Investigation of various factors affecting encapsulation on the In-Cap automatic capsule-filling machine

The purpose of this study was to determine the factors that influence fill weight and weight variability of capsules produced on the In-Cap and to assess any differences in terms of capsule defects between gelatin and HPMC (Quali-V) shells. The In-Cap is an automatic tamping type capsule-filling machine and the low output of ≈3000 capsules/hour makes it ideal for early formulation development and phase I/IIa clinical supplies manufacture. Four commonly used excipients (Avicel PH101, Avicel PH302, A-Tab, and Prosolv HD90) and a poorly flowing drug blend were encapsulated at various pin settings and powder bed heights. The average fill weight and coefficient of weight variation were determined. The percentage of defective capsules formed during encapsulation was calculated. Results of the study showed that pin setting was critical for controlling the fill weight and the weight variation. The order of pin setting with pin 1 (closer to the powder chute) set to a relatively higher position and pin 4 (before ejection) set to a lower position was found to give higher fill weights with relatively lower weight variability. The powder bed height influenced the fill weight for poorly flowing powders. The capsule machine speed did not appear to significantly influence the fill weight. The fill weight and weight variation were found to depend on the flow property of the material. A large percentage of defective capsules was obtained using HPMC shell size #00. Some of the commonly observed defects included split caps and improperly closed filled capsules. In general, appropriate selection of pin settings and bed height can reduce the weight variability seen, especially with poorly flowing high-dose formulations.     

青龙胶丸治疗脑梗塞后慢性脑功能不全50例疗效观察

采用青龙胶丸治疗脑梗塞后慢性脑功能不全５０例。结果表明,在连续治疗３个月后,慢性脑功能不全所致的头痛、头晕、失眠、生活主动性减退、对周围事物反应能力减退等症状的有效率均达８０％以上。神经心理学检查证实其对指向记忆、联想学习、人像特点联想回忆、认识能力等均有较好的改善作用。治疗前后血液流变学指标的改善,提示青龙胶丸降低纤维蛋白原、降低血液粘度,具有抗凝、解聚、溶栓、扩张血管、改善微循环的作用。认为是其对慢性脑功能不全发挥较好治疗作用的药理基础之一。     

双歧三联活菌胶囊对急性胰腺炎患者肠黏膜屏障功能的保护作用

目的探讨双歧三联活菌胶囊对急性胰腺炎患者肠黏膜屏障功能的保护作用。方法选取急性胰腺炎患者66例,随机分为观察组和对照组。两组患者均予以禁食水、持续胃肠减压、解痉镇痛、抗感染、抑制胃酸分泌、生长抑素、改善局部微循环和保持水电解质酸碱平衡等常规治疗。观察组患者加用双歧杆菌三联活菌胶囊420mg水化后自胃管灌注,夹管1．5h,3次／d,连用7d。观察两组患者的治疗前后肠黏膜屏障功能的变化情况,并比较其临床疗效。结果治疗7d后,两组患者血清内毒素、TNF—α和D-乳酸水平均有明显下降（P〈0．05或P〈0．01）,且观察组下降值比对照组更明显（P〈0．05）;同时观察组患者临床总有效率为93．94％,明显高于对照组的75．76％（χ2=4．24,P〈0．05）。结论双歧杆菌三联活菌胶囊治疗急性胰腺炎效果较好,能降低血清内毒素、TNF-α和D-乳酸水平,对患者肠黏膜屏障功能具有良好的保护作用。     

益坤精胶囊对骨质疏松模型小鼠骨形态和血清中IL-6表达的影响

目的:观察益坤精胶囊对骨质疏松模型小鼠骨形态计量学指标及血清白介素-6(IL-6)的影响。方法:取60只C57雌性小鼠随机分为:模型组(等体积生理盐水)、雌激素组(尼尔雌醇,0.25 mg/kg)、益坤精胶囊高剂量组(1.44 g/kg)、中剂量组(0.72 g/kg)、低剂量组(0.36 g/kg)及假手术组(等体积生理盐水),各组灌胃均70 d。采用酶联免疫吸附测定(ELISA)法检测血清中IL-6浓度,BI-2000医学图像分析系统进行骨形态计量学指标检测,使用CT测量分析各组小鼠股骨远侧干骺端血管数量。结果:与假手术组比较,模型组骨小梁平均宽度、骨皮质平均厚度、骨小梁面积、成骨细胞数以及骨密度、骨血管数量均明显减小,而破骨细胞数、血清中IL-6的浓度明显上升(P0.05)。与模型组比较,雌激素组、益坤精胶囊高、中、低剂量组上述指标均明显改善(P0.05),且益坤精胶囊高剂量组与雌激素组疗效相当(P0.05)。结论:益坤精胶囊可明显改善骨质疏松模型小鼠的骨形态计量学指标,降低血清中IL-6水平,增加骨血管数量,且以1.44 g/kg益坤精胶囊灌胃效果最佳。     

他克莫司联合黄葵胶囊治疗难治性膜性肾病的临床疗效

目的:探讨他克莫司联合黄葵胶囊治疗难治性膜性肾病疗效及安全性。方法:选取2014年3月-2015年10月我院收治的60例难治性膜性肾病患者,按随机数字表法分为观察组和对照组各30例,对照组给予泼尼松治疗,观察组在此基础上增加他克莫司联合黄葵胶囊口服,两组均治疗6个月,观察两组临床疗效,检测并对比两组治疗前后尿蛋白(uPRO)、血清白蛋白(sALB)、血清肌酐(sCr)、血谷丙转氨酶(sALT)、肿瘤坏死因子α(TNF-α)、转化生长因子β1(TGF-β1)以及不良反应情况。结果:观察组的有效率高于对照组(P0.05);治疗后两组uPRO、TNF-α、TGF-β1均明显降低,sALB、sCr明显升高(P0.05),且观察组uPRO、TNF-α、TGF-β1低于对照组(P0.05);两组不良反应发生率比较差异无统计学意义(P0.05)。结论:他克莫司联合黄葵胶囊治疗难治性膜性肾病具有较好的疗效,降低肾功能损伤,不良反应低,值得临床推广。     

通滞苏润江胶囊联合塞来昔布对早期膝骨关节炎患者血清炎症因子和疼痛介质的影响

摘要 目的：观察通滞苏润江胶囊联合塞来昔布对早期膝骨关节炎（KOA）患者血清炎症因子和疼痛介质的影响。方法：选择2021年6月-2022年12月期间石家庄市人民医院收治的早期KOA患者80例,采用随机数字表法将患者分为对照组（塞来昔布,40例）和观察组（通滞苏润江胶囊联合塞来昔布,40例）。对比两组疗效、疼痛视觉模拟评分（VAS）、西安大略和麦克马斯特大学骨关节炎指数（WOMAC）评分、炎症因子和疼痛介质。结果：观察组临床总有效率高于对照组（P<0.05）。两组治疗1个月后VAS、WOMAC评分下降,且观察组低于对照组同时间点（P<0.05）。两组治疗1个月后肿瘤坏死因子-α（TNF-α）、白细胞介素-1β（IL-1β）、白细胞介素-6（IL-6）下降,且观察组低于对照组同时间点（P<0.05）。两组治疗1个月后前列腺素E₂（PGE₂）、P物质（SP）下降,且观察组低于对照组同时间点（P<0.05）。两组不良反应发生率对比未见统计学差异（P>0.05）。结论：塞来昔布和通滞苏润江胶囊联合治疗早期KOA患者,可缓解疼痛,提高临床治疗效果,改善关节功能,同时还可改善血清炎症因子和疼痛介质水平。     

Boar sperm changes after sorting and encapsulation in barium alginate membranes

A routine use of boar-sexed semen is limited by the long sorting time necessary to obtain an adequate number of sexed spermatozoa for artificial insemination and by the high susceptibility of spermatozoa of this species to damages induced by sorting procedure and subsequent cryopreservation. The aim of this work was to study the impact of encapsulation in barium alginate membrane on sorted boar spermatozoa by evaluating membrane integrity, chlortetracycline staining patterns, protein tyrosine phosphorylation, and Hsp70 immunolocalization during storage over 72 hours in liquid or encapsulated form. The encapsulation procedure significantly (P < 0.05) decreased the overall membrane integrity of control unsorted semen (81.8 vs. 57.4, CTR vs. CPS), but did not negatively affect the overall viability and the chlortetracycline staining patterns of sorted encapsulated cells. Moreover, encapsulation significantly decreased (P < 0.05) the overall phosphotyrosin A pattern cell percentage in unsorted (98.4 vs. 92.6, CTR vs. CPS) but not in sorted semen (64.0 vs. 74.2; SORT CTR vs. SORT CPS). As for Hsp70, the overall percentage of cells displaying the different patterns was significantly influenced (P < 0.05) by treatment but not by storage time. The sorting procedure seems to induce the major changes, whereas encapsulation tends to exert a protective effect on sorted semen by increasing the percentage of spermatozoa displaying the T pattern (2.8 vs. 24.3; SORT CTR vs. SORT CPS). In conclusion, our data confirm that the damaging impact of the encapsulation in barium alginate capsules seems to be limited when compared with that of the sorting procedure and, moreover, the association of the two procedures does not result in an algebraic sum of the negative effects. These results suggest the possibility of a future utilization of the encapsulation technology in order to store sorted spermatozoa and permit their controlled release in the female genital tract.     

枳术宽中胶囊联合益生菌对 老年幽门螺杆菌阳性慢性萎缩性胃炎患者的疗效

目的探讨枳术宽中胶囊联合益生菌对老年幽门螺杆菌(H.pylori)阳性慢性萎缩性胃炎(chronic atrophic gastritis,CAG)患者的临床疗效。方法将80例H.pylori阳性的老年慢性萎缩性胃炎患者随机分为2组,各40例。其中对照组患者给予包含雷贝拉唑、阿莫西林、克拉霉素和胶体果胶铋的标准四联疗法治疗。观察组患者将四联疗法中的胶体果胶铋替代为枳术宽中胶囊,并在此基础上加用益生菌。7天为1个疗程,全部患者治疗2个疗程。停药1个月后比较两组患者治疗前后临床症状缓解率、H.pylori根除率、不良反应发生率等情况。结果治疗后两组患者病情均有所改善,但与对照组相比,观察组患者的症状缓解率及H.pylori根除率较高,不良反应发生率较低,差异均有统计学意义(P0.05)。结论枳术宽中胶囊联合益生菌可明显缓解老年CAG患者的临床症状,提高幽门螺杆菌的根除率,同时减轻患者不良反应发生率,对临床治疗CAG具有指导性意义。     

乳杆菌微胶囊化培养的研究

采用MaCSPDMDAAC微胶囊对两种乳杆菌进行了固定化发酵研究。结果表明,两种乳杆菌能够在微胶囊内很好地生长和繁殖,菌浓度可分别达到18×1011/mL 胶囊和269×1011/mL胶囊,比游离培养高出十倍以上,并且能与游离发酵一样产生乳酸,糖耗时间可缩短1/3～2/3。进行的多批次发酵显示了巨大的产酸能力。