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Simultaneous Determination of n-acetyl Cysteine and Taurine by HPTLC Method in Active Pharmaceutical Ingredient and Pharmaceutical Dosage Form

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American Journal of Analytical Chemistry 2017年第11期8卷 742-751页

作者： A. R. Magesh Magharla Dasaratha Dhanaraju GIET School of Pharmacy Rajahmundry India

Specific, precise and sensitive TLC-Densitometric method was developed and validated for the simultaneous estimation of n-acetyl cysteine and Taurine in active pharmaceutical ingredient and pharmaceutical dosage form. An effective separation was achieved on pre-coated silica gel HPTLC plates by using n-butanol:acetic acid:water (8:0.5:1.5 v/v/v). The spots were scanned densitometrically at 295 nm. The RF values of n-acetyl cysteine and Taurine were found to be 0.29 and 0.52, respectively. Calibration curves were linear in the range of 30 - 180 and 100 - 600 ng/band for n-acetyl cysteine and Taurine, correspondingly with correlation coefficients of 0.999. The developed method was validated as per ICH guidelines. The limits of detection were 11.24 and 63.40 ng/spot for nAC and TAU respectively. The method developed was found to be precise and specific for the simultaneous analysis of n-acetyl cysteine and Taurine in pure and tablet dosage form.

关键词： High Performance Thin Layer Chromatography n-acetyl Cysteine Taurine Validation

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Reversal Effects of n-acetyl Cysteine on <i>Moringa oleifera</i>Leaves-Induced Sub-Acute Hepatotoxicity in Wistar Albino Rats

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neuroscience & Medicine 2019年第4期10卷 385-397页

作者： Josephine n. Kasolo Agnes namaganda Godfrey S. Bbosa Haruna Muwonge Robert Lukande Joshua nfambi Ivan Kimuli Isaac Okullo Department of Medical Physiology College of Health Sciences Makerere University Kampala Uganda Department of Pharmacology and Therapeutics College of Health Sciences Makerere University Kampala Uganda Department of Pathology College of Health Sciences Makerere University Kampala Uganda Department of Dental Surgery College of Health Sciences Makerere University Kampala Uganda

Background: M. oleifera is a highly valued medicinal plant used widely from time immemorial to treat various ailments. However, with continued un-standardized use of the plant leaves, studies have reported organ toxicity to the liver, kidney and the heart. As communities continue to use M. oleifera leaves for its medicinal and nutritional values, there is need to find an antidote for its hepatotoxicity. Aim: The study established the reversal effect of n-acetyl Cysteine (nAC) on M. oleifera aqueous leaf extract-induced hepatotoxicity in Wistar albino rats. Methods: Twenty-four (24) rats received a toxic dose (8.05 g/kg bwt) of M. oleifera leaf extract for 28 days to cause sub-acute hepatotoxicity. They were divided into 4 groups of 6 rats each. Group I received 1 ml normal (control group), Group II received 1000 ng/kg nAC, Group III received 1200 mg/kg nAC and Group IV received 1500 mg/kg nAC. Another group of 6 rats (Group V) received 0.75 mg/kg Paracetamol to cause hepatotoxicity. Group V (a positive control) received the prescribed clinical dose of 1200 mg/kg nAC which reverses the hepatotoxicity. All the nAC doses were given once a day intragastric for 7 days. On days: 1, 3 and 7 of receiving nAC, liver serum enzymes and bilirubin were measured. On day 7 the animals were sacrificed and liver tissue harvested for histopathology analysis. Results: A dose of 8.05 g/kg of M. oleifera leaf extract and 0.75 mg/kg Paracetamol were able to induce hepatotoxicity in Wister albino rats in 28 days. The M. oleifera extract induced hepatotoxic rats treated with nAC at doses of 1000 mg/kg, 1200 mg/kg and 1500 mg/kg, had a reduction in mean serum liver enzymes, plus reduced mean serum bilirubin levels. The liver histopathological analysis showed reduced inflammation after treatment with nAC for 3 and 7 days in the M. oleifera and paracetamol induced hepatotoxic rats. Conclusion: nAC can reverse M. oleifera leaf aqueous extract-induced sub-acute hepatotoxicity in Wistar Albino r

关键词： M. oleifera Sub-Acute Hepatotoxicity n-acetyl Cysteine Wistar Albino Rat

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Amelioration of hepatotoxicity by biocleavable aminothiol chimeras of isoniazid: Design, synthesis, kinetics and pharmacological evaluation

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World Journal of Hepatology 2018年第7期10卷 496-508页

作者： neha Vithal Bhilare Suneela Sunil Dhaneshwar Kakasaheb Ramoo Mahadik Department of Pharmaceutical Chemistry Poona College of Pharmacy Bharati Vidyapeeth University

AIM To overcome the hazardous effects on liver caused by long-term use of antitubercular agent isoniazid(InH) by developing a novel hepatoprotective prodrug strategy by conjugating InH with aminothiols as antioxidant promoities for probable synergistic *** InH was conjugated with n-acetyl cysteine(nAC) and n-(2)-mercaptopropionyl glycine using the SchottenBaumann reaction and with L-methionine using Boc-anhydride through a biocleavable amide linkage. Synthesized prodrugs were characterized by spectral analysis, and in vitro and in vivo release studies were carried out using HPLC. Their hepatoprotective potential was evaluated in male Wistar rats by performing liver function tests, measuring markers of oxidative stress and carrying out histopathology *** Prodrugs were found to be stable in acidic(pH 1.2) and basic(pH 7.4) buffers and in rat stomach homogenates, whereas they were hydrolysed significantly(59.43%-94.93%) in intestinal homogenates over a period of 6 h. Upon oral administration of prodrug nI to rats, 52.4%-61.3% InH and 47.4%-56.8% of nAC were recovered in blood in 8-10 h. Urine and faeces samples pooled over a period of 24 h exhibited 1.3%-2.5% and 0.94%-0.9% of nAC, respectively, without any presence of intact nI or InH. Prodrugs were biologically evaluated for hepatoprotective activity. All the prodrugs were effective in abating oxidative stress and re-establishing the normal hepatic physiology. The effect of prodrug of InH with nAC in restoring the levels of the enzymes superoxide dismutase and glutathione peroxidase and abrogating liver damage was noteworthy especially. COnCLUSIOn The findings of this investigation demonstrated that the reported prodrugs can add safety and efficacy to future clinical protocols of tuberculosis treatment.

关键词： Aminothiols antioxidants n-acetyl cysteine n-(2-mercaptopropionyl)glycine isoniazid L-methionine liver injury tuberculosis

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