Drug Development and Industrial Pharmacy最新文献

{"title":"Stability-indicating green HPLC method for fixed-dose tablets containing remogliflozin etabonate and teneligliptin: an AQbD approach.","authors":"Raj Patel, Rajendra Kotadiya","doi":"10.1080/03639045.2024.2400199","DOIUrl":"10.1080/03639045.2024.2400199","url":null,"abstract":"<p><strong>Background: </strong>In June 2021, the Central Drug Standards Control Organization approved a fixed-dose combination tablet containing remogliflozin etabonate (100 mg) and teneligliptin (10 mg) to manage type II diabetes.</p><p><strong>Objective: </strong>This study aims to develop a stability-indicating RP-HPLC method for quantifying remogliflozin etabonate and teneligliptin in tablet formulations <i>via</i> analytical quality by design (AQbD) principles.</p><p><strong>Methods: </strong>Risk assessment, Plackett-Burman design, and central composite design were employed to understand the impact of independent variables on critical analytical attributes. The stationary phase was a HyperClone BDS C18 column, and the mobile phase consisted of acetonitrile and phosphate buffer (20 mM, pH 5) at a 45:55% (v/v) ratio.</p><p><strong>Results: </strong>The method, validated per ICH Q2 (R1), resulted in retention times of 3.395 and 12.308 min for teneligliptin and remogliflozin etabonate, respectively. Forced degradation studies confirmed robustness, with clear peak separation and no interference from degradation products. The AGREE score of 0.65 supports its green applicability for tablet analysis in quality control.</p><p><strong>Conclusion: </strong>The AQbD-assisted RP-HPLC method developed in this study offers environmental friendliness, efficient separation with well-defined peaks, and simple mobile phase combination.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"750-762"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142125131","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanocrystal formulations of mebendazole employing quality by design and molecular level insights by atomistic simulations.","authors":"Elisavet Vardaka, Kyriakos Kachrimanis","doi":"10.1080/03639045.2024.2398597","DOIUrl":"10.1080/03639045.2024.2398597","url":null,"abstract":"<p><strong>Objective: </strong>The present study investigates the production of mebendazole nanocrystal formulations by wet media milling.</p><p><strong>Significance: </strong>Nanocrystal formulations are expected to enhance the dissolution properties of mebendazole, which possesses poor solubility, highly dependent on crystal polymorphism.</p><p><strong>Methods: </strong>A Box-Behnken design was employed to study the effects of formulation and process variables on the nanocrystal size and ζ-potential. The optimal nanosuspensions were solidified by spay-drying and freeze-drying with and without mannitol, and the effects of the drying method on the reconstitution of the nanosuspension was studied. Additionally, their physicochemical properties were determined, while the mechanism of fracture and stabilizer adsorption were investigated by atomistic simulations.</p><p><strong>Results: </strong>Poloxamer 407 is the most suitable stabilizer, while the bead size, milling speed, and stabilizer content significantly affect the diameter. The ζ-potential is affected by the stabilizer concentration depending on bead size. Energy-vector diagrams revealed a slip plane in the lattice of form C, while molecular dynamics simulations revealed strong interactions between stabilizer and crystal surface. Both drying processes induce polymorphic transformation to form A, which, however, can be partially prevented by the addition of mannitol in freeze-drying, at the expense of suspension redispersibility. The spray-dried nanosuspensions exhibited substantially enhanced dissolution profile compared to neat mebendazole, probably due to reduction of particle size, despite transformation to the unfavorable form A.</p><p><strong>Conclusions: </strong>Nanocrystal formulations exhibited significant dissolution enhancement, while experimental design and atomistic simulations provided useful insights into the mechanism of their formation and stability.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"735-749"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105394","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Industrial manufacturing method and characterization of Ayurvedic marine drugs: mother pearl, cowry, coral and pearl.","authors":"Sandeep Chavan, Sushama Bhuvad, Vidya Gupta, Vineeta Deshmukh, Sadanand Sardeshmukh","doi":"10.1080/03639045.2024.2396902","DOIUrl":"10.1080/03639045.2024.2396902","url":null,"abstract":"<p><strong>Introduction: </strong>Ayurvedic marine drugs derived from mollusc shells and coral are regularly used by Ayurvedic physicians to treat several disease conditions like acid peptic disease, irritable bowel syndrome, osteoporosis, etc. However, standard operating procedures for manufacturing these drugs and their complete characterization have not been published in the Ayurvedic Formulary and Ayurvedic Pharmacopeia of India to date.</p><p><strong>Methods: </strong>Present study describes the traditional manufacturing process and thorough characterization using classical and advanced analytical tools. The raw materials characters, in-process parameters, and finished product specifications have been elaborated to develop monographs. Especially, the identity and purity of raw coral and pearl were checked by Raman Spectroscopy and Energy Dispersive X-ray Fluorescence analysis.</p><p><strong>Results: </strong>In the finished product analysis, the X-Ray Diffraction study revealed that incineration after trituration with <i>Aloe barbadensis</i> leaf pulp or rose water converted the aragonite phase of calcium carbonate into calcite phase in mother pearl, cowry, and pearl while the calcite form of raw coral was retained. The prominent bands around 1390, 870, and 712 cm^-1 detected by Fourier Transform-Infrared Spectroscopy and mass loss between 39-44% (w/w) revealed by thermogravimetric analysis confirmed the carbonate form of these calcium-based drugs. The finished products were very fine grayish-white powders constituted by irregularly shaped nano-micro particulate calcium carbonate exhibiting particle size between 600 nm (D10 value) to 1.2 µm (D90 value).</p><p><strong>Conclusion: </strong>The quality control and assurance achieved in this study may be further utilized by the pharmaceutical industries to manufacture quality marine drugs and conduct efficacy studies.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"721-734"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142105393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Correction.","authors":"","doi":"10.1080/03639045.2024.2406315","DOIUrl":"10.1080/03639045.2024.2406315","url":null,"abstract":"","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"i"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142281918","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Correction.","authors":"","doi":"10.1080/03639045.2024.2416335","DOIUrl":"10.1080/03639045.2024.2416335","url":null,"abstract":"","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"776"},"PeriodicalIF":2.4,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142496930","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Modeling moisture change of packaged dry tablet dosage forms under consumer use condition.","authors":"Duck Soon An, Dong Sun Lee","doi":"10.1080/03639045.2024.2382415","DOIUrl":"10.1080/03639045.2024.2382415","url":null,"abstract":"<p><p>A simple mathematical model based on product's moisture sorption isotherm and package's moisture transmission was developed to predict moisture content of dry solid tablets during consumers' use, which is useful for determination of in-use shelf life (ISL) or secondary shelf life. The moisture increase depending on amount of product remaining in the package was accounted for in the mass balance equation on the package. The model was first verified by literature data of desiccant canisters in a plastic bottle of high density polyethylene exposed to two environmental conditions (25 °C and 60% relative humidity (RH); 40 °C and 75% RH) simulating in-use of removing one canister each day. Then an experimental work was conducted on dry refresher candies in a polyethylene terephthalate bottle at 25 °C with two tablets taken out every day, which confirmed the model's capability to predict the product moisture content during in-use storage of 76% and 90% RH. Its use can provide science-based accurate determination of ISL, which may work as consumer guideline. The model is also expected to be helpful for recommending management scheme of whole product life.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"639-645"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141726963","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phytochemical profiling and antioxidant evaluation of <i>Rhododendron arboreum</i> Sm leaf and flower: integrative analysis using advanced analytical techniques.","authors":"Yangchen Dolma Kom, Karthiyayini Ramaswamy, Surya Suresh","doi":"10.1080/03639045.2024.2390029","DOIUrl":"10.1080/03639045.2024.2390029","url":null,"abstract":"<p><strong>Objective: </strong>This study investigates the biological activities of <i>Rhododendron arboreum</i> Sm from the eastern Himalayas, addressing a literature gap on its properties. It explores the plant's phytochemical, antioxidant, and medicinal characteristics.</p><p><strong>Significance: </strong>Evaluating methanolic extracts of <i>R. arboreum</i> offers valuable insights into its bioactive potential. Comprehensive GC-MS analysis identified a diverse array of compounds, highlighting the plant's chemical composition.</p><p><strong>Methods: </strong>Methanolic leaf and flower extracts underwent sequential extraction and phytochemical profiling using column chromatography, TLC, and GC-MS analysis. Spectral studies aided compound identification, and antioxidant activity was assessed <i>via</i> spectrophotometric assays.</p><p><strong>Results: </strong>Column chromatography separated methanol leaf and flower extracts into 17 and 24 distinct fractions, respectively. TLC analysis showed specific R_f values for leaf (0.58, 0.65, 0.75, 0.8, 0.86, 0.9) and flower samples (0.91, 0.38, 0.48, 0.51, 0.56, 0.6, 0.65, 0.75, 0.85, 0.96). GC-MS analysis revealed a variety of organic functional groups, including aliphatic hydrocarbons, aromatic compounds, heterocyclic molecules, phenolic compounds, steroids, terpenoids, alcohols, esters, and other bioactive compounds. FTIR spectra identified functional groups such as hydroxyls, primary amines, alkanes, and alkynes. NMR data indicated a complex molecular composition with diverse proton environments. Leaf extracts demonstrated superior antioxidant activity compared to flower extracts in DPPH, ABTS, hydrogen peroxide scavenging, lipid peroxidation inhibition, and FRAP assays.</p><p><strong>Conclusion: </strong>The study identifies diverse phytochemicals in <i>R.arboreum</i> extracts and highlights their potential applications in pharmaceuticals, nutraceuticals, and functional foods, owing to the superior antioxidant activity of leaf extracts compared to flowers.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"687-705"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141901280","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Gingerol containing polymeric nanofibers: a healing touch for accelerated wound recovery.","authors":"Heybet Kerem Polat, Sefa Gözcü, Sedat Ünal, Timur Paçacı, Eren Aytekin, Nasıf Fatih Karakuyu, Esra Köngül Şafak, Yakup Gültekin, Yonca Yazıksız, Nihat Kurt","doi":"10.1080/03639045.2024.2390033","DOIUrl":"10.1080/03639045.2024.2390033","url":null,"abstract":"<p><strong>Objective: </strong>In the current research, 6-gingerol (GA)-loaded <i>nanofiber drug delivery system</i> were developed, and their potential usage in wound healing was evaluated.</p><p><strong>Significance: </strong>This study investigates the effectiveness of nanofibrous membranes composed of sodium alginate (SA), poly(vinyl alcohol) (PVA), and 6-gingerol (GA) as delivery systems for anti-inflammatory agents in the context of wound dressings.</p><p><strong>Methods: </strong>GA-loaded SA/PVA nanofiber was prepared using electrospinning. <i>In vitro</i> characterization of this nanofiber included the examination of comprehensive <i>in vitro</i> characterization, anti-inflammatory and antioxidant activities, cytotoxicity, a scratch tes and <i>in vivo</i> skin test.</p><p><strong>Results: </strong>GA was extracted from <i>Zingiber officinale</i>, and its successful isolation was confirmed through analyses such as H-NMR, C-NMR. Then GA was electrospuned into the SA/PVA nanofibers, and scanning electron microscopy (SEM) imaging revealed that the fiber diameters of the formulations ranged between 148 nm and 176 nm. Anti-inflammatory and antioxidant studies demonstrated that the effectiveness of GA increased with higher doses; however, this increase was accompanied by decreased cell viability. In vitro release studies revealed that GA exhibited a burst release within the first 8 h, followed by a controlled release, reaching completion within 24 h. Within the scope of <i>in vitro</i> release kinetics, release data are mathematically compatible with the Weibull model with high correlation. The scratch test results indicated that TB2 (%1 GA) promoted epithelialization. Furthermore, it was determined that TB2 (%1 GA) did not cause any irritation.</p><p><strong>Conclusions: </strong>As a result, TB2 shows promise as a formulation for wound dressings, offering potential benefits in the field of wound care.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"706-719"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141901279","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Quantitative analysis of solid dosage forms of Atenolol by Raman spectroscopy.","authors":"Arslan Ali, Haq Nawaz, Muhammad Irfan Majeed, Madiha Ghamkhar","doi":"10.1080/03639045.2024.2377331","DOIUrl":"10.1080/03639045.2024.2377331","url":null,"abstract":"<p><strong>Objective: </strong>To develop a Raman spectroscopy-based analytical model for quantification of solid dosage forms of active pharmaceutical ingredient (API) of Atenolol.Significance: For the quantitative analysis of pharmaceutical drugs, Raman Spectroscopy is a reliable and fast detection method. As part of this study, Raman Spectroscopy is explored for the quantitative analysis of different concentrations of Atenolol.</p><p><strong>Methods: </strong>Various solid-dosage forms of Atenolol were prepared by mixing API with excipients to form different solid-dosage formulations of Atenolol. Multivariate data analysis techniques, such as Principal Component Analysis (PCA) and Partial least square regression (PLSR) were used for the qualitative and quantitative analysis, respectively.</p><p><strong>Results: </strong>As the concentration of the drug increased in formulation, the peak intensities of the distinctive Raman spectral characteristics associated with the API (Atenolol) gradually increased. Raman spectral data sets were classified using PCA due to their distinctive spectral characteristics. Additionally, a prediction model was built using PLSR analysis to assess the quantitative relationship between various API (Atenolol) concentrations and spectral features. With a goodness of fit value of 0.99, the root mean square errors of calibration (RMSEC) and prediction (RMSEP) were determined to be 1.0036 and 2.83 mg, respectively. The API content in the blind/unknown Atenolol formulation was determined as well using the PLSR model.</p><p><strong>Conclusions: </strong>Based on these results, Raman spectroscopy may be used to quickly and accurately analyze pharmaceutical samples and for their quantitative determination.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"619-627"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141558309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Quality-by-design driven approach in the formulation of an anti-ulcer and gastro-protective oral suspension.","authors":"Georgia Hanley, Silvia Vargas Jiménez, Eleaneth Baltodano Viales, Juan Miguel Zúñiga Umaña, José Vega Baudrit, Yesenia Murillo Rodríguez, Luis Castillo Henríquez","doi":"10.1080/03639045.2024.2383932","DOIUrl":"10.1080/03639045.2024.2383932","url":null,"abstract":"<p><strong>Objective: </strong>This work aims to present a Quality-by-Design (QbD) step-by-step methodology to formulate anti-ulcer and gastro-protective oral suspensions.</p><p><strong>Methods: </strong>Sucralfate was used as a drug model. The Quality Target Product Profile was established early during preformulation. Viscosity, resuspendability, pH, and density were assessed through the screening of several suspension platforms based on different prototype compositions. A compatibility study between the active pharmaceutical ingredient and the excipients was performed by thermal analysis and infrared spectroscopy. An Ishikawa fishbone diagram and Failure Mode and Effect Analysis were employed to identify the Critical Material Attributes (CMAs), Critical Process Parameters (CPPs), and Critical Quality Attributes (CQAs). CMAs' and CPPs' impact on identified CQAs was further assessed through a 2² full factorial experimental design at normal conditions after manufacture and one month at super-accelerated stress conditions. <b>Results:</b> The lead prototype exhibited no physicochemical incompatibilities. The risk assessment tools revealed that the concentration of the wetting agent and the total concentration of thickening agents represented critical factors for the quality profile of the preparation in terms of viscosity. The optimized formulation comprising 1.125 w/v% total concentration of Natrosol 250 HX and Avicel RC 591 exhibited an enhanced performance according to the established profile.</p><p><strong>Conclusions: </strong>The analytical and physicochemical tests showed the robustness and compliance of the final preparation with the quality profile. The proposed step-by-step methodology based on QbD, Design of Experiments, and Quality Risk Management presented in our research holds practical implications for local industries and formulation scientists involved in the development of oral suspensions.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"646-657"},"PeriodicalIF":2.4,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141787493","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}