AbstractIn this study, we investigated the effects of certain respiratory drugs, which are mainly used on human serum paraoxonase‐1 (hPON1; EC 3.1.8.1). hPON1 was purified from human serum, with 354.91 fold and 45% yield by using two simple step procedures including, first, ammonium sulfate precipitation, then, Sepharose‐4B‐l‐tyrosine‐1‐naphthylamine hydrophobic interaction chromatography. SDS‐polyacrylamide gel electrophoresis showed a single protein band belonging to hPON1 with 43 kDa. All the pharmaceutical compounds inhibited the PON1 enzyme highly at the micromolar level. The obtained IC50 values for nine different pharmaceutics ranged from 0.219 μM (salbutamol sulfate) to 67.205 μM (montelukast sodium). So, all drugs could be considered as potent hPON1 inhibitors. Ki values and inhibition types were determined by Lineweaver‐Burk graphs. While varenicline tartrate and moxifloxacin hydrochloride inhibited the enzyme in a noncompetitive manner, others inhibited it in a mixed manner.

01 Jan 2011·BioMed Research International

Effects of Theophylline on Anesthetized Malignant Hyperthermia‐Susceptible Pigs

Article

Author: Gerbershagen, Mark U. ; Fiege, Marko ; Weisshorn, Ralf ; Kolodzie, Kerstin ; Wappler, Frank

Background. Theophylline was shown to induce contracture development in porcine malignant hyperthermia (MH) susceptible (MHS) skeletal muscles in vitro. The purpose of the current study was to investigate the in vivo effects of theophylline in MHS and MH normal (MHN) swine.Methods. MH‐trigger‐free general anesthesia was performed in MHS and MHN swine. Theophylline was administered intravenously in cumulative doses up to 93.5 mg·kg−1. The clinical occurrence of MH was defined by changes of central‐venous pCO2, central‐venous pH, and body core temperature.Results. Theophylline induced comparable clinical alterations in the anesthetized MHS and MHN swine, especially in regard to hemodynamic data. No pig developed hypermetabolism and/or MH according to defined criteria. All animals died with tachycardia followed by ventricular fibrillation.Conclusions. The cumulative theophylline doses used in this study were much higher than doses used therapeutically in humans, as demonstrated by measured blood concentrations. Theophylline is thus not a trigger of MH in genetically determined swine.

15 Aug 2006·International Journal of Pharmacology

Effect of Bio-adhesive Polymers like HPMC, Gelatin, Na-CMC and Xanthan Gum on Theophylline Release from Respective Tablets

Author: Islam, Kazi Mehedul ; Shaheen, Sharif Mohammad ; Rashid, Mamunur ; Hossen, Nazir Md. ; Amran, Shah Md. ; Ahmed, Maruf

In order to evaluate the feasible application of bio-adhesive polymers like HPMC-15 cps and 50 cps; gelatin; Na-CMC and xantham gum in sustained release dosage form (SRDF), tablets containing various amount of bio-adhesive polymers with a model drug like anhydrous Theophylline sodium glycinate were prepared by compression in a hydraulic press (Perkin Elmer) compression machine using 5 ton pressure.The release characteristics of Theophylline (TH) from sustained release tablets were analyzed in triplicate using a thermal shaker (Memmert) with a shaking speed of 50 rpm at 37±0.5°C in 250 mL of simulated gastric fluid without enzyme for 8 h.At the end of 8 h of dissolution it was found that 61.60% (for 300 mg HPMC-15 cps) and 42.92% (for 500 mg HPMC-15 cps) of TH was released from HPMC-15 cps based tablets, resp.When HPMC-15 cps was increased to 50 cps, 52.12 and 59.66% of TH was released, resp.Both concentration and viscosity depended sustained release of TH was found.74.13 And 94.15% of TH was released from Gelatin based SR tablets of the same concentrations, resp.Gelatin also showed the same concentration effects i.e. release was reduced with an increase in concentration of polymer.52.40 And 50.95% of TH was released from Na-CMC based SR tablets of the same concentrations, resp. and that of 76.96 and 78.26% of TH from xanthan gum based tablets.It means that there was no remarkable concentration effect of these two polymers on the TH release.In all cases there was almost zero order release fashion.Bio-adhesive polymers like HPMC and gelatin might be successfully applicable in SRDF rather than Na-CMC and xanthan gum studied here.

100 Deals associated with Theophylline Sodium Glycinate

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KEGG	Wiki	ATC	Drug Bank
D06104	-	R03DA04	-

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Indication	Country/Location	Organization	Date
Asthma	China	Dandong Yichang Pharmaceutical Co., Ltd.	01 Jan 1995
Bronchitis	China	Dandong Yichang Pharmaceutical Co., Ltd.	01 Jan 1995
Pulmonary Edema	China	Dandong Yichang Pharmaceutical Co., Ltd.	01 Jan 1995

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