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1.
Pak J Pharm Sci ; 32(5(Supplementary)): 2299-2304, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31894058

RESUMO

Chitosan nanoparticles (CSNPs) have proven their excellent drug delivery potential through various routes of administration and therefore, the need for large scale production of CSNPs for the commercialization is paramount. Their particle size and surface charge, drug loading capacity, and morphology were characterized in this study. Finally, drug release studies of both continuous and scalable modes were undertaken to ascertain suitability of CSNPs as a carrier for HC. The particle size of the large and small scale of HC-CSNPs was 253.3±16.4 nm and 225.4 ±9.6 nm, respectively. Besides, the surface charge of the large and small scale of HC-CSNPs was +35.3±0.3 mV and +32.6±2.5 mV, respectively. The size and surface charge of both HC-CSNPs were not proven to be statistically different. Drug loading capacity of large and small scale production of HC-CSNPs was high with 89%, and 83% of HC was loaded into CSNPs, respectively. Moreover, the morphology of both large and small scale production of HC-CSNPs had a similar shape and particle size. The drug release profile of CSNPs prepared by both methods showed a significantly (p<0.05) higher percentage release as compared to the free form. It is expected that positively charged nano-sized HC-CSNPs with high drug loading capacity could enhance the efficiency of drug delivery system to carry and diffuse into the target cells. The results obtained also suggested that the modified method applied could be further developed for large scale production of HC-CSNPs.


Assuntos
Quitosana/química , Dermatite Atópica/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Hidrocortisona/química , Nanopartículas/química , Análise Custo-Benefício , Liberação Controlada de Fármacos , Géis , Humanos , Hidrocortisona/administração & dosagem , Tamanho da Partícula
2.
Drug Dev Ind Pharm ; 44(12): 2061-2070, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30081679

RESUMO

OBJECTIVE: This study was designed to optimize and develop matrix type transdermal drug delivery system (TDDS) containing tizanidine hydrochloride (TZH) using different polymers by solvent evaporation method. SIGNIFICANCE: A strong need exists for the development of transdermal patch having improved bioavailability at the site of action with fewer side effects at off-target organs. METHODS: The patches were physically characterized by texture analysis (color, flexibility, smoothness, transparency, and homogeneity), in vitro dissolution test and FTIR analysis. Furthermore, functional properties essential for TDDS, in vitro percentage of moisture content, percentage of water uptake, in vitro permeation by following different kinetic models, in vivo drug content estimation and skin irritation were determined using rabbit skin. RESULTS: The optimized patches were soft, of uniform texture and thickness as well as pliable in nature. Novel transdermal patch showed ideal characteristics in terms of moisture content and water uptake. FTIR analysis confirmed no interaction between TZH and cellulose acetate phthalate (CAP). The patch showed sustained release of the drug which increased the availability of short acting TZH at the site of action. The patch also showed its biocompatibility to the in vivo model of rabbit skin. CONCLUSIONS: The results demonstrated that topically applied transdermal patch will be a potential medicated sustain release patch for muscle pain which will improve patient compliance.


Assuntos
Clonidina/análogos & derivados , Sistemas de Liberação de Medicamentos/métodos , Relaxantes Musculares Centrais/administração & dosagem , Adesivo Transdérmico , Administração Cutânea , Animais , Disponibilidade Biológica , Clonidina/administração & dosagem , Clonidina/farmacocinética , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/farmacocinética , Liberação Controlada de Fármacos , Excipientes/química , Teste de Materiais , Relaxantes Musculares Centrais/farmacocinética , Mialgia/tratamento farmacológico , Polímeros/química , Coelhos , Pele/efeitos dos fármacos , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos
3.
Acta Pol Pharm ; 74(2): 477-487, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29624252

RESUMO

The study was conducted to formulate and assess a novel polypill comprising of atorvastatin calci- um (ATVC), clopidogrel bisulfate (CLB) and aspirin (ASP) which, after in vivo correlation, can be intended for use in hyperlipidemic chronic heart disease patients. Polypill was made by the compression coating technique (CCT) with multiple active ingredients along with different concentrations of mucoadhesive and sustained release polymers, i.e., Carbopol 934 (CAB), Methocel k15 (MTH) and sodium carboxymethyl cellulose (NaCMC). The effect of different concentration of polymers on physical properties, wash off time, mucoadhe- sion strength, swelling behavior, surface pH and drug release kinetics were investigated. In vitro drug release studies showed that combination of CAB-NaCMC (1 : 1) retarded drug release up to 96.7 ± 1.15%, while com- bination of CAB-MTH and MTH-NaCMC retarded drug release up to 81.9 ± 1.5% and 101.4 ± 1.3%, respec- tively, at the same polymer concentration. Core enteric coated tablet of ATVC (K 11) was compressed over with CLB and ASP granules with the help of CCT and produced the desired results with zero order release rate thus indicating successful formulation of proposed polypill.


Assuntos
Aspirina/química , Atorvastatina/química , Inibidores de Hidroximetilglutaril-CoA Redutases/química , Inibidores da Agregação Plaquetária/química , Polimedicação , Tecnologia Farmacêutica/métodos , Ticlopidina/análogos & derivados , Acrilatos/química , Adesividade , Administração Oral , Animais , Aspirina/administração & dosagem , Atorvastatina/administração & dosagem , Carboximetilcelulose Sódica/química , Química Farmacêutica , Clopidogrel , Preparações de Ação Retardada , Combinação de Medicamentos , Composição de Medicamentos , Liberação Controlada de Fármacos , Concentração de Íons de Hidrogênio , Inibidores de Hidroximetilglutaril-CoA Redutases/administração & dosagem , Derivados da Hipromelose/química , Mucosa Intestinal/química , Cinética , Modelos Químicos , Inibidores da Agregação Plaquetária/administração & dosagem , Polímeros/química , Coelhos , Solubilidade , Propriedades de Superfície , Comprimidos com Revestimento Entérico , Ticlopidina/administração & dosagem , Ticlopidina/química
6.
Front Pharmacol ; 10: 317, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31068804

RESUMO

Introduction: Athletes train physically to reach beyond their potential maximum aerobic threshold. Whey protein supplements (WPS) are often used in conjunction with physiotherapy and psychotherapy to regain better vital sign and physical performances. This review aimed to explore the clinical evidence on the efficacy and safety of WPS in sports performance and recovery among athletes. Methodology: A comprehensive literature search was performed to identify relevant randomized control trials (RCTs) that investigated the efficacy and safety of WPS on the vital sign and physical performance among athletes. The Cochrane Risk of Bias (ROB) Assessment tools were used to assess the quality of the studies. Meta-analysis was conducted using the frequentist model with STATA version 14.2®. Results: A total of 333,257 research articles were identified out of which 20 RCTs were included for qualitative synthesis and network meta-analysis with 351 participants. Among the studies, 7 had low ROB and 3 RCTs had high ROB. Of these 20 trials, 16 trials were randomized clinical trials which compared whey protein supplements (WPS) with various comparators i.e., L-alanine, bovine colostrum, carbohydrate, casein, leucine, maltodextrin, rice, protein + caffeine were compared with placebo. Analysis from the pairwise meta-analysis revealed that for respiratory exchange ratio (RER) WPS was found to be significantly improving compared to maltodextrin (WMD = 0.012; 95%CI = 0.001, 0.023). Similarity to RPE (Rate Perceived Exertion), slight difference between WPS and the comparators, however, when the estimation was favorable to the comparators, there was moderate-high heterogeneity. For VO 2max, high heterogeneity appeared when WPS compared to maltodextrin with the I 2 = 97.8% (WMD = 4.064; 95% CI = -4.230, 12.359), meanwhile bovine colostrum (WMD = -2.658; 95%CI = -6.180, 0.865) only comparator that was better than WPS. According to the estimated effect of the supplements on physical performance outcome results, maximum power (8 studies, 185 athletes), highest ranked was bovine colostrum (SUCRA = 70.7%) and the lowest ranked was placebo (SUCRA = 17.9%), yet all insignificant. Then again, on average power (nine studies, 187 athletes), WPS was the highest ranked (SUCRA = 75.4 %) about -112.00 watt (-187.91, -36.08) and most of the estimations were significant. Body mass was reported in 10 studies (171 athletes), carbohydrate may be at the highest ranked (SUCRA = 66.9%) but it is insignificant. Thought the second highest ranked was WPS (SUCRA = 64.7%) and it is significant (WMD = -6.89 kg; CI = -8.24, -5.54). Conclusion: The findings of this review support the efficacy and safety of WPS as an ergogenic aid on athletes' sports performance and recovery. The overall quality of clinical evidence was found to be valid and reliable from the comprehensive search strategy and ROB assessment.

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