Acta pharmaceutica Nordica最新文献

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Model systems in iontophoresis--transport efficacy. 离子导入-运输效能的模型系统。
Acta pharmaceutica Nordica Pub Date : 1992-09-01 DOI: 10.1016/0169-409X(92)90026-M
B. Sage, J. Riviere
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引用次数: 66
Use of chemical penetration enhancers in transdermal drug delivery--possibilities and difficulties. 化学渗透促进剂在经皮给药中的应用——可能性和困难。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
J Wiechers
{"title":"Use of chemical penetration enhancers in transdermal drug delivery--possibilities and difficulties.","authors":"J Wiechers","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 2","pages":"123"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12560672","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}
引用次数: 0
Improvement of oral bioavailability of fenbufen by cyclodextrin complexations. 环糊精络合改善芬布芬的口服生物利用度。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
T Miyaji, Y Inoue, F Acartürk, T Imai, M Otagiri, K Uekama
{"title":"Improvement of oral bioavailability of fenbufen by cyclodextrin complexations.","authors":"T Miyaji,&nbsp;Y Inoue,&nbsp;F Acartürk,&nbsp;T Imai,&nbsp;M Otagiri,&nbsp;K Uekama","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The interactions of fenbufen (FB) with alpha-, beta-, gamma-cyclodextrins (CyDs) were studied in aqueous solution and in solid state. beta-CyD formed water soluble complex with FB in the molar ratio of 1:2 (guest:host). The solid complex of FB with alpha-CyD was obtained in the molar ratio of 1:2 (guest:host), while the same with gamma-CyD was obtained as 1:1 ratio. The dissolution rate and bioavailability of FB were significantly increased by the formation of inclusion complexes (alpha greater than gamma-CyD complex). CyDs had no effect on the metabolic time of FB forming two active metabolites, and the bioavailability of metabolites was also increased by complexation of FB with CyDs. The bitter taste of FB powder was reduced by alpha-CyD complexation. The enhanced bioavailability and reduced bitterness of FB by CyD complexations suggested the possibility of applying FB in smaller doses with fewer side-effects.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"17-22"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12683877","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}
引用次数: 0
Properties of suction de-epithelialized skin relative to drug delivery. 抽吸去上皮皮肤与药物递送的特性。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
P Svedman, S Lundin
{"title":"Properties of suction de-epithelialized skin relative to drug delivery.","authors":"P Svedman,&nbsp;S Lundin","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 2","pages":"115-6"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12560663","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}
引用次数: 0
Skin absorption of drugs. 药物的皮肤吸收。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
R C Wester
{"title":"Skin absorption of drugs.","authors":"R C Wester","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 2","pages":"116"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12560664","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}
引用次数: 0
Predicting percutaneous absorption. 预测经皮吸收。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
J E Riviere
{"title":"Predicting percutaneous absorption.","authors":"J E Riviere","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 2","pages":"119-20"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12560668","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}
引用次数: 0
Bioactive compounds from nature. 来自大自然的生物活性化合物。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
K Nakanishi
{"title":"Bioactive compounds from nature.","authors":"K Nakanishi","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 4","pages":"319-28"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12469304","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}
引用次数: 0
N-substituted (aminomethyl)benzoate 21-esters of corticosteroids as water-soluble, solution-stable and biolabile prodrugs. 糖皮质激素的n-取代(氨基甲基)苯甲酯21-酯作为水溶性、溶液稳定性和生物稳定性的前药。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
E Jensen, H Bundgaard
{"title":"N-substituted (aminomethyl)benzoate 21-esters of corticosteroids as water-soluble, solution-stable and biolabile prodrugs.","authors":"E Jensen,&nbsp;H Bundgaard","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Various N-substituted 3- or 4-(aminomethyl)benzoate 21-esters of hydrocortisone, prednisolone and methylprednisolone were synthesized and evaluated as water-soluble prodrug forms, with the aim of developing improved preparations for parenteral or ophthalmic administration. All esters were readily hydrolyzed enzymatically by human plasma. The half lives of hydrolysis in 80% plasma ranged from 8 min to 342 min, the rate being dependent on the structure of the amino group and its position relative to the ester moiety, as well as on the structure of the steroid. The esters showed maximal stability in aqueous solution at pH 3-4. From temperature-accelerated studies of the 3-[(4-methylpiperazin-1-yl)methyl)]benzoate ester of hydrocortisone, the shelf life of an aqueous solution (pH 4.0) of this ester was predicted to be 6 years at 25 degrees C. This estimated shelf life is not reduced by precipitation of the slightly soluble parent drug since the ester was shown to be capable of solubilizing hydrocortisone, possibly by self-micelization.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"35-42"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12683771","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}
引用次数: 0
In vitro diffusion cell design and validation. II. Temperature, agitation and membrane effects on betamethasone 17-valerate permeation. 体外扩散池的设计与验证。2温度、搅拌和膜对17-戊酸倍他米松渗透的影响。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
E W Smith, J M Haigh
{"title":"In vitro diffusion cell design and validation. II. Temperature, agitation and membrane effects on betamethasone 17-valerate permeation.","authors":"E W Smith,&nbsp;J M Haigh","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>An in vitro permeation cell has been designed and validated for use in monitoring the transmembrane permeation of betamethasone 17-valerate. The design utilizes common laboratory equipment and incorporates as many beneficial features as possible from other designs. The importance of fully validating the hydrodynamic performance of the cell prior to experimentation is stressed. The cell was validated by monitoring the diffusion of betamethasone 17-valerate in isopropyl myristate solution into purified isopropyl myristate receptor phase at different temperatures, different agitation rates and through different synthetic and biological membranes. The results of the hydrodynamic validation agree with data from other researchers and show that the permeation cell is adequately sensitive to these experimental parameters. The results of the membrane evaluation allow appropriate selection of the barrier material for representative transdermal experiments to be conducted. While human and porcine stratum corneum/epidermis are similar in diffusive properties, hairless mouse skin appears to be the most convenient animal membrane for these studies. Although silicone and cellulose membranes appear to be useful in this application, porous filter membranes and egg-shell membranes are insufficiently discriminatory to betamethasone 17-valerate diffusion to provide useful in vitro permeation data.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 3","pages":"171-8"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12590843","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}
引用次数: 0
Macromolecular prodrugs. XX. Factors influencing model dextranase-mediated depolymerization of dextran derivatives in vitro. 大分子高活性化合物。XX。影响模型葡聚糖酶介导葡聚糖衍生物体外解聚的因素。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
L S Nielsen, H Weibel, M Johansen, C Larsen
{"title":"Macromolecular prodrugs. XX. Factors influencing model dextranase-mediated depolymerization of dextran derivatives in vitro.","authors":"L S Nielsen,&nbsp;H Weibel,&nbsp;M Johansen,&nbsp;C Larsen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Endo-dextranase-mediated depolymerization of dextran and dextran derivatives under various experimental conditions in vitro was determined. By a simultaneous determination of Mn and MW of dextrans treated with the enzyme in aqueous buffer, an initial increase of the polydispersity of the polysaccharide sample was observed, indicating that dextranase cleaved the dextran molecules into chains which differed significantly in length. A pH optimum of 5 for the enzyme action was found. However, in the pH range 5-8, which prevails in the colon, the initial depolymerization rates differed by a factor of less than 2. Dextranase treatment of a dextran sample resulted in a constant increase of the concentration of terminal reducing glucose residues per time unit suggesting, that the initial depolymerization reaction followed zero-order kinetics. For degrees of substitution below 12 the efficacy of dextranase fragmentation of dextran conjugates decreased almost linearly with increasing DS. The chemical nature of the attached drug did not significantly affect the depolymerization rates. Maximally depolymerized dextran derivatives were obtained by the combined action of dextranase and various alpha-glucosidases. Treatment of such solutions with: a) model esterases b) 80% plasma and c) 20% liver homogenate did not give rise to an acceleration of the initial drug regeneration, as compared to identical experiments carried out in pure buffer solution (pH 7.4 and 37 degrees C).</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"23-30"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12554268","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}
引用次数: 0
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