微丸的进展

通过查阅近年国内外有关文献,对微丸的释药机制,制备方法及辅料作了综述。     

高效液相色谱法测定暖胃舒乐颗粒剂中芍药苷的含量

目的：建立暖胃舒乐颗粒剂中芍药苷含量测定的质量标准。方法：用高效液相色谱法测定。结果：平均加样回收率为99．1％（RSD＝0．8％）。结论：此方法简便，准确，稳定，重现性好，且成药中其它组分对测定无干扰，能有效地控制该制剂的质量。     

HPLC法测定枣仁安神颗粒中丹酚酸B的含量

目的：建立以高效液相色谱法测定枣仁安神颗粒中丹酚酸B含量的方法。方法：色谱柱为phenomenex Lu-nar C18（150 mm×4.6 mm id,5μm）,流动相为甲醇-乙腈-甲酸-水（30∶10∶1∶59）,流速为1.0 mL.min-1,检测波长为286 nm。结果：丹酚酸B进样量在0.1664～1.6640μg范围内与峰面积分值呈良好的线性关系（r=0.9999）;平均加样回收率为99.95%,RSD=0.09%（n=9）。结论：本方法操作简便,准确,可用于该制剂中丹酚酸B的含量测定。     

Development and in vitro Evaluation of Enteric Coated Multiparticulate System for Resistant Tuberculosis

The multiparticulate formulation of sodium para aminosalicylate for oral administration was developed by extrusion spheronization technique. Microcrystalline cellulose was used as filler in concentration of 14.4% w/w. Pellets were coated with Eudragit L 30 D-55 using fluidized bed processor. Different weight gains of acrylic polymer were applied onto the pellets and evaluated for in vitro dissolution behavior in 0.1 N HCl for two hours and then media was changed to phosphate buffer pH 6.8. A 60% w/w coating level of Eudragit L30 D 55 has produced the most acceptable results against the gastric attack. 3% Seal coat of HPMC E5 was also applied in order to protect the drug from migration into the Eudragit coat and film coat was applied in order to prevent aggregation of pellets in the dissolution media. Morphological characteristics of developed pellets were also investigated by scanning electron microscopy and found to be smooth and spherical. Developed system was found to be suitable for the delivery of Sod PAS in to intestinal region.     

芩百清肺浓缩丸含药血清抗甲型流感病毒的实验研究

目的:观察芩百清肺浓缩丸(黄芩.百部等)含药血清(S-QQCP)对甲型流感病毒的抑制作用。方法:应用体外细胞培养技术进行MDCK细胞培养,运用血清药理学方法制备芩百清肺浓缩丸(QQCP)低、中、高剂量含药血清,观察S-QQCP对甲型流感病毒生物合成、吸附和直接杀伤的作用。结果:与空白血清比较,QQCP各剂量含药血清对甲型流感病毒生物合成均有抑制作用(P<0.01);高剂量含药血清对甲型流感病毒吸附MDCK细胞有明显的抑制作用(P<0.01);各剂量含药血清对甲型流感病毒未显示出直接杀伤作用(P>0.05)。结论:S-QQCP对甲型流感病毒生物合成和吸附有一定的抑制作用。     

Upgrading wet granulation monitoring from hand squeeze test to mixing torque rheometry

With over 50 years of research in granulation technology, however more research is required to elucidate this widely applicable technology. Wetting phenomena could influence redistribution of individual ingredients within a granule according their solubility and also could affect the drying processes. Binder selection for a particular system is quite often empirical and dependent on the skills and experience of the formulator. Hand squeeze test was and still the main way for determination of wet granulation end point, but it is subjected to individual variation. It depends mainly on operator experience, so it is not possible to be validated. Literature reveals a variety of advanced monitoring techniques following up different wet massing stages. Torque measurement has been proved to be the most reliable control method as its tight relation to mass resistance. Many reports showed successful applications of mixing torque rheometer (MTR) for monitoring the wet massing procedure and scale up in addition to some preformulation applications. MTR as a new approach allows formulators to select a liquid addition range where the granule growth behavior is more predictable.     

Improvement of the Material Motion in a Rotary Processor

ABSTRACT

The purpose of this paper is to reject or to confirm the hypothesis that the influence of the water addition rate on the size and size distribution of pellets is caused by insufficient spreading of the added water at higher water addition rates. To overcome insufficient spreading of the added water, the agitation in the rotary processor is intensified by improving the spiral, rope-like movement by means of two baffles and a permanent PTFE coating, and by installing a chopper. Improvement of the spiral, rope-like movement moderates the influence of the water addition rate on the pellet size. The chopper has no significant influence on pellet size, pellet size distribution, or percentage of agglomerates for the pellets, which are investigated in this study. Furthermore, the implementation of the technical modifications does not influence the dissolution characteristics of the pellets directly. It is therefore concluded that the water added is well spread over the mass by ensuring an optimal spiral, rope-like movement, so that incorporation of a chopper is superfluous. The remaining influence of the water addition rate on the pellet size can most probably be explained by differences in processing time, resulting in different volumes of air capable of extracting water from the powder mass.     

Tableting and tablet properties of alginates: Characterisation and potential for Soft Tableting

The aim of the study was to evaluate the suitability of alginates for Soft Tableting. For this purpose the compaction properties of alginates, varying in molecular weight, guluronic acid/mannuronic acid ratio and salt, were investigated and compared to MCC. Based on the mechanical properties, the suitability of the tested excipients for Soft Tableting was predicted. In order to test the prediction the tested materials were used to tablet enteric coated pellets, which served as a pressure sensitive material. The tableting behaviour was analysed by the 3-D modeling technique. The tablet properties were analysed by determining the elastic recovery and the compactibility. Alginates in general deformed elastically. The compression behaviour depended on the chemical composition of the alginates with sodium alginates being more elastic than potassium alginates. Tablets containing alginates with low guluronic acid content exhibited higher elasticity than tablets with alginates having a low mannuronic acid content. The plasticity of potassium alginates was higher than for sodium alginates. However, the plasticity of all tested alginates was lower than the plasticity of MCC. The compactibility of the tested alginates was sufficient. The proposed prediction, which states that tableting excipients with higher elasticity are more suitable for tableting sensitive materials than plastic excipients, was valid for the tested materials. The elastic alginates inflicted less damage on the pellets than the plastic MCC. Thus, all alginates were more appropriate for tableting pressure sensitive materials than MCC.     

Description and evaluation of cocaine body-packers management in French Guiana (2016–2019)

IntroductionFrench Guiana is a hub for drugs trafficking between South America and Europe. In Corpore transport, or Body-packing, is one of the options favored. In 2018, 577 people were arrested for smuggling cocaine from French Guiana to mainland France. The objective of this study was to update the epidemiological data and to evaluate the overall management of body-packers.MethodsA monocentric retrospective and observational study included patients admitted to the emergency department of the Cayenne General Hospital from January 1st, 2016 to December 31st, 2019 after ingestion of cocaine pellets.ResultsDuring the period, 668 people were referred to Cayenne hospital's emergency department by for suspected body-packing. Two hundred nineteen were excluded due to the absence of cocaine pellets in the initial X-ray or because they were carrying cannabis pellets. The mean age was 25.2 years with a sex ratio of 2.21 males per female. Among them, 13.7% of cases were complicated without endangering the vital prognosis. The mean number of pellets was similar between the population with and without complications (respectively 54.1 [50.9–57.4] and 57.8 [48.9–66.6], p = 0.22). The presence of cocaine in the urine was not significantly associated with the risk of complications (OR = 0.5, [95%CI = 0.1–1.8], p = 0.23). Compared to the CT-scanner which has the highest diagnostic accuracy (Se 100%, Sp 94%), the sensitivity of the Abdominal X-ray was 44%.ConclusionThis study showed that complications were rare, most of which were digestive stagnation requiring endoscopy. Given the low rate of complications and their low severity the average duration of hospitalization was relatively short. The type 3, micro-industrial quality packaging, almost exclusively used in body-packing in French Guiana, seems to be the main factor in this reduction of complications. This observation suggests possible adaptations of the current protocol for body-packers monitoring.     

Formulation of immediate release pellets containing famotidine solid dispersions

Famotidine (FM) is a potent H2-receptor antagonist used for the treatment of peptic ulcer. It has a low and variable bioavailability which is attributed to its low water solubility. In this study, the dissolution of the drug was enhanced by a preparation of solid dispersion using two hydrophilic carriers, namely Gelucire 50/13 and Pluronic F-127. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), which indicated that there were no signs of interaction of the drug with the carriers used in the case of solid dispersions containing higher polymeric contents (1:3 and 1:5). FM solid dispersions in the matrices of Gelucire 50/13 and Pluronic F-127 (1:3) were used to prepare pellets. The scanning electron microscope (SEM) images of pellets showed that the pellets have spherical shape and their size depends on the carrier used. The dissolution of the drug from either solid dispersion or pellets was performed. The dissolution study depicted that, the presence of the drug in solid dispersion enhanced its dissolution in comparison with the drug itself. Also, the drug release from the manufactured pellets was found to be improved in the case of solid dispersions (drug:carrier 1:3). A complete drug release occurred after 30 min from pellets containing solid dispersions, while only about 30% of the loaded FM was released from pellets containing untreated drug after 2 h.