RESUMO
BACKGROUND: Starch is a potential biomaterial used for various pharmaceutical applications because of its unique physicochemical and functional characteristics. A number of modification techniques, such as physical, chemical, enzymatic and genetic or a combination of any of these methods have been reported with the aim of enhancing the positive attributes and eliminating the shortcomings of the native starches. OBJECTIVES: The present studies deal with the development of co-precipitates of corn starch with different silicates (Mg, Ca, Al) with an aim of using it as a tablet superdisintegrant. Co-precipitates of starch with different silicates were prepared and FTIR-ATR, XRD and SEM techniques were used for the characterization of conjugates. MATERIAL AND METHODS: The conjugate were analyzed for various powder evaluation test like angle of repose, bulk density, tapped density, Hausner's ratio, Carr's index, swelling index and effective pore radius. RESULTS: The prepared co-precipitates were found to possess good powder flow properties. The swelling and effective pore radius of all co-precipitates (SMgC, SAlC and SCaC) was found in the range between 30-100% and 15.89-21.71 µm respectively. Different ratios of the prepared co-precipitates were used to formulate fast disintegrating tablets. Fast disintegrated tablets formulated using starch silicate conjugates as superdisintegrant were evaluated for diameter, thickness, hardness, friability, tensile strength, in vitro tablet disintegration, water absorption ratio, wetting time and in vitro dissolution studies. The effective pore radius and swelling of the co-precipitates were correlated with the in vitro disintegration, water absorption ratio and wetting time of the tablets. CONCLUSIONS: It was concluded that silicated co-precipitates of starch could be used as superdisintegrants in pharmaceutical tablet formulations.
Assuntos
Química Farmacêutica/métodos , Silicatos/química , Amido/química , Comprimidos/química , Precipitação Química , Dureza , Metais/química , Pós/química , SolubilidadeRESUMO
The novel polysaccharide (NPS) PolyGlycopleX (PGX) has been shown to reduce glycemia. Pharmacological treatment with sitagliptin, a dipeptidyl peptidase 4 (DPP4) inhibitor, also reduces glycemia by increasing glucagon-like peptide-1 (GLP-1). Our objective was to determine if using NPS in combination with sitagliptin reduces hyperglycemia in Zucker diabetic fatty (ZDF) rats more so than either treatment alone. Male ZDF rats were randomized to: 1) cellulose/vehicle [control (C)]; 2) NPS (5% wt:wt)/vehicle (NPS); 3) cellulose/sitagliptin [10 mg/(kg · d) (S)]; or 4) NPS (5%) + S [10 mg/(kg · d) (NPS+S)]. Glucose tolerance, adiposity, satiety hormones, and mechanisms related to DPP4 activity and hepatic and pancreatic histology were examined. A clinically relevant reduction in hyperglycemia occurred in the rats treated with NPS+S (P = 0.001) compared with NPS and S alone. Blood glucose, measured weekly in fed and feed-deprived rats and during an oral glucose tolerance test, was lower in the NPS+S group compared with all other groups (all P = 0.001). At wk 6, glycated hemoglobin was lower in the NPS+S group than in the C and S (P = 0.001) and NPS (P = 0.06) groups. PGX (P = 0.001) and S (P = 0.014) contributed to increased lean mass. Active GLP-1 was increased by S (P = 0.001) and GIP was increased by NPS (P = 0.001). Plasma DPP4 activity was lower in the NPS+S and S groups than in the NPS and C groups (P = 0.007). Insulin secretion and ß-cell mass was increased with NPS (P < 0.05). NPS alone reduced LDL cholesterol and hepatic steatosis (P < 0.01). Independently, NPS and S improve several metabolic outcomes in ZDF rats, but combined, their ability to markedly reduce glycemia suggests they may be a promising dietary/pharmacological co-therapy for type 2 diabetes management.
Assuntos
Alginatos/farmacologia , Hiperglicemia/tratamento farmacológico , Polissacarídeos Bacterianos/farmacologia , Pirazinas/farmacologia , Saciação/efeitos dos fármacos , Triazóis/farmacologia , Animais , Glicemia/análise , Diabetes Mellitus Tipo 2/tratamento farmacológico , Dipeptidil Peptidase 4/sangue , Inibidores da Dipeptidil Peptidase IV/farmacologia , Combinação de Medicamentos , Peptídeo 1 Semelhante ao Glucagon/sangue , Teste de Tolerância a Glucose , Insulina/sangue , Insulina/metabolismo , Secreção de Insulina , Células Secretoras de Insulina/efeitos dos fármacos , Células Secretoras de Insulina/metabolismo , Masculino , Obesidade/tratamento farmacológico , Ratos , Ratos Zucker , Fosfato de SitagliptinaRESUMO
Melioidosis, endemic in Southeast Asia and Northern Australia, is an uncommon but frequently fatal opportunistic infection caused by the Gram-negative saprophyte Burkholderia pseudomallei. We describe the first reported case of activation of latent melioidosis concurrent with COVID-19-associated lymphopenia and neutropenia in the setting of poorly controlled diabetes. A 43-year-old HIV-positive, diabetic man presented to the emergency department with persistent chills and progressive dyspnea. He was admitted for hypoxia. Chest X-ray showed bilateral parenchymal infiltrates suspicious for COVID-19. Shortly after admission, he became acutely encephalopathic, had a generalized seizure, and was transferred to the intensive care unit after intubation. Further workup showed severe neutropenia and lymphopenia. The patient received empiric antimicrobial coverage and was found to be severe acute respiratory syndrome coronavirus 2 positive. He deteriorated rapidly with refractory shock and persistent hypoxemia, and died 40 hours after admission. Blood cultures and sputum cultures obtained via bronchoalveolar lavage returned positive for Burkholderia pseudomallei. Given confirmed compliance with antiretrovirals, stable CD4 counts, and no recent foreign travel, the patient likely contracted the B. pseudomallei infection from travel to Southeast Asia many years prior and only became symptomatic after succumbing to severe acute respiratory syndrome coronavirus 2 infection. This case highlights the importance of considering activation of latent opportunistic infections by COVID-19 in immunocompromised patients.
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In the present study, corn Starch-Neusilin UFL2 conjugates were prepared by physical, chemical, and microwave methods with the aim of using the conjugates as tablet superdisintegrant. Various powder tests, namely, angle of repose, bulk density, tapped density, Hausner's ratio, Carr's index, swelling index, and powder porosity were conducted on the samples. The conjugates were characterized by ATR-FTIR, XRD, DSC, and SEM techniques. Heckel and Kawakita models were applied to carry out compression studies for the prepared conjugates. Fast disintegrating tablets of domperidone were prepared using corn starch and corn Starch-Neusilin UFL2 conjugates as tablet superdisintegrants in different concentrations. Conjugates were found to possess good powder flow and tabletting properties. Heckel analysis indicated that the conjugates prepared by microwave method showed the slowest onset of plastic deformation while Kawakita analysis indicated that the conjugates prepared by microwave method exhibited the highest amount of total plastic deformation. The study revealed that the corn Starch-Neusilin UFL2 conjugates possess improved powder flow properties and could be a promising superdisintegrant for preparing fast disintegrating tablet. Also, the results sugessted that the microwave method was found to be most effective for the preparation of corn Starch-Neusilin UFL2 conjugates.
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OBJECTIVE: Evidence supports the role of dietary fiber in improving metabolic health. PolyGlycopleX (PGX), a viscous functional polysaccharide improves lipidemia and glycemia in healthy adults. Our objective was to examine the effects of PGX on risk factors associated with the metabolic syndrome in Japanese adults with abdominal obesity. DESIGN AND METHODS: Sixty four subjects assigned to 14 weeks of 15 g day(-1) of PGX or placebo were assessed in a randomized, double-blind, placebo-controlled, parallel group trial. At week 0 and 14, primary outcome measures were serum lipids, abdominal adiposity, glucose tolerance and blood pressure. RESULTS: Total and LDL cholesterol were reduced at week 14 with PGX but not placebo (P < 0.05). The reduction in waist circumference at week 14 was greater with PGX versus placebo (P < 0.05). In females, abdominal visceral fat was decreased to a greater extent with PGX versus placebo (P < 0.05). While glucose tolerance worsened with placebo over time, PGX reduced glucose total area under the curve from week 0 to 6 (P = 0.039). Serum concentrations of resistin and IL6 increased slightly in placebo and decreased slightly with PGX . CONCLUSIONS: PGX is a functional fiber that shows promise in reducing risk factors related to the metabolic syndrome in Japanese adults with abdominal obesity.