Improved Static Compression Behaviors and Tablettabilities of Spherically Agglomerated Crystals Produced by the Spherical Crystallization Technique with a Two-Solvent System

Purpose. Poorly compressible crystals of acebutolol hydrochloride were agglomerated by the spherical crystallization technique with a two-solvent system to improve the compressibility for direct tabletting. The mechanism of improvements in static compression behaviors and tablettabilities of the spherically agglomerated crystals were investigated. Methods. The improvement of static compression behaviors of the agglomerated crystals was determined by measuring the stress relaxations and elastic recoveries of compressed powder of original and agglomerated crystals. The improved tablettability of agglomerated crystals was evaluated by the pressure transmission ratio upon compression, the ejection pressure for releasing the tablet from the die and the tablet strength, i.e., tensile strength required for breaking. Results. The higher relaxation pressure and the lower elastic recovery of the agglomerated crystals than of the original crystals were found. The pressure transmission ratio data showed that the friction pressures of the two crystals were similar during the compression period. The ejection pressure of the agglomerated crystals was lower than that of the original crystals. The tensile strength of the tablet of agglomerated crystals was greater than that of the original crystals. Conclusions. The compressibility and tablettability of the spherically agglomerated crystals prepared by the spherical crystallization technique were much improved due to their increased plastic property and reduced adhesive property compared to the original crystals.     

Acute and chronic losartan administration: effect on angiotensin II content and modulation of [3H]norepinephrine release from rat interscapular brown adipose tissue

Summary To determine if acute or chronic (21 days) losartan (10mg/kg, s.c.) regulates the renin-angiotensin system in interscapular brown adipose tissue, angiotensin II (AII) content and [³H]overflow from slices preloaded with [³H]norepinephrine were examined. Acute or chronic losartan administration had no effect on AII content. AII increased evoked [³H]overflow from slices from control rats. Losartan administration did not alter basal [³H]outflow or evoked [³H]overflow. Acute losartan administration inhibited AII-induced enhancement of evoked [³H]overflow. Tolerance developed to the inhibitory effect of losartan following chronic administration.Supported by a grant from the American Heart Association (Local Kentucky Affiliate) and by a gift from DuPont Merck Pharmaceuticals. Portions of this work have been presented in abstract form [The Pharmacologist 34(3): 157, 1992]     

心房颤动犬心房肌细胞2型理阿诺受体的分布和表达

目的探讨心房颤动(房颤)时心房肌细胞2型理阿诺受体表达和分布的改变。方法杂种犬10只,分为正常对照组和单纯房颤组,每组5只。单纯房颤组用起搏器进行房颤式快速起搏,起搏频率(500±20)次/min,正常对照组不植入起搏器。24周后取出心脏,用逆转录聚合酶链反应、免疫荧光染色技术检测犬心房肌细胞2型理阿诺受体在mRNA水平的表达和蛋白水平的表达和分布。结果与正常对照组比较,单纯房颤组犬2型理阿诺受体在mRNA和蛋白水平的表达明显低于正常对照组(P<0.05);在细胞质、细胞膜2型理阿诺受体分布均显著减少。结论房颤时心房肌细胞2型理阿诺受体表达下调,2型理阿诺受体可能不是心房肌细胞主要的钙信号调控的受体。     

微囊化吲哚美辛片剂的研讨

以明胶-CAP 为囊材,经复凝聚法制备吲哚美辛微囊,再按所筛选的最佳处方制备微囊化片剂。该片与市售片相比,体外 T_(50)延长约5.6倍,家兔体内达峰时间滞后,能明显减轻对大鼠胃的刺激性。     

Release of neuroactive substances: homocysteic acid as an endogenous agonist of the NMDA receptor

Summary Sulfur containing amino acids such as homocysteic acid (HCA), cysteinsulfinic acid, homocysteinsulfinic acid are released by depolarization of slices from various rat brain regions in a Ca⁺⁺-dependent manner. L-HCA excites caudate neurons through their N-methyl-D-aspartic acid (NMDA) receptor and potentiates their cortically evoked excitatory postsynaptic potentials.³⁵S-methionine can label the releasable pool of HCA, and thus appears as a precursor of HCA. Thus HCA is a transmitter candidate which acts predominantly on the NMDA receptor.     

Functional outcome and general health status in patients after arthroscopic release in adhesive capsulitis

Frozen shoulder is said to be a self-limiting entity but full recovery often takes more than 2 years. For that, most patients are unwilling to tolerate painful restriction while awaiting resolution. We prospectively investigated 30 patients (16 women, 14 men) for the outcome of arthroscopic capsular release in idiopathic frozen shoulder. Results were determined by the assessment of subjective and objective parameters to estimate both shoulder function and general health status. Symptoms persisted without improvement for a minimum of 6 months of conservative treatment. Preoperative average American shoulder and elbow surgeons score (ASES) was 35, visual analog scale (VAS) to measure pain was 7, and simple shoulder test (SST) was 4. Mean scores of the physical component of SF-36 were considerably reduced. Mean forward elevation was 85°, average abduction was 70°, mean internal rotation was 15°, and mean external rotation was 10°. Patients were followed-up at 6 weeks, 3, 6, 12 months and by a mean of 36 months. Range of motion for all planes improved (P < 0.05). Median VAS reduced to 2, average ASES increased to 91, and SST enhanced to a mean of 10 (P < 0.05). We stated improvement of the physical components in the SF-36 questionnaire in particular bodily pain and the role-physical score. There were no significant differences between the measurements in the early postoperative phase compared to the mid-term follow-up (P > 0.05). Our results demonstrate that arthroscopic release of refractory idiopathic frozen shoulder combined with a gentle manipulation provides reliable expectations for improvement in both clinical and general health status for most patients. We recommend the use of a limb-specific and a general-health-status questionnaire to conclude the benefit of the surgical intervention and contribute the optimization of a therapy concept more effectively.     

手术及综合康复治疗膝关节僵直

目的 探讨膝关节纤维性僵直手术及围手术期、术后综合康复治疗的方法和意义.方法 26例膝关节纤维性僵直患者,采用髌骨外上方小切口,辅助关节镜下行关节内粘连松解,并结合徒手推拿松解.术前进行心理宣教,术后第2天开始经止痛泵维持在CPM机上行慢速全范围关节活动度功能锻炼,并行主被动伸屈膝功能锻炼、髌骨内推训练.结果 术后平均随访19个月(8～32个月),膝关节活动度从术前平均32°增至113°,平均提高81°.无皮肤坏死、创口裂开、肌腱断裂、骨折等并发症发生.结论 关节镜辅助下小切口松解治疗膝关节纤维性僵直的手术操作简单,创伤小,康复快.膝关节僵直围手术期及术后综合康复治疗,对膝关节功能恢复有重要意义.     

火把花根片对哮喘豚鼠气道炎症抑制作用的实验研究

目的 研究火把花根片对哮喘豚鼠气道炎症的作用。方法 建立哮喘豚鼠动物模型。豚鼠17只随机分为2组，即对照组(8只)和火把花根组(9只)。测定支气管肺泡灌洗液(BAIF)细胞总数、嗜酸性粒细胞、淋巴细胞、中性粒细胞数量及蛋白浓度，图像分析软件测定气道壁厚度及腺体厚度。结果 火把花根组BAIF细胞总数、嗜酸性较细胞为主的炎性细胞数量及蛋白浓度均低于对照组(P＜0．01)，图像分析表明火把花根组气道壁厚度及腺体厚度均较对照组减低(P＜0．01)。结论 火把花根片可抑制哮喘豚鼠的气道慢性炎症，对支气管哮喘有治疗作用。     

Comparison of Quantiferon-TB Gold With Tuberculin Skin Test for Detecting Latent Tuberculosis Infection Prior to Liver Transplantation

Screening for latent tuberculosis infection (LTBI) is recommended prior to organ transplantation. The Quantiferon-TB Gold assay (QFT-G) may be more accurate than the tuberculin skin test (TST) in the detection of LTBI. We prospectively compared the results of QFT-G to TST in patients with chronic liver disease awaiting transplantation. Patients were screened for LTBI with both the QFT-G test and a TST. Concordance between test results and predictors of a discordant result were determined. Of the 153 evaluable patients, 37 (24.2%) had a positive TST and 34 (22.2%) had a positive QFT-G. Overall agreement between tests was 85.1% (kappa= 0.60, p < 0.0001). Discordant test results were seen in 12 TST positive/QFT-G negative patients and in 9 TST negative/QFT-G positive patients. Prior BCG vaccination was not associated with discordant test results. Twelve patients (7.8%), all with a negative TST, had an indeterminate result of the QFT-G and this was more likely in patients with a low lymphocyte count (p = 0.01) and a high MELD score (p = 0.001). In patients awaiting liver transplantation, both the TST and QFT-G were comparable for the diagnosis of LTBI with reasonable concordance between tests. Indeterminate QFT-G result was more likely in those with more advanced liver disease.     

The expression of somatostatin receptors 1 and 2 in benign,pre‐malignant and malignant laryngeal lesions

The expression of somatostatin receptors 1 and 2 in benign, pre‐malignant and malignant laryngeal lesions The role of chemotherapy in squamous cell carcinoma of the larynx has not been clearly defined. Whilst toxic chemotherapy regimes may confer a marginal improvement in survival, surgery and radiotherapy remain the mainstay of treatment. Somatostatin is a naturally occurring peptide, which exerts antiproliferative and antiangiogenic effects via five membrane‐bound receptor subtypes. The expression of somatostatin receptor subtypes (SSTRs) 1 and 2 was studied in benign, pre‐malignant and malignant laryngeal specimens. Epithelial expression of SSTR1 was detected in 4/6 (67%) Reinke's oedema, 5/6 (83%) pre‐malignant and 8/12 (67%) malignant specimens, with virtually no stromal or vascular expression. High levels of epithelial SSTR2 expression were noted in all Reinke's oedema specimens, compared with low‐to‐moderate levels in only 2/6 (33%) pre‐malignant and 3/12 (25%) malignant specimens (P < 0.01). This ‘loss’ of epithelial SSTR2 expression may provide a growth advantage in pre‐malignant and malignant laryngeal lesions. Vascular expression of SSTR2 was ubiquitous in all groups, with scant stromal expression. Overall, most (>80%) pre‐malignant and malignant laryngeal specimens expressed at least one of the two SSTR subtypes studied. Somatostatin analogues may have a therapeutic role in squamous cell carcinoma of the larynx.