{"title":"Acoustic emission during the deformation of alpha-lactose monohydrate and anhydrous alpha-lactose monocrystals.","authors":"D. Wong, M. Waring, P. Wright, M. Aulton","doi":"10.3109/03639048809152005","DOIUrl":"https://doi.org/10.3109/03639048809152005","url":null,"abstract":"During the deformation of single crystals of alpha-lactose monohydrate and anhydrous alpha-lactose in a crushing strength rig, their acoustic activity was monitored using a portable activity meter. The acoustic parameters measured were the average signal level (ASL), count rates and total acoustic counts. Both types of lactose, even though deformed by fragmentation, differed fundamentally in the degree and nature of this fragmentation. Close correlation was observed between the ASL, count rate profiles and the force-displacement profiles. The monohydrate form is acoustically more active than the anhydrous form during deformation. Small internal fractures which were neither visually observed nor detected in the force-displacement profiles (in particular the anhydrous alpha-lactose) were detected by monitoring the acoustic signals during the deformation of these crystals. This work illustrates the potential of using the acoustic emission technique as an aid in the assessment of the deformation characteristics of pharmaceutical materials during single crystal compression studies.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114959823","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Nagata, Y. Hidaka, M. Hidaka, Y. Kawano, T. Iwakiri, M. Okumura, K. Arimori
{"title":"Effect of acute hepatic failure on the hepatic first-pass effect of 5-fluorouracil in rats.","authors":"M. Nagata, Y. Hidaka, M. Hidaka, Y. Kawano, T. Iwakiri, M. Okumura, K. Arimori","doi":"10.1211/jpp/62.05.0006","DOIUrl":"https://doi.org/10.1211/jpp/62.05.0006","url":null,"abstract":"OBJECTIVES\u0000In cancer chemotherapy for hepatocellular carcinoma, 5-fluorouracil is widely used and has typically been given by intrahepatic arterial (i.a.) infusion to increase treatment efficacy and reduce systemic toxicity. 5-Fluorouracil is eliminated primarily by the liver and so the hepatic first-pass effect after intrahepatic arterial administration of 5-fluorouracil may be lower in patients with hepatic failure, and systemic toxicity may not be reduced. In this study, we have investigated the effect of acute hepatic failure on the first-pass effect of 5-fluorouracil in rats.\u0000\u0000\u0000METHODS\u0000Experimental acute hepatic failure was induced by treatment with carbon tetrachloride (CCl4). 5-Fluorouracil was infused for 15 min into the hepatic artery or the saphenous vein of rats at a dose of 1.25 mg/kg.\u0000\u0000\u0000KEY FINDINGS\u0000Hepatic availability in 50% CCl4-treated (severe hepatic failure) rats was higher than in controls.\u0000\u0000\u0000CONCLUSIONS\u0000The hepatic first-pass effect after intrahepatic arterial administration of 5-fluorouracil was lower in severe hepatic failure. Therefore, the reducing effect of the systemic toxicity after intrahepatic arterial administration may be lower in severe hepatic failure.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"62 5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129398939","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
F. Bigucci, B. Luppi, L. Monaco, T. Cerchiara, V. Zecchi
{"title":"Pectin-based microspheres for colon-specific delivery of vancomycin.","authors":"F. Bigucci, B. Luppi, L. Monaco, T. Cerchiara, V. Zecchi","doi":"10.1211/jpp/61.01.0006","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0006","url":null,"abstract":"OBJECTIVES\u0000The aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan.\u0000\u0000\u0000METHODS\u0000Hydrogels were prepared at different weight ratios (4:1, 7:1, 10:1; pectin/chitosan), loaded with vancomycin hydrochloride (2:1, 4:1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency. The influence of different pectin/chitosan hydrogels on the release behaviour of microspheres at pH 2.0, 5.5 and 7.4 were evaluated in vitro with and without pectinolytic enzyme.\u0000\u0000\u0000KEY FINDINGS\u0000The results showed that water uptake was increased by raising the environmental pH (from 2.0 to 7.4) and the pectin/chitosan weight ratio, while drug availability was increased by raising the environmental pH (from 2.0 to 7.4) and decreased by raising the pectin/chitosan weight ratio. In the presence of pectinase, the glycoside bonds of pectin were degraded and a considerable amount of drug was released in a short time.\u0000\u0000\u0000CONCLUSIONS\u0000This study suggested that pectin/chitosan microspheres were able to limit the release of vancomycin under acidic conditions and release it under simulated colonic conditions, confirming their potential for a colon-specific drug delivery system.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"35 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121080794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
N. Nishimura, Tomichika Uemura, K. Iwamoto, K. Naora
{"title":"Change in tolbutamide permeability in rat jejunum and Caco-2 cells by Sho-saiko-to (Xiao Chai Hu Tang), a Chinese traditional medicine.","authors":"N. Nishimura, Tomichika Uemura, K. Iwamoto, K. Naora","doi":"10.1211/jpp/62.05.0014","DOIUrl":"https://doi.org/10.1211/jpp/62.05.0014","url":null,"abstract":"OBJECTIVES\u0000This study was designed to investigate the effects of Sho-saiko-to (Xiao Chai Hu Tang), a Chinese traditional medicine, on the membrane permeability of tolbutamide in the intestinal tract. We carried out an in-situ loop study with rat jejunum and a transport study with Caco-2 cell monolayers.\u0000\u0000\u0000METHODS\u0000In the in-situ loop study, absorption clearance of tolbutamide was estimated from the drug concentrations in the loop and plasma. The apical-to-basolateral and basolateral-to-apical transport of tolbutamide and d-mannitol, a paracellular transport marker, was assessed using Caco-2 cell monolayers cultured on a polycarbonate membrane.\u0000\u0000\u0000KEY FINDINGS\u0000The absorption clearance of tolbutamide was enhanced by a concomitant dose of Sho-saiko-to over 10 min in the rat in-situ loop. Sho-saiko-to increased the apical-to-basolateral transport of tolbutamide, whereas the basolateral-to-apical transport of this drug was reduced by Sho-saiko-to. On the other hand, in both directions the P(app) of d-mannitol was reduced by the presence of Sho-saiko-to. Furthermore, the apical-to-basolateral transport of tolbutamide in ATP-depleted Caco-2 cells was diminished by Sho-saiko-to. These findings suggest that Sho-saiko-to can facilitate the epithelial membrane permeability of tolbutamide across the rat jejunum in-situ and Caco-2 cell monolayers. Since Sho-saiko-to suppressed the passive transport of tolbutamide from the apical-to-basolateral side, enhanced permeability may be related to effects of Sho-saiko-to on the energy-dependent transport of tolbutamide in the intestine.\u0000\u0000\u0000CONCLUSIONS\u0000Our findings suggest that Sho-saiko-to might facilitate the energy-dependent transport of tolbutamide across the rat jejunum in-situ and Caco-2 cell monolayers.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"23 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123886026","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
G. Cirillo, O. I. Parisi, M. Curcio, F. Puoci, F. Iemma, U. G. Spizzirri, N. Picci
{"title":"Molecularly imprinted polymers as drug delivery systems for the sustained release of glycyrrhizic acid.","authors":"G. Cirillo, O. I. Parisi, M. Curcio, F. Puoci, F. Iemma, U. G. Spizzirri, N. Picci","doi":"10.1211/jpp/62.05.0003","DOIUrl":"https://doi.org/10.1211/jpp/62.05.0003","url":null,"abstract":"OBJECTIVES\u0000The aim was to synthesize molecularly imprinted polymers (MIPs) with high recognition properties towards glycyrrhizic acid and to evaluate the performance of these materials to act as base excipients in glycyrrhizic acid sustained release in gastrointestinal simulating fluids.\u0000\u0000\u0000METHODS\u0000MIPs were synthesized using methacrylic acid (MAA) as acidic, 2-(dimethylamino)ethyl methacrylate (DMAEMA) as basic, and 2-hydroxyethylmethacrylate (HEMA) as neutral functional monomers, while ethylene glycol dimethacrylate (EGDMA) was chosen as a crosslinking agent. The imprinting effect was evaluated by binding experiments using glycyrrhizic acid and glycyrrhetic acid (analogue molecule) solutions and in-vitro release studies were performed in gastrointestinal simulating fluids.\u0000\u0000\u0000KEY FINDINGS\u0000Good recognition and selectivity properties were found in all the synthesized materials in both ethanol and ethanol-water mixture. The release from non-imprinted polymers was indeed higher at acidic pH, while a slower release was observed in MIPs' case, because of the presence of imprinted cavities in the polymeric structure. The stronger capacity of MAA to interact by hydrogen bonds with the template makes MAA-containing MIPs the most effective materials in both rebinding and release experiments.\u0000\u0000\u0000CONCLUSIONS\u0000The release tests confirm the applicability of imprinted polymer for glycyrrhizic acid sustained release in gastrointestinal simulating fluids.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"28 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"122311905","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
N. Wittschier, C. Lengsfeld, S. Vorthems, U. Stratmann, J. Ernst, E. Verspohl, A. Hensel
{"title":"Large molecules as anti-adhesive compounds against pathogens.","authors":"N. Wittschier, C. Lengsfeld, S. Vorthems, U. Stratmann, J. Ernst, E. Verspohl, A. Hensel","doi":"10.1055/S-2007-986869","DOIUrl":"https://doi.org/10.1055/S-2007-986869","url":null,"abstract":"Anti-adhesive compounds are potential prophylactic tools in alternative treatment regimes against bacterial infection, as bacterial adhesion is commonly mediated by carbohydrate-protein interactions between surface adhesions of microorganisms and the host cell. The use of exogenous polyvalent, high-molecular carbohydrates and tannin-like plant-derived compounds should antagonize the adhesive interaction. A range of carbohydrates and carbohydrate- and proanthocyanidin-enriched plant extracts were screened for potential anti-adhesive effects against Helicobacter pylori, Campylobacter jejuni, Porphyromonas gingivalis and Candida albicans in different in-situ assays on primary tissue. The adhesion of H. pylori on human stomach tissue was effectively blocked by glucuronic acid-enriched polysaccharides from immature okra fruits (Abelmoschus esculentus). These compounds also had strong in-vitro effects against C. jejuni (inhibition up to 80%), but were ineffective in an in-vivo study in infected chicken broilers due to metabolism in the gastrointestinal system. Polysaccharides from Glycyrrhizia glabra, also enriched with glucuronic acid, showed strong anti-adhesive properties against H. pylori and P. gingivalis (inhibition 60-70%). Pelargonium sidoides extract, containing mainly polymeric proanthocyanidins, was effective against H. pylori in a dose-dependent manner. Due to the multifunctional adhesive strategy of C. albicans, no effective compounds were detected against this yeast. Structure-activity relationships are presented and the potential in-vivo use of carbohydrate-based anti-adhesives is discussed.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"59 6 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130117260","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Cancer, chitosan nanoparticles and catalytic nucleic acids.","authors":"M. Tan, P. Choong, C. Dass","doi":"10.1211/jpp/61.01.0002","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0002","url":null,"abstract":"OBJECTIVES\u0000The aim of this review was to examine gene therapy involving DNAzyme and siRNA encapsulation into chitosan nanoparticles, discussing the current and future status of this drug delivery system in enhancing drug delivery and cancer therapy.\u0000\u0000\u0000KEY FINDINGS\u0000Cancer is a disease state in which the cells in our body undergo mutations at the genetic level and are transformed, acquiring the ability to replicate limitlessly. Conventional cancer treatment involves the use of surgery and cytotoxic chemotherapy and/or radiotherapy, which have the potential of harming normal, otherwise healthy, non-neoplastic cells. Newer forms of therapy such as immunotherapy and gene therapy have shown initial promise, but still require better ways to limit exposure to cancerous lesions in the body. As a result drug delivery systems have been developed in attempts to deliver therapeutics specifically to the target lesion site. One recent drug delivery system has revolved around the use of chitosan nanoparticle technology, where therapeutics are encapsulated into nanoparticles and targeted to tumours.\u0000\u0000\u0000SUMMARY\u0000Though few, attempts at encapsulating therapeutics such as deoxyribozymes and small or short interfering RNA have been optimistic and encouraging.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"61 1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129687724","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Curcuma zedoaria Rosc. (white turmeric): a review of its chemical, pharmacological and ethnomedicinal properties.","authors":"R. Lobo, K. Prabhu, A. Shirwaikar, A. Shirwaikar","doi":"10.1211/jpp/61.01.0003","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0003","url":null,"abstract":"OBJECTIVES\u0000Curcuma zedoaria Rosc is a perennial herb found in tropical countries, such as India, Japan and Thailand. Various parts of this plant are used in Ayurveda and other folk medicines for the treatment of different ailments such as diarrhoea, cancer, flatulence and dyspepsia. This study is an attempt to compile an up-to-date and comprehensive review of C. zedoaria that covers its traditional and folk medicinal uses, phytochemistry and pharmacology.\u0000\u0000\u0000KEY FINDINGS\u0000Research carried out using different in-vitro and in-vivo techniques of biological evaluation supports most of the claims.\u0000\u0000\u0000SUMMARY\u0000This review presents the botany, chemistry, traditional uses and pharmacological data of the plant.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"51 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"124653548","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hui Li, Shu-ling Li, Zhi-hong Wu, Li Gong, Jiu-Ling Wang, Yu-Zhu Li
{"title":"Effect of traditional Chinese herbal Bu-Wang-San on synaptic plasticity in ovariectomised rats.","authors":"Hui Li, Shu-ling Li, Zhi-hong Wu, Li Gong, Jiu-Ling Wang, Yu-Zhu Li","doi":"10.1211/jpp/61.01.0013","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0013","url":null,"abstract":"OBJECTIVES\u0000The neuroprotective effects of Bu-Wang-San (BWS) and its effects on spine synapse plasticity were investigated in ovariectomised rats.\u0000\u0000\u0000METHODS\u0000Thirty-six ovariectomised rats were divided into three groups: untreated controls, treatment with 17beta-estradiol or with BWS. After 3 months, spatial acquisition and spatial retention were measured using the Morris water maze. Swim time, swim distance, swim speed, quadrant time and platform crossing were recorded. Spine synapse density in the hippocampus was examined by transmission electron microscopy. The expression of synaptophysin P38 (P38) mRNA was examined by real-time PCR and the protein expression of P38 was examined by Western blot.\u0000\u0000\u0000KEY FINDINGS\u0000In spatial acquisition and spatial retention, the BWS group functioned significantly better than the control group. Ultrastructural observation of the hippocampus showed that BWS significantly increased spine synapse density compared with the ovariectomised group. In addition, BWS significantly increased P38 mRNA and protein expression in the hippocampus. Thus, the positive effect of BWS on learning and memory in rats was associated with increased spinal synapse density and increased P38 mRNA and protein expression in the hippocampus following menopause-induced injury.\u0000\u0000\u0000CONCLUSIONS\u0000These results suggest that BWS could improve cognitive ability following menopause-induced impairment of learning and memory.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"21 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115950384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"HYPOGLYCAEMIC AGENTS.","authors":"D. F. Hayman, V. Petrow, O. Stephenson","doi":"10.1201/9781315383293-33","DOIUrl":"https://doi.org/10.1201/9781315383293-33","url":null,"abstract":"","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131027428","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}