Clinical treatmemt of pheumonia with nifedipine

AIM: To study efficacy of nifedipine(Nif) treating pneumonia. METHODS: In experimental group, 44 cases were given routine treatment and simultaneously took supplementarily Nil (0.3-0.5 mg·kg~(-1)) tid, for 3d. In control group, 30 cases were given routine treatment.     

Study of the Complexation Behaviour of Fexofenadine with β-Cyclodextrin

Fexofenadine is a selective histamine H(1) receptor antagonist, used for relief of the symptoms of allergy. However its aqueous solubility is very poor. Solid inclusion complexes of fexofenadine and β-cyclodextrin were prepared at the molar ratios of 1:1 and 1:2 by kneading, and coprecipitation methods to improve its solubility. Characterization of the complexes was performed using infrared spectroscopy, X-ray diffractometry, and in vitro dissolution studies. Fexofenadine was found to exhibit interaction with β-cyclodextrin both in solid and liquid state. Phase solubility studies indicated that fexofenadine forms a stable complex with β-cyclodextrin. Both IR spectroscopy and X-ray diffractometry studies indicated interaction of fexofenadine with β-cyclodextrin. Kneading method at 1:1 and co-precipitation method at 1:1 and 1:2 molar ratios showed significant interaction. In vitro dissolution studies confirmed the same results.     

Acute exacerbation of psychosis with buspirone?

We report a patient with schizophrenia who suffered an acute exacerbation of psychosis when treated with buspirone to alleviate anxiety. This psychotic reaction appeared to be dose dependent. Discontinuing buspirone resulted in a rapid improvement of psychotic symptoms. Re-introduction of buspirone at a modest dose helped to alleviate anxiety without exacerbating his schizophrenic symptoms. The other case studies of psychosis due to buspirone are reviewed and possible mechanisms for this association are discussed, particularly the role of dopamine and serotonin.     

Reduction of bitterness of antihistaminic drugs by complexation with β-cyclodextrins

Reduction of bitterness of antihistaminic drugs by cyclodextrin (CyD) complexation was examined. The stability constant (Kc) of the 1:1 CyD inclusion complexes with antihistaminic drugs increased in the order of 2-hydroxypropyl-β-CyD (HP-β-CyD) ≈ β-CyD > γ-CyD > α-CyD for diphenhydramine and epinastine, and HP-β-CyD ≈ β-CyD > α-CyD > γ-CyD for hydroxyzine, cetirizine, and dl-chlorpheniramine. The inclusion complexes inhibited the adsorption of antihistaminic drugs to lipid membrane using liposomes, as the magnitude of Kc increased. From human gustatory sensation tests, β-CyD and HP-β-CyD potently suppressed the bitterness of antihistaminic drugs in a dose-dependent manner. Further, an artificial taste sensor analysis revealed that β-CyD and HP-β-CyD inhibited the bitterness of antihistaminic drugs in solution. The results suggest that CyDs suppress the bitterness of antihistaminic drugs in solutions through the formation of inclusion complexes. These results may provide useful information for masking or elimination of bitterness of drugs using CyDs.     

Interaction of Puerarin with Phospholipid in Solid Dispersion

Aim:To study the interaction of puerarin(PU) with phospholipid(PL)in solid dispersion.Methods:PU/PL solid dispersion was prepared with solvent evaporation and the interaction between PU and PL was studied by analysis of their ultraviolet spectra,infrared spectra,1H NMR spectra and thin layer chromatogram.Results:In chloroform the maximum absorption peak of pu in PU/PL mixture was located at 243nm,but 251nm for that of PU in solid dispersion.Howerver in methanol,QU in mixture or solid dispersion had the same maximum absorption peak location in ultraviolet spectra.Compared with the infrared spectra of mixture,that of solid dispersion showed the specific absorption peak location of berzene ring framework in PU molecule was markedly changed,the stretching vibration peak of P=O in PL molecule was shifted to high wavernumbers and the stretching vibration peak of C=C in PL molecule was disappeared.In 1H NMR spectra,most of the signals form PU in solid dispersion were weaken markedly or disappeared and the signals from the polar part of PL molecule were significantly changed.PU and PL in solid dispersion could be spearated on silica gel plate with the mixed solvent of chloroform,methanol and water (65:25:5)or ethyl acetate and methanol(10:1).Conclusion:In solid dispersion the benzene ring framework of PU molecule could act with the polar part and unsaturated part of PL molecule through charges transfer,and the interacted part could be surrounded by fat chains of PL molecule.     

Prevention of vascular structural changes with antihypertensive therapy

<正> The primary aim of antihypertensive therapy is to reduce or normalize blood pressure of the patients, so that we can lower the incidence of morbidity and mortality which are related to cardiovascular complications due to hypertension. It is also desirable that antihypertensive treatments can prevent or reverse cardiovascular changes, so that after a certain treat ment period, it may be possible to withdraw the treat ments without the risk of hypertension. However, most studies to date have shown that withdrawal of treat ments usually resulted in rebound hypertension, with the re-establishment of hypertension within a very     

The condensation of γ-butyrolactone with ethyl acetate

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 22, No. 12, pp. 1465–1469, December, 1988.     

Announcement of new partnership with the Blackwell Publishing

InanewcollaborationwiththeBlackwellPublishing，theShanghaiInstituteofMateriaMedica(SIMM)，ChinesAcademyofSciences(CAS)，andtheChinesePharmacologicalSociety，arepleasedtoannounceanewpublishinpartnership.AsofDecember2004BlackwellwillbeginpublicationoftheActaPharmacologicaSinica(APS)，theofficialjournaofSIMM，CAS，andtheChinesePharmacologicalSociety.EditedbyAcademicianKai－xianCHEN，APSendeavorstopromotepharmacologicalresearchandaimstobecomaninternationaljournalofgreatinfluencei…     

Study of the dissolution characteristics of oxazepam via complexation with β-cyclodextrin

Complex formation of oxazepam and β-cyclodextrin in solution was studied by phase solubility and spectral shift methods. The value of the apparent stability constant, K_c, calculated using these techniques, was 205 and 498 M⁻¹, respectively. Solid complexes of oxazepam and β-CD were prepared using the kneading and spray-drying methods. These complexes led to an improvement in the dissolution rate over free oxazepam, spray-drying being the most efficient technique. These complexes were characterized by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray diffraction.     

Irreversible blockade of β-adrenergic receptors with a bromoacetyl derivative of pindolol

Summary A potent irreversible -adrenergic derivative of pindolol possessing a chemically reactive group (Br-AAM-pindolol) was synthesized. This compound devoid of agonist properties, competed for all (³H)-dihydroalprenolol (³H-DHA) binding sites in C₆ glioma cell and rat cerebellum membranes. Pretreatment of C₆ glioma cell membranes with Br-AAM-pindolol and subsequent washing resulted in a time- and dose-dependent blockade of -adrenergic receptors. A 50% blockade was achieved in the presence of 1.6 nM Br-AAM-pindolol.This blockade occurs specifically at the -adrenergic receptor level, as: 1) it induced a decrease of maximal isoproterenol stimulated adenylate cyclase activity with no modification of basal and sodium fluoride stimulated activity and 2) decreases of (³H)-DHA binding and stimulation of adenylate cyclase activity by the agonist were suppressed in the presence of isoproterenol, a -adrenergic agonist. Furthermore, Br-AAM-pindolol treatment did not affect (³H)-diazepam binding in C₆ glioma cell membranes.Pretreatment of C₆ glioma cells with Br-AAM-pindolol also reduced the response of adenylate cyclase to isoproterenol and the number of -adrenergic receptors. The blockade of -adrenergic receptors of C₆ glioma cells by Br-AAM-pindolol was non-competitive, whereas the blockade obtained with AM-pindolol, a derivative of pindolol devoid of alkylating properties, was competitive.The irreversible blockade of -adrenergic receptors by Br-AAM-pindolol in rat erythrocyte membranes was substantiated by the demonstration that no recovery of -adrenergic receptors occurred during long term incubation of the membranes (48 h) following Br-AAM-pindolol treatment and subsequent washing.Double reciprocal plotting of equiactive isoproterenol concentrations in dose-response curves of adenylate cyclase from membranes of control and Br-AAM-pindolol treated C₆ glioma cells permitted calculation of the dissociation constant for isoproterenol from its binding sites (1.5±0.2×10^–7 M, n=11). This is very close to the dissociation constant of the agonist derived from binding experiments (1.7±0.5×10^–7 M, n=13).These results suggest that Br-AAM-pindolol is a potent irreversible -adrenergic antagonist and may be useful for pharmacological and physiological studies of -adrenergic receptors.     

Expression of β-catenin in lung tissues of mice with pulmonary fibrosis

目的 观察β-连环蛋白在肺纤维化模型小鼠肺组织中的表达.方法 昆明小鼠40只随机均分成实验组和对照组,气管内分别一次性注入博来霉素5 mg/kg(0.04 ml)和生理盐水0.04 ml.给药后第3、7、14、28天,每组处死小鼠5只,取肺组织做病理切片和HE染色;用碱水解法检测肺组织羟脯氨酸含量,免疫组化法及Western blot检测肺组织中β-连环蛋白表达.结果 实验组肺泡炎和肺纤维化程度均明显高于对照组(P＜0.05),羟脯氨酸的含量在第7-28天明显高于对照组(P＜0.01).实验组在各时间点肺组织中的β-连环蛋白表达高于对照组(P＜0.05);其表达高峰在第14天.结论 β-连环蛋白在模型小鼠肺纤维化发生过程中存在高表达.     

Characteristics of 10 kDa protein in sera of patients with myasthenia gravis

Background and purpose: Myasthenia gravis (MG) is an autoimmune disease of the neuromuscular junction characterized by increased fatigability and weakness of skeletal muscles, and is caused by the autoantibodies against acetylcholine receptor (AChR).However, levels of the antibody against AChR in sere are poorly related to severity of the disease.The opinion that the antibody against AChR is not only pathogenic factor of myasthenia gravis has been accepted, multiple factors and their interrelation     

Topical treatment of actinic keratosis with fluorouracil: is irritation associated with efficacy?

Actinic keratoses (AKs) are common dysplastic epidermal lesions that share clinical, histologic, and molecular features with squamous cell carcinoma. Therapeutic options include destructive modalities (i.e., cryosurgery, curettage) or topical fluorouracil treatment. The efficacy of topical fluorouracil for the treatment of widespread AK lesions has been demonstrated in multiple studies, but treatment is often associated with significant skin irritation. Various approaches to decrease irritation while maintaining efficacy have been attempted, including altered treatment regimens, combination therapies, and variations in vehicle formulations. Recently, a novel topical fluorouracil cream that contains 0.5% 5-fluorouracil in a microsphere vehicle has been approved for the treatment of AK. Data demonstrate that this low-dose formulation is effective in reducing AK lesions while maintaining a tolerable irritation profile.