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1.
ISA Trans ; 105: 230-239, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32475537

RESUMEN

Fuzzy Logic Speed Controller (FLSC) has been widely used for motor drive due to its robustness and its non-reliance to real plant parameters. However, it is computationally expensive to be implemented in real-time and prone to the fuzzy rules' selection error which results in the failure of the drive's system. This paper proposes an improved simplified rules method for Fuzzy Logic Speed Controller (FLSC) based on the significant crisp output calculations to address these issues. A systematic procedure for the fuzzy rules reduction process is first described. Then, a comprehensive evaluation of the activated crisp output data is presented to determine the fuzzy dominant rules. Based on the proposed method, the number of rules was significantly reduced by 72%. The simplified FLSC rule is tested on the Induction Motor (IM) drives system in which the real-time implementation was carried out in the dSPACE DS1103 controller environment. The simulation and experimental results based on the proposed FLSC have proved the workability of the simplified rules without degrading the motor performance.

2.
Eur J Pharm Sci ; 138: 105009, 2019 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-31306781

RESUMEN

Permeation enhancer strategy is used to develop Benzoylaconitine (BA) of high molecular weight (603.7 Da) into transdermal patch. The present study was to achieve a patch with good analgesic and anti-inflammatory effects and investigate the relationship between physicochemical parameters of enhancers and enhancement strength. In vitro skin permeation study was used to evaluate the effect of enhancers, and correlation study was conducted to clarify the relationship between physicochemical parameters of enhancer and permeation amount. The enhancement molecular mechanism was characterized using FT-IR and molecular modeling. Finally, pharmacodynamic effect of BA patch was evaluated with analgesic and anti-inflammatory assessment. The correlation analysis indicated that the optimized patch containing permeation enhancer Plurol® Oleique CC497 with high surface tension (43.0 dyne/m), demonstrated the strongest skin permeation amount of 5.50 ±â€¯0.21 µg/cm2. According to the FT-IR and molecular modeling study, the enhancer with high surface tension demonstrated maximum interaction strength (Emix = -9.20 kcal/mol) with skin lipid and affected the skin protein region, which strongly disturbed skin lipid arrangement according to the results of ATR-FTIR study (wavenumber variation of νas CH2 of skin lipid > 2.00 cm-1) and molecular modeling (Cohesive Energy Density of skin lipid bilayer = 1.04E + 08 kcal/mol). It was indicated that only based on sufficient interaction strength and disturbing of both lipophilic and hydrophilic area of stratum corneum, permeation enhancer was able to demonstrated great permeation enhancement effect. Finally, BA transdermal patch was developed and showed excellent analgesic and anti-inflammatory effect, which was a potential preparation for the treatment of inflammatory pain.


Asunto(s)
Aconitina/análogos & derivados , Antiinflamatorios/farmacología , Permeabilidad/efectos de los fármacos , Absorción Cutánea/efectos de los fármacos , Aconitina/farmacología , Administración Cutánea , Animales , Química Farmacéutica/métodos , Interacciones Hidrofóbicas e Hidrofílicas/efectos de los fármacos , Masculino , Ratones , Ratas , Ratas Wistar , Piel/efectos de los fármacos , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Parche Transdérmico
3.
Drug Dev Ind Pharm ; 44(10): 1642-1649, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29851521

RESUMEN

OBJECTIVE: The aim of this study was to develop a drug-in-adhesive patch for transdermal delivery of daphnetin (DA), which is a coumarin derivative in Girald Daphne, and to investigate the role of Transcutol P (TP) in the release and percutaneous permeation processes of DA. METHODS: Backing films, permeation enhancers and enhancer content in the transdermal patch were investigated through in vitro experiments using rat skin. Anti-inflammatory and analgesic effects of the optimized formulation were evaluated using the adjuvant arthritis model and the pain model induced by acetic acid, respectively. In addition, the enhancement effect of TP was investigated using differential scanning calorimetry (DSC), FTIR, and molecular dynamic simulation. RESULTS: The optimal formulation, composed of DURO-TAK® 87-2852, CoTranTM 9680, 1% DA, and 10% TP showed anti-inflammatory and analgesic effects. It was found that TP only promoted the release process of DA from its transdermal patch. Furthermore, the decrease of interaction between drug and pressure sensitive adhesive (PSA) as well as the improvement of PSA mobility due to TP addition were the main factors that enhanced the release of DA from patch. CONCLUSIONS: This study successfully used TP to develop a DA patch with good anti-inflammatory and analgesic effects, proving that TP promotes the release of DA by reducing the interaction between DA and PSA and increasing the mobility of PSA.


Asunto(s)
Glicoles de Etileno/síntesis química , Glicoles de Etileno/farmacocinética , Absorción Cutánea/efectos de los fármacos , Parche Transdérmico , Umbeliferonas/síntesis química , Umbeliferonas/farmacocinética , Administración Cutánea , Animales , Glicoles de Etileno/administración & dosificación , Masculino , Ratones , Ratas , Ratas Wistar , Absorción Cutánea/fisiología , Umbeliferonas/administración & dosificación
4.
Curr Drug Deliv ; 10(5): 548-56, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-23607649

RESUMEN

The potential of Compritol(®)888 ATO as a release modifier to retard the release of highly water soluble drug, metoprolol succinate (MPL) was exploited. Different ratios of Compritol(®)888 ATO versus MPL were utilized and the effect of various formulation methods was evaluated to sustain the release of MPL. MPL: Compritol(®)888 ATO in 1:2 ratio could successfully retard the release of MPL. Melt granulation method "as hot process" was found to be effective when compared to direct compression and wet granulation. The in vitro release characteristics of tablets were studied in pH 6.8 phosphate buffer at 50 rpm using USP Type II apparatus. Formulation F7 retarded MPL release with ~90% release after 20 h. Stability studies showed no significant difference (f2>50) in MPL release profile after three months of storage period at 25 ± 2°C/60 ± 5% RH and 40 ± 2°C/75 ± 5% RH. The bioavailability of sustained release tablets, F7 was compared with commercially available tablets, MetXL50 in 12 healthy human volunteers in a crossover design. Plasma concentration of MPL was determined using HPLC with fluorescence detector. IVIVC correlation was obtained by deconvoluting the plasma concentration-time curve using a model independent Wagner-Nelson method. Correlations of fraction of drug dissolved in vitro and fraction of drug absorbed in vivo displayed a significant linear relationship for sustained release tablets of MPL.


Asunto(s)
Antagonistas Adrenérgicos beta/química , Excipientes/química , Ácidos Grasos/química , Metoprolol/análogos & derivados , Antagonistas Adrenérgicos beta/farmacocinética , Adulto , Química Farmacéutica , Estudios Cruzados , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Estabilidad de Medicamentos , Femenino , Humanos , Masculino , Metoprolol/química , Metoprolol/farmacocinética , Solubilidad , Comprimidos , Agua/química , Adulto Joven
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