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Effects Of Combined Methotrexate On The Pharmacokinetics Of Biqi Capsule In Normal Rats

Posted on:2016-07-30Degree:MasterType:Thesis
Country:ChinaCandidate:Y Q LiFull Text:PDF
GTID:2134330461492957Subject:Clinical pharmacy
Abstract/Summary:PDF Full Text Request
Biqi includ Strychnos (modulation powder), Chen medicine Codonopsis, Atractylodes, Poria, Salvia, adjuvant Panax, Chuanxiong, Achyranthes, earthworm, and make medicine licorice. The side with BNI, Qufengchushi Huoxuezhitong effect. Its anti-inflammatory, analgesic, a very significant role in regulating the immune system, and effective. For the treatment of rheumatism, rheumatoid arthritis is often used in conjunction with Western medicine, can enhance its efficacy.Strychnos for dry mature seeds Loganiaceae plant Strychnosnux-vomica L. Marchand, the warm, bitter, big drug, Tongluozhitong, Sanjie swelling, numbness good except Pianku is pain to the drug. Strychnos although a significant effect, but it has a big drug, a small safe range, the small changes in the plasma concentration will reach therapeutic effect or produce toxic side effects. Therefore, to study the changes in the plasma concentration in the case of combination therapy is essential for rational drug use has an important role in guiding.From the point of view of clinical pharmacy legislation questions, select Biqi Strychni active ingredient rather brucine and disabilities as observed indicators of drug use in vitro dissolution under the joint, in vivo pharmacokinetics study drug were explored, mainly content and results are as follows:1. Artificial gastric juice in vitro dissolution test cases: â‘  Strychnos powder brucine and strychnine, persons belonging to burst dissolution, the dissolution of the largest brucine and strychnine disabilities were 2.60 mg and 4.64 mg, and elution amount at the time of 5mi n reached 2.36 mg and 4.27 mg, respectively, is the largest elution amount of 91% and 92%;â‘¡ Biqi group strychnine, persons affected due to the dissolution of the capsule shell, to 15mi n dissolution equilibrium is reached, followed by dissolution and Strychnos powder group similar to the dissolution profiles of these two groups were compared, f2 values were> 50, it indicates that the dissolution behavior Biqi Strychnos powder similar to the same kind of dissolution; â‘¢ 3 group co-administration group (Biqi with MTX and put into groups, the first group Biqi vote, the first vote MTX group) compared to just throw Biqi Group 2 index components f2 values were greater than 99, indicating that two kinds whether drugs while taking MTX or before the first service or service Biqi, methotrexate were no significant effect on the dissolution Biqi. This is to simulate the in vitro dissolution because, after combination therapy for Biqi whether in vivo pharmacokinetics dynamics have an impact, you need to do further experiments in vivo metabolism.2. The paper establishes the HPLC analysis of rat plasma rather brucine and disabilities, the parties are to meet legal verification index analysis requirements, specific, days brucine and strychnine with disabilities, day RSD values were less than 15%; different concentrations were greater than 60% recovery; the operation more convenient and suitable for in vivo drug brucine and strychnine quantitative analysis of pharmacokinetic requirements.3. In combination with methotrexate for Biqi dynamics influence of drug metabolism in normal rats:healthy rats were fed 0.216 g/kg Strychnos powder,0.432 g/kg Biqi first gavage 0.432 g/kg Biqi capsules after 30 min reperfusion with 3.6 mg/kg MTX, first orally 3.6 mg/ kg MTX reperfusion after 30 min to 0.432 g/kg Biqi, MTX and Biqi while after gavage pharmacokinetic comparison results show that strychnine:â‘  Dynamics affect Biqi strychnine in the pharmacokinetics of methotrexate (MTX): Methotrexate promote the absorption of strychnine, and to extend its elimination half-life, so that strychnine can continue role in the body, improve the outcome. The results reported in the literature in the two drugs can enhance the unity of rheumatoid arthritis clinical results from a clinical pharmacy provides an experimental basis for enhanced efficacy.â‘¡ combination therapy, the medication order two drugs metabolic behavior Biqi strychnine in vivo greater impact on the bioavailability of the size of the sort:Two drugs while taking> the first service of methotrexate (MTX)> first served Biqi> Biqi taken alone. The first group to take affect Biqi minimum; before taking MTX group and the two groups were also taking drugs to speed up the strychnine peak time Tmax, prolonging its half-life t1/2 (respectively, taken alone Biqi 7.01 fold and 9.68 fold) and in vivo residence time M RT, an increase of the maximum plasma concentration Cmax and AUC AUC, especially while changing the treatment group than more obvious. Therefore recommend the best way for the two drugs administered at the same time taking.â‘¢ combination should strengthen blood concentration monitoring. From the experimental results were also observed under the joint drug use because of the increased strychnine maximum plasma concentration Cmax, so the earlier group taking MTX or when taking the two drugs should be strengthened to monitor the plasma concentration, to prevent the occurrence of side effects.Through in vitro, in vivo in two parts, namely the impact of the in vitro dissolution studies in combination with methotrexate for Biqi and pharmacokinetics of normal rats for pharmacokinetic studies of combination therapy provides a certain case reference value, while this paper to further optimize clinical Biqi when administered in combination with methotrexate method, dosage, treatment provide experimental data in the case of combination therapy is recommended for patients with drug monitoring Blood Circulation to ensure drug safety,In this paper, based on actual clinical medicine, from a clinical point of view to study pharmacy, using pharmacokinetic method to effectively solve clinical use in combination therapy risk issues, practical, provide reference for the rational use of medicine containing Strychnos future.
Keywords/Search Tags:Biqi capsule, methotrexate(MTX), drug combination, brucine, strychnine, drug cumulative effect
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