White crystalline powder
rhizomes of Ligusticum chuanxiong Hort.
Pyrazine, tetramethyl-, hydrochloride/Pyrazine, 2,3,5,6-tetramethyl-, hydrochloride (1:1)/tetramethylpyrazine hydrochloride/T6N DNJ B1 C1 E1 F1 &&HCl/Ligustrazine hydrochloride/2,3,5,6-tetramethylpyrazine hydrochloride/Tetramethylpyrazine hydrochloride (1:1)/Ligustrazine HCl,hydrochloride/Ligustrazine Hydrochloride
192.7ºC at 760mmHg
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provides coniferyl ferulate(CAS#:76494-51-4) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Management of chronic pain is restricted by the lack of effective tools. This study evaluated the efficacies of sinomenine combined gabapentin or ligustrazine hydrochloride in treating peripheral and central chronic neuropathic pain. The study was conducted in mice with photochemically induced sciatic nerve injury, and in rats with photochemically induced spinal cord injury. For assessing the effectiveness of combined therapy, sinomenine, gabapentin or ligustrazine hydrochloride was injected intraperitoneally (i.p.), and pain behavioral tests were performed. At sub-effective dosages, pre-administration of sinomenine (for 60 min) plus gabapentin or ligustrazine hydrochloride, generated significant anti-allodynic effects in mice or rats with peripheral or central neuropathic pain. However, these effects were abolished when gabapentin or ligustrazine hydrochloride was pre-administered, and then sinomenine was given 60 min later. The combined efficacies of sinomenine and gabapentin or ligustrazine hydrochloride, cannot be blocked or reversed by the naloxone, suggesting the underlying mechanism is not mediated by opioid receptors. Moreover, following repeated treatments, sinomenine and gabapentin combination increased the baseline mechanical threshold, while generating prolonged analgesia, without introducing notable side effects. Sinomenine can enhance the efficacy of gabapentin or ligustrazine hydrochloride in rodent models of peripheral or central neuropathic pain, without introducing tolerance or other notable side effects. Findings of current study suggest that combing sinomenine and gabapentin or ligustrazine hydrochloride could be highly beneficial in neuropathic pain therapies.
Copyright © 2019 Elsevier B.V. All rights reserved.
Drug combination; Gabapentin; Ligustrazine hydrochloride; Neuropathic pain; Sinomenine
Sinomenine facilitates the efficacy of gabapentin or ligustrazine hydrochloride in animal models of neuropathic pain.
Gao T1, Shi T2, Wiesenfeld-Hallin Z3, Li T4, Jiang JD5, Xu XJ6.
2019 Jul 5
This study investigates the preparation of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres. This experiment investigates effects of the ratio of carboxymethyl chitosan and collagen blend, water to oil ratio, stirring speed, and other factors on the microsphere properties. The experiment had the following conditions: a 1:2 proportion of carboxymethyl chitosan and collagen, a 1:2 proportion of drugs and materials, a 5:1 proportion of oil phase and water phase, 0.5% of span80, a 600r/min stirring speed, 3 ml of a cross-linking agent, 3 h of cross-linking curing, 1.25 ± 0.05 mm diameter LTH microcapsules, a 54.08% envelop rate, and a 14.16% carrier rate. The microspheres release rate reached 66% within 1 h, then steadily released within 5 h in vitro. The experimental results showed that the ligustrazine hydrochloride microsphere production process was stable and exhibited a good release effect compared with other ligustrazine hydrochloride tablets and pills.
carboxymethyl chitosan; collagen; ligustrazine hydrochloride; micro spheres
Development of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres: Formulation optimization, characterization, and vitro release.
Lin Q1, Huo Q2, Qin Y1, Zhao Z1, Tao F2.
2017 Jan 2
The purpose of this study was to compare the pharmacokinetic profile of tetramethylpyrazine hydrochloride (TMPH) in rat plasma and tissues following intravenous (iv), intragastric (ig) and intraocular (io) administration. After io, ig and iv administration of a single dose at 10 mg/kg, tissue and plasma samples drawn from the femoral artery were collected at timed intervals. The concentration of TMPH in the samples was analyzed using high-performance liquid chromatography (HPLC). The area under the concentration-time curve (AUC) and the drug targeting efficiency percentage (DTE(%)) were calculated to evaluate the targeting efficiency of the drug with the three different administration routes. After io administration, TMPH was rapidly absorbed to reach its peak plasma and brain concentration within 5 min. The systemic bioavailability obtained with io administration was greater than that obtained through the ig route (63.22% vs. 16.88%). The AUCt rank order of the iv administration group was AUCkidney >AUCheart >AUCliver >AUCbrain >AUCspleen >AUClung; that of the ig administration group as AUCkidney >AUCliver >AUCheart >AUCspleen >AUCbrain >AUClung; while that of the io administration group was AUCkidney >AUCbrain >AUCheart >AUCliver >AUCspleen >AUClung. The ratio of the AUCbrain value between the io route and iv injection was 1.05, which was greater than that obtained after ig administration (0.30). The DTE after io administration was calculated: brain (165.72%), heart (97.76%), liver (113.06%), spleen (105.31%), lung (163.40%) and kidney (135.31%). The io administration group showed obvious drug transport to the brain. These results indicate that TMPH is rapidly absorbed from the eye into the systemic circulation, and there may be a direct translocation pathway for TMPH from the eye to the brain. Therefore, io administration of TMPH could be a promising alternative to intravenous and oral approaches.
Tetramethylpyrazine hydrochloride; bioavailability; intraocular administration; pharmacokinetics; tissue distribution
Intraocular administration of tetramethylpyrazine hydrochloride to rats: a direct delivery pathway for brain targeting?
Mao D1,2, Li F1, Ma Q1, Dai M1, Zhang H1, Bai L1, He N1,3,4,5.
Ligustrazine (hydrochloride) is a natural product.IC50 value:Target:In vitro: Ligustrazine hydrochloride displayed a protection effect on injured ECV304 cells, NOS and NO formation were significantly increased compared with the model group .In vivo: