Journal of ocular pharmacology最新文献

Prevention and treatment of ocular inflammation with a new class of non-steroidal anti-inflammatory agents. 一类新的非甾体类抗炎药预防和治疗眼部炎症。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.335

G C Chiou, Q S Yao, M S Chang, T Okawara

引用次数: 16

Modulation of intraocular pressure by adenosine agonists. 腺苷激动剂对眼压的调节作用。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.379

C E Crosson, T Gray

{"title":"Modulation of intraocular pressure by adenosine agonists.","authors":"C E Crosson, T Gray","doi":"10.1089/jop.1994.10.379","DOIUrl":"https://doi.org/10.1089/jop.1994.10.379","url":null,"abstract":"Adenosine receptors have been shown to modulate a variety of physiological functions; however, little is known about the role these receptors play in the modulation of ocular function. To investigate the potential role of adenosine receptors in modulating intraocular pressure (IOP), the A1 agonist N6-cyclopentyladenosine (CPA), the nonselective adenosine agonist 5'-N-ethylcarboxamideadenosine (NECA) and the A2 agonist 8-phenylaminoadenosine (CV-1808) were evaluated. Topical administration of NECA produced a dose-related reduction in IOP. However, an initial ocular hypertension of 1 to 2 hours was also observed in rabbits treated with NECA. The administration of CPA (165 micrograms) resulted only in a reduction in IOP, while the administration of CV-1808 produced only an initial ocular hypertension. As adenosine A1 receptors have been shown to be negatively coupled to adenylate cyclase in several systems, CPA was evaluated for its ability to suppress cAMP formation in the isolated iris/ciliary body. CPA produced a dose-related suppression of cAMP accumulation induced by 10(-6) M forskolin (EC50 = 3.2 nM). These results indicate that selected adenosine agonists can modulate IOP. The ocular hypotension induced by adenosine agonists is consistent with the activation of adenosine A1 receptors and may involve the modulation of cAMP levels in the iris/ciliary body.","PeriodicalId":16638,"journal":{"name":"Journal of ocular pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.1994.10.379","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19198748","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: 32

Ion exchange resins for ophthalmic delivery. 眼用离子交换树脂。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.57

R Jani, O Gan, Y Ali, R Rodstrom, S Hancock

{"title":"Ion exchange resins for ophthalmic delivery.","authors":"R Jani, O Gan, Y Ali, R Rodstrom, S Hancock","doi":"10.1089/jop.1994.10.57","DOIUrl":"https://doi.org/10.1089/jop.1994.10.57","url":null,"abstract":"A new novel delivery system for ophthalmic drugs was developed using an antiglaucoma agent Betaxolol Hydrochloride as a model. The new delivery system involved both the binding and release of drug from ion exchange resin particles. Betaxolol was studied in-vitro via a release model analysis. The ocular comfort of Betaxolol was greatly enhanced by reducing the availability of free drug molecules in the precorneal tear film. The amount of resin concentration was selected to obtain optimum binding of the drug. The zeta potential of suspended particles was adjusted to produce flocculated suspension. Drug resin particles were then incorporated into the structured vehicle, containing Carbomer 934P as a polymer, to enhance the physical stability and ease of resuspendability of the product. This delivery system also optimized the bioavailability of Betaxolol, reducing the total drug concentration in half to 0.25% Betaxolol in 0.25% BETOPTIC S Ophthalmic Suspension as compared with 0.5% Betaxolol in BETOPTIC 0.5% Sterile Ophthalmic Solution dosage form. Increased comfort of 0.25% BETOPTIC S Ophthalmic Suspension, as well as its bioequivalency data in animal models (rabbits), was confirmed in actual clinical trials of the product 0.25% BETOPTIC S Ophthalmic Suspension. The 0.25% BETOPTIC S Ophthalmic Suspension product has been approved gamma FDA and is marketed in U. S. since February 1990. The 0.25% BETOPTIC S Ophthalmic Suspension formulation has an increased bioavailability (equivalent to BETOPTIC 0.5% Sterile Ophthalmic Solution at half the concentration of drug); and pharmaceutically, is an elegant suspension product which settles slowly providing uniform dosage and increased ocular comfort.","PeriodicalId":16638,"journal":{"name":"Journal of ocular pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.1994.10.57","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19196722","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: 70

Studies on the ocular hypotensive effects of prostaglandin F2 alpha ester prodrugs and receptor selective prostaglandin analogs. 前列腺素F2 α酯前药及受体选择性前列腺素类似物降压作用的研究。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.177

D F Woodward, M F Chan, J A Burke, A Cheng-Bennett, G Chen, C E Fairbairn, T Gac, M E Garst, C Gluchowski, L J Kaplan

{"title":"Studies on the ocular hypotensive effects of prostaglandin F2 alpha ester prodrugs and receptor selective prostaglandin analogs.","authors":"D F Woodward, M F Chan, J A Burke, A Cheng-Bennett, G Chen, C E Fairbairn, T Gac, M E Garst, C Gluchowski, L J Kaplan","doi":"10.1089/jop.1994.10.177","DOIUrl":"https://doi.org/10.1089/jop.1994.10.177","url":null,"abstract":"The use of natural prostaglandins (PG), such as PGD2, PGE2, PGF2 alpha, and PGI2, for treating glaucoma is limited by their ocular side effects. One approach to achieve the required separation of ocular hypotensive activity from side effects is to employ ester prodrugs. From a novel series of 11- and 15-mono and 11,15-diacyl esters of PGF2 alpha we identified prodrugs where PGF2 alpha formation rates in the iris-ciliary body exceeded those in the conjunctiva, sclera, and corneal endothelium. Compared to PGF2 alpha-1-isopropyl ester the ocular tissue hydrolysis rates of the 11-monopivaloyl, the 11,15-dipivaloyl ester and the 1,11-lactone were up to 1000 fold less. Despite this large disparity in hydrolysis rates, the pivaloyl esters and the 1,11-lactone were potent ocular hypotensives in our animal models. In studying prostaglandin analogs, we found that a diverse variety of prostanoid receptor selective agonists lowered intraocular pressure in dogs and/or monkeys. These included DP-, EP1-, EP2-, EP3-, and FP-receptor selective compounds. These findings were surprising and prompted us to re-examine the receptor selectivity of these agonists by radioligand binding studies. Using radiolabelled PGE2, 17-phenyl PGF2 alpha, and sulprostone we were able to confirm the selectivity of the agonists currently used for receptor characterization directly by radioligand binding competition studies. It appears that multiple prostanoid receptor subtypes may be involved in regulating intraocular pressure.","PeriodicalId":16638,"journal":{"name":"Journal of ocular pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.1994.10.177","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19197490","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: 26

Designing safer ophthalmic drugs by soft drug approaches. 采用软性药物途径设计更安全的眼科药物。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.3

N Bodor

{"title":"Designing safer ophthalmic drugs by soft drug approaches.","authors":"N Bodor","doi":"10.1089/jop.1994.10.3","DOIUrl":"https://doi.org/10.1089/jop.1994.10.3","url":null,"abstract":"There are two major novel metabolism-based drug design concepts which have significant advantages when used in the design of safe, specific ophthalmic drugs. One is based on predictable enzymatic activation processes by enzymes found exclusively or preferentially at the site of action--in this case, within the eye, primarily in the iris-ciliary body. The second major retrometabolic design technique involves soft drug approaches. Among the various soft drug design strategies, it was found that the \"inactive metabolite\" and the \"soft analog\" approaches are the most useful for designing safe and selective ophthalmic drugs. In the first case, the design process starts with a known (or predicted) inactive metabolite (Mi) of the drug (D). This Mi is then structurally modified in the \"chemical activation\" stage to the soft drug (SD), which is isosteric and/or isoelectronic with D to produce activity at the target receptors, similar to that of D. By design, however, SD is also subject to a facile, predictable (generally hydrolytic) metabolism leading in one step to the starting inactive Mi. As this deactivation takes places everywhere in the body, the desired activities are produced virtually exclusively at the target site at or near the place of application. Successful use of this general concept has led to soft beta-blockers as safe antiglaucoma agents, soft anticholinergics as short acting mydriatic agents, and soft corticosteroids as a type of novel, safe anti-inflammatory agents, which due to their unique design, do not elevate intraocular pressure IOP and do not produce other systemic and local side effects.","PeriodicalId":16638,"journal":{"name":"Journal of ocular pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.1994.10.3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"18909547","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: 21

Arachidonic acid stimulates corneal epithelial migration. 花生四烯酸刺激角膜上皮细胞迁移。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.453

M Nakamura, T Fujihara, H Mibu, M Hikida

引用次数: 11

Efficacy of insulin eyedrops. 胰岛素滴眼液的功效。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.461

D J Pillion, J A Atchison, J Stott, D McCracken, C Gargiulo, E Meezan

{"title":"Efficacy of insulin eyedrops.","authors":"D J Pillion, J A Atchison, J Stott, D McCracken, C Gargiulo, E Meezan","doi":"10.1089/jop.1994.10.461","DOIUrl":"https://doi.org/10.1089/jop.1994.10.461","url":null,"abstract":"Systemic absorption of insulin delivered via eyedrops has been studied in rats made transiently hyperglycemic by anesthesia with xylazine/ketamine. Insulin at a concentration of 2 mg/ml was not absorbed significantly when saline alone was used as the formulation for the eyedrops (0.04 ml). When various emulsant agents were added to the eyedrop formulation, systemic insulin levels were increased and concomitantly, blood D-glucose levels were decreased. Saponin, Brij-78, BL-9 and several alkylglycosides all increased the systemic absorption of insulin following delivery in eyedrops. Not all surfactant agents were effective in promoting systemic insulin absorption from eyedrops, as evidenced by the failure of some non-ionic surfactants to increase insulin absorption. Similar results were obtained when nosedrops containing insulin plus non-ionic surfactants were administered to rats. In conclusion, systemic insulin absorption was greatly accelerated by the addition of certain emulsants to the eyedrop formulation and physiologically important levels of insulin could be delivered systemically following eyedrop administration.","PeriodicalId":16638,"journal":{"name":"Journal of ocular pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.1994.10.461","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19076671","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: 19

The effects of naloxone on retinal ischemia in rats. 纳洛酮对大鼠视网膜缺血的影响。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.481

T T Lam, K Takahashi, M O Tso

引用次数: 22

Prevention of ocular inflammation induced by lens protein, endotoxin, and interleukin-1 with synthetic interleukin-1 blockers. 人工合成白细胞介素-1阻滞剂预防晶状体蛋白、内毒素和白细胞介素-1引起的眼部炎症。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.577

G C Chiou, Q S Yao, T Okawara

引用次数: 21

Mucoadhesive ophthalmic vehicles: evaluation of polymeric low-viscosity formulations. 黏合剂眼科载具:聚合物低粘度配方的评价。

Journal of ocular pharmacology Pub Date : 1994-01-01 DOI: 10.1089/jop.1994.10.83

M F Saettone, D Monti, M T Torracca, P Chetoni

{"title":"Mucoadhesive ophthalmic vehicles: evaluation of polymeric low-viscosity formulations.","authors":"M F Saettone, D Monti, M T Torracca, P Chetoni","doi":"10.1089/jop.1994.10.83","DOIUrl":"https://doi.org/10.1089/jop.1994.10.83","url":null,"abstract":"A series of polyanionic natural or semi-synthetic polymers (polygalacturonic acid, hyaluronic acid, carboxymethylamylose, carboxymethylchitin, chondroitin sulfate, heparan sulfate and mesoglycan) were evaluated as potential mucoadhesive carriers for ophthalmic drugs. Solutions containing cyclopentolate (CY) or pilocarpine (PI) as salts (or polyanionic complexes) with the acidic polymers, all showing a low viscosity, were tested for miotic (resp. mydriatic) activity in albino rabbits. In the case of some polymeric complexes, small but significant increases of the areas under the activity vs. time curves (AUC) over reference cyclopentolate hydrochloride (CYHC1) or pilocarpine nitrate (PINO3) vehicles, and significant AUC decreases after removal of precorneal mucin by treatment with N-acetylcysteine were observed. A correlation was found between these data, considered indicative of the occurrence of a mucoadhesive interaction \"in vivo\", and \"in vitro\" viscometric data expressing the polymers-mucin force of interaction. The advantages and limitations of the mucoadhesive non-viscous approach in the formulation of ophthalmic vehicles are presented and discussed.","PeriodicalId":16638,"journal":{"name":"Journal of ocular pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.1994.10.83","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19196724","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: 75