• Bulletin of the Korean Chemical Society
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• v.27 no.7
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• pp.1025-1030
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• 2006

A 3D-CoMFA model with pranlukast analogues was constructed, which could be applied to predict the antagonistic activity of aryl benzyl ether analogues against LTD4. Molecular modeling and 3D-CoMFA studies were performed on 78 pranlukast analogues and 14 aryl benzyl ethers to evaluate the antagonistic behavior of aryl benzyl ethers and provide information for further modification of this kind of compounds. The aryl benzyl ether core was found to be in excellent three dimensional match with the central planar moiety of pranlukast analogues, and the pranlukast 3D-CoMFA model could be successfully applied to predict the biological activity of aryl benzyl ether analogues.

• Polymer(Korea)
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• v.36 no.1
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• pp.41-46
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• 2012

In this study, poly(ethylene glycol) (PEG) was used as a hydrophilic polymer carrier to develop solid dispersion formulations for enhancing solubility and dissolution rate of pranlukast, one of poorly soluble drugs that has been broadly used for the treatment of asthma. PEG based solid dispersions with or without poloxamer were prepared by hot melting and solvent evaporation methods. The resultant solid dispersions were characterized by DSC and powder X-ray measurements, and their morphological properties were observed to be partially changed to amorphous state with reduced crystallinity. Dissolution and solubility tests showed that the solubility and dissolution rate of the solid dispersions were significantly enhanced. The solid dispersion formulation prepared by the hot melting method with a chemical composition of pranlukast:PEG:poloxamer = 1:5:1 demonstrated the most enhanced solubility and dissolution rate. The results suggest that the solid dispersions based on PEG and poloxamer are promising systems for the enhancement of solubility and bioavailability of pranlukast.

• Polymer(Korea)
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• v.35 no.4
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• pp.277-283
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• 2011

Solid dispersion is mainly used for improved dissolution of poorly water-soluble drugs. Solid dispersion of pranlukast was prepared by spray-drying with plasdone S-630. When pH of water was high, pranlukast was highly soluble in the solubility experiment of solid dispersions with varying pH. The particle size of pranlukast particles in solid dispersions was measured to be in nanometers scale based on particle size analysis. Zeta-potential analysis confirmed the negative charge of solid dispersion. SEM was used to observe the surface of solid dispersion, which confirmed spherical morphology, DSC and XRD confirmed the amorphous nature of solid dispersions. The in vitro test was carried out to find improved dissolution rate of pranlukast solid dispersion in simulated juice gastric and a controlled experiment was carried out to compare pranlukast solid dispersions with a conventional drug (Onon$^{(R)}$), These results showed the dissolution properties of pranlukast solid dispersions prepared by spray drying proper for the oral pharmaceutical formulation.

• Tuberculosis and Respiratory Diseases
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• v.46 no.5
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• pp.697-708
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• 1999

Background : Leukotriene (LT) $C_4$, $D_4$, and $E_4$, the main components of slow-reacting substance of anaphylaxis (SRS-A), have been suggested to play an important role in bronchial asthma such as antigen-induced bronchoconstriction, airway hyperreactivity, and pulmonary eosinophil accumulation. The purpose of this study was to evaluate the effects of treatment with the cysteinyl-LTs (cys-LTs) antagonist, pranlukast on allergen-induced guinea pig asthma model. Methods : Guinea pigs of treatment and placebo groups were sensitized by subcutaneous injection of ovalbumin(OVA) and challenged by inhalation of aerosolized OVA (1% weight/volume OVA). Normal control group did not sensitize with OVA. Oral ingestion of pranlukast and normal saline to the treatment and placebo groups was performed. In the treatment and placebo groups, airway resistance was measured before and after oral ingestion. Serum $LTC_4$ and eosinophilic infiltration of the bronchiolar and peribronchiolar tissues were measured after ingestion in the treatment and placebo groups. Results : Allergen-induced airway constriction developed in 20 (8 in treatment group, 12 in placebo group) among 35 guinea pigs. Airway resistance was significantly decreased at 3 and 6 minutes after OVA challenge in the pranlukast treatment group. In the placebo group, there was no difference of airway resistance between before and after saline ingestion. Serum $LTC_4$ levels showed 348.4 pg/ml in the treatment group, 373.9 pg/ml in the placebo group, and 364.4 pg/ml in the control group. There were no statistically significant difference between treatment and placebo group (p=0.232), and treatment and control group (p=0.501). Eosinophilic infiltrations in the peribronchiolar region per one-microscopic field ($\times$400 high power fields) demonstrated 7.06 in the treatment group, 19.2 in the placebo group, and 4.50 in the control group. There was significant decrement of eosinophilic infiltration in the treatment group which was compared with placebo group (p=0.001). Conclusion : These results demonstrate that pranlukast, a cys-LTs receptor antagonist, can attenuate allergen induced early-phase bronchoconstriction and eosinophilic infiltration in the bronchiolar tissues.

• Journal of Integrative Natural Science
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• v.9 no.4
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• pp.228-233
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• 2016

Cysteinyl leukotrienes are inflammatory mediators having important role in pathophysiological conditions such as asthma and allergic rhinitis. CysLT1 receptor mediates most of the disease regulatory actions of the CysLTs and it is been implicated in a number of inflammatory conditions including gastrointestinal and cardiovascular diseases. Hence in the present study, molecular docking of CysLT1 was performed with its potent and orally efficacious antagonist CP-199330 and CP-199331. The aim of this study was to compare the interaction of CP-199330 and CP-199331 with known drugs such as Zafirlukast, Pranlukast and Montelukast which had already showed clinical efficacy in the treatment of asthma. The residues such as TYR83, GLN274, LYS311 and SER313 were found to interact with both the antagonist and the known drugs. Also, we noticed the docking scores and interaction of the antagonists were comparable with the known drugs. Hence these antagonists could serve as better drugs for the treatment of allergy.