Advances in Pharmacological and Pharmaceutical Sciences最新文献

{"title":"Busting the Breast Cancer with AstraZeneca's Gefitinib","authors":"S. Chemmalar, A. R. I. Shameha, Che Azurahanim, Che Abdullah, Nor Asma, Ab Razak, L. M. Yusof, M. Ajat, Kim Wei Chan, Md Zuki, Abu Bakar Zakaria","doi":"10.1155/2023/8127695","DOIUrl":"https://doi.org/10.1155/2023/8127695","url":null,"abstract":"Breast cancer is the most common cancer diagnosed in women, and in 2020, there were 684, 996 deaths due to this disease. Epidermal growth factor receptors (EGFRs) and their respective ligands have been blamed for the pathogenesis and resistance to treatment in specific breast cancer cases. With EGFR having four homologues: EGFR1, EGFR2, EGFR3, and EGFR4, in-depth understanding of EGFR biology led to the discovery of small-molecule inhibitors and antibodies against this receptor. Gefitinib (GEF), a tyrosine kinase inhibitor of EGFR1, possesses a vast potential for treatment against breast cancer and is supported by a multiplicity of experiments. Unfortunately, in clinical trials, GEF did not show the outcomes expected with complete response and disease progress. This is due to incomplete understanding of the molecular mechanisms involved in EGFR signaling and endocrine sensitivity. Hence, additional in-depth experiments are needed regarding various molecular pathways and crosstalk pathways to comprehend GEF's action mechanism thoroughly in breast cancer patients. In this review, the role of EGFR in the development and pathogenesis of breast cancer and the pharmacokinetics and pharmacotherapy of GEF for the treatment of breast cancer have been elaborated. Nanomedicines synthesized with GEF have shown positive experimental response, paving a promising path for GEF against breast cancer.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"17 9","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138602810","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":"Antistaphylococcal Efficacy of Cefepime, Meropenem, and Piperacillin-Tazobactam in Patients with Polymicrobial Infection with MSSA Bacteremia or Pneumonia","authors":"Laila M. Najia, Eric Pyles, Arnaldo Lopez-Ruiz, Bibidh Subedi","doi":"10.1155/2023/7684613","DOIUrl":"https://doi.org/10.1155/2023/7684613","url":null,"abstract":"There is a paucity of literature describing de-escalation techniques in patients with polymicrobial infections with one offending organism being methicillin-susceptible Staphylococcus aureus (MSSA) being treated with β-lactam therapy. The purpose of this study is to determine treatment outcomes for patients with polymicrobial infections with MSSA bacteremia or pneumonia who are treated with cefepime (FEP), meropenem (MEM), or piperacillin-tazobactam (TZP). This trial design represents a retrospective observational three-group comparison study of patients at a community teaching hospital system. Patients reviewed included those who had a MSSA bacteremia or pneumonia in addition to a confirmed polymicrobial infection or presence of a coinfection and received definitive therapy with FEP, MEM, or TZP. The primary outcome is defined as the resolution of fever of ≥100.4°F, hypothermia (≤95°F), leukocytosis (WBC °>° 12,000 cells/mm3), and leukopenia with WBC °<° 4,000 cells/mm3. Secondary outcomes included duration of definite therapy, in-hospital mortality, hospital and ICU length of stay (LOS), 30-day readmission rates for a presumed infection, and hospital-acquired Clostridioides difficile infection (HCDI). From August 1, 2016, to August 30, 2019, 45 patients met eligibility criteria. There were no observed differences in primary endpoint (p = 0.65) or secondary endpoints, i.e., in-hospital mortality (p = 0.10), hospital LOS (p = 0.75), ICU LOS (p = 0.53), 30-day readmission rates for presumed infection (p = 0.07), or HCDI (p = 0.34). There was no difference in treatment success with FEP, MEM, or TZP for polymicrobial infections with one offending organism being MSSA. Due to the lack of evidence in this unique patient population and observed results of our study, randomized studies are warranted to determine appropriate therapy in this complex patient population.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"115 18","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138607597","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":"Exploring the Effect of Compound Glycyrrhizin and Silybinin on the Metabolism of Pexidartinib in Rats Based on CYP3A4 and CYP2C9","authors":"Yan-Ding Su, Xinyi Wei, Q. Cheng, He Qi, Jianghui Chen, Xiang-jun Qiu","doi":"10.1155/2023/6737062","DOIUrl":"https://doi.org/10.1155/2023/6737062","url":null,"abstract":"Pexidartinib offered a new therapeutic option for adult patients with symptomatic tenosynovial giant cell tumor (TGCT) who were refractory to surgical treatment and had severe morbidity or functional limitations. Meanwhile, the metabolism of pexidartinib was mainly mediated through the oxidation of cytochrome P450 (CYP) 3A and glucuronidation by uridine glucuronosyltransferase (UGT) 1A4 and attention shall be paid to CYP450-based drug-drug interactions during therapeutic dosing. This study aimed to examine the changes in the pharmacokinetics of pexidartinib by silymarin and compound glycyrrhizin on pexidartinib in vivo in rats by high-performance liquid chromatography (HPLC)-UV approach and to detect its expression in CYP3A4 and CYP2C9 using the western blot. The findings of chromatography experiments revealed that silybinin as well as compound glycyrrhizin increased the exposure of pexidartinib in rats and had a significant inhibitory effect on the metabolism of pexidartinib. The results of immunoblotting assays suggested that silybinin as well as compound glycyrrhizin inhibited the protein expression of CYP3A4 and CYP2C9 in rats. Therefore, the combination of pexidartinib with silybinin and compound glycyrrhizin should be monitored to avoid clinical adverse effects.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"110 3","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138608482","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":"Trends of Antihypertensive, Antidiabetic, and Nonsteroidal Anti-Inflammatory Drugs Use among the Health Workers Cohort Study, Mexico 2004 to 2018.","authors":"Janinne Ortega-Montiel, Alejandra Montoya, René Soria-Saucedo, Katia Gallegos-Carrillo, Paula Ramírez-Palacios, Jorge Salmerón, Eduardo Salazar-Martínez","doi":"10.1155/2023/5555274","DOIUrl":"10.1155/2023/5555274","url":null,"abstract":"<p><strong>Background: </strong>Hypertension and type 2 diabetes (T2D) are the most prevalent noncommunicable diseases in Mexico and worldwide. According to international practice management guidelines, the principal chronic management therapy is daily oral medication.</p><p><strong>Aim: </strong>We aim to describe the trends of antihypertensive, antidiabetic, and nonsteroidal anti-inflammatory (NSAID) drugs use among the Mexican adult population from 2004-2018.</p><p><strong>Methods: </strong>We analyzed data from the Health Workers Cohort Study (HWCS) for males and females aged >18 years. We calculated the prevalence of chronic diseases and utilization for every kind of antihypertensive, antidiabetic, and NSAIDs (measured by self-reported utilization) at baseline and two follow-ups (2004, 2010, and 2017). Trends were analyzed using Fisher's exact test.</p><p><strong>Results: </strong>Hypertension prevalence increased from 19.8 to 30.3%, higher than T2D prevalence from 7.0 to 12.8% through fourteen years of follow-up. Like the self-reported dual therapy, the proportion of patients using beta-blockers and angiotensin II receptor blockers increased. Regarding T2D, the prevalence of metformin utilization increased to 83.9%. The utilization of common NSAIDs, mainly for muscular pain, remained around 13 to 16%.</p><p><strong>Conclusions: </strong>Our findings showed a changing prevalence of drug utilization for hypertension and T2D between 2004 and 2018 and consistent use of NSAIDs in the adult Mexican population.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5555274"},"PeriodicalIF":2.1,"publicationDate":"2023-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10684324/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138457176","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhancement of Liver Targetability through Statistical Optimization and Surface Modification of Biodegradable Nanocapsules Loaded with Lamivudine.","authors":"Srikar Grandhi, Moawia Al-Tabakha, Prameela Rani Avula","doi":"10.1155/2023/8902963","DOIUrl":"https://doi.org/10.1155/2023/8902963","url":null,"abstract":"<p><p>The intention of the current work was to develop and optimize the formulation of biodegradable polymeric nanocapsules for lamivudine (LMV) in order to obtain desired physical characteristics so as to have improved liver targetability. Nanocapsules were prepared in this study as aqueous-core nanocapsules (ACNs) with poly(lactide-co-glycolide) using a modified multiple emulsion technique. LMV was taken as a model drug to investigate the potential of ACNs developed in this work in achieving the liver targetability. Three formulations factors were chosen and 3³ factorial design was adopted. The selected formulation factors were optimized statistically so as to have the anticipated characteristics of the ACNs viz. maximum entrapment efficiency, minimum particle size, and less drug release rate constant. The optimized LMV-ACNs were found to have 71.54 ± 1.93% of entrapment efficiency and 288.36 ± 2.53 nm of particle size with zeta potential of -24.7 ± 1.2 mV and 0.095 ± 0.006 h^-1 of release rate constant. This optimized formulation was subjected to surface modification by treating with sodium lauryl sulphate (SLS), which increased the zeta potential to a maximum of -41.6 ± 1.3 mV at a 6 mM concentration of SLS. The results of <i>in vivo</i> pharmacokinetics from blood and liver tissues indicated that hepatic bioavailability of LMV was increased from 13.78 ± 3.48 <i>μ</i>g/mL <i>∗</i> h for LMV solution to 32.94 ± 5.12 <i>μ</i>g/mL <i>∗</i> h for the optimized LMV-ACNs and to 54.91 ± 6.68 <i>μ</i>g/mL <i>∗</i> h for the surface-modified LMV-ACNs.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"8902963"},"PeriodicalIF":2.8,"publicationDate":"2023-11-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10676277/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138457175","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Use of Monoterpenes as Potential Therapeutics in Diabetes Mellitus: A Prospective Review.","authors":"Leonardo da Rocha Sousa, Nildomar Ribeiro Viana, Angélica Gomes Coêlho, Celma de Oliveira Barbosa, Débora Santos Lula Barros, Maria do Carmo de Carvalho E Martins, Ricardo Martins Ramos, Daniel Dias Rufino Arcanjo","doi":"10.1155/2023/1512974","DOIUrl":"https://doi.org/10.1155/2023/1512974","url":null,"abstract":"<p><p>Monoterpenes are secondary metabolites of plants belonging to the terpenoid class of natural products. They are the most abundant components of essential oils that are generally considered to have various pharmacological properties. These compounds are reported to have antidiabetic effects in recent years. Due to nature's complex biosynthetic machinery, they also exhibit a reasonable degree of structural complexity/diversity for further analysis in structure-activity studies. Therefore, monoterpenes as antidiabetic agents have been investigated by recent in vitro and in vivo studies extensively reported in the scientific literature and claimed by patent documents. The purpose of this survey is to provide a comprehensive and prospective review concerning the potential applications of monoterpenes in the treatment of diabetes. The data for this research were collected through the specialized databases PubMed, Scopus, Web of Science, and ScienceDirect between the years 2014 and 2022, as well as the patent databases EPO, WIPO, and USPTO. The research used 76 articles published in the leading journals in the field. The main effect observed was the antidiabetic activity of monoterpenes. This review showed that monoterpenes can be considered promising agents for prevention and/or treatment of diabetes as well as have a marked pharmaceutical potential for the development of bioproducts for therapeutics applications.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"1512974"},"PeriodicalIF":2.8,"publicationDate":"2023-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10665111/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138457177","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Drug Utilization Evaluation of Erythropoietin at a Referral Teaching Hospital in Iran","authors":"Iman Karimzadeh, Hanieh Rasekh, Ava Karimian, Mojtaba Shabani-Borujeni, Afsaneh Vazin","doi":"10.1155/2023/6685602","DOIUrl":"https://doi.org/10.1155/2023/6685602","url":null,"abstract":"Objectives. Drug utilization evaluation (DUE) studies aim to survey the appropriateness of drug use. DUE is an executive approach used to improve the use of medications as well as reduce the cost of treatment, ensure drug adequacy, and improve patient safety. The aim of this study was to evaluate the pattern of erythropoietin use, according to standard guidelines, in patients admitted to Namazi Hospital in Shiraz, Iran. Methods. In this descriptive, retrospective study, 230 patients were assessed. All patients who were hospitalized in different wards of Namazi Hospital, affiliated to Shiraz University of Medical Sciences, and received at least three doses of erythropoietin from September 2019 to March 2020 participated in this study. The following standard indicators of erythropoietin use were evaluated through reviewing medical charts of the cohort: drug dose, dosing intervals, route of administration, indication, monitoring of laboratory parameters, drug dose adjustment based on the response rate as well as target hemoglobin ≥12 g/dl, attention to major drug interactions, and administration of injectable or oral iron supplementation during treatment. Results. Most (65.2%) of the participants were male. The mean ± SD age of the patients was 47.55 ± 22.71 years. More than half (51.3%) of the included subjects were hospitalized in the nephrology ward. PDpoetin® and Cinnapoietin® were given to 52.6% and 47.4% of the study participants, respectively. Treatment of anemia due to chronic kidney disease was the most frequent indication of erythropoietin. The time interval of erythropoietin administration was three times a week for 68.3% of the patients. The most frequently administered weekly dose of erythropoietin was 12,000 units. The weekly dose, dose interval, and route of administration of erythropoietin were appropriate in 52.6%, 77.4%, and 100% of the patients, respectively. Dose adjustment based on the response rate, attention to major drug interactions as well as absolute-relative contraindications, and attention to the target hemoglobin ≥12 g/dl to decide whether or not to continue treatment were based on standard guideline in 98.1%, 98.7%, and 93% of the patients, respectively. The sum indexes of erythropoietin use were in line with standard guidelines in 75.84% of the cases. Conclusion. According to our results, in the setting of erythropoietin use in hospitals, physicians need more attention and education in areas such as selecting the proper dose of medication, correct indication of the drug, temporal arrangement of monitoring laboratory items, and the patient’s need for iron supplements.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"12 3","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135539646","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":"Pharmacovigilance and Adverse Drug Reactions Reporting: Healthcare Providers' Experiences from Southern Highland Tanzania.","authors":"Dorkasi L Mwakawanga,&nbsp;Manase Kilonzi,&nbsp;Erick G Philipo,&nbsp;Aron Martine,&nbsp;Tusaligwe Mbilinyi,&nbsp;Nancy F Kileo,&nbsp;Bryceson Mkinga,&nbsp;Cleopatra Justine Shonyella,&nbsp;Juma A Mohamedi,&nbsp;Aurelia Clement,&nbsp;Davance Mwasomola,&nbsp;Stella E Mushy,&nbsp;Nathanael Sirili","doi":"10.1155/2023/5537592","DOIUrl":"10.1155/2023/5537592","url":null,"abstract":"<p><strong>Purpose: </strong>This exploratory qualitative study aimed to analyze the experiences of healthcare providers (HCPs) in pharmacovigilance (PV) and ADR reporting in the southern highland zone of Tanzania.</p><p><strong>Methods: </strong>In 2022, an exploratory qualitative case study using in-depth interviews (IDIs) was conducted to explore the experiences of PV and ADR reporting among HCPs (doctors, nurses, and pharmacists). The study was carried out in a zonal referral hospital and a regional referral hospital of the Tanzanian southern highlands zone. Inductive-deductive thematic analysis was adopted for data analysis.</p><p><strong>Results: </strong>Participants demonstrated adequate knowledge of PV and its related activities including ADR reporting. Knowing the interactions and wrong medication dosage as sources of ADR, signs, and symptoms, stopping the drug, and treating the symptoms following ADR emerged as subthemes linked with adequate knowledge in identifying and managing ADR. Participants perceived reporting ADR as laborious, posing a subjective burden and that not all ADRs needed to be reported. The latter contributed to limited participation in ADR reporting despite that participants were conversant with both physical and online ADR reporting platforms.</p><p><strong>Conclusion: </strong>Although HCPs are well informed about PV and ADR reporting including the benefits to public health, their involvement in ADR reporting is low. In addition to the ongoing on-the-job training and regular supportive supervision for HCPs to improve the ADR practice, there is still a need to explore other strategies to be used as motives for HCPs to report ADR regularly.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5537592"},"PeriodicalIF":2.8,"publicationDate":"2023-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10593552/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50156288","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Brazilin from <i>Caesalpinia sappan</i> L. as a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor: Pharmacophore-Based Virtual Screening, <i>In Silico</i> Molecular Docking, and <i>In Vitro</i> Studies.","authors":"Muhammad Iqbal,&nbsp;Nur Hasanah,&nbsp;Aimee Detria Arianto,&nbsp;Widya Dwi Aryati,&nbsp;Meidi Utami Puteri,&nbsp;Fadlina Chany Saputri","doi":"10.1155/2023/5932315","DOIUrl":"https://doi.org/10.1155/2023/5932315","url":null,"abstract":"<p><strong>Background: </strong>Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a crucial regulator of low-density lipoprotein cholesterol (LDL-c) levels, as it binds to and degrades the LDL receptor (LDLR) in the lysosome of hepatocytes. Elevated levels of PCSK9 have been linked to an increased LDL-c plasma levels, thereby increasing the risk of cardiovascular disease (CVD), making it an attractive target for therapeutic interventions. As a way to inhibit PCSK9 action, we searched for naturally derived small molecules which can block the binding of PCSK9 to the LDLR.</p><p><strong>Methods: </strong>In this study, we carried out <i>in silico</i> studies which consist of virtual screening using an optimized pharmacophore model and molecular docking studies using Pyrx 0.98. Effects of the candidate compounds were evaluated using <i>in vitro</i> PCSK9-LDLR binding assays kit.</p><p><strong>Results: </strong>Eleven natural compounds that bind to PCSK9 were virtually screened form HerbalDB database, including brazilin. Next, molecular docking studies using Pyrx 0.98 showed that brazilin had the highest binding affinity with PCSK9 at -9.0 (Kcal/mol), which was higher than that of the other ten compounds. Subsequent <i>in vitro</i> PCSK9-LDLR binding assays established that brazilin decreased the binding of PCSK9 to the EGF-A fragment of the LDLR in a dose-dependent manner, with an IC₅₀ value of 2.19 <i>μ</i>M.</p><p><strong>Conclusion: </strong>We have identified brazilin, which is derived from the <i>Caesalpinia sappan</i> herb, which can act as a small molecule inhibitor of PCSK9. Our findings suggest that screening for small molecules that can block the interaction between PCSK9 and the LDLR <i>in silico</i> and <i>in vitro</i> may be a promising approach for developing novel lipid-lowering therapy.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5932315"},"PeriodicalIF":2.8,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10584496/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49673049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comparative Direct Compression Property of a Novel Pregelatinized Starch in Paracetamol Tablets.","authors":"Tamrat Balcha Balla,&nbsp;Nisha Mary Joseph,&nbsp;Anteneh Belete","doi":"10.1155/2023/5573176","DOIUrl":"10.1155/2023/5573176","url":null,"abstract":"<p><strong>Background: </strong>Among all the pharmaceutical dosage forms, tablets are still the most preferred and the most commonly used option because of their advantages. The direct compression method of tablet preparation exempts several steps needed in the granulation method. Therefore, the pursuit of better direct compression tablet excipients is evident in contemporary research endeavors. Pregelatinized Taro Boloso-I starch has comparable flow properties and higher compressibility and compactibility than Starch 1500®. However, there is no evidence in the literature regarding the lubricant sensitivity and dilution potential of pregelatinized Taro Boloso-I starch. This study was aimed at performing the <i>in vitro</i> evaluation of paracetamol tablets prepared using pregelatinized Taro Boloso-I starch as a direct compression excipient using paracetamol as a model drug.</p><p><strong>Methods: </strong>Taro Boloso-I starch was pregelatinized, and its properties including amylose to amylopectin ratio, densities, flow properties, swelling power, water solubility index, particle morphology, moisture content, and moisture sorption profile were evaluated. Furthermore, the lubricant sensitivity test, dilution potential study, and compatibility test with the paracetamol drug using ATR spectroscopy were performed. The properties of the directly compressed tablets prepared accordingly were evaluated. The majority of evaluations were performed in comparison with Starch 1500®. <i>Results and Discussion</i>. PGTBIS had a significantly lower amount of amylose than Starch 1500®. In the ATR-IR spectra of the mixture of the paracetamol and pregelatinized PGTBIS, all the major absorbance peaks of the drug were maintained indicating the absence of chemical modifications. PGTBIS showed better flow properties than Starch 1500®. The modified starch was shown to withstand magnesium stearate up to 0.5% concentration.</p><p><strong>Conclusion: </strong>PGTBIS could accommodate higher drug cargo than Starch 1500® with acceptable tablet properties. Accordingly, PGTBIS starch could be taken as a potential direct compression excipient.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5573176"},"PeriodicalIF":2.8,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10567489/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41188025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}