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.     

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。     

苏云金芽孢杆菌以色列变种发泡块剂灭白纹伊蚊幼虫的效果研究

目的：比较苏云金芽孢杆菌Bti－951发泡块剂（由本所研制）和Bti－Ft发泡块剂（德国提供）灭白纹伊蚊效果。方法：模拟现场试验和现场试验。结果：室内生物测定，Bti－951发泡块剂LD50为0.2365μg／ml；Bti－Ft发泡块剂LD50为0．0903μg／ml。在3．4～3．7m2现场水池中，两种发泡块剂使用剂量为0．5、1．0、1．5g／m2，制剂24小时灭蚊效果均达100％；当剂量为1．5g／m2时，Bti-951发泡块剂持效15天，Bti－Ft可达20天。结论：该剂型运用于小型水体，便于贮存、携带和使用，比乳剂、粉剂持效更长。     

Pharmacokinetics of Controlled Release and Immediate Release Morphine Sulphate Tablets after a Single Dose and Multiple Doses in Chinese Volunteers

健康志愿者１０名，随机交叉口服硫酸吗啡控释片（ＣＲＭＳ）３０ｍｇ（３０ｍｇ×１）和硫酸吗啡普通片（ＩＲＭＳ）２０ｍｇ（１０ｍｇ×２），分别于服药前后各时点取静脉血，用ＧＣＭＳ测定血浆中吗啡含量。以药代软件程序处理，分别求得ＣＲＭＳ和ＩＲＭＳ的Ｃｍａｘ为１９．３８±３．８０和２１．２７±６．２１ｎｇ／ｍｌ；ｔｍａｘ为２．３６±０．３７ｈ和０．５５±０．１６ｈ；ｔ１／２β为３．５３±０．８７ｈ和３．０３±０．７４ｈ，曲线下面积ＡＵＣ为１４５．１５±１７．６５和９３．０８±１６．６５ｎｇ·ｈ／ｍｌ。癌症病人多次口服硫酸吗啡至稳态，ＣＲＭＳ和ＩＲＭＳ的峰浓度分别为２７．４３±０．３３ｎｇ／ｍｌ，２２．６８±０．１６ｎｇ／ｍｌ；谷浓度分别为１９．４５±１．４４ｎｇ／ｍｌ；１８．１４±０．４９ｎｇ／ｍｌ。     

白松片对慢性应激抑郁模型大鼠行为学及血浆CORT、ACTH的影响

目的：观察白松片对慢性应激抑郁大鼠模型行为学和血浆CORT、ACTH含量的影响。方法：SD雄性大鼠28只随机分为空白对照组、模型对照组、氟西汀对照组及白松片试验组，选用慢性轻度不可预见性应激加孤养造模，观察各组大鼠敞箱实验和液体消耗等行为学指标变化，采用放射免疫方法检测大鼠血浆皮质醇(CORT)和促肾上腺皮质激素(ACTH)含量。结果：慢性应激抑郁大鼠体重增加缓慢，敞箱实验中的水平运动、垂直运动得分、清洁动作次数显著减少，中央格停留时间显著延长；糖水消耗明显下降，纯水消耗显著增多，而且其血浆皮质醇和促肾上腺皮质激素含量增加。氟西汀和白松片均显著改善慢性应激抑郁大鼠模型的行为学和神经内分泌变化。结论：慢性轻度不可预见性应激可使大鼠行为及神经内分泌发生异常改变，引起抑郁状态，白松片对此具有一定拮抗作用。     

金芪降糖片联合西药治疗糖尿病对患者血浆ET-1和sICAM-1水平的影响

目的：探讨金芪降糖片对糖尿病患者血浆ET-1和sICAM-1水平的影响及临床应用价值。方法：金芪降糖片和降糖类西药同时服用治疗糖尿病，并与只服西药治疗组进行比较。采用酶联免疫法检测两组患者治疗前后血浆中血管内皮细胞活性因子ET-1和sICAM-1水平，同时观察血糖和血脂、HbA1c等各项指标的变化。结果：金芪组治疗后血糖和血脂、HbA1c均有显著变化（P〈0．05），对照组仅血糖有明显变化（P〈0．05）；金芪组治疗后ET-1和sICAM-1均显著降低，分别为P〈0．05和P〈0．01，对照组两者水平皆无明显变化（P〉0．05）。结论：金芪降糖片通过降低糖尿病患者血浆中ET-1和s／CAM-1水平，从而保护患者的血管内皮细胞，在西药常规治疗糖尿病的基础上，再加以中药辨证施治，可以提高临床对糖尿病的疗效。     

藿香正气片增强镇静催眠药的镇静与催眠作用的研究

目的研究藿香正气片增强镇静催眠药对小鼠的镇静催眠作用.为临床增添了一个中西药结合的镇静催眠合剂提供药理依据.方法应用抖笼换能器法观察藿香正气片对小鼠的自发活动的影响.由此观察藿香正气片与镇静催眠药的协同作用.测定藿香正气片与镇静催眠药对小鼠的入睡时间及睡眠持续时间的作用.两个实验均分成四组,生理水组、藿香正气片组、安定组、安定+藿香正气片组.结果1.对小鼠自发活动的影响.(1)藿香正气片组与生理盐水组比较,具有极显著性差异(P＜0.01).(2)安定组与安定+藿香正气片组比较具有显著性差异(P＜0.05).2.藿香正气片增强镇静催眠药对小鼠的睡眠作用.(1)藿香正气片组与生理盐水组比较具有显著性差异(P＜0.05).(2)藿香正气片+安定组与安定组比较具有极显著性差异(P＜0.01).结论藿香正气片与安定合用对镇静及催眠确有协同作用.     

关节灵片镇痛、抗炎作用的实验研究

为探讨关节灵片的镇痛、抗炎作用,用热板法和扭体法观察该药镇痛作用,结果关节灵片为不同剂量灌胃给药对小鼠热致痛和醋酸致痛均有明显抗痛作用,呈现一定的量效关系;关节灵片对二甲苯所致炎性水肿亦有显著的抑制作用。提示关节灵具有较好的镇痛抗炎作用。     

Controlled Release of Theophylline Monohydrate from Amylodextrin Tablets: In Vitro Observations

Amylodextrin is a linear dextrin and can be produced by enzymatic hydrolysis of the -1,6 glycosidic bonds of amylopectin. Tablets compacted from pure amylodextrin showed good binding properties and did not disintegrate in aqueous media. Extended and decreasing drug release rates were found for tablets of 300 mg with a diameter of 9 mm containing 70% amylodextrin and 30% theophylline monohydrate, when compacted at 5 kN. Almost-constant drug release rates were obtained for these tablets when compacted at 10 or 15 kN. Nearly constant drug release rates were also shown for amylodextrin tablets with a drug load up to 75% compacted at 10 kN. Both release rate and release profile could be adjusted by selecting tablet thickness and incorporation of either lactose as a highly soluble excipient or talc as a hydrophobic excipient.     

海通片的毒理学研究

①目的　对海通片进行安全性评价。②方法　应用小鼠急性毒性实验及大鼠的亚急性毒性实验测定ＬＤ５０ ．③结果　小鼠的ＬＤ５０为８ ０６４．００ｍ ｇ／ｋｇ 体质量,ＬＤ５０的９５％ 可信限为７ ４４１．３２～８ ７３３．９１ｍ ｇ／ｋｇ 体质量,大鼠能耐受ＬＤ５０１／２０的海通片,其中毒靶器官是肝脏。④结论　海通片为低毒药物,肝功能不良者应慎用。