Pub Date : 2024-05-07DOI: 10.22159/ijap.2024v16i3.50223
Ahmed Elgendy, Adeboye Adejare
Oral administration of drugs is highly preferred for almost all human beings than any other route of drug delivery except during some health challenges. Therefore, permeability assessment of drugs across intestinal membrane is essential in the early stages of drug discovery for time and cost reasons. Animals, including humans, have been used for decades as in vivo models for determining intestinal drug permeability and absorption. However, in vivo models are very invasive, time-consuming, and not cost-effective methods. Numerous in vitro models have been used to screen drug permeability and absorption through intestinal membranes. In this article partitioning based physicochemical models that can predict a compound/drug permeability potential across intestinal membrane will be elaborated upon.
{"title":"PARTITIONING BASED PHYSICOCHEMICAL MODELS FOR ASSESSING INTESTINAL PERMEABILITY AND ABSORPTION OF DRUGS","authors":"Ahmed Elgendy, Adeboye Adejare","doi":"10.22159/ijap.2024v16i3.50223","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50223","url":null,"abstract":"Oral administration of drugs is highly preferred for almost all human beings than any other route of drug delivery except during some health challenges. Therefore, permeability assessment of drugs across intestinal membrane is essential in the early stages of drug discovery for time and cost reasons. Animals, including humans, have been used for decades as in vivo models for determining intestinal drug permeability and absorption. However, in vivo models are very invasive, time-consuming, and not cost-effective methods. Numerous in vitro models have been used to screen drug permeability and absorption through intestinal membranes. In this article partitioning based physicochemical models that can predict a compound/drug permeability potential across intestinal membrane will be elaborated upon.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"28 S87","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003789","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.48787
Meghana Raykar, M. Velraj
Objective: Tofacitinib citrate is a commonly used therapeutic agent for various diseases. Mouth-dissolving formulations provide potential benefits for patient compliance. This study aims to evaluate the acute oral toxicity of tofacitinib citrate in these formulations to ensure their safety and efficacy. Methods: This study aimed to assess the acute oral toxicity of tofacitinib citrate in mouth-dissolving formulations and evaluate its effects on food and water consumption, hematological and biochemical parameters, and organ histopathology. Male and female Wistar rats were divided into four groups. The control group received distilled water, while the treated groups were orally administered tofacitinib citrate at 5 mg/kg, 100 mg/kg, and 300 mg/kg. Observations were made over 14 d, assessing general appearance, behavior, food and water consumption, and mortality. Hematological and biochemical analyses and histopathological examinations were conducted on vital organs. Results: In acute toxicity studies, Wistar rats showed no toxicity at up to 300 mg/kg tofacitinib citrate. Compared to controls, food/water intake and hematological, biochemical, and histopathological parameters of major organs remained unchanged, indicating no systemic effects and affirming the compound's safety in mouth-dissolving formulations. Conclusion: Tofacitinib citrate in mouth-dissolving formulations demonstrated a favorable safety profile with no acute oral toxicity. Normal consumption, unchanged parameters, and no organ abnormalities support its safety. Further investigation is required to assess chronic toxicity and long-term safety.
{"title":"ACUTE ORAL TOXICITY OF TOFACITINIB CITRATE IN WISTAR RATS: IMPLICATIONS FOR NOVEL MOUTH DISSOLVING FORMULATIONS","authors":"Meghana Raykar, M. Velraj","doi":"10.22159/ijap.2024v16i3.48787","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.48787","url":null,"abstract":"Objective: Tofacitinib citrate is a commonly used therapeutic agent for various diseases. Mouth-dissolving formulations provide potential benefits for patient compliance. This study aims to evaluate the acute oral toxicity of tofacitinib citrate in these formulations to ensure their safety and efficacy.\u0000Methods: This study aimed to assess the acute oral toxicity of tofacitinib citrate in mouth-dissolving formulations and evaluate its effects on food and water consumption, hematological and biochemical parameters, and organ histopathology. Male and female Wistar rats were divided into four groups. The control group received distilled water, while the treated groups were orally administered tofacitinib citrate at 5 mg/kg, 100 mg/kg, and 300 mg/kg. Observations were made over 14 d, assessing general appearance, behavior, food and water consumption, and mortality. Hematological and biochemical analyses and histopathological examinations were conducted on vital organs.\u0000Results: In acute toxicity studies, Wistar rats showed no toxicity at up to 300 mg/kg tofacitinib citrate. Compared to controls, food/water intake and hematological, biochemical, and histopathological parameters of major organs remained unchanged, indicating no systemic effects and affirming the compound's safety in mouth-dissolving formulations.\u0000Conclusion: Tofacitinib citrate in mouth-dissolving formulations demonstrated a favorable safety profile with no acute oral toxicity. Normal consumption, unchanged parameters, and no organ abnormalities support its safety. Further investigation is required to assess chronic toxicity and long-term safety.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"91 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141002889","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.50412
D. Saritha, P. S. CHANDRA BOSE, R. Osmani, Padmini Iriventi, S. Kanna, Gundawar Ravi
Objective: The main aim of the present study was to improve the dissolution rate of Haloperidol nanocrystals and thereby increase their bioavailability. Haloperidol is a typical antipsychotic drug and it is used to treat schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Haloperidol falls into the Biopharmaceutics Classification System (BCS-II) class of drugs (poorly soluble aqueous and highly permeable) and has poor bioavailability. Methods: The present study involves the preparation and optimization of Haloperidol nanocrystals by the anti-solvent precipitation method using Polaxomer407 and polyvinyl pyrrolidone K30 (PVP K30). The prepared nanocrystals were evaluated for various parameters like particle size, zeta potential, % drug content, % yield, surface morphology, drug-excipient compatibility studies (Fourier-transform infrared spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)), and in vitro dissolution studies. Results: Nine preparations were done and the best preparation amongst them was selected for further studies. F7 preparation containingpolaxomer407 and PVP K30 was selected as optimized preparation based on their evaluation parameters. 32 factorial design was used in the preparation. The particle size of the F7 nanocrystals was 300.2±2.7 nm and the zeta potential-36.3±3.2 mV. The % yield was in the range of 63.62±0.3%-98.21±0.8 %. The drug content of various preparations was found to be in the range of 58.46±0.8%-93.54±0.5 %. In vitro dissolution studies showed the highest % drug release for F7(91.54±0.03%) in 10 h. Conclusion: F7 preparation was found to be having acceptable characteristics and thus selected as optimized preparation.
{"title":"DEVELOPMENT, OPTIMIZATION AND IN VITRO CHARACTERIZATION OF HALOPERIDOL NANOCRYSTALS USING 32 FACTORIAL DESIGN","authors":"D. Saritha, P. S. CHANDRA BOSE, R. Osmani, Padmini Iriventi, S. Kanna, Gundawar Ravi","doi":"10.22159/ijap.2024v16i3.50412","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50412","url":null,"abstract":"Objective: The main aim of the present study was to improve the dissolution rate of Haloperidol nanocrystals and thereby increase their bioavailability. Haloperidol is a typical antipsychotic drug and it is used to treat schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Haloperidol falls into the Biopharmaceutics Classification System (BCS-II) class of drugs (poorly soluble aqueous and highly permeable) and has poor bioavailability.\u0000Methods: The present study involves the preparation and optimization of Haloperidol nanocrystals by the anti-solvent precipitation method using Polaxomer407 and polyvinyl pyrrolidone K30 (PVP K30). The prepared nanocrystals were evaluated for various parameters like particle size, zeta potential, % drug content, % yield, surface morphology, drug-excipient compatibility studies (Fourier-transform infrared spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)), and in vitro dissolution studies.\u0000Results: Nine preparations were done and the best preparation amongst them was selected for further studies. F7 preparation containingpolaxomer407 and PVP K30 was selected as optimized preparation based on their evaluation parameters. 32 factorial design was used in the preparation. The particle size of the F7 nanocrystals was 300.2±2.7 nm and the zeta potential-36.3±3.2 mV. The % yield was in the range of 63.62±0.3%-98.21±0.8 %. The drug content of various preparations was found to be in the range of 58.46±0.8%-93.54±0.5 %. In vitro dissolution studies showed the highest % drug release for F7(91.54±0.03%) in 10 h.\u0000Conclusion: F7 preparation was found to be having acceptable characteristics and thus selected as optimized preparation.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"156 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141001756","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.50320
Yadla Pavani, S. Aravind, Charitha Annam, Mannam SUBBA RAO
Objective: A seven-day regimen consisting of vonoprazan (VNP), amoxicillin (AXC) and clarithromycin (CRC), administered twice daily, has been permitted and reimbursed by health coverage as initial therapy. No technique has been implemented yet to determine the quantities of VNP, AXC, and CRC combination. This work effectively aimed at estimating these medications (VNP, AXC, and CRC) at the same time by developing an HPLC technique that saves money and time. Methods: The VNP, AXC, and CRC were separated in a “Waters” column (C18 nature; 250 mm sized length; 4.6 mm sized internal diameter; 5 µm sized particle; 25 °C temperature). Phosphoric acid (0.1% in water; pH 4.2) and absolute methanol (50:50, v/v) comprise the mobile phase. The drug product, Voqueznatripak, was subjected to hydrolysis, oxidation, photolysis, and thermal stressors with the intent to cause enforced degradation. The suggested "HPLC conditions" were verified in compliance with ICH guidance. Results: The measurements had a linear range of 10–20 µg/ml for VNP and 250–750 µg/ml for AXC and CRC. The AXC, CRC, and VNP had LOQ’s 5.302 µg/ml, 5.487 µg/ml and 0.523 µg/ml, respectively. Precision measurements were<0.2% RSD and accuracy ranges were 99.40% to 101.46%. The newly devised “HPLC conditions” specificity attribute and stability-indicating quality were also validated by forced degradation tests. Conclusion: The newly devised “HPLC conditions” for analysing AXC, CRC, and VNP in formulation dosage form and stability samples might be adapted by quality control laboratories. The devised “HPLC conditions” is qualified and consistent to reveal and detect any probable change in the drug product assessments throughout stability experiments.
{"title":"QUANTIFICATION AND QUALITY CONTROL OF TRIPLE-DRUG COMBINATION EMPLOYED FOR GASTRIC ULCER USING STABILITY-INDICATING SELECTIVE RP-HPLC TECHNIQUE","authors":"Yadla Pavani, S. Aravind, Charitha Annam, Mannam SUBBA RAO","doi":"10.22159/ijap.2024v16i3.50320","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50320","url":null,"abstract":"Objective: A seven-day regimen consisting of vonoprazan (VNP), amoxicillin (AXC) and clarithromycin (CRC), administered twice daily, has been permitted and reimbursed by health coverage as initial therapy. No technique has been implemented yet to determine the quantities of VNP, AXC, and CRC combination. This work effectively aimed at estimating these medications (VNP, AXC, and CRC) at the same time by developing an HPLC technique that saves money and time.\u0000Methods: The VNP, AXC, and CRC were separated in a “Waters” column (C18 nature; 250 mm sized length; 4.6 mm sized internal diameter; 5 µm sized particle; 25 °C temperature). Phosphoric acid (0.1% in water; pH 4.2) and absolute methanol (50:50, v/v) comprise the mobile phase. The drug product, Voqueznatripak, was subjected to hydrolysis, oxidation, photolysis, and thermal stressors with the intent to cause enforced degradation. The suggested \"HPLC conditions\" were verified in compliance with ICH guidance.\u0000Results: The measurements had a linear range of 10–20 µg/ml for VNP and 250–750 µg/ml for AXC and CRC. The AXC, CRC, and VNP had LOQ’s 5.302 µg/ml, 5.487 µg/ml and 0.523 µg/ml, respectively. Precision measurements were<0.2% RSD and accuracy ranges were 99.40% to 101.46%. The newly devised “HPLC conditions” specificity attribute and stability-indicating quality were also validated by forced degradation tests.\u0000Conclusion: The newly devised “HPLC conditions” for analysing AXC, CRC, and VNP in formulation dosage form and stability samples might be adapted by quality control laboratories. The devised “HPLC conditions” is qualified and consistent to reveal and detect any probable change in the drug product assessments throughout stability experiments.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"8 36","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004428","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.49937
D. N B, B. E. O., A. M. N., M. A. G., P. M. V., R. O. V., B. A. I., K. I I
In the perspective of the pharmaceutical industry development, manufacturers expand their product portfolios by updating generic drugs. Complex Generics (CG) or Nonbiological Generic Drugs (NBGD) contain known pharmaceutical substances are out of patent protection and are made by using new technologies, excipients, nanocarriers, dosage form modernization, etc. These drugs are developed in the patients’ interests to improve their life quality and increase drugs’ efficacy and safety. The article discusses the categories and characteristics of CG, shows examples available on the pharmaceutical market, API and dosage forms. This article discusses approaches to quality control that pose challenges for developers and regulators. The fundamental importance of the innovative drugs manufacturing process and the ingredients standardization in the dosage forms formulations to create the standard product are indicated. First, a comprehensive control of polymers is required as an important tool to make the necessary pharmacokinetics. The influence degree on the API release and the effectiveness of dosage form (DF) depends on the polymer’s physicochemical characteristics. In this regard, it is important to create databases of these excipients accessible to developers containing information about properties, use, dosages and safety. In view of the complexity structure and manufacturing processes of the NBGD and insufficiency of pharmacopeial requirements for standard approaches for resolving issues of comparability and bioequivalence the current regulatory documents should be expanded and revise for a correct quality assessment. There is a need to create new scientific and regulatory roadmaps for the development and approval of complex generic drugs.
{"title":"COMPLEX GENERICS AS A TREND OF MODERN PHARMACEUTICAL DEVELOPMENT","authors":"D. N B, B. E. O., A. M. N., M. A. G., P. M. V., R. O. V., B. A. I., K. I I","doi":"10.22159/ijap.2024v16i3.49937","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.49937","url":null,"abstract":"In the perspective of the pharmaceutical industry development, manufacturers expand their product portfolios by updating generic drugs. Complex Generics (CG) or Nonbiological Generic Drugs (NBGD) contain known pharmaceutical substances are out of patent protection and are made by using new technologies, excipients, nanocarriers, dosage form modernization, etc. These drugs are developed in the patients’ interests to improve their life quality and increase drugs’ efficacy and safety.\u0000The article discusses the categories and characteristics of CG, shows examples available on the pharmaceutical market, API and dosage forms. This article discusses approaches to quality control that pose challenges for developers and regulators. The fundamental importance of the innovative drugs manufacturing process and the ingredients standardization in the dosage forms formulations to create the standard product are indicated. First, a comprehensive control of polymers is required as an important tool to make the necessary pharmacokinetics. The influence degree on the API release and the effectiveness of dosage form (DF) depends on the polymer’s physicochemical characteristics. In this regard, it is important to create databases of these excipients accessible to developers containing information about properties, use, dosages and safety.\u0000In view of the complexity structure and manufacturing processes of the NBGD and insufficiency of pharmacopeial requirements for standard approaches for resolving issues of comparability and bioequivalence the current regulatory documents should be expanded and revise for a correct quality assessment. There is a need to create new scientific and regulatory roadmaps for the development and approval of complex generic drugs.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"116 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141002723","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.49491
Asha Eluru, K. S. Babu
Objective: This investigation demonstrates a stability-indicating and reliable “reverse-phase ultra-performance liquid chromatography” method to simultaneously quantify timolol maleate and dorzolamide HCl in the pharmaceutical dosage form. Methods: Successful separation was accomplished using Phenyl column (100 mm x 2.1 mm, 1.7μm) with isocratic type of elution using mobile phase containing Acetonitrile+Ammonium Formate buffer (30:70), respectively with 0.2 ml/min flow rate. The wavelength sensor was attuned at 266 nm to quantify timolol maleate and dorzolamide HCl. Results: Dorzolamide HCl and timolol maleate peaks were eluted with fine resolution at retention times 0.7 min and 1.5 min, respectively. In the 55.75-334.5 μg/ml and 6.25-37.5 μg/ml concentration ranges for dorzolamide HCl and timolol maleate, the calibration graphs were linear, with regression coefficients of 0.99997 and 0.99991, respectively. The suggested ultra-performance liquid chromatography approach has been shown as sensitive, precise, robust, accurate, specific and stability, indicating through the resolution of dorzolamide HCl and timolol maleate from its degradation-based compounds. Conclusion: The established ultra-performance liquid chromatography technique was effectively extended to the evaluation of dorzolamide HCl and timolol Maleate in the pharmaceutical dosage form and the test results appeared satisfactory.
{"title":"A NEW RP-UPLC METHOD FOR THE SEPARATION AND SIMULTANEOUS QUANTIFICATION OF DORZOLAMIDE HCl AND TIMOLOL MALEATE","authors":"Asha Eluru, K. S. Babu","doi":"10.22159/ijap.2024v16i3.49491","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.49491","url":null,"abstract":"Objective: This investigation demonstrates a stability-indicating and reliable “reverse-phase ultra-performance liquid chromatography” method to simultaneously quantify timolol maleate and dorzolamide HCl in the pharmaceutical dosage form.\u0000Methods: Successful separation was accomplished using Phenyl column (100 mm x 2.1 mm, 1.7μm) with isocratic type of elution using mobile phase containing Acetonitrile+Ammonium Formate buffer (30:70), respectively with 0.2 ml/min flow rate. The wavelength sensor was attuned at 266 nm to quantify timolol maleate and dorzolamide HCl.\u0000Results: Dorzolamide HCl and timolol maleate peaks were eluted with fine resolution at retention times 0.7 min and 1.5 min, respectively. In the 55.75-334.5 μg/ml and 6.25-37.5 μg/ml concentration ranges for dorzolamide HCl and timolol maleate, the calibration graphs were linear, with regression coefficients of 0.99997 and 0.99991, respectively. The suggested ultra-performance liquid chromatography approach has been shown as sensitive, precise, robust, accurate, specific and stability, indicating through the resolution of dorzolamide HCl and timolol maleate from its degradation-based compounds.\u0000Conclusion: The established ultra-performance liquid chromatography technique was effectively extended to the evaluation of dorzolamide HCl and timolol Maleate in the pharmaceutical dosage form and the test results appeared satisfactory.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"4 18","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004536","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.49550
Novi Nurleni, Arie Firdiawan, Agnes Rendowaty, Resti Kurniasari
Objective: Current research work aimed to develop a formulation of red ginger into a stable soap preparation, effective as an antibacterial and safe for long-term use. Methods: The maceration method was used to extract red ginger rhizome. In the formulation, there are variations in the concentration of the extract, where Formulation I (FI) 3%, Formulation II (FII) 5%, Formulation III (FIII) 7%, and Formulation IV (FIV) 0%. The evaluation of the preparation includes tests such as sensory evaluation, homogeneity, pH, viscosity and flow properties, density, foam height, and stability, as well as antibacterial activity using the agar diffusion method against Staphylococcus aureus ATCC 25932 and Escherichia coli ATCC 25922. Results: The percentage of extract yield obtained was 2.38%. All three formulations of soap have shown good stability during the 28-day evaluation (significant>0.05), indicating no significant changes during storage, and the inhibitory power of Staphylococcus aureus ATCC 25923 bacteria in the three successive formulations was 9.03±0.4; 12.21±0.3; 15.26±0.4 (mm) respectively, while that of Escherichia coli ATCC 25922 was 6.01±0.6; 10.32±0.4; 12.58±0.6 (mm). Conclusion: The evaluation results, all formulations have good stability during storage. The variation in concentration of red ginger extract will affect the inhibitory power against test bacteria. F III, with an extract content of 7% has better antibacterial activity compared to other formulations.
目的：目前的研究工作旨在将红姜制成一种稳定的肥皂制剂：目前的研究工作旨在将红姜配制成一种稳定的肥皂制剂，作为抗菌剂有效且可长期安全使用：方法：采用浸渍法提取红姜根茎。在配方中，提取物的浓度各不相同，其中配方 I (FI) 为 3%，配方 II (FII) 为 5%，配方 III (FIII) 为 7%，配方 IV (FIV) 为 0%。制剂的评估包括感官评估、均匀性、pH 值、粘度和流动性、密度、泡沫高度和稳定性等测试，以及采用琼脂扩散法对金黄色葡萄球菌 ATCC 25932 和大肠杆菌 ATCC 25922 的抗菌活性测试：萃取率为 2.38%。在 28 天的评价中，三种肥皂配方均表现出良好的稳定性（显著性>0.05），表明在贮藏期间没有发生显著变化，三种连续配方对金黄色葡萄球菌 ATCC 25923 的抑菌力分别为 9.对大肠杆菌 ATCC 25922 的抑菌力分别为 6.01±0.6；10.32±0.4；12.58±0.6（mm）：评价结果表明，所有配方在储存期间都具有良好的稳定性。红姜提取物浓度的变化会影响对试验细菌的抑制能力。与其他配方相比，提取物含量为 7% 的 F III 具有更好的抗菌活性。
{"title":"FORMULATION AND EVALUATION OF RED GINGER RHIZOME EXTRACT SOAP AS AN ANTIBACTERIAL","authors":"Novi Nurleni, Arie Firdiawan, Agnes Rendowaty, Resti Kurniasari","doi":"10.22159/ijap.2024v16i3.49550","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.49550","url":null,"abstract":"Objective: Current research work aimed to develop a formulation of red ginger into a stable soap preparation, effective as an antibacterial and safe for long-term use.\u0000Methods: The maceration method was used to extract red ginger rhizome. In the formulation, there are variations in the concentration of the extract, where Formulation I (FI) 3%, Formulation II (FII) 5%, Formulation III (FIII) 7%, and Formulation IV (FIV) 0%. The evaluation of the preparation includes tests such as sensory evaluation, homogeneity, pH, viscosity and flow properties, density, foam height, and stability, as well as antibacterial activity using the agar diffusion method against Staphylococcus aureus ATCC 25932 and Escherichia coli ATCC 25922.\u0000Results: The percentage of extract yield obtained was 2.38%. All three formulations of soap have shown good stability during the 28-day evaluation (significant>0.05), indicating no significant changes during storage, and the inhibitory power of Staphylococcus aureus ATCC 25923 bacteria in the three successive formulations was 9.03±0.4; 12.21±0.3; 15.26±0.4 (mm) respectively, while that of Escherichia coli ATCC 25922 was 6.01±0.6; 10.32±0.4; 12.58±0.6 (mm).\u0000Conclusion: The evaluation results, all formulations have good stability during storage. The variation in concentration of red ginger extract will affect the inhibitory power against test bacteria. F III, with an extract content of 7% has better antibacterial activity compared to other formulations.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"127 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141002007","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.50267
Sanjay Dinkar Sawant, Shital Digambar Godse
Mirabegron is a beta-3 adrenergic receptor agonist and is specified for the treatment of overactive Bladder. This review covers analytical methods aimed at the identification and quantification of mirabegron in bulk, commercial dosage forms, and Biological fluids. Using various techniques such as UV-spectroscopy, spectro-fluorimetry, planer chromatography, High Performance-Thin Layer Chromatography (HPTLC), HPLC, High-Performance Liquid Chromatography-MS/MS (HPLC-MS/MS), Ultra-Pressure Liquid Chromatography-MS/MS (UPLC-MS/MS), and capillary electrophoresis. HPLC is the most used analytical technique for the identification and quantification of mirabegron in bulk and commercial dosage forms.
{"title":"ANALYTICAL TECHNIQUES FOR DETERMINATION OF MIRABEGRON FROM BULK, PHARMACEUTICAL FORMULATION, AND BIOLOGICAL MATRICES: A CRITICAL REVIEW","authors":"Sanjay Dinkar Sawant, Shital Digambar Godse","doi":"10.22159/ijap.2024v16i3.50267","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50267","url":null,"abstract":"Mirabegron is a beta-3 adrenergic receptor agonist and is specified for the treatment of overactive Bladder. This review covers analytical methods aimed at the identification and quantification of mirabegron in bulk, commercial dosage forms, and Biological fluids. Using various techniques such as UV-spectroscopy, spectro-fluorimetry, planer chromatography, High Performance-Thin Layer Chromatography (HPTLC), HPLC, High-Performance Liquid Chromatography-MS/MS (HPLC-MS/MS), Ultra-Pressure Liquid Chromatography-MS/MS (UPLC-MS/MS), and capillary electrophoresis. HPLC is the most used analytical technique for the identification and quantification of mirabegron in bulk and commercial dosage forms.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"170 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141001953","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.50043
Nabila Apriliani, L. Laila, B. Prasetyo
Objective: The aim of this study was to formulate an oral thin film strip (OTFS) contained the red dragon fruit peel (RDFP) ethanol extract (Hylocereus polyrhizus) and evaluate the characteristic, stability and antibacterial activity against Streptococcus mutans (S. mutans). Methods: The film was made using the solvent casting method by adding a variety of concentration ethanol extract of red dragon fruit peel (5%, 10%, and 15%). The films were evaluated in organoleptic test, weight, thickness, pH, disintegration time, folding endurance, stability test and antibacterial activity. Results: The results showed that the film provided a distinctive color, aroma, and taste of the extract. The result of film evaluation had weight between 0.07-0.21 g, thickness between 0.10-0.20 mm, pH between 5.70-5.99, disintegration time between 34.99-49.13 s, and folding endurance between 321.00-812.83 times. The films were stable for 2 mo at a variety storage temperature (4±2 ℃, 28±2 ℃, and 40±2 ℃). The films showed antibacterial activity for 5%, 10% and 15% with the diameter of inhibition 8.5 mm, 10.8 mm, and 12.9 mm, respectively. Conclusion: Ethanol extract of RDFP can be utilized as a mouth freshener film that is stable for 2 mo and has antibacterial activity against S. mutans.
{"title":"UTILIZATION RED DRAGON FRUIT PEEL (HYLOCEREUS POLYRHIZUS) ETHANOL EXTRACT IN ORAL THIN FILM STRIP AS A MOUTH FRESHENER","authors":"Nabila Apriliani, L. Laila, B. Prasetyo","doi":"10.22159/ijap.2024v16i3.50043","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50043","url":null,"abstract":"Objective: The aim of this study was to formulate an oral thin film strip (OTFS) contained the red dragon fruit peel (RDFP) ethanol extract (Hylocereus polyrhizus) and evaluate the characteristic, stability and antibacterial activity against Streptococcus mutans (S. mutans).\u0000Methods: The film was made using the solvent casting method by adding a variety of concentration ethanol extract of red dragon fruit peel (5%, 10%, and 15%). The films were evaluated in organoleptic test, weight, thickness, pH, disintegration time, folding endurance, stability test and antibacterial activity.\u0000Results: The results showed that the film provided a distinctive color, aroma, and taste of the extract. The result of film evaluation had weight between 0.07-0.21 g, thickness between 0.10-0.20 mm, pH between 5.70-5.99, disintegration time between 34.99-49.13 s, and folding endurance between 321.00-812.83 times. The films were stable for 2 mo at a variety storage temperature (4±2 ℃, 28±2 ℃, and 40±2 ℃). The films showed antibacterial activity for 5%, 10% and 15% with the diameter of inhibition 8.5 mm, 10.8 mm, and 12.9 mm, respectively.\u0000Conclusion: Ethanol extract of RDFP can be utilized as a mouth freshener film that is stable for 2 mo and has antibacterial activity against S. mutans.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"10 27","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004778","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 : 2024-05-07DOI: 10.22159/ijap.2024v16i3.50220
Aulia UL HAFIZAH, Purwantiningsih Sugita, Mohammad Khotib, Umi Cahyaningsih, Siti Sadiah
Objective: This study aimed to develop, characterize, and conduct stability evaluations to ensure compliance with intravenous administration for microemulsion ibuprofen injection. In addition, hematology assessment and profile of drug release kinetics were analyzed. Methods: The formulation process commenced by introducing various chitosan concentrations into microemulsion ibuprofen injection, following a method established in a previous study. Formulation parameters studied include particle size, polydispersity index (PDI), zeta potential, kinetic of drug release, anti-inflammation activity using the 1% carrageenin induction method, and hematology assessment. Results: The results showed that the addition of 1% chitosan solution allowed for the development of the ideal microemulsion formula, with droplet size, zeta potential, and PDI of 19.37±0.32 nm,-1.53±0.12 mV, and 0.38±0.02, respectively. Kinetics of chitosan-coated ibuprofen microemulsion (MK) were governed by the squared root of time paradigm, suggesting that drug release proceeded by diffusion and was influenced by the carrier. Compared to the other groups, the paw injected with MK indicated a strong anti-inflammatory effect and did not differ significantly from the control group (p>0.05). However, Hematology analysis showed no statistically significant variations in leukocyte and erythrocyte profiles between the treatment and control groups (p>0.05). Conclusion: MK met the criteria as an intravenous preparation based on the characteristics and safety.
{"title":"IBUPROFEN INJECTABLE MICROEMULSION PREPARATION COATED BY CHITOSAN: FORMULATION, CHARACTERIZATION, IN VITRO PERFORMANCE, ANTI-INFLAMMATION ACTIVITY, AND HEMATOLOGY ASSESSMENT","authors":"Aulia UL HAFIZAH, Purwantiningsih Sugita, Mohammad Khotib, Umi Cahyaningsih, Siti Sadiah","doi":"10.22159/ijap.2024v16i3.50220","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50220","url":null,"abstract":"Objective: This study aimed to develop, characterize, and conduct stability evaluations to ensure compliance with intravenous administration for microemulsion ibuprofen injection. In addition, hematology assessment and profile of drug release kinetics were analyzed.\u0000Methods: The formulation process commenced by introducing various chitosan concentrations into microemulsion ibuprofen injection, following a method established in a previous study. Formulation parameters studied include particle size, polydispersity index (PDI), zeta potential, kinetic of drug release, anti-inflammation activity using the 1% carrageenin induction method, and hematology assessment.\u0000Results: The results showed that the addition of 1% chitosan solution allowed for the development of the ideal microemulsion formula, with droplet size, zeta potential, and PDI of 19.37±0.32 nm,-1.53±0.12 mV, and 0.38±0.02, respectively. Kinetics of chitosan-coated ibuprofen microemulsion (MK) were governed by the squared root of time paradigm, suggesting that drug release proceeded by diffusion and was influenced by the carrier. Compared to the other groups, the paw injected with MK indicated a strong anti-inflammatory effect and did not differ significantly from the control group (p>0.05). However, Hematology analysis showed no statistically significant variations in leukocyte and erythrocyte profiles between the treatment and control groups (p>0.05).\u0000Conclusion: MK met the criteria as an intravenous preparation based on the characteristics and safety.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"23 38","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004791","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}
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