Meta-analysis of efficacy and safety of sinomenine combined with methotrexate in treatment of rheumatoid arthritis / 中国中药杂志

To systemically evaluate the efficacy and safety of sinomenine combined with methotrexate(SIN+MTX) in the treatment of rheumatoid arthritis(RA). Literature databases of Wanfang, CNKI, VIP, SinoMed, PubMed, Cochrane Library and Web of Science were retrieved comprehensively for relevant clinical trials. The literature retrieval time was from database establishment to February 4, 2020. The quality of literatures was assessed by the Cochrane Evaluation Handbook 5.1.0, and qualified literature was reviewed and analyzed by using the RevMan 5.3 statistical software. Twenty randomized controlled trials met the inclusion criteria, and were enrolled in the Meta-analysis. The results showed that SIN+MTX remarkably reduced DAS28(MD=-0.85, 95%CI[-1.03,-0.67], P<0.000 01), and improved total efficiency(P<0.000 01). SIN+MTX could inhibit swollen joint count(MD=-1.19, 95%CI[-1.75,-0.63], P<0.000 1), tender joint count(MD=-1.58, 95%CI[-2.89,-0.28], P=0.02) and reduce morning stiffness time(MD=-8.44, 95%CI[-11.82,-5.07], P<0.000 01) compared with control group. The results showed that SIN+MTX was equal to control group in grip strength(SMD=0.20,95%CI[-1.11,1.51],P=0.77). SIN+MTX remarkably alleviated the erythrocyte sedimentation rate(MD=-9.87, 95%CI[-14.52,-5.22], P<0.000 1), C-reactive protein(SMD=-0.30, 95%CI[-0.51,-0.09], P=0.005), and rheumatoid factor(MD=-11.23,95%CI[-13.81,-8.65],P<0.000 01). The frequency of adverse reactions were reduced compared with that in the control group(P<0.000 01). Current clinical studies demonstrate that the efficacy and safety of SIN+MTX in the treatment of RA were superior to control group. However, due to the low quality and quantity of the included studies, high-quality randomized controlled trials are necessary to support the clinical evidences.

Inhibition of lipopolysaccharide-induced inflammation in RAW264.7 macrophages by sinomenine through regulating heme oxygenase-1 expression and autophagy / 中南大学学报(医学版)

To investigate the effect of sinomenine on lipopolysaccharide (LPS)-induced inflammation in RAW264.7 macrophages and the underlying mechanisms.
 Methods: The mouse RAW264.7 macrophages were treated with sinomenine and/or LPS with or without heme oxygenase-1 (HO-1) inhibitor Znpp. Real-time PCR, ELISA, immunofluenscence, and Western blot were used to detect the mRNA expression of TNF-α and IL-6, the release of TNF-α and IL-6, the protein expression of HO-1 and autophagy, respectively.
 Results: Compared with the control group, the mRNA expression and release of inflammatory cytokines TNF-α and IL-6 were increased, the green fluorescence of autophagy-related protein LC3 was accumulated and the protein expression of HO-1 was increased in RAW264.7 cells after LPS treatment (P<0.05). Compared with the LPS group, sinomenine treatment could reduce the mRNA expression and release of TNF-α and IL-6, accompanied by increasess in green fluorescence aggregation of LC3 and HO-1 production (P<0.05). HO-1 inhibitor Znpp could weaken the ability of sinomenine through suppressing TNF-α and IL-6 expression and decreasing the aggregation of LC3 green fluorescence (P<0.05).
 Conclusion: Sinomenine could alleviate LPS-induced inflammation in RAW264.7 macrophages, which might be related to HO-1 mediated autophagy. This study provides an experimental and theoretical basis for the clinical application of sinomenine in prevention and treatment of inflammation.

Preparation and evaluation of intra-articular injectable sinomenine hydrochloride-loaded in situ liquid crystals / 药学学报

Phytantriol (PT), ethanol (ET) and water were used to prepare in situ cubic liquid crystal (ISV2). The pseudo-ternary phase diagram of PT-ET-water was constructed and isotropic solution formulations were chosen for further optimization. The physicochemical properties of isotropic solution formulations were evaluated to optimize the composition of ISV2. In situ hexagonal liquid crystals (ISH2) were prepared based on the composition of ISV2 with the addition of vitamin E acetate (VitEA) and the amount of VitEA was optimized by in vitro release behavior. The phase structures of liquid crystalline gels formed by ISV2 and ISH2 in excess water were confirmed by crossed polarized light microscopy and small angle X-ray scattering, respectively. Rheological properties of ISV2 and ISH2 were studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using a dialysis membrane diffusion method. Pharmacokinetics was investigated by determination of sinomenine hydrochloride (SMH) concentration in synovial membrane after intra-articular injection of SMH-loaded ISH2 in adjuvant-induced arthritis rats. The optimal ISV2 (PT/ET/water, 64 : 16 : 20, w/w/w) loaded with 6 mg x g(-1) of SMH showed a suitable pH, injectable and formed a cubic liquid crystalline gel in situ with minimum water absorption in the shortest time. The optimal ISV2 was able to sustain the drug release for 144 h. The optimal ISH2 system was prepared by addition of 5% VitEA into PT in the optimal ISV2 system. This ISH2 (PT/VitEA/ET/water, 60.8 : 3.2 : 16 : 20, w/w/w/w) was an injectable isotropic solution with suitable pH. The new ISH2 was able to sustain the drug release for more than 240 h. Local pharmacokinetics study indicated that the retention time and AUC(0-∞) of ISH2 group were increased significantly compared with that of SMH solution group and the AUC(0-∞) of ISH2 group was 6.01 times higher than that of SMH solution group. The developed ISH2 was suitable for intra-articular injection that may apply to patients in the treatment of rheumatoid arthritis.

Influence of sinomenine on protein profiles of peripheral blood mononuclear cells from ankylosing spondylitis patients: a pharmacoproteomics study / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Ankylosing spondylitis (AS) is a common inflammatory rheumatic disease which lacks satisfactory treatment so far. Sinomenine (SIN) is an alkaloid and has recently been utilized in treating multiple rheumatic diseases including AS in China, but its exact mechanism remains to be explored. This study investigated the alteration of proteome in peripheral blood mononuclear cells (PBMCs) from AS patients.</p><p><b>METHODS</b>Thirty AS patients were enrolled in this study. PBMCs from each AS patient were cultured in medium with or without SIN respectively. Then PBMCs proteins from both groups were separated by two-dimensional electrophoresis (2-DE) and analyzed by mass spectrometry (MS). Two differentially expressed proteins were then chosen to be verified using Western blotting.</p><p><b>RESULTS</b>Seven proteins, including a-synuclein (SNCA), calmodulin (CALM), acidic leucine-rich nuclear phosphoprotein 32 family member A (ANP32A), chloride intracellular channel protein 1 (CLIC1), guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 (GNB1), gelsolin (GSN) and histone H2B type 1-M (HISTH2BM) were over-expressed, while coronin- 1A (CORO1A) was under-expressed in the SIN-treated PBMCs. Further bioinformatics search indicated that the changes of SNCA, ANP32A and CLIC1 pertained to apoptosis, while changes of GSN and CORO1A were associated with both apoptosis and inhibition of immunological function. Subsequently GSN and CORO1A were selected to validate by Western blotting and the results were consistent with those of 2-DE.</p><p><b>CONCLUSION</b>There were 8 differentially expressed proteins in the SIN-treated PBMCs, which might shed some light on the mechanism of SIN in the treatment of AS.</p>

Analgesic effect of sinomenine on SSNI model rats and monoamine neurotransmitters in striatal extracellular fluid / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the analgesic effect of sinomenine on the neuropathic pain rat model induced by SSNI, and discuss its impact on monoamine neurotransmitters in striatal extracellular fluid.</p><p><b>METHOD</b>Male SD rats were randomly divided into the sham operation group, the SSNI model group, the gabapentin group (100 mg x kg(-1)), the sinomenine high dose group (40 mg x kg(-1)) and the sinomenine low dose group (20 mg x kg(-1)). Mechanical hyperalgesia and cold pain sensitivity were evaluated by Von Frey hairs and cold spray. Striatum was sampled by microdialysis. High performance liquid chromatography-electrochemical detector (HPLC-ECD) were used to detect the content of such neurotransmitters as monoamine neurotransmitters noradrenaline (NE), dopamine (DA), 5-hydroxy tryptamine (5-HT) and their metabolites dihydroxyphenylacetic phenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA).</p><p><b>RESULT</b>SSNI model rats showed significant improvement in mechanical withdrawal threshold and cold pain sensitivity, significant decrease in intracerebral NE and notable increase in DA, 5-HT and their metabolites. Compared with the model group, the sinomenine high dose group showed significant increase in mechanical withdrawal threshold at 60, 90, 180 and 240 min after abdominal administration (P < 0.01), significant decrease in cold pain sensitivity score during 30-240 min (P < 0.05). Sinomenine can significantly up-regulated NE content in striatal extracellular fluid during 45-135 min (P < 0.05), remarkably reduce DA content and DOPAC at 45, 75 and 135 min (P < 0.05), 5-HT content during 45-135 min, DOPAC during 75-165 min (P < 0.05), and 5-HIAA during 45-135 min (P < 0.05).</p><p><b>CONCLUSION</b>Sinomenine has the intervention effect on neuropathic pain in SSNI model rats. Its mechanism may be related to disorder of monoamine neurotransmitters in striatal extracellular fluid.</p>

The role of sinomenine in treatment of allergic rhinitis mice model and its mechanism / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To explore the role of sinomenine in treatment of allergic rhinitis mice model and its possible mechanism.@*METHOD@#We used ovalbumin (OVA) to make allergic rhinitis model of BALB/c mice. Saline was used in the control group. When we challenged the mice with OVA intranasally, the mice in sinomenine treatment group were feed by the food containing sinomenine. Mice were then killed 24 h after the last OVA challenge. The noses of mice from each group were removed en bloc and fixed, then each section was stained with hematoxylin and eosin. ELISA assay was used to measure the concentration of anti-OVA IgE, IL-4 and IFN-gamma. The proteins expressive level of T-bet and GATA3 were examined.@*RESULT@#Nasal mucosa of the mice in sinomenine treatment group were not hyperplasia and without obvious infiltration of eosinophils. The concentration of anti-OVA IgE, IL-4 and IFN-gamma in the serum and T-bet and GATA3 expression levels of sinomenine treatment group were lower than those of allergic rhinitis group.@*CONCLUSION@#The sinomenine can be used to treat allergic rhinitis mice, and the mechanism may rely on the improvements of the Th1/Th2 imbalance.

Torsion of the gallbladder in pregnancy / 대한외과학회지

Torsion of the gallbladder is a rare condition that is difficult to diagnose preoperatively, but prompt surgical intervention is necessary to avoid possible sepsis and death. A 36-year-old pregnant woman presented to Emergency Department with a constant epigastric pain at 17 weeks of gestation. Abdominal ultrasonography and magnetic resonance imaging demonstrated a distended gallbladder that contained no stones but had mild wall thickening. Laparoscopic cholecystectomy using three ports was performed under the impression of an acalculous cholecystitis. The gallbladder was found to be rotated 180 degrees clockwise on gallbladder mesentery and to be gangrenous. The postoperative course was uneventful and the patient was discharged on the 4th day after surgery. It is important to keep in mind gallbladder torsion in the differential diagnosis from acute cholecystitis when the patient has an acute onset of abdominal pain and a severely distended gallbldder. Prompt cholecystectomy via a laparoscopic approach should be performed.

Effects of sinomenine and methotrexate on fibroblast-like synoviocytes in rheumatoid arthritis / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To investigate the effects of sinomenine (SIN) and methotrexate (MTX) on the proliferation and apoptosis of in vitro cultured fibroblast-like synoviocytes (FLS) in rheumatoid arthritis (RA) patients, as well as the expression of osteoclast differentiation factor in FLS.</p><p><b>METHODS</b>FLS were isolated from the synovium of RA patients and cultured in vitro. FLS were incubated with different concentrations of SIN and MTX respectively or combined: 0.001, 0.010, 0.100, 1.000 mg/mL SIN; 0.001, 0.010, 0.100, 1.000 mg/mL MTX; 0.001 mg/mL SIN + 0.001 mg/mL MTX, 0.010 mg/mL SIN + 0.010 mg/mL MTX, 0.100 mg/mL SIN + 0.100 mg/mL MTX, 1.000 mg/mL SIN + 1.000 mg/mL MTX, namely SIN1, 2, 3, 4 groups; MTX1, 2, 3, 4 groups and the combination 1, 2, 3, 4 groups. The medium without drugs was used as a control group. There was a total of 13 groups, each group with 3 complex holes. MTT was applied to detect the growth of FLS. The flow cytometry was applied to detect the apoptosis of FLS. The expressions of FLS receptor activator of nuclear factor kappa B ligand (RANKL) mRNA and osteoprotegerin (OPG) mRNA were observed by semi-quantitative RT-PCR.</p><p><b>RESULTS</b>Compared with the control group, RA FLS proliferation OD values of all the drug groups were lower (P < 0.05). The RA FLS apoptosis OD value of the combination 3 group increased, the OPG mRNA expression increased, the expression of RANKL mRNA decreased with statistical difference (P < 0.05). The RA proliferation OD values of the SIN3 group and the MTX3 group increased when compared with the combination 3 group (P < 0.05).</p><p><b>CONCLUSIONS</b>SIN and MTX had synergistic effects in inhibiting FLS. This might be one of the mechanisms for inhibiting RA bone damage.</p>

Investigation of articular cavity medicating for treatment of knee osteoarthritis / 中国骨伤

Osteoarthritis (OA) is a common chronic progressing disease in the elderly. In current there are many methods of drug treatment for knee osteoarthritis, the intra-articular injection belongs to local application, can direct effect on arthritis, is the most used and most effective methods in osteoarthritis treatment. A single medication may exist that anti-inflammatory effects produce a marked effect but articular cartilage injury is induced, or articular cartilage repairing are promoted but anti-inflammatory effects is not ideal. Therefore,the best method of treatment should be a comprehensive analysis of articular structure, function and possible pathogenic factor to understand the expectations of level of recovery and use in patients to design an individualized treatment plan.

Therapeutic effect of an injectable sustained-release sinomenine hydrochloride and sodium hyaluronate compound in a rabbit model of osteoarthritis / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>While intra-articular injection of sinomenine hydrochloride has a therapeutic effect on osteoarthritis, it has a short half-life, and is thermolabile and photolabile. The aim of this research was to evaluate the sustained-release of sinomenine hydrochloride from an injectable sinomenine hydrochloride and sodium hyaluronate compound (CSSSI) and its therapeutic effect in a rabbit model of osteoarthritis following intra-articular injection.</p><p><b>METHODS</b>An injectable compound consisting of 1% sodium hyaluronate and 2.5% sinomenine hydrochloride was prepared and kept as the experiment group, and 2.5% sinomenine hydrochloride was prepared and kept as the control group. The cumulative mass release was measured at different time points in each group in vitro. Sixty-five male Zelanian rabbits were randomly divided into five groups: 15 (30 knees) each for the control, sodium hyaluronate, sinomenine hydrochloride, and CSSSI groups respectively, and five (10 knees) for the modeling group. Papain was injected into both knees of each rabbit for model establishment. Subsequently, 0.2 ml of the corresponding drugs was injected into the articular cavities of the remaining experiment groups, while the control group was treated with 0.2 ml normal saline. All groups were treated once a week for 4 weeks. Seven days after the last treatment, knees were anatomized to perform pathological observations and Mankin's evaluation of the synovium. Four groups were compared using the SPSS 13.0 software package.</p><p><b>RESULTS</b>In the in vitro sustained-release experiments, 90% of the drug was released in the experiment group 360 minutes following the injection. Comparison of the Mankin's evaluations of the four groups illustrated statistical discrepancies (P < 0.05). In further paired comparisons of the CSSSI group vs. modeling control/sodium hyaluronate/sinomenine hydrochloride groups, statistical significance was uniformly obtained. Moreover, sodium hyaluronate and sinomenine hydrochloride treatments showed significant improvement over the modeling control (P < 0.05), whereas sodium hyaluronate vs. sinomenine hydrochloride comparison failed to reach significance (P > 0.05).</p><p><b>CONCLUSIONS</b>CSSSI has a sustained-release effect on sinomenine hydrochloride. Intra-articular injection of CSSSI was significantly better than the sole sodium hyaluronate or sinomenine hydrochloride for the treatment of osteoarthritis in a rabbit model.</p>

Determination of o-methylflavinantine in a Tibetan medicine Meconopsis quintuplinervia by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To develop an HPLC method for the determination of a Tibetan medicine Meconopsis quintuplinervia.</p><p><b>METHOD</b>A Hypersil-Keystone-C18 column (4.6 mm x 250 mm, 5 microm) was used with the isocratic elution of acetonitrile and 0.012% glacial acetic acid. The flow rate was 1.0 mL x min(-1), and the detection wavelength was set at 237 nm.</p><p><b>RESULT</b>The linear range of 0-methylflavinantine was 0.2-2.4 microg (r = 0.999 7). The average recovery was 96.26%.</p><p><b>CONCLUSION</b>The developed method was reliable, and can be used for the quality control of M. quintuplinervia Regel.</p>

Hyponatremia Induced Coma during Risperidone Treatment in 2 Cases of Schizophrenia / 대한정신약물학회지

Antipyschotics have been frequently reported being associated with hyponatremia. We have experienced two cases of severe hyponatremia with neurological symptoms in patients with acute schizophrenia who were treated with risperidone. Case 1 was a 33-year-old female who developed hyponatremia (Na+114 mEq/L) at 17 days after initiation of treatment with risperidone. Case 2 was a 41-year-old female who developed hyponatremia (Na+107 mEq/L) 5 months after treatment with risperidone. In both cases, polydipsia was not obvious. The exact cause of hyponatremia was uncertain, but we suggest that syndrome of inappropriate secretion of antidiuretic hormone due to risperidone may be the mechanism of hyponatremia in both cases. Although there have been many recent studies about the pathophysiology of hyponatremia among psychiatric patients, the exact mechanism remains unclear. There have been many case reports in the literature of hyponatremia associated with antipsychotics. We suggest that risperidone may be a potential drug that can cause hyponatremia and lead to life-threatening neurological symptoms in the early stage treatment, and that clinicians should monitor patients on a regular basis.

A Case of Transient Psychosis after Sustained Release Bupropion Overdose / 대한정신약물학회지

Bupropion is a unique antidepressant with enhancing both noradrenergic and dopaminergic neurotransmission without altering serotonergic system. Given its pharmacodynamics and structural similarity to amphetamine, the possibility of bupropionrelated psychosis has been reported. The authors describe a 22-year-old woman who presented psychotic symptoms after taking 10 tablets of sustained release bupropion (bupropion SR) 150 mg (total 1,500 mg) and lorazepam 0.5 mg (total 5 mg). Visual hallucinations developed at 17 hours after overdose, while paranoid ideation and aggressive behaviors developed at 24 hours after overdose. The psychotic symptoms remitted on the fifth day of antipsychotics treatment. She remained psychiatrically stable without any clinically significant symptoms during 3-month follow-up. This case raises issue about the possible relationship between bupropion overdose and transient psychosis.

Extranodal NK/T Cell Lymphoma Accompanied by Heavy Eosinophilic Infiltration and Peripheral Blood Eosinophilia, Involving Skeletal Muscles

The patient was a 52-year-old female with swelling in both lower legs and peripheral blood eosinophilia. Biopsy specimen revealed the heavy infiltration of eosinophils with sparse small lymphocytes showing mild atypia. The diagnosis was Kimura disease. The symptoms including eosinophilia were relieved by steroid treatment. At 17 months from initial biopsy, the patient developed swelling of the buttock. At 25 months, fever and dyspnea with multiple lung nodules developed. Wedge resection revealed multiple aggregates of CD3(+), CD56(+), Epstein-Barr virus(+) large atypical lymphocytes with necrosis. The patient was finally diagnosed with extranodal NK/T cell lymphoma (NKTL). Epstein-Barr virus in situ hybridization retrospectively performed on the previous biopsies demonstrated Epstein-Barr virus infection in small CD3(+) lymphocytes. The patient expired after 26 months despite chemotherapy. Blood eosinophilia correlated well with disease activity during the clinical course. This case shows not only unusual histologic features, which hampered the correct diagnosis, but also a unique clinical manifestation of NKTL.

Extranodal NK/T Cell Lymphoma Accompanied by Heavy Eosinophilic Infiltration and Peripheral Blood Eosinophilia, Involving Skeletal Muscles

The patient was a 52-year-old female with swelling in both lower legs and peripheral blood eosinophilia. Biopsy specimen revealed the heavy infiltration of eosinophils with sparse small lymphocytes showing mild atypia. The diagnosis was Kimura disease. The symptoms including eosinophilia were relieved by steroid treatment. At 17 months from initial biopsy, the patient developed swelling of the buttock. At 25 months, fever and dyspnea with multiple lung nodules developed. Wedge resection revealed multiple aggregates of CD3(+), CD56(+), Epstein-Barr virus(+) large atypical lymphocytes with necrosis. The patient was finally diagnosed with extranodal NK/T cell lymphoma (NKTL). Epstein-Barr virus in situ hybridization retrospectively performed on the previous biopsies demonstrated Epstein-Barr virus infection in small CD3(+) lymphocytes. The patient expired after 26 months despite chemotherapy. Blood eosinophilia correlated well with disease activity during the clinical course. This case shows not only unusual histologic features, which hampered the correct diagnosis, but also a unique clinical manifestation of NKTL.

A Case Report of a Gastric Cancer Patient with a Good Quality of Life after Radiotherapies to 17 Metastases for 4 Years / 대한방사선종양학회지

Five and half years ago, a 45-year-old female metastatic gastric cancer patient underwent a metastatectomy and chemotherapy. Over the last 4 years and 2 months, she received radiotherapy for every new distant metastasis with intermittent TS-1 oral chemotherapy. She received 8 courses of radiotherapy at 17 metastatic sites for more than 4 years. Metastatic sites which received a curative radiation dose achieved and maintained local control. The patient is now 51 years of age and lives without difficulty in performing her daily activities.

Research progress on immunosuppressive activity of monomers extracted from Chinese medicine / 中国中药杂志

The clinical or experimental study proves that Chinese medicine such as Tripteryglum wilfordii, Lignum Sappan, Caulis Sinomenii, Radix Trichosanthis and Herba Artemisiae Annuae have good immunosuppressive activity. Further researches on the immunosuppressive active components from Chinese medicine have been the main direction in recent years. The recent researches on immunosuppressive effect and possible mechanisms for the monomers such as triperine, triptolide, bazilein, potosappanin A, sinomenine, trichosanthin and artemisinin extracted from those Chinese medicine are introduced in this review.

Rat in vitro plasma-binding percentage determination of sinomenine hydrochloride by using microdialysis method and ultrafiltration / 中国中药杂志

<p><b>OBJECTIVE</b>To assess feasibility of plasma protein-binding percentage by using microdialysis method.</p><p><b>METHOD</b>Sinomenine hydrochloride was selected as model drug. The in vitro rat plasma protein-binding percentage of three kinds of concentration was determinated by using microdialysis sampling tool and HPLC-UV. At the same time the classical study method, such as ultrafiltration method, was also used to determinate the protein-binding percentage to compare the difference between the two methods.</p><p><b>RESULT</b>The in vitro rat plasma protein-binding percentage of sinomenine hydrochloride using microdialysis method was about 26% and kept relative stable at the concentration range. There was no significant difference between the two methods.</p><p><b>CONCLUSION</b>The results shows that the binding percentage is relative low. Microdialysis method is a new method for the study of protein-binding degree.</p>

Effect of sinomenine on tumor necrosis factor-alpha and nuclear factor-kappaB in the heterotopic tissue in rats with endometriosis / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effect of sinomenine on the level of tumor necrosis factor-alpha (TNF-alpha) and nuclear factor-kappaB (NF-kappaB) and in the heterotopic tissue in rats with endometriosis.</p><p><b>METHODS</b>The rats with endometriosis were divided into sinomenine lavage group, blank control group, model group and danazol group, and the levels of TNF-alpha and NF-kappaB in the heterotopic tissues of the rats were detected with immunohistochemistry.</p><p><b>RESULTS</b>Sinomenine lavage and danazol treatment both significantly decreased the levels of levels of TNF-alpha and NF-kappaB in the heterotopic tissues of the rats as compared with the model group (P<0.05), and lesions were significantly smaller in sinomenine lavage group than in danazol group.</p><p><b>CONCLUSION</b>Sinomenine can inhibit the production and activity of TNF-alpha and NF-kappaB to suppress the adhesion, implantation, infiltration and growth of the endometrial cells in the rat model of endometriosis.</p>

Preparation of sinomenine hydrochloride delayed-onset sustained-release tablets / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare sinomenine hydrochloride delayed-onset sustained-release tablets.</p><p><b>METHOD</b>The tablets containing sinomenine hydrochloride were prepared by dry-compression coating technique with the ratio of HPMC in core tablet and the ratio of HPMC in coating film as the influence factors and the lag-time and release rate as the evaluation parameters. Experiments were done on the central composite design, the data were simulated by using multi-linear equation and second-order polynomial equation. The possibly optimal formulation was predicted by response surface method. The dissolution date (lag-time and release rate) of the tablets prepared under the optimum condition were compared with the predicted. The drug released mechanism of the tablet were studied by Model-fitted of drug released within 6-15 h with zero-order, Higuchi and Peppas equation, respectively.</p><p><b>RESULT</b>The lag-time and release rate were simulated using second-order polynomial equation, regression coefficients of the two parameters were 0.9901 and 0.9876, respectively. Bias between the observed and predicted values of lag-time and release rate were -3.15% and -0.34%, respectively. The lag-time of the tablet prepared under the optimum condition in vitro was about 6 h, then drug released from the tablet within 6-15 h was found to conform to zero-order kinetics and was controlled by bulk erosion mechanism.</p><p><b>CONCLUSION</b>Sinomenine hydrochloride delayed-onset sustained-release tablets release drug slowly after lag time. The models developed in this study are proved to be highly predictable.</p>