Drug design and delivery最新文献_第2页

Controlled release microspheres based on Eudragit L100 for the oral administration of erythromycin. 红霉素口服控释微球的研制。

Drug design and delivery Pub Date : 1991-07-01

I Morishita, M Morishita, Y Machida, T Nagai

引用次数: 0

Conjugate of N4-(4-carboxybutyryl)-ara-C and ethylenediamine-introduced dextran. Drug release profiles and further in vivo study of its antitumor effects. N4-(4-羧基丁基)-ara- c与乙二胺引入的葡聚糖的缀合物。药物释放谱及其抗肿瘤作用的进一步体内研究。

Drug design and delivery Pub Date : 1991-04-01

H Onishi, Y Seno, P Pithayanukul, T Nagai

{"title":"Conjugate of N4-(4-carboxybutyryl)-ara-C and ethylenediamine-introduced dextran. Drug release profiles and further in vivo study of its antitumor effects.","authors":"H Onishi, Y Seno, P Pithayanukul, T Nagai","doi":"","DOIUrl":"","url":null,"abstract":"In vitro and further in vivo work with a conjugate formed from the cytotoxic drug 1-beta-arabinofuranosylcytosine (ara-C) and dextran 2000 are described. In the preparation of this conjugate, functionalisation of ara-C was via N4-(4-carboxybutyryl)-ara-C (glu-ara-C), permitting conjugation with amino groups introduced by prior reaction of the oxidised dextran with ethylenediamine; by varying the proportions of the reaction components, 5.4 to 7.7% w/w loadings of ara-C were obtained. At physiological pH, in vitro, drug release from a 5.4% loaded conjugate was gradual and was dominantly ara-C; at lysosomal pH (pH 5) the release rate was much slower and more ara-U was formed. Antitumour effects were evaluated in L1210 leukaemic mice following single (1 day after inoculation) or double (2 and 6 days after inoculation) intraperitoneal injection of ara-C, glu-ara-C, or a 7.7% loaded conjugate at three dose levels. In all cases, the increase in lifespan was greatest following use of the conjugate, but the differences in the effects of ara-C and the conjugate were only significant at the lowest dose level. Glu-ara-C was virtually inactive under all conditions.","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"7 2","pages":"139-45"},"PeriodicalIF":0.0,"publicationDate":"1991-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12880674","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

Nonleast-squares jackknife regression in drug design. 药物设计中的非最小二乘折刀回归。

Drug design and delivery Pub Date : 1991-04-01

P P Mager

引用次数: 0

New approaches to drug design and delivery based on drug-membrane interactions. 基于药物-膜相互作用的药物设计和递送新方法。

Drug design and delivery Pub Date : 1991-04-01

L G Herbette, D G Rhodes, R P Mason

引用次数: 0

Enhanced skin permeation of papaverine by a medium chain glyceride. 中链甘油酯增强罂粟碱的皮肤渗透性。

Drug design and delivery Pub Date : 1991-04-01

M Okumura, Y Nakamori, K Sugibayashi, Y Morimoto

{"title":"Enhanced skin permeation of papaverine by a medium chain glyceride.","authors":"M Okumura, Y Nakamori, K Sugibayashi, Y Morimoto","doi":"","DOIUrl":"","url":null,"abstract":"The mode and mechanism of action of Sefsol-318, a medium chain glyceride and a potent percutaneous absorption enhancer, on the in vitro permeation of papaverine hydrochloride through hairless rat skin were investigated and compared with those of laurocapram (Azone). The total amount of the drug delivered through excised skin over 28 h from aqueous solutions of the drug in which 5% S-318 or Azone was suspended was about 820 or 420 times higher, respectively, than from the solution alone. Experiments using liposomes as models, indicated that both the enhancers markedly increased the fluidity of lipid membranes. Skin conductance measurements in hairless rats indicated that they both also increased in vivo skin moisturizing and water holding capacity. These results suggest that the mechanism of action of Sefsol-318 and Azone in enhancing skin permeation are similar. But following in vitro pretreatment of the excised skin with 5% Sefsol-318 and aqueous emulsion for 2 h, skin permeation of papaverine hydrochloride through the pretreated skin was much lower than through non-treated skin in the presence of Sefsol-318. In contrast, the enhancing effect of Azone on the pretreated skin was similar to that of Azone on the in vitro non-treated skin. We found that, unlike Azone, Sefsol-318 disappeared from skin completely one day after 24 h-in vivo pretreatment of skin with aqueous gels containing each agent. In agreement, drug permeation through skin excised one day after the in vivo pretreatment with Sefsol-318 was almost the same as in non-pretreated controls without Sefsol-318. This difference in the mode of action of Sefsol-318 and Azone may arise from the difference in the residence times of these enhancers in skin.","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"7 2","pages":"147-57"},"PeriodicalIF":0.0,"publicationDate":"1991-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13071438","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

Quantitative structure-activity relationship studies of inhibitors of gastric (H+/K+)-ATPase. 胃(H+/K+)- atp酶抑制剂的定量构效关系研究。

Drug design and delivery Pub Date : 1991-04-01

P Singh, R C Sharma, T N Ojha

引用次数: 0

Thermo-responsive hydrogels based on acryloyl-L-proline methyl ester and their use as long-acting testosterone delivery systems. 基于丙烯酰- l-脯氨酸甲酯的热反应性水凝胶及其作为长效睾酮输送系统的应用。

Drug design and delivery Pub Date : 1991-04-01

M Yoshida, M Asano, M Kumakura, R Kataki, T Mashimo, H Yuasa, H Yamanaka

{"title":"Thermo-responsive hydrogels based on acryloyl-L-proline methyl ester and their use as long-acting testosterone delivery systems.","authors":"M Yoshida, M Asano, M Kumakura, R Kataki, T Mashimo, H Yuasa, H Yamanaka","doi":"","DOIUrl":"","url":null,"abstract":"New thermo-responsive hydrogels were synthesized by copolymerizing acryloyl-L-proline methyl ester (A-ProOMe) with minor amounts of 2-hydroxypropyl methacrylate (HPMA) or polyethylene glycol 600 dimethacrylate (14G), using gamma-rays from a 60Co source. In water, extensive swelling of the hydrogels occurred at 10 degrees C, but there was marked deswelling as the temperature was raised to 37 degrees C. The poly(A-ProOMe-co-HPMA) hydrogel was characterized by an initial rapid shrinkage at the surface in the deswollen state; this shrinkage arose because of the formation of a rigid membrane barrier devoid of micropores. The system is therefore 'surface regulated'. In contrast, no such a barrier formed in the deswollen poly(A-ProOMe-co-14G) hydrogel. The whole matrix shrunk without the disappearance of micropores, and it is therefore a 'matrix pumping' system. Testosterone was incorporated into both these types of hydrogels, and the drug-loaded hydrogels were implanted subcutaneously into the backs of castrated rats. The daily dose of testosterone released in vivo from the poly(A-ProOMe-co-HPMA) hydrogel was constant at approximately 30 micrograms/day throughout an experimental period of 54 weeks. In contrast, drug release from the poly(A-ProOME-co-14G) hydrogel reached a maximum after one week and then decreased linearly with time down to the 7th week, when it was undetectable. These conclusions were supported by the changes in weight of the ventral prostates and right-side seminal vesicles of the rats, which were restored to normal when delivery of the testosterone was sustained.","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"7 2","pages":"159-74"},"PeriodicalIF":0.0,"publicationDate":"1991-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13071439","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

Linear free energy-related and quantitative structure-activity relationships of inhibitors of thymidylate synthetase. 胸苷酸合成酶抑制剂的线性自由能相关和定量构效关系。

Drug design and delivery Pub Date : 1991-01-01

P P Mager

引用次数: 0

5-HT3 receptor antagonists. 5-HT3受体拮抗剂。

Drug design and delivery Pub Date : 1991-01-01

M B Tyers

引用次数: 0

5-HT3 receptor antagonists. 5-HT3受体拮抗剂。

Drug design and delivery Pub Date : 1991-01-01 DOI: 10.1016/b0-44-451005-2/00569-6

M. Tyers

引用次数: 1