scholarly journals Original article. Pharmacodynamics of dry powder formulations of salbutamol for delivery by inhalation

2011 ◽  
Vol 5 (4) ◽  
Author(s):  
Nichakorn Sukasame ◽  
Narumon Nimnoo ◽  
Tan Suwandecha ◽  
Teerapol Srichana

AbstractBackground: Salbutamol is a βObjective: Evaluate the relationship of in vitro particle size characteristics and pharmacodynamics of formulations of inhaled salbutamol dry powder.Methods: Three formulations contained micronized salbutamol and a lactose carrier with different size ranges (40- 80, 20-40, and 10-20 μm for formulations 1, 2, and 3, respectively). Following formulation of the drug, resultant powders were characterized using scanning electron microscopy and the aerosolization performance determined using an Andersen Cascade Impactor analysis. A high-performance liquid chromatography method was used for measuring the salbutamol drug content. The in vivo pharmacodynamics of the formulations was monitored in 12 healthy and 12 asthmatic volunteers.Results: The percentage of the fine particle fractions (FPF) for formulations 1, 2, and 3 were 24.87±0.52%, 33.82±3.80%, and 41.50±2.86%, respectively. The mass median aerodynamic diameters (MMAD) were around 3 μm for all formulations. The pharmacodynamic parameters, forced vital capacity (FVC), forced expiratory volume in one second (FEVConclusion: The formulations of salbutamol dry powder aerosols with a fine lactose carrier produced a high deposition in the lower regions of the respiratory tract. Although the FEF

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110350
Author(s):  
Lijun Cheng ◽  
Yang Deng

Gastrodin (GAS) and its aglycone, p-hydroxybenzyl alcohol (HBA), are both bioactive compounds extracted from Gastrodia elata Blume (GEB). In the current Chinese pharmacopoeia, they are regarded as quality control markers for GEB. In this study, we developed a high-performance liquid chromatography method coupled with a diode array detector to quantify GAS and HBA concentrations in plasma following oral ingestion by rats. For the first time, GAS was detected in vivo after HBA administration. GAS and HBA both had similar pharmacological effects, but the influence of the glucose moiety resulted in different pharmacokinetic characteristics. In this study, the effects of GAS and HBA at different administration durations were investigated in zebrafish larvae. These compounds were found to induce a sedative effect but had different onset times. In conclusion, a biotransformation of HBA to GAS could be observed in the rats. This may be a new insight into the pharmacokinetic characteristics of these bioactive compounds and also relates to the different ways in which they take effect.


1995 ◽  
Vol 269 (2) ◽  
pp. R287-R293 ◽  
Author(s):  
N. Yamaguchi

The aim of the present study was to investigate if either dihydropyridine-sensitive L-type Ca2+ channels or cholinergic receptor-mediated mechanisms are implicated in endothelin-1 (ET)-induced adrenal catecholamine (CA) secretion in anesthetized dogs. ET was locally administered to the left adrenal gland via the left adrenolumbar artery. Plasma CA concentrations in adrenal venous and aortic blood were determined by a high-performance liquid chromatography method. In the control group, local infusion (1 min, 0.5 ml/min) of ET (the fixed total dose of 0.5 microgram given to the gland or approximately 0.0197 microgram/kg of body weight) resulted in a sharp increase in the basal CA output, followed by a rapid decline, and a relatively slow secondary response lasted over a period of 15-30 min. In the second group treated with nifedipine (5 micrograms or approximately 0.207 microgram/kg) similarly administered 10 min before ET infusion, the ET-induced first steep increase in CA output was significantly attenuated by approximately 75% (P < 0.05, n = 6). In dogs similarly receiving either pentolinium (1 mg or approximately 0.041 mg/kg) or atropine (0.5 mg or approximately 0.018 mg/kg), the ET-induced CA response remained unchanged. The results indicate that ET-induced adrenal CA release was largely mediated by the activation of dihydropyridine-sensitive L-type Ca2+ channels. Furthermore, neither nicotinic nor muscarinic receptors were functionally implicated in the CA response to ET. The study suggests the existence of noncholinergic mechanisms involved in the secretory action of ET on the adrenal medulla in the dog in vivo.


2020 ◽  
Vol 7 (1) ◽  
pp. 24-31
Author(s):  
Rajeshree Khambadkar ◽  
Selvan Ravindran ◽  
Digamber Singh Chahar ◽  
Srushti Utekar ◽  
Amlesh Tambe

Introduction: Resveratrol and its monooxygenated metabolite oxyresveratrol were the subject matter of intense research due to their medicinal value. Absorption, distribution, metabolism and excretion are important to understand the bioavailability and pharmacokinetic profile of resveratrol and oxyresveratrol. Quantification of resveratrol and oxyresveratrol is essential for both in vitro and in vivo studies. Methods: During in vitro drug metabolism studies, both qualitative and quantitative information are essential to understand the metabolic profile of resveratrol and oxyresveratrol. In the present study, a simple and stable method is outlined using high performance liquid chromatography to quantify both resveratrol and oxyresveratrol. This method is suitable to understand the metabolic stability, plasma stability, pharmacokinetics and toxicokinetics of resveratrol and oxyresveratrol. Results: Generally, in vitro incubation studies are performed at high concentrations and in vivo studies are carried out at both high and low concentrations, therefore high performance liquid chromatography method is demonstrated as a suitable technique to quantify resveratrol and oxyresveratrol. Conclusion: Retention time of resveratrol and oxyresveratrol from liquid chromatography qualitatively confirm its identity.


Author(s):  
Olga Yuryeva ◽  
Yuliya Kondratova ◽  
Liliya Logoyda

 Objective: A simple, rapid, and reproducible high-performance liquid chromatography method was developed for the simultaneous determination of amlodipine and valsartan in their combined dosage forms and for drug dissolution studies.Methods: A C18 column (Zorbax Eclipse ХDB-C18, 5 μm, 2.1 mm × 150 mm) and a mobile phase of water:acetonitrile:trifluoroacetic acid (55:45:0.1 v/v/v) mixture were used for separation and quantification. Analyses were run at a flow rate of 0.4 mL/min and at ambient temperature. The injection volume was 5 μL and the ultraviolet detector was set at 265 nm. The method was validated as per ICH guidelines.Results: Under these conditions, amlodipine and valsartan were eluted at 1.64 min and 4.08 min, respectively. Total run time was shorter than 7 min. The results were 99.6 ± 0.6 and 98.5 ± 0.8 for amlodipine and valsartan, respectively. Valsartan was released within 15 min (98.32%) and amlodipine was also released within 30 min (96.16%) both at a pH of 6.8.Conclusion: The developed method was applied successfully for quality control assay of amlodipine and valsartan in their combination drug product and in vitro dissolution studies.


Author(s):  
Rajasekhar Reddy Alavala ◽  
Prathusha Katahala ◽  
Ganapathi Thipparapu ◽  
Umasankar Kulandaivelu ◽  
Shireesha Boyapati ◽  
...  

Objective: Tacrine is a potent acetylcholine esterase inhibitor (AChEI), and curcumin has been recently proven to possess AChEI, amyloid β aggregation inhibitory activity in addition to its diverse pharmacodynamic nature. Tacrine undergoes biological transformation by cytochrome P450 (CYP 1A2) to a hydroxy metabolite, which is hepatotoxic. Curcumin is known for its inhibitory nature for various metabolic enzymes along with CYP1A2. The present study was undertaken to evaluate the influence of curcumin on the disposition kinetics of tacrine and to assess its impact on dosage regimen.Methods: It was hypothesized that the simultaneous administration of curcumin and tacrine can minimize the toxicity along with increased absorption of tacrine and curcumin into the biological system during the treatment of Alzheimer’s patients.Results and Discussion: Hence, an attempt was made to develop a simple, precise, accurate, and cost-effective reversed-phase high-performance liquid chromatography method for simultaneous determination of curcumin and tacrine and also to estimate the effect of curcumin on absorption of tacrine, in rat plasma.Conclusion: Concomitant administration of curcumin with tacrine improved the parameters such as Cmax and AUC, which indicates that the curcumin would improve the absorption of tacrine.


2008 ◽  
Vol 52 (9) ◽  
pp. 3047-3051 ◽  
Author(s):  
Stephanie J. Wallace ◽  
Jian Li ◽  
Craig. R. Rayner ◽  
Kingsley Coulthard ◽  
Roger L. Nation

ABSTRACT Colistin methanesulfonate (CMS) has the potential to hydrolyze in aqueous solution to liberate colistin, its microbiologically active and more toxic parent compound. While conversion of CMS to colistin in vivo is important for bactericidal activity, liberation of colistin during storage and/or use of pharmaceutical formulations may potentiate the toxicity of CMS. To date, there has been no information available regarding the stability of CMS in pharmaceutical preparations. Two commercial CMS formulations were investigated for stability with respect to colistin content, which was measured by a specific high-performance liquid chromatography method. Coly-Mycin M Parenteral (colistimethate lyophilized powder) was stable (<0.1% of CMS present as colistin) for at least 20 weeks at 4°C and 25°C at 60% relative humidity. When Coly-Mycin M was reconstituted with 2 ml of water to a CMS concentration of 200 mg/ml for injection, Coly-Mycin M was stable (<0.1% colistin formed) for at least 7 days at both 4°C and 25°C. When further diluted to 4 mg/ml in a glucose (5%) or saline (0.9%) infusion solution as directed, CMS hydrolyzed faster at 25°C (<4% colistin formed after 48 h) than at 4°C (0.3% colistin formed). The second formulation, CMS Solution for Inhalation (77.5 mg/ml), was stable at 4°C and 25°C for at least 12 months, as determined based on colistin content (<0.1%). This study demonstrated the concentration- and temperature-dependent hydrolysis of CMS. The information provided by this study has important implications for the formulation and clinical use of CMS products.


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