International Journal of Applied Pharmaceutics最新文献

{"title":"DEVELOPMENT AND OPTIMIZATION OF SUPER SATURABLE SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM FOR DASATINIB BY DESIGN OF EXPERIMENT","authors":"C. Rajinikanth, K. Kathiresan","doi":"10.22159/ijap.2024v16i3.50434","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50434","url":null,"abstract":"Objective: In current research, Self-Nanoemulsifying Super Saturable Drug Delivery Systems S‑SNEDDS was formulated to attain superior drug dissolution and stability.\u0000Methods: Using saturated solubility, capryol ® 90, cremophor®-EL, and transcutol HP were used to make S-SNEDDS. Its composition was optimized using the ternary phase diagram. Using the central composite design of Response Surface Methodology, dasatinib-SNEDDS developed responses for droplet size (Y1), polydispersity index (Y2), and % drug released in 15 min (Y3). Various Precipitation Inhibitors were added to optimize SNEDDS (S3) to make S-SNEDDS and evaluate.\u0000Results: The optimum formulation was S3, with a particle size of 128 nm and zeta potential of-21 mV. Methylcellulose was shown better supersaturation than other inhibitors. The optimized formulation (F3) was more stable than ordinary SNEDDS due to its more significant zeta potential (-25 mV) and lower particle size (128 nm). Dasatinib was shown to be amorphous in S-SNEDDS using Differential Scanning Calorimetry and X-ray Powder Diffraction. F3 had a higher 90 min release rate (>99%) than pure drug dispersion (26%) and SNEDDS formulation (95%).\u0000Conclusion: The results concluded that S-SNEDDS formulation successfully enhanced the dissolution and stability of dasatinib.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"24 15","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141005948","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}

{"title":"EFFECT OF POLYMER CONCENTRATION AND SURFACTANTS ON PHYSICAL CHARACTERISTICS, DRUG RELEASE AND ANTIOXIDANT ACTIVITY OF GLUTATHIONE-KAPPA CARRAGEENAN NANOSPHERES","authors":"Yuyun Nailufa, Bambang Widjaja","doi":"10.22159/ijap.2024v16i3.49242","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.49242","url":null,"abstract":"Objective: Glutathione is one of the antioxidants widely used as an antiaging and skin lightener. Glutathione at a dose of 250 mg/d orally proved useful as an antiaging. At the same time, glutathione topical night cream is effective at a dose of 0.1% for the skin of Indonesian women. Glutathione is one of the antioxidants that has easily oxidized properties in storage. Research purpose to optimize the concentration of kappa carrageenan polymer and surfactan to obtain the optimal physical characteristics of nanosphere system analyzed based on size, PDI, yield, drug loading, entrapment efficiency, dissolution and antioxidant activity.\u0000Methods: The most commonly used method of making nanospheres is ionotropic gelation because it has proven effective, easy, and easy to apply. Ionotropic gelation is depend on the tendency of polyelectrolytes to cross connect to develop hydrogel beads often called gelispheres in the existence of counter ions. Nanospheres were prepared by aerosolization ionotropic gelation technique followed by freeze-drying. This method uses carrageenan polymers of 0.5% and 1.0% with the addition of surfactant as a stabilizer. Evaluation parameters are particle size, entrapment efficiency, drug loading, drug release and antioxidant activity.\u0000Results: The results of the nanospheres obtained were tested physically and drug activity. Nanospheres successfully formed, with size 382.67±52.24 nm, F2 325.20±4.62 nm, F3 495.39±30.61 nm, and F4 409.80±4.11 nm. The greater the polymer concentration, the greater the value of entrapment efficiency and drug content in the nanosphere. The morphology of the nanosphere is quite good, spherical, with a smooth surface. The release profile shows that glutathione release is quite good but takes a long time, namely F1 73.91±2.17%, F2 75.91±2.76%, F3 78.56±2.82%, and F4 79.56±1.34% in 480 min or 8 h. Antioxidant activity of glutathione-Kappa carrageenan nanospheres with the DPPH method showed that nanospheres have medium or medium category antioxidant activity.\u0000Conclusion: The most optimal formula is F4 with 1% kappa-carrageenan concentration and 0.6% KCl.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"10 S6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141003538","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}

{"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}

{"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}

{"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}

{"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}

{"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}

{"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}

{"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}

{"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}