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Gao R.,Shenyang Pharmaceutical University | Ren T.,Shenyang Pharmaceutical University | Feng J.,Shenyang Pharmaceutical University | Wang J.,Shenyang Pharmaceutical University | And 3 more authors.
European Journal of Lipid Science and Technology | Year: 2013

A lipid emulsion delivery system was developed to improve the anti-inflammatory and anti-nociceptive activities of dexketoprofen. The dexketoprofen isopropyl ester (DE) lipid emulsion (DEE) with a particle size of 208.1±33.1nm and a charge of -34.81mV was administered to rats and then compared with dexketoprofen injection solution (DS). There was no statistical significance in their pharmacokinetic parameters. The anti-inflammatory effect of DEE was evaluated by experiments involving egg-albumin-induced paw edema in rats and xylene-induced ear swelling in mice. In the paw edema test, the swelling of the DEE group recovered quickly from 1 to 3h (p<0.05), compared with the DS group. In the ear swelling test, the inhibition rate produced by DEE and DS was 57.79 and 28.57%, respectively. Acetic acid-induced abdominal constriction and hot-plate experiments were used to evaluate the peripheral and central anti-nociceptive actions of DEE. In the acetic acid-induced abdominal constriction test, DEE significantly restrained the writhing responses with a pain inhibition rate of 66.38% compared with 30.06% for the DS group. In the hot-plate test, both preparations had a similar pain threshold increasing percentage. This study shows that the anti-inflammatory and anti-nociceptive activities of dexketoprofen are markedly improved after incorporation into a lipid emulsion. Practical applications: Dexketoprofen is an important drug for the management of inflammation and treatment of pain. However, its commercial preparations have usually been applied to treat diseases which are less serious because of their limited efficiencies. In this study, the anti-inflammatory and anti-nociceptive activities of dexketoprofen are markedly improved by incorporating its prodrug into the lipid emulsion. Therefore, the lipid emulsion preparation can be used to treat more kinds of inflammation and pain in clinic. The efficacy of dexketoprofen could be improved by its prodrug in lipid emulsion because the emulsion drops could accumulate in the inflamed tissue and release more dexketoprofen after degradation. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Choi D.-H.,Chosun University | Piao Y.-J.,Shenzhen Salubris Pharmaceuticals Co. | Choi E.-J.,Chosun University | Choi J.-S.,Chosun University
Biomolecules and Therapeutics | Year: 2011

The aim of this study was to investigate the effect of amlodipine on the pharmacokinetics of warfarin after oral and intravenous administration of warfarin in rats. Warfarin was administered orally (0.2 mg/kg) or intravenously (0.05 mg/kg) without or with oral administration of amlodipine (0.1 or 0.4 mg/kg) in rats. The effect of amlodipine on the P-glycoprotein (P-gp) as well as cytochrome P450 (CYP) 3A4 activity was also evaluated. Amlodipine inhibited CYP3A4 enzyme activity with 50% inhibition concentration (IC 50) of 9.1 μM. Compared to those animals in the oral control group (warfarin without amlodipine), the area under the plasma concentration-time curve (AUC) of warfarin was significantly greater (0.1 mg/kg, p<0.05; 0.4 mg/kg, p<0.01) by 26.5-53.5%, and the peak plasma concentration (C max) was significantly higher (0.4 mg/kg, p<0.05) by 26.2% after oral administration of warfarin with amlodipine, respectively. Consequently, the relative bioavailability of warfarin increased by 1.26-to 1.53-fold and the absolute bioavailability of warfarin with amlodipine was significantly greater by 61.7-72.5% compared to that in the control group (47.4%). In contrast, amlodipine had no effect on any pharmacokinetic parameters of warfarin given intravenously. Therefore, the enhanced oral bioavailability of warfarin may be due to inhibition of CYP 3A4-mediated metabolism in the intestine and/or liver rather than renal elimination and P-gp by amlodipine. © 2011 The Korean Society of Applied Pharmacology. Source


Sun Y.,Sun Yat Sen University | Chen J.,Sun Yat Sen University | Chen X.,Shenzhen Salubris Pharmaceuticals Co. | Huang L.,Sun Yat Sen University | Li X.,Sun Yat Sen University
Bioorganic and Medicinal Chemistry | Year: 2013

A series of Tacrine-Homoisoflavonoid hybrids were designed, synthesised and evaluated as inhibitors of cholinesterases (ChEs) and human monoamine oxidases (MAOs). Most of the compounds were found to be potent against both ChEs and MAO-B. Among these hybrids, compound 8b, with a 6 carbon linker between tacrine and (E)-7-hydroxy-3-(4-methoxybenzylidene)chroman-4-one, proved to be the most potent against AChE and MAO-B with IC50 values of 67.9 nM and 0.401 μM, respectively. This compound was observed to cross the blood-brain barrier (BBB) in a parallel artificial membrane permeation assay for the BBB (PAMPA-BBB). The results indicated that compound 8b is an excellent multifunctional promising compound for development of novel drugs for Alzheimer's disease (AD). © 2013 Elsevier Ltd. All rights reserved. Source


Trademark
Shenzhen Salubris; Pharmaceuticals Co. | Date: 2013-05-07

Pharmaceutical preparations, for treating diseases of cardiovascular system, for use in haematology, dermatology, ophthalmology and gastroenterology, anti-infectives, antitumor drugs, for treating metabolic diseases, for treating nervous system diseases, for treating diseases of respiratory system, digestive system, endocrine system and immune system, for treating hypersensitivity diseases and for treating musculo-skeletal disorders; Chemico-pharmaceutical preparations, for the prevention and treatment of disorders of the nervous system, the immune system, the cardiovascular system, the metabolic system, the respiratory system, the musculo-skeletal system, digestive system and endocrine system, for the treatment of infective diseases, for use in dermatology, oncology, hematology and in tissue and organ transplantation, in ophthalmology and for treating hypersensitivity diseases; Chemical preparations for pharmaceutical purposes, for treating diseases of cardiovascular system, for use in haematology, dermatology, ophthalmology and gastroenterology, anti-infectives, antitumor drugs, for treating metabolic diseases, for treating nervous system diseases, for treating diseases of respiratory system, digestive system, endocrine system and immune system, for treating hypersensitivity diseases and for treating musculo-skeletal disorders; Medicines for human purposes, for treating diseases of cardiovascular system, for use in haematology, dermatology, ophthalmology and gastroenterology, anti-infectives, antitumor drugs, for treating metabolic diseases, for treating nervous system diseases, for treating diseases of respiratory system, digestive system, endocrine system and immune system, for treating hypersensitivity diseases and for treating musculo-skeletal disorders; Medicated troches, for the prevention and treatment of disorders of the nervous system, the immune system, the cardiovascular system, the metabolic system, the respiratory system, the musculo-skeletal system, digestive system, and endocrine system, for the treatment of infective diseases, for use in dermatology, oncology, hematology and in tissue and organ transplantation, in ophthalmology and for gastroenterological disorders; Active pharmaceutical ingredients in the nature of pharmaceutical preparations, which are used for the prevention and treatment of disorders of the nervous system, the immune system, the cardiovascular system, the metabolic system, the respiratory system, the musculo-skeletal system, digestive system, and endocrine system, for the treatment of infective diseases, for use in dermatology, oncology, hematology and in tissue and organ transplantation, in ophthalmology and for gastroenterological disorders; Prepared Chinese medicines, for treating diseases of cardiovascular system, for use in haematology, dermatology, ophthalmology and gastroenterology, anti-infectives, antitumor drugs, for treating metabolic diseases, for treating nervous system diseases, for treating diseases of respiratory system, digestive system, endocrine system and immune system, for treating hypersensitivity diseases and for treating musculo-skeletal disorders; Biochemical medicines, for treating diseases of cardiovascular system, for use in haematology, dermatology, ophthalmology and gastroenterology, anti-infectives, antitumor drugs, for treating metabolic diseases, for treating nervous system diseases, for treating diseases of respiratory system, digestive system, endocrine system and immune system, for treating hypersensitivity diseases and for treating musculo-skeletal disorders; Dietetic substances adapted for medical use, namely, beverages or food in the nature of vitamin, protein, minerals, lecithin, glucose, amino acid, folic acid, fruit juice, fruit oil, honey, seaweed glue, fish oil, cod-liver oil, cubilose, and mineral food-supplements, which are used for treating diseases of cardiovascular system, for use in haematology, dermatology, ophthalmology and gastroenterology, anti-infectives, antitumor drugs, for treating metabolic diseases, for treating nervous system diseases, for treating diseases of respiratory system, digestive system, endocrine system and immune system for treating hypersensitivity diseases and for treating musculo-skeletal disorders; Drugs for medical purposes, namely, medicines for the prevention and treatment of disorders of the nervous system, the immune system, the cardiovascular system, the metabolic system, the respiratory system, the musculo-skeletal system, digestive system, and endocrine system, for the treatment of infective diseases, for use in dermatology, oncology, hematology and in tissue and organ transplantation, in ophthalmology and for gastroenterological disorders.


Li A.-Z.,Shenzhen Salubris Pharmaceuticals Co. | Xu W.-J.,Shenzhen Salubris Pharmaceuticals Co.
Acta Crystallographica Section E: Structure Reports Online | Year: 2014

The title compound (trivial name moexipril hydrochloride) crystallizes as the acetonitrile monosolvate, C27H35N2O7 + Cl- C2H3N, with the salt comprising a U-shaped cation and a chloride anion. The conformation of the cation is stabilized by a weak intramolecular N+-H⋯O hydrogen bond and the tetrahydropyridine ring adopts a boat conformation. The dihedral angle between the planes of the benzene rings is 85.6(1)°. In the crystal, the cations and anions form tight ionic pairs by strong intermolecular O-H⋯Cl hydrogen bonds. C-H⋯Cl and C-H⋯N hydrogen bonds link these ionic pairs and the acetonitrile solvate molecules into puckered layers parallel to (100). Source

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