Dextromethorphan HBr, Guaifenesin, and Diphenhydramine HCl in the range 200-400 nm wavelength using experimentally calculated absorbance. Results: The maximum wavelengths of Dextromethorphan HBr, Guaifenesin, and Diphenhydramine HCl were obtained at 278 nm, 273 nm, and 252 nm, respectively. The average % accuracy obtained was 99.60% for Dextromethorphan HBr, 98.98% for Guaifenesin, and 100.32% for Diphenhydramine HCl in dosage forms. Conclusion: This method was successfully applied with simultaneous estimation to determine Dextromethorphan HBr, Guaifenesin, and Diphenhydramine HCl levels in tablet preparations and met the validation requirements.
{"title":"QUANTITATIVE ANALYSIS OF DEXTROMETHORPHAN-HBr, GUAIFENESIN, AND DIPHENHYDRAMINE-HCl IN TABLET DOSAGE FORM BY RATIO DIFFERENCE SPECTROPHOTOMETRY METHOD","authors":"R. E. Tarigan, Muhammad Andry, Annisa Tifany ZULMI MARPAUNG, Muhammad Amin Nasution, Muhammad Fauzan Lubis","doi":"10.22159/ijap.2024v16i1.49218","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49218","url":null,"abstract":"Objective: This study aims to develop a spectrophotometric method with the Ratio Difference method using ethanol pro analysis solvent to obtain the results of Dextromethorphan Hydrobromide (HBr) levels of Guaifenesin and Diphenhydramine Hydrochloride (HCl) in tablets.\u0000Methods: The Ratio Difference Sprctrophotography method involves dividing the mixture spectrum by the standard spectrum of each analyte and reducing the ratio to obtain a spectrum that does not depend on the concentration of the analyte used as a divider and can directly determine the levels of Dextromethorphan HBr, Guaifenesin, and Diphenhydramine HCl in the range 200-400 nm wavelength using experimentally calculated absorbance.\u0000Results: The maximum wavelengths of Dextromethorphan HBr, Guaifenesin, and Diphenhydramine HCl were obtained at 278 nm, 273 nm, and 252 nm, respectively. The average % accuracy obtained was 99.60% for Dextromethorphan HBr, 98.98% for Guaifenesin, and 100.32% for Diphenhydramine HCl in dosage forms.\u0000Conclusion: This method was successfully applied with simultaneous estimation to determine Dextromethorphan HBr, Guaifenesin, and Diphenhydramine HCl levels in tablet preparations and met the validation requirements.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"67 23","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139449223","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49340
Deni Noviza, T. Julianto, A. B. Abdul Majeed, K. A. Hamid
Objective: A simple, straightforward, ultra-performance liquid chromatography (UPLC) with a fluorescence detector method was developed and validated to determine xanthorrhizol in rat plasma. This method was successfully applied to an oral pharmacokinetic study. Methods: Xanthorrhizol was separated using a C18 column in an isocratic mode using a mobile phase of acetonitrile: water (85:15 v/v) at a 0.4 ml/min flow rate. The fluorescence detector was set at 230 nm excitation and 320 nm emission wavelengths. The method was then applied in the pharmacokinetic study involving 12 Sprague-Dawley rats. Results: The developed bioanalytical methods were found to be linear in the range of 0.078–5 mg/ml with a correlation coefficient of r2=0.999. The percentage recovery of xanthorrhizol was more than 95%, and the relative standard deviation was less than 2. These results indicate that the method is accurate and precise. The limit of detection (LOD) and limit of quantification (LOQ) of the technique were 0.123 µg/ml and 0.373 µg/ml, respectively. Furthermore, the stability studies demonstrated that xanthorrhizol is stable under various analytical conditions. The pharmacokinetic study revealed that the area under the curve (AUC) was 27.23±19.65 (µg. h/ml), the half-life (t 1/2) was 7.71±2.89 h, the mean residence time (MRT) was 13.86±4.06 h while the maximum concentration (Cmax) was 1.58±0.62 µg/ml, and the time to reach the maximum concentration (Tmax) was 1.33±0.20 h. Conclusion: The developed bioanalytical method was reliable and successfully met all validation criteria, making it a robust choice for quantifying xanthorrhizol. Therefore, it may be effectively utilized to determine xanthorrhizol in rat plasma following a pharmacokinetic study.
{"title":"BIOANALYTICAL OF UPLC METHOD DEVELOPMENT AND VALIDATION OF XANTHORRIZOL AND ITS APPLICATION TO PHARMACOKINETIC STUDY","authors":"Deni Noviza, T. Julianto, A. B. Abdul Majeed, K. A. Hamid","doi":"10.22159/ijap.2024v16i1.49340","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49340","url":null,"abstract":"Objective: A simple, straightforward, ultra-performance liquid chromatography (UPLC) with a fluorescence detector method was developed and validated to determine xanthorrhizol in rat plasma. This method was successfully applied to an oral pharmacokinetic study.\u0000Methods: Xanthorrhizol was separated using a C18 column in an isocratic mode using a mobile phase of acetonitrile: water (85:15 v/v) at a 0.4 ml/min flow rate. The fluorescence detector was set at 230 nm excitation and 320 nm emission wavelengths. The method was then applied in the pharmacokinetic study involving 12 Sprague-Dawley rats.\u0000Results: The developed bioanalytical methods were found to be linear in the range of 0.078–5 mg/ml with a correlation coefficient of r2=0.999. The percentage recovery of xanthorrhizol was more than 95%, and the relative standard deviation was less than 2. These results indicate that the method is accurate and precise. The limit of detection (LOD) and limit of quantification (LOQ) of the technique were 0.123 µg/ml and 0.373 µg/ml, respectively. Furthermore, the stability studies demonstrated that xanthorrhizol is stable under various analytical conditions. The pharmacokinetic study revealed that the area under the curve (AUC) was 27.23±19.65 (µg. h/ml), the half-life (t 1/2) was 7.71±2.89 h, the mean residence time (MRT) was 13.86±4.06 h while the maximum concentration (Cmax) was 1.58±0.62 µg/ml, and the time to reach the maximum concentration (Tmax) was 1.33±0.20 h.\u0000Conclusion: The developed bioanalytical method was reliable and successfully met all validation criteria, making it a robust choice for quantifying xanthorrhizol. Therefore, it may be effectively utilized to determine xanthorrhizol in rat plasma following a pharmacokinetic study.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"9 11","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448357","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49377
Bhargavi Posinasetty, Srividya Kommineni, R. K. Kumarachari, Kishore Bandarapalle, Syed Naziya, Chanambatla Yamini, Daruri Seemanthini
Objective: The current study’s objective is to develop and optimize nanoencapsulated bio compounds of Asparagus racemosus (BCAR) utilizing the ionic gelation process to target the kidney for antiurolithiatic activity. Methods: Nanoencapsulated BCAR was prepared employing the ionic gelation method. Box Behnken Design (BBD) 3-factor, 3-level is used to examine the effects of formulation parameters and to enhance the desired responses. Characterization studies include Fourier transform infrared (FTIR), X-ray diffraction (XRD), particle size, zeta potential, scanning electron microscopy (SEM), and transmission electron microscopy (TEM) performed to study the quality of optimized nanoparticles. Results: Mathematical equations and response surface plots were used to relate the dependent and independent variables. Diagnostic charts were used to show the varied factor-level permutations. The percentages of entrapment efficiency (% EE) and drug release (% DR) used in evaluation studies of optimized bio compounds of BCAR nanoparticles (OBCARNPs) were determined to be 80.67% and 77.4%, respectively. The Fourier transform infrared (FTIR) results showed that chitosan, sodium tripolyphosphate (NaTPP), and BCAR were compatible. Due to chitosan and NaTPP gelation in the case of OBCBANPs, X-ray diffraction (XRD) analyses have acknowledged the crystallinity. The particle size and zeta potential of the optimized formulation, found to be 48.8 nm and 14.1 mV, respectively, indicate the nanoparticles are in the nanorange and possess extreme stability by preventing particle convergence. Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) studies reveal that the optimized formulation nanoparticles are spherical in shape, homogeneous, and have little aggregation. The accelerated stability studies showed that the optimized formulation was stable at different temperatures and relative humidity. Conclusion: The stable, optimized formulation was prepared, evaluated, and characterized. BBD is employed to optimize the formulation by minimizing the number of experimental runs and enhancing the desired responses. The optimized formulation further needs to investigate the in vivo studies for antiurolithiatic activity by targeting the kidney.
{"title":"DESIGN AND OPTIMIZATION OF NANO ENCAPSULATED BIO COMPOUNDS OF ASPARAGUS RACEMOSUS: BOX BEHNKEN APPROACH","authors":"Bhargavi Posinasetty, Srividya Kommineni, R. K. Kumarachari, Kishore Bandarapalle, Syed Naziya, Chanambatla Yamini, Daruri Seemanthini","doi":"10.22159/ijap.2024v16i1.49377","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49377","url":null,"abstract":"Objective: The current study’s objective is to develop and optimize nanoencapsulated bio compounds of Asparagus racemosus (BCAR) utilizing the ionic gelation process to target the kidney for antiurolithiatic activity.\u0000Methods: Nanoencapsulated BCAR was prepared employing the ionic gelation method. Box Behnken Design (BBD) 3-factor, 3-level is used to examine the effects of formulation parameters and to enhance the desired responses. Characterization studies include Fourier transform infrared (FTIR), X-ray diffraction (XRD), particle size, zeta potential, scanning electron microscopy (SEM), and transmission electron microscopy (TEM) performed to study the quality of optimized nanoparticles.\u0000Results: Mathematical equations and response surface plots were used to relate the dependent and independent variables. Diagnostic charts were used to show the varied factor-level permutations. The percentages of entrapment efficiency (% EE) and drug release (% DR) used in evaluation studies of optimized bio compounds of BCAR nanoparticles (OBCARNPs) were determined to be 80.67% and 77.4%, respectively. The Fourier transform infrared (FTIR) results showed that chitosan, sodium tripolyphosphate (NaTPP), and BCAR were compatible. Due to chitosan and NaTPP gelation in the case of OBCBANPs, X-ray diffraction (XRD) analyses have acknowledged the crystallinity. The particle size and zeta potential of the optimized formulation, found to be 48.8 nm and 14.1 mV, respectively, indicate the nanoparticles are in the nanorange and possess extreme stability by preventing particle convergence. Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) studies reveal that the optimized formulation nanoparticles are spherical in shape, homogeneous, and have little aggregation. The accelerated stability studies showed that the optimized formulation was stable at different temperatures and relative humidity.\u0000Conclusion: The stable, optimized formulation was prepared, evaluated, and characterized. BBD is employed to optimize the formulation by minimizing the number of experimental runs and enhancing the desired responses. The optimized formulation further needs to investigate the in vivo studies for antiurolithiatic activity by targeting the kidney.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"30 13","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448639","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.48052
Sanjay Kumar Gupta, S. Patra
Objective: The principal objective of this research was to develop and optimize cost-effective sustained-release Vildagliptin (VLN) tablets using the wet granulation method. Methods: The tablets were prepared by the non-aqueous wet granulation method. A Box-Behnken design was used to study the effect of the independent variables, i.e., HPMC K100 M, Eudragit RSPO and PVP K30, on the dependent variables swelling index, in vitro drug release at 8 and 12 h. The drug's physiochemical properties were investigated using ultraviolet (UV), Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The hardness, thickness, weight variation, content uniformity, swelling index, and in vitro drug release study of the formulated tablets were all evaluated. The optimized formulation Opt-VLD-SR was evaluated for pharmacokinetic parameters like AUC, Cmax, tmax and MRT. Results: The FTIR and DSC studies confirmed that no interaction occurred between the drug, polymers and excipients. The crystalline nature of VLN remained unchanged in the optimised formulation tablet, according to DSC studies. With the optimal concentration of both polymers, formulation Opt-VLN delayed drug release for up to 12 h. The formulated Optimized Sustained-release tablets (Opt-VLD-SR) showed significantly lower Cmax±3.01ng/ml) than conventional IR tablets (256.17±8.02ng/ml). In the pharmacokinetic study, the MRT for Optimized-VLD-SR is (7.40h) showed a better result than the Vildagliptin IR marketed product (3.70 h.), which leads to higher bioavailability of Vildagliptin. Conclusion: Sustained release tablets of VLN with a combination of diffusion and erosion-controlled drug release mechanisms have been successfully developed.
{"title":"DEVELOPMENT, CHARACTERIZATION AND PHARMACOKINETIC EVALUATION OF OPTIMIZED VILDAGLIPTIN SUSTAINED RELEASE MATRIX TABLET USING BOX-BEHNKEN DESIGN","authors":"Sanjay Kumar Gupta, S. Patra","doi":"10.22159/ijap.2024v16i1.48052","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.48052","url":null,"abstract":"Objective: The principal objective of this research was to develop and optimize cost-effective sustained-release Vildagliptin (VLN) tablets using the wet granulation method.\u0000Methods: The tablets were prepared by the non-aqueous wet granulation method. A Box-Behnken design was used to study the effect of the independent variables, i.e., HPMC K100 M, Eudragit RSPO and PVP K30, on the dependent variables swelling index, in vitro drug release at 8 and 12 h. The drug's physiochemical properties were investigated using ultraviolet (UV), Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The hardness, thickness, weight variation, content uniformity, swelling index, and in vitro drug release study of the formulated tablets were all evaluated. The optimized formulation Opt-VLD-SR was evaluated for pharmacokinetic parameters like AUC, Cmax, tmax and MRT.\u0000Results: The FTIR and DSC studies confirmed that no interaction occurred between the drug, polymers and excipients. The crystalline nature of VLN remained unchanged in the optimised formulation tablet, according to DSC studies. With the optimal concentration of both polymers, formulation Opt-VLN delayed drug release for up to 12 h. The formulated Optimized Sustained-release tablets (Opt-VLD-SR) showed significantly lower Cmax±3.01ng/ml) than conventional IR tablets (256.17±8.02ng/ml). In the pharmacokinetic study, the MRT for Optimized-VLD-SR is (7.40h) showed a better result than the Vildagliptin IR marketed product (3.70 h.), which leads to higher bioavailability of Vildagliptin. \u0000Conclusion: Sustained release tablets of VLN with a combination of diffusion and erosion-controlled drug release mechanisms have been successfully developed.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"30 9","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139448643","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49422
Yenni Puspita Tanjung, M. Barliana, I. Joni, A. Chaerunisaa
Objective: This study aims to report the optimum formula for BSA nanoparticles cholecalciferol (BSA-NP cholecalciferol), which can increase the solubility of cholecalciferol.Methods: BSA cholecalciferol nanoparticles was prepared by desolvation method with variations in solvent/non-solvent ratio, BSA concentration, pH of BSA solution, and cholecalciferol concentration. For this purpose, particle size, polydispersity index, and zeta potential were measured. Furthermore, the solubility test of the best BSA-NPs cholecalciferol formula was carried out.Results: The most optimal BSA nanoparticle cholecalciferol characterization results have a particle size of 166.6±50.3 nm, a zeta potential of-32.1 mV, and a percentage encapsulation efficiency (%EE) for cholecalciferol of 82.9±0.72%. The solubility of BSA-NP cholecalciferol is four times higher than that of pure cholecalciferol.Conclusion: The optimum formula for BSA-NP cholecalciferol with a solvent/non-solvent ratio of 1/2, a concentration of BSA of 2.5%, a BSA solution pH 6, and a cholecalciferol concentration of 0.1% will increase the solubility of cholecalciferol by four times compared to pure cholecalciferol.
{"title":"IMPROVED SOLUBILITY OF CHOLECALCIFEROL AS BOVINE SERUM ALBUMIN (BSA) NANOPARTICLES","authors":"Yenni Puspita Tanjung, M. Barliana, I. Joni, A. Chaerunisaa","doi":"10.22159/ijap.2024v16i1.49422","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49422","url":null,"abstract":"Objective: This study aims to report the optimum formula for BSA nanoparticles cholecalciferol (BSA-NP cholecalciferol), which can increase the solubility of cholecalciferol.Methods: BSA cholecalciferol nanoparticles was prepared by desolvation method with variations in solvent/non-solvent ratio, BSA concentration, pH of BSA solution, and cholecalciferol concentration. For this purpose, particle size, polydispersity index, and zeta potential were measured. Furthermore, the solubility test of the best BSA-NPs cholecalciferol formula was carried out.Results: The most optimal BSA nanoparticle cholecalciferol characterization results have a particle size of 166.6±50.3 nm, a zeta potential of-32.1 mV, and a percentage encapsulation efficiency (%EE) for cholecalciferol of 82.9±0.72%. The solubility of BSA-NP cholecalciferol is four times higher than that of pure cholecalciferol.Conclusion: The optimum formula for BSA-NP cholecalciferol with a solvent/non-solvent ratio of 1/2, a concentration of BSA of 2.5%, a BSA solution pH 6, and a cholecalciferol concentration of 0.1% will increase the solubility of cholecalciferol by four times compared to pure cholecalciferol.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"65 32","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139449083","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 : 2024-01-07DOI: 10.22159/ijap.2024v16i1.49765
M. P., R. G. V.
Objective: The objective of the study was to evaluate the pharmacokinetic parameters of abacavir sulphate mucoadhesive buccal films in vivo. Methods: Abacavir sulphate mucoadhesive buccal films were developed using the solvent casting method and the prepared buccal films were evaluated for qualitative and quantitative parameters. Pharmacokinetic parameters (maximum plasma concentration [Cmax], maximum plasma concentration [Tmax], area under the curve [AUC], and biological half-life [t1/2]) were evaluated in vivo using healthy albino white rabbits. The blood samples were collected evaluated and the results were compared with Ziagen a reference standard. The Modern Version 6 software and the pharmacokinetic function (Microsoft Excel add-in) applications were used to conduct the statistical study. Results: The abacavir sulphate mucoadhesive buccal films were prepared successfully and the evaluated qualitative and quantitative parameters were within in the acceptable range. The results of the study stated that Cmax, Tmax, AUC0-t, AUC0-α, and t1/2 of abacavir sulphate mucoadhesive buccal film were found to be 93.86 ng/ml, 8 h, 1652.21 ng/ml×h, 2939.76 ng/ml×h, and 17.96 h, respectively. These results were comparable with the reference standard. Conclusion: The overall absorption of abacavir sulphate was more in the test formulation with respect to the reference product at the same dose. Hence the study concludes that abacavir sulphate mucoadhesive buccal films achieved prolonged muchoadhesion and improved bioavailability compared to the conventional formulation.
{"title":"DEVELOPMENT AND IN VIVO EVALUATION OF ABACAVIR SULPHATE MUCOADHESIVE BUCCAL FILMS","authors":"M. P., R. G. V.","doi":"10.22159/ijap.2024v16i1.49765","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i1.49765","url":null,"abstract":"Objective: The objective of the study was to evaluate the pharmacokinetic parameters of abacavir sulphate mucoadhesive buccal films in vivo.\u0000Methods: Abacavir sulphate mucoadhesive buccal films were developed using the solvent casting method and the prepared buccal films were evaluated for qualitative and quantitative parameters. Pharmacokinetic parameters (maximum plasma concentration [Cmax], maximum plasma concentration [Tmax], area under the curve [AUC], and biological half-life [t1/2]) were evaluated in vivo using healthy albino white rabbits. The blood samples were collected evaluated and the results were compared with Ziagen a reference standard. The Modern Version 6 software and the pharmacokinetic function (Microsoft Excel add-in) applications were used to conduct the statistical study.\u0000Results: The abacavir sulphate mucoadhesive buccal films were prepared successfully and the evaluated qualitative and quantitative parameters were within in the acceptable range. The results of the study stated that Cmax, Tmax, AUC0-t, AUC0-α, and t1/2 of abacavir sulphate mucoadhesive buccal film were found to be 93.86 ng/ml, 8 h, 1652.21 ng/ml×h, 2939.76 ng/ml×h, and 17.96 h, respectively. These results were comparable with the reference standard.\u0000Conclusion: The overall absorption of abacavir sulphate was more in the test formulation with respect to the reference product at the same dose. Hence the study concludes that abacavir sulphate mucoadhesive buccal films achieved prolonged muchoadhesion and improved bioavailability compared to the conventional formulation.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"67 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139449236","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：