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1.
Cureus ; 16(4): e58296, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38752039

RESUMO

Background Nonselective beta-blockers (NSBBs) have been used in the management of portal hypertension and the prevention of initial and recurrent variceal bleeding in patients with liver cirrhosis. However, there is controversy regarding the use of NSBBs in patients with decompensated cirrhosis (DC) due to concerns over potential adverse effects, such as worsening of hepatic function and risk of hepatorenal syndrome (HRS). HRS is a serious complication of DC characterized by acute kidney injury (AKI) and progressive renal failure, and its development can lead to significant morbidity and mortality in this setting. Therefore, using NSBBs in patients with DC remains an area of ongoing research and debate. Our study aims to investigate the potential effect of NSBBs on HRS development. Methodology A retrospective chart review of 404 patients with cirrhosis was performed across all Northwell Health institutions between January 01, 2019, and December 31, 2020. An analysis was done on 516 patient encounters. Inclusion criteria included patients with an established International Classification of Diseases 10th Revision code of cirrhosis and AKI. After adjusting for clinical predictors, the Student's t-test or Mann-Whitney U-test was used to compare variables between the two outcome groups (HRS vs. no HRS) for the continuous variables. Pearson's chi-square test or Fisher's exact test was used for the categorical variables to test if an association existed between the use of NSBBs at home and HRS. A two-sided p-value <0.05 was considered statistically significant. SAS 9.4 (SAS Institute Inc., Cary, NC, USA) was used for statistical analysis. Results The primary outcome was the development of HRS during the hospital stay. With a total of 109 visits with HRS, we had 21 (23.60%) reported HRS in the 89 visits where NSBBs were used at home before the hospitalization, while 88 (20.61%) HRS were observed in the 427 visits with no NSBB use at home. The use of NSBBs at home was not significantly associated with the development of HRS (odds ratio = 1.1, 95% confidence interval = 0.6-1.9, p = 0.7321). We also found that higher serum albumin on admission is associated with lower odds of HRS. In contrast, increased serum creatinine, bilirubin, presence of ascites, and use of pressors were associated with a higher risk of HRS. Conclusions Our study highlights the relevant safety of NSBB use in end-stage liver disease. Their use did not appear to increase the risk of developing HRS during hospitalization with DC. Further randomized controlled trials are warranted to shed more light on the efficacy, dose tolerance limits, and safety of NSBBs in decompensated end-stage liver disease.

2.
ACG Case Rep J ; 10(10): e01181, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37899956

RESUMO

Cytomegalovirus (CMV) belongs to the Herpesviridae family, and it is considered the largest virus to infect humans. Primary CMV infection frequently targets immunodeficient patients and is often symptomatic. However, it may remain latent or clinically unapparent for years in immunocompetent individuals. CMV infection rarely presents as an invasive disease in the latter group of individuals, in which case, the most common site of involvement in the gastrointestinal tract. When CMV affects the gastrointestinal tract, the colon and stomach are the 2 frequently involved sites. This case report describes a unique case of an immunocompetent patient who presented with acute excruciating periumbilical pain and was diagnosed with acute gastritis secondary to CMV infection and possible Helicobacter pylori-associated chronic active gastritis. Symptoms resolved entirely soon after treatment with antimicrobials that cover for both infections. The diagnosis was based on histopathologic findings from biopsies taken from the stomach during the endoscopic evaluation combined with positive CMV serology and positive CMV-deoxyribonucleic acid.

3.
Ann Med Surg (Lond) ; 85(7): 3386-3395, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37427170

RESUMO

Despite the recommendations to avoid using corticosteroids systematically for hospitalized coronavirus disease of 2019 (COVID-19) patients, healthcare professionals used personalized treatments, including corticosteroids, as adjuncts to treat their patients due to their limited access to treatment options. This study aims to evaluate the use of corticosteroids among hospitalized COVID-19 patients with all-cause mortality as the primary outcome and to assess the predictors of all-cause mortality associated with the characteristics of the patients and the corticosteroid regimens adopted. Methods: A multicenter retrospective study was performed over three months targeting 422 COVID-19 patients from six hospitals in Lebanon. Data were collected from patients' medical charts retrospectively and covered a period of one year (September 2020-August 2021). Results: The study sample included 422 patients, predominantly males, with 59% of cases classified as severe or critical cases. Dexamethasone and methylprednisolone were the most used corticosteroids. Around 22% of the patients died during hospitalization. After adjusting for covariates, performing a polymerase chain reaction before admission increased the mortality rate by 424% compared to doing it at hospital admission (aHR 4.24, 95% CI 1.35-13.3), with 18.11 times higher mortality rate among critical cases (aHR 18.11, 95% CI 9.63-31.05). Exposure to side effects from corticosteroids increased the mortality rate by 514% compared to others (aHR 5.14, 95% CI 1.28-8.58). In particular, the mortality rate among patients having hyperglycemia dropped by 73% compared to others (aHR 0.27, 95% CI 0.06-0.98). Conclusion: Corticosteroids are frequently used in treating hospitalized COVID-19 patients. The all-cause mortality rate was higher among older and critical cases and lower among smokers and those treated for more than 7 days. Research exploring the safety and efficacy of corticosteroids is required to allow better in-hospital management of COVID-19 cases.

4.
Blood Sci ; 5(2): 131-135, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37228771

RESUMO

Hemochromatosis, either hereditary hemochromatosis (HH) or secondary hemochromatosis, consists of the accumulation of iron in the liver, heart, and other organs. It leads to end-organ damage in a proportion of affected subjects. Although liver-related morbidity (cirrhosis and hepatocellular carcinoma [HCC]) and mortality are well established, the frequency of these complications remains controversial. The aim of this study is to examine the rate of hospitalization and the incidence of iron overload-related comorbidities in patients with hemochromatosis between the years of 2002 and 2010. We queried the Nationwide Inpatient Sample (NIS) database from the year 2002 to 2010. We included adults (age ≥18 years) and used the ICD-CM 9 code 275.0x to identify hospitalized patients with a diagnosis of hemochromatosis. Data analysis for this study was generated using SAS software version 9.4. A total of 168,614 hospitalized patients between 2002 and 2010 had a diagnosis of hemochromatosis. The majority were males (57%) with a median age of 54 years (37-68), with a predominance of white patients (63.3%) followed by black (26.8%). The rate of hospitalization among patients with hemochromatosis increased by 79% between the years 2002 and 2010 (34.5/100,000 in 2002 vs 61.4/100,000 in 2010). The main associated diagnoses were diabetes mellitus (20.2%), cardiac disease, including arrhythmias (14%) and cardiomyopathy (dilated 3.8%; peri-, endo-, myocarditis 1.3%), liver cirrhosis (8.6%), HCC (1.6%), and acute liver failure (0.81%). Of note, HCC was associated with cirrhosis in 1188 patients (43% of HCC patients) and male sex (87%). Diagnostic biopsies were performed in 6023 (3.6%) of those patients and liver transplant was performed in 881 (0.5%). In-hospital mortality occurred in 3638 (2.16%) patients. In this large database study, we found a rising trend in hospitalization for hemochromatosis, possibly due to the increased recognition of this entity and billing for the condition. The incidence of cirrhosis in hemochromatosis was found to be similar to other studies (8.6% vs 9%). However, the rate of HCC was lower than previous reports (1.6% vs 2.2%-14.9%), and only 43% of HCC was associated with cirrhosis. This raises important pathophysiologic questions regarding the impact of iron overload in HCC. There has been an increase in the rate of hospitalization for patients with a diagnosis of hemochromatosis. This may be related to an increased recognition of hemochromatosis as the underlying etiology for conditions such as diabetes, cardiomyopathy, cirrhosis, and HCC. Further prospective studies are needed to clarify the burden of liver disease in HH and secondary iron overload.

6.
Respir Med Case Rep ; 43: 101826, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37008194

RESUMO

We herein present the case of a 79-year-old female patient who presents with a single asymptomatic pulmonary nodule, melanocytic in nature, later identified as a remote secondary lesion of a primary cutaneous melanoma that was resected 22 years before presentation. Although quite atypical, the patient underwent resection of the affected pulmonary lobe; follow-up imaging did not reveal any local or distant recurrences.

8.
Gastroenterology Res ; 15(4): 180-187, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36128183

RESUMO

Background: Since their introduction in the early 1980s, proton pump inhibitors (PPIs) have been used worldwide for a broad range of indications. Unfortunately, however, PPIs have become overly prescribed by healthcare providers, sometimes in the absence of clear indications. Although PPIs were initially presumed to have an excellent safety profile, emerging studies have shed light on the association between their long-term use and a myriad of side effects, including the possibility of an increased risk of spontaneous bacterial peritonitis (SBP). Data available to date regarding the association between PPI use and SBP development in cirrhotic patients is conflicting. While some observational studies provide no association between PPI use in cirrhotic patients and an increased risk of SBP development, many others support this association. As a result of the conflicting conclusions from case controls, cohorts, and meta-analyses, we aimed to carry out this retrospective cohort analysis of data from cirrhotic patients included in the electronic medical record-based commercial database, EXPLORYS (IMB-WATSON, Cleveland, Ohio). Our aim was to evaluate for a possible association between PPIs use and the risk of SBP development in cirrhotic patients and to compare the prevalence of SBP development between cirrhotic patients who were actively using PPIs and those who were not. Methods: A retrospective cohort analysis with chart review was conducted on patients with cirrhosis who were included in the electronic medical record-based commercial database, EXPLORYS (IMB-WATSON, Cleveland, Ohio). Using this database, records were reviewed between December 2017 and 2020. Included patients were adults aged 30 to 79 years with a Systematized Nomenclature of Medicine-Clinical Terms (SNOMED-CT) diagnosis of liver cirrhosis. Included patients with a SNOMED-CT diagnosis of liver cirrhosis were divided into two groups: the first group included all cirrhotic patients who did not use PPIs and the second group included all cirrhotic patients who were on PPIs at home. Results: In our analysis, SBP occurred in 1.7% (1,860 patients) of the included cirrhotic patients whether they were actively taking PPIs or not. Among the 40,670 cirrhotic patients who were on PPIs at home, 1,350 (3.3%) patients developed SBP. On multivariate analysis, PPI use was the strongest predictor for SBP in cirrhotic patients (odds ratio (OR) = 4.24; 95% confidence interval (CI): 3.83 - 4.7, P value < 0.0001), with cirrhotic patients taking PPIs being 4.24 more likely to develop SBP than those not on PPIs. In addition, PPI use, history of bleeding varices, age, race, and gender were found to be independent predicting factors for SBP, in descending order of importance. Conclusions: Our retrospective cohort analysis has shown that the use of PPIs in patients with liver cirrhosis is an independent predicting risk factor for SBP development. It solidified the argument that cirrhotic patients receiving this form of therapy seem to have a higher risk of developing SBP. In the setting of the emerging evidence that PPIs might impose health risks in cirrhotic patients, further studies are needed to settle the current debate between supporters and opponents of this proposition. In addition, future studies may help clarify the relationship between the occurrence of SBP in cirrhotic patients and the type, dose, and duration of PPIs used. We recommend that unless it is clearly indicated, PPI therapy should be avoided or administered with caution in patients with cirrhosis.

9.
Cureus ; 14(5): e25520, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35800801

RESUMO

Introduction Sarcoidosis is a multisystemic disorder of an unclear etiology. It has been postulated that sarcoidosis is a chronic autoimmune inflammation, which may predispose to venous thromboembolism (VTE). Recent studies showed increased VTE events in patients with sarcoidosis and other autoimmune disorders. This multicenter retrospective study aims at determining a possible correlation between VTE and sarcoidosis. Subjects and Method We reviewed charts from a commercial database (Explorys Inc, Cleveland, OH, USA), which is an aggregate of electronic health records from 26 major health care systems. We included patients between 30 and 69 of age. Patients with a condition known to cause a hypercoagulable state were excluded. We calculated the prevalence of VTE in patients with and without a diagnosis of sarcoidosis and compared the results. A multivariate analysis was performed to adjust for gender, race, age, tobacco use, and obesity. Results The overall prevalence of the VTE in patients without sarcoidosis was 1.4% compared to 4.9% in patients with sarcoidosis. Patients with sarcoidosis were more likely to develop VTE (OR: 2.96; 95% CI: 2.84-3.08; p < 0.001). Predictors of VTE in patients with sarcoidosis were gender, age, race, and obesity. Conclusion Our study indicates that sarcoidosis poses a risk of developing VTE. Further prospective studies are needed to shed light on this association and explain the prothrombotic phenotype of sarcoidosis.

10.
Arch Ital Urol Androl ; 94(2): 237-247, 2022 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-35775354

RESUMO

Priapism is a persistent penile erection lasting longer than 4 hours, that needs emergency management. This disorder can induce irreversible erectile dysfunction. There are three subtypes of priapism: ischemic, non-ischemic, and stuttering priapism. If the patient has ischemic priapism (IP) of less than 24-hours (h) duration, the initial management should be a corporal blood aspiration followed by instillation of phenylephrine into the corpus cavernosum. If sympathomimetic fails or the patient has IP from 24 to 48h, surgical shunts should be performed. It is recommended that distal shunts should be attempted first. If distal shunt failed, proximal, venous shunt, or T-shunt with tunneling could be performed. If the patient had IP for 48 to 72h, proximal and venous shunt or T-shunt with tunneling is indicated, if those therapies failed, a penile prosthesis should be inserted. Non-ischemic priapism (NIP) is not a medical emergency and many patients will recover spontaneously. If the NIP does not resolve spontaneously within six months or the patient requests therapy, selective arterial embolization is indicated. The goal of the management of a patient with stuttering priapism (SP) is the prevention of future episodes. Phosphodiesterase type 5 (PDE5) inhibitor therapy is considered an effective tool to prevent stuttering episodes but it is not validated yet. The management of priapism should follow the guidelines as the future erectile function is dependent on its quick resolution. This review briefly discusses the types, pathophysiology, and diagnosis of priapism. It will discuss an updated approach to treat each type of priapism.


Assuntos
Priapismo , Gagueira , Algoritmos , Humanos , Masculino , Ereção Peniana , Pênis/cirurgia , Inibidores da Fosfodiesterase 5 , Priapismo/etiologia , Priapismo/terapia
12.
Diabetol Metab Syndr ; 14(1): 85, 2022 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-35725489

RESUMO

INTRODUCTION: Starting December 2019, the world has been devastated by the rapid spread of coronavirus disease 2019 (Covid-19). Many risk factors have been associated with worse outcomes and death from Covid-19 pneumonia including having diabetes mellitus. To date, it is not clear if all group of diabetics share the same risk of complications with COVID-19 infection. This study aims to compare disease severity and mortality rate in insulin users versus non-insulin users. METHODS: In this retrospective case-control study conducted at the largest health care network in New York state, we included adult, diabetic patients admitted from March 2020 to October 2020 with Covid-19 pneumonia. We compared the baseline characteristics in addition to outcomes of diabetic patients on home insulin (cases) and non-insulin user diabetics (controls). In addition, to determine if home insulin use is associated with an increased mortality, we conducted a cox regression analysis. RESULTS: We included 696 patients in the study period with a median age of 57 years, interquartile range [IQR] 51-62, and median body mass index 29.9 (IQR: 26-34.7). The majority (476 [68%]) were males. We identified 227 cases (33%) and 469 controls (67%). More cases than controls were hypertensive (74% vs 67%, p = 0.03), on ACE/ARB (50% vs 42%, p = 0.05), and had a hemoglobin A1c > 8.1 (71% vs 44%, p < 0.001). More cases had AKI (52% vs 38%, p < 0.001), however no significant differences were found in intubation rates (26% vs 24%, p = 0.54), detection of pulmonary embolism (4% vs 6%, p = 0.19) or death rate (15% vs 11%, p = 0.22) comparing cases and controls. In a multivariate analysis, we found that home insulin use was independently associated with increased risk of death: Hazard ratio: 1.92, 95% confidence interval (1.13-3.23). CONCLUSION: We showed herein that diabetic patients on home insulin with COVID-19 pneumonia, have worse outcomes and increased mortality compared to diabetics on oral antihyperglycemic agents. Close monitoring of insulin-dependent type II diabetic patients is needed in the current pandemic.

13.
Cureus ; 14(3): e23450, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35494982

RESUMO

Background Patients with liver cirrhosis were previously considered as anticoagulated; thus, their risk of developing venous thromboembolism (VTE) is lower. Recently, several studies showed contradicting results regarding deep venous thrombosis (DVT) occurrence in cirrhotic patients. The aim of this study is to evaluate the prevalence and risk associated with developing DVT in hospitalized cirrhotic patients in a large US population. Methods We queried the commercial database Explorys (IMB Inc., Armonk, New York), an aggregate of electronic health record data from 26 US healthcare systems. After excluding patients under 20 years old, a cohort of patients with a Systematized Nomenclature of Medicine - Clinical Terms of "cirrhosis of the liver" and "inpatient care" between 2015-2019 were identified, and prevalence of DVT was calculated in the exposure and the control groups. Statistical analysis for a multivariable model was performed. Factors adjusted for include gender, race, obesity, hypoalbuminemia, diabetes mellitus, viral hepatitis, and liver malignancy. Results Among 9,990,290 patients who were hospitalized between 2015 and 2019, 157,400 patients had a diagnosis of liver cirrhosis. The prevalence of DVT in hospitalized patients with liver cirrhosis was 3.29% compared to 3.18% in non-cirrhotic patients. Using the multivariate analysis model, DVT was inversely associated with cirrhosis in hospitalized patients [OR: 0.921; p<0.0001] compared to patients without liver cirrhosis. Predictors of developing DVT among patients with cirrhosis were non-Caucasian race, obesity (BMI>30), liver malignancy, hypoalbuminemia, and diabetes mellitus. Cirrhotic patients due to viral hepatitis were less likely to develop DVT [OR: 0.775; p<0.001] compared to non-cirrhotic patients. Conclusion In this database, although the prevalence of DVT in cirrhotic hospitalized patients was slightly higher than in non-cirrhotic patients (3.29% vs. 3.18%, respectively), cirrhosis as an independent factor was associated with less risk of DVT during hospitalization. This poses a question regarding DVT prophylaxis necessity in this group of patients. Further studies are needed to clarify the benefit and risks of DVT prophylaxis in cirrhotic patients.

14.
Cureus ; 14(12): e32544, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36654566

RESUMO

We herein present two cases of spontaneous pneumothorax. The first one is occurring in an elderly female who has an extensive history of smoking and an underlying chronic obstructive lung disease, whereas the second case represents a congenital bleb in a male patient who has no other underlying pulmonary disorder. Both cases presented to our facility with a spontaneous pneumothorax following pulmonary bleb rupture. Both patients underwent thoracoscopic surgery with subsequent partial pleurectomy and pleurodesis.

15.
J Clin Med ; 10(23)2021 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-34884323

RESUMO

Hepatorenal syndrome (HRS) is a type of acute kidney injury (AKI), occurring in patients with decompensated liver cirrhosis and is associated with high mortality. We aim to describe the predictors associated with the development of HRS in cirrhotic patients with AKI. We retrospectively analyzed 529 cirrhotic patient encounters with AKI across all Northwell Health institutions between 1 January 2015 and 31 December 2018. We performed multivariate analyses to determine independent predictors of development of HRS. Alcoholic cirrhosis was the most common identified etiology of cirrhosis. The mean Model for End-Stage Liver Disease Scorewas18 (±7). Ascites was the most commonly identified clinical feature of portal hypertension. Infection was identified in 38.4% of patients with urinary tract infection/pyelonephritis being the most common. Spontaneous bacterial peritonitis occurred in 5.9% of patients. The most common cause of AKI was pre-renal. Hepatorenal syndrome was identified in 9.8% of patient encounters. Predictors of HRS were history of ascites, serum creatinine >2.5 mg/dL, albumin <3 g/dL, bilirubin >2 mg/dL and spontaneous bacterial peritonitis. We demonstrate strong predictors for the development of HRS which can aid clinicians to attain an early diagnosis of HRS, leading to prompt and targeted management and improving outcomes.

16.
Gastroenterology Res ; 14(3): 184-189, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34267834

RESUMO

BACKGROUND: Proton pump inhibitors (PPIs) increase gastric pH by reducing acid production. The resulting alkaline milieu in the stomach increases the risk of bacterial translocation. This study aimed to investigate if there is a correlation between PPI use and developing pyogenic liver abscesses. METHODS: In this retrospective case-control analysis, we studied adult patients diagnosed with cryptogenic liver abscess at Northwell hospitals between 2015 and 2019. Adult patients with the diagnosis of liver abscess were included. We excluded patients with history of liver abscess prior to admission, biliary disease, hepatobiliary malignancy, or intra-abdominal infections. A group of randomly selected patients without liver abscess from the same hospitals' database were enrolled as the control group. A multivariate logistic regression analysis was performed to adjust for potential confounding factors. RESULTS: We identified 277 patients diagnosed with first episode of pyogenic liver abscess. Cases were compared to 554 controls. Klebsiella pneumonia was the most common pathogen. PPI use was associated with an increased risk of developing a first episode of pyogenic liver abscess in univariate (odds ratio (OR): 2.36, 95% confidence interval (CI): 1.70 - 3.27), and multivariate analysis (adjusted OR: 2.27, 95% CI: 1.55 - 3.32). CONCLUSION: This study is the first US population-based analysis to demonstrate that PPI use is associated with increased risk of developing pyogenic liver abscesses. Further prospective studies are needed to shed more light on this association and better evaluate the impact of dose and duration of PPI exposure.

17.
J Pharm Sci ; 108(10): 3319-3328, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31145923

RESUMO

The use of multifunctional excipients is gaining interest as it simplifies formulations by replacing the need of multiple monofunctional excipients. In previous work, coprocessed chitin-calcium carbonate (CC) showed to have good potential as a multifunctional excipient for fast disintegrating tablets produced by direct compression. It allowed for good tablet strength, enhanced powder flowability, and higher true and bulk densities with fast disintegrating properties. The objective of this work is to gain insight on CC tableting properties under different tablet manufacturing conditions (different lubrication levels, compression speeds, and dwell times) and in formulations with drug models: ibuprofen and paracetamol. Results showed that CC exhibited good tabletability, compressibility, and compactibility profiles. CC does not require the addition of lubricant and can be used at high compression speeds and different dwell times. When included in formulations with ibuprofen and paracetamol at different percentages, CC enhanced tablets strength and promoted fast disintegration and drug dissolution. In conclusion, this study shows that CC can be used as a multifunctional excipient (filler-disintegrant-binder) for fast disintegrating tablets produced by direct compression.


Assuntos
Carbonato de Cálcio/química , Quitina/química , Excipientes/química , Comprimidos/química , Acetaminofen/química , Química Farmacêutica/métodos , Força Compressiva/efeitos dos fármacos , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Ibuprofeno/química , Pós/química , Pressão , Solubilidade/efeitos dos fármacos , Resistência à Tração/efeitos dos fármacos
18.
J Pharm Sci ; 107(8): 2152-2159, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29698724

RESUMO

Owing to the increasing interest in multifunctional excipients for tableting, coprocessing of individual excipients is regularly used to produce excipients of improved multifunctionality superior to individual excipients or their physical mix. The use of chitin as an excipient in tablet formulation is limited because of certain drawbacks such as poor flowability and low true density. The objective of this work is to improve these properties through coprocessing of chitin with calcium carbonate (CaCO3) by precipitating CaCO3 on chitin particles using different methods. In addition, optimization of the coprocessed chitin was carried out to improve the excipient's properties. Physicochemical (CaCO3 content, true density, X-ray diffraction, infrared spectroscopy, and scanning electron microscopy) and functional testing (swelling force, flowability, tensile strength, deformation mechanism, and disintegration time) were used to characterize the coprocessed product. Results showed that the calcite CaCO3 polymorph is precipitated on the chitin surface and that it interacts with chitin at carbonyl- and amide-group level. In addition, the coprocessed excipient has an improved true density and powder flowability, with CaCO3 forming single layer on the chitin particles surface. Tableting studies showed that the coprocessed powder exhibited an intermediate deformation behavior between CaCO3 (most brittle) and chitin (most plastic). Tablets showed acceptable tensile strength and rapid disintegration (2-4 s). These results show the potential use of coprocessed chitin-CaCO3 as a multifunctional excipient for fast disintegration of tablets produced by direct compression.


Assuntos
Carbonato de Cálcio/química , Quitina/química , Composição de Medicamentos/métodos , Excipientes/química , Precipitação Química , Difração de Pó , Pressão , Solubilidade , Comprimidos , Resistência à Tração , Difração de Raios X
19.
J Pharm Sci ; 106(7): 1839-1848, 2017 07.
Artigo em Inglês | MEDLINE | ID: mdl-28392454

RESUMO

Disintegrants are used as excipients to ensure rapid disintegration of pharmaceutical tablets and further ensure proper dissolution of the active pharmaceutical ingredient. This study investigates disintegration mechanisms of chitin and common disintegrants. Swelling assessment (swelling force and swelling ratio) in different media, and compaction behavior (pure or mixed with other excipients) tabletability, deformation (Heckel modeling), and compact disintegration times were investigated on the tested disintegrants (alginic acid calcium salt, crospovidone, sodium starch glycolate, croscarmellose sodium, and chitin). Results show that the physicochemical properties of the disintegration medium such as pH and ionic strength, as well as other formulation ingredients, affect the disintegrant functionalities. Heckel analysis using the mean yield pressure "Py" shows that alginic acid calcium salt is the most brittle among the studied disintegrants, while crospovidone has the most plastic deformation mechanism, followed by chitin. Chitin showed good tabletability and disintegration properties that were not influenced by the physicochemical formulation environment. Chitin is largely available and easily modifiable and thus a promising material that could be used as a multifunctional excipient in tablet formulation.


Assuntos
Quitina/química , Excipientes/química , Benchmarking , Química Farmacêutica , Força Compressiva , Concentração de Íons de Hidrogênio , Concentração Osmolar , Pós , Solubilidade , Comprimidos
20.
Pharm Biol ; 54(6): 1035-41, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26511200

RESUMO

CONTEXT: Several plant-derived natural products have been used in clinical phase for applications in neurological, cardiovascular, and inflammatory diseases. Arbutus andrachne L. (Ericacea) is an evergreen shrub native to the Mediterranean region. Traditionally, the fruits and leaves of Arbutus tree are well known and used as antiseptics, diuretics, blood tonic, and laxatives. OBJECTIVE: Data regarding the biological effects of compounds derived from the Lebanese Arbutus andrachne are not available. In the present work, we studied the antioxidant activity of methanol extracts of leaves, fruits, and roots of the plant against electrolysis; together with their effects on the cardiodynamics of isolated perfused rabbit hearts. MATERIALS AND METHODS: In vitro electrolysis of the different root, leaves, and fruits methanol extracts was evaluated by the amount of free radicals that has been reduced by increasing the concentration of root extracts ranging from 0.5 to 2 mg after 1, 2, 3, and 4 min. Left ventricular pressure (LVP), heart rate (HR), and coronary flow (CR) were investigated in isolated rabbit heart after administration of 0.5, 1, 2, and 2 mg of each methanol extracts plotted against time (0, 0.5, 1.5, 5, and 10 min), according to the Langendorff method. Lipid peroxidation study was performed by the colorimetric method on myocard tissue after incubation with 500 µl of the different methanol extracts. The amount of MDA was determined at 500 nm absorbance after 5 min incubation. RESULTS: Among the different methanol extracts, the roots showed the highest in vitro antioxidant activity, particularly observed at concentration of 2 mg which completely inhibits free radical generation after 4 min. LVP decreases by 32% at the dose of 2 mg of root extracts after 5 min. No significant effect was observed by the three tested extracts on the heart rate. The three methanol extracts did not show any significant effect on the coronary flow. Moreover, the roots show an increase in the coronary flow at a concentration of 1 and 2 mg/ml during 1 min. Electrolysis on heart tissue treated with the roots extracts shows a decrease in the MDA level from 70.51 ± 6.71 to 48.58 ± 4.15 nmole/g of tissue. DISCUSSION AND CONCLUSION: Methanol extracts of the roots possess antihypertensive effect that may result from its ability to decrease the LVP together with its protective role by inhibiting free radical generation and significantly decreasing the MDA level of heart tissue.


Assuntos
Antioxidantes/farmacologia , Ericaceae/química , Coração/efeitos dos fármacos , Miocárdio/metabolismo , Extratos Vegetais/farmacologia , Animais , Antioxidantes/isolamento & purificação , Relação Dose-Resposta a Droga , Ericaceae/crescimento & desenvolvimento , Frutas/química , Frutas/crescimento & desenvolvimento , Coração/fisiopatologia , Técnicas In Vitro , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Metanol/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Folhas de Planta/crescimento & desenvolvimento , Raízes de Plantas/química , Raízes de Plantas/crescimento & desenvolvimento , Coelhos , Espécies Reativas de Oxigênio/metabolismo , Função Ventricular Esquerda/efeitos dos fármacos , Pressão Ventricular/efeitos dos fármacos
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