Anti-inflammatory effect of topically applied pranoprofen-gel

The anti-inflammatory activity and mode of action of topically applied pranoprofen-gel were investigated in comparison with indomethacin-gel in experimental animals. Applied topically, 0.3 ?? 3% pranoprofen-gel inhibited carrageenin-induced paw edema, fracture-induced paw edema, carrageenin-induced...

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Veröffentlicht in:Folia Pharmacologica Japonica 1985, Vol.85(4), pp.283-296
Hauptverfasser: TERASAWA, Michio, IMAYOSHI, Tomonori, IWAHISA, Yoshinori, MARUYAMA, Yutaka
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container_title Folia Pharmacologica Japonica
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creator TERASAWA, Michio
IMAYOSHI, Tomonori
IWAHISA, Yoshinori
MARUYAMA, Yutaka
description The anti-inflammatory activity and mode of action of topically applied pranoprofen-gel were investigated in comparison with indomethacin-gel in experimental animals. Applied topically, 0.3 ?? 3% pranoprofen-gel inhibited carrageenin-induced paw edema, fracture-induced paw edema, carrageenin-induced increase in vascular permeability and adjuvant arthritis in rats and ultraviolet ray-induced erythema in guinea pigs dose-dependently, with a potency slightly greater than that of indomethacin-gel. In addition, pranoprofen-gel inhibited dosedependently the formation of granuloma caused by a cotton pellet implantation, without affecting the weight of the thymus or adrenals and without inducing gastrointestinal lesions. Moreover, applied topically to carrageenin treated rats, pranoprofen-gel inhibited dose-dependently, and more potently than indomethacin-gel, the production of a prostaglandin E2 (PGE2)-like substance in both the exudate of the carrageenin air pouch and the inflamed synovial membrane. Both drugs inhibited the potentiation of bradykinin-induced vascular permeability in rabbit skin by arachidonic acid, but not by PGE2. Pranoprofen was only one third as potent as indomethacin in inhibiting the production of PGE2 from the phagocytosing of killed bacteria by rat peritoneal leucocytes in vitro. These results show that pranoprofen-gel, applied topically, permeates well from the skin to the deep inflammatory site, relieving potently and long lastingly the inflammation by inhibiting PG production. As a topical anti-inflammatory agent, pranoprofen-gel is at least as effective as indomethacin-gel, so it may have good clinical use.
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Applied topically, 0.3 ?? 3% pranoprofen-gel inhibited carrageenin-induced paw edema, fracture-induced paw edema, carrageenin-induced increase in vascular permeability and adjuvant arthritis in rats and ultraviolet ray-induced erythema in guinea pigs dose-dependently, with a potency slightly greater than that of indomethacin-gel. In addition, pranoprofen-gel inhibited dosedependently the formation of granuloma caused by a cotton pellet implantation, without affecting the weight of the thymus or adrenals and without inducing gastrointestinal lesions. Moreover, applied topically to carrageenin treated rats, pranoprofen-gel inhibited dose-dependently, and more potently than indomethacin-gel, the production of a prostaglandin E2 (PGE2)-like substance in both the exudate of the carrageenin air pouch and the inflamed synovial membrane. Both drugs inhibited the potentiation of bradykinin-induced vascular permeability in rabbit skin by arachidonic acid, but not by PGE2. Pranoprofen was only one third as potent as indomethacin in inhibiting the production of PGE2 from the phagocytosing of killed bacteria by rat peritoneal leucocytes in vitro. These results show that pranoprofen-gel, applied topically, permeates well from the skin to the deep inflammatory site, relieving potently and long lastingly the inflammation by inhibiting PG production. 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Applied topically, 0.3 ?? 3% pranoprofen-gel inhibited carrageenin-induced paw edema, fracture-induced paw edema, carrageenin-induced increase in vascular permeability and adjuvant arthritis in rats and ultraviolet ray-induced erythema in guinea pigs dose-dependently, with a potency slightly greater than that of indomethacin-gel. In addition, pranoprofen-gel inhibited dosedependently the formation of granuloma caused by a cotton pellet implantation, without affecting the weight of the thymus or adrenals and without inducing gastrointestinal lesions. Moreover, applied topically to carrageenin treated rats, pranoprofen-gel inhibited dose-dependently, and more potently than indomethacin-gel, the production of a prostaglandin E2 (PGE2)-like substance in both the exudate of the carrageenin air pouch and the inflamed synovial membrane. Both drugs inhibited the potentiation of bradykinin-induced vascular permeability in rabbit skin by arachidonic acid, but not by PGE2. Pranoprofen was only one third as potent as indomethacin in inhibiting the production of PGE2 from the phagocytosing of killed bacteria by rat peritoneal leucocytes in vitro. These results show that pranoprofen-gel, applied topically, permeates well from the skin to the deep inflammatory site, relieving potently and long lastingly the inflammation by inhibiting PG production. 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IMAYOSHI, Tomonori ; IWAHISA, Yoshinori ; MARUYAMA, Yutaka</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c394t-994eec38fb75f664201dcb8ccd259901669341c686fd90497992a1490a85013e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>jpn</language><creationdate>1985</creationdate><topic>Administration, Topical</topic><topic>Animals</topic><topic>Anti-Inflammatory Agents - administration &amp; dosage</topic><topic>Anti-Inflammatory Agents - pharmacology</topic><topic>Anti-Inflammatory Agents - therapeutic use</topic><topic>Benzopyrans - administration &amp; dosage</topic><topic>Benzopyrans - pharmacology</topic><topic>Benzopyrans - therapeutic use</topic><topic>Capillary Permeability - drug effects</topic><topic>Edema - therapy</topic><topic>Erythema - drug therapy</topic><topic>Female</topic><topic>Gels</topic><topic>Granuloma - prevention &amp; control</topic><topic>Guinea Pigs</topic><topic>Indomethacin - therapeutic use</topic><topic>Inflammation - drug therapy</topic><topic>Male</topic><topic>Propionates - administration &amp; dosage</topic><topic>Propionates - pharmacology</topic><topic>Propionates - therapeutic use</topic><topic>Prostaglandins E - biosynthesis</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Rats, Inbred Lew</topic><topic>Rats, Inbred Strains</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>TERASAWA, Michio</creatorcontrib><creatorcontrib>IMAYOSHI, Tomonori</creatorcontrib><creatorcontrib>IWAHISA, Yoshinori</creatorcontrib><creatorcontrib>MARUYAMA, Yutaka</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Folia Pharmacologica Japonica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>TERASAWA, Michio</au><au>IMAYOSHI, Tomonori</au><au>IWAHISA, Yoshinori</au><au>MARUYAMA, Yutaka</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Anti-inflammatory effect of topically applied pranoprofen-gel</atitle><jtitle>Folia Pharmacologica Japonica</jtitle><addtitle>Nihon Yakurigaku Zasshi</addtitle><date>1985-01-01</date><risdate>1985</risdate><volume>85</volume><issue>4</issue><spage>283</spage><epage>296</epage><pages>283-296</pages><issn>0015-5691</issn><eissn>1347-8397</eissn><abstract>The anti-inflammatory activity and mode of action of topically applied pranoprofen-gel were investigated in comparison with indomethacin-gel in experimental animals. Applied topically, 0.3 ?? 3% pranoprofen-gel inhibited carrageenin-induced paw edema, fracture-induced paw edema, carrageenin-induced increase in vascular permeability and adjuvant arthritis in rats and ultraviolet ray-induced erythema in guinea pigs dose-dependently, with a potency slightly greater than that of indomethacin-gel. In addition, pranoprofen-gel inhibited dosedependently the formation of granuloma caused by a cotton pellet implantation, without affecting the weight of the thymus or adrenals and without inducing gastrointestinal lesions. Moreover, applied topically to carrageenin treated rats, pranoprofen-gel inhibited dose-dependently, and more potently than indomethacin-gel, the production of a prostaglandin E2 (PGE2)-like substance in both the exudate of the carrageenin air pouch and the inflamed synovial membrane. Both drugs inhibited the potentiation of bradykinin-induced vascular permeability in rabbit skin by arachidonic acid, but not by PGE2. Pranoprofen was only one third as potent as indomethacin in inhibiting the production of PGE2 from the phagocytosing of killed bacteria by rat peritoneal leucocytes in vitro. These results show that pranoprofen-gel, applied topically, permeates well from the skin to the deep inflammatory site, relieving potently and long lastingly the inflammation by inhibiting PG production. As a topical anti-inflammatory agent, pranoprofen-gel is at least as effective as indomethacin-gel, so it may have good clinical use.</abstract><cop>Japan</cop><pub>The Japanese Pharmacological Society</pub><pmid>3874127</pmid><doi>10.1254/fpj.85.283</doi><tpages>14</tpages><oa>free_for_read</oa></addata></record>
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source MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals
subjects Administration, Topical
Animals
Anti-Inflammatory Agents - administration & dosage
Anti-Inflammatory Agents - pharmacology
Anti-Inflammatory Agents - therapeutic use
Benzopyrans - administration & dosage
Benzopyrans - pharmacology
Benzopyrans - therapeutic use
Capillary Permeability - drug effects
Edema - therapy
Erythema - drug therapy
Female
Gels
Granuloma - prevention & control
Guinea Pigs
Indomethacin - therapeutic use
Inflammation - drug therapy
Male
Propionates - administration & dosage
Propionates - pharmacology
Propionates - therapeutic use
Prostaglandins E - biosynthesis
Rabbits
Rats
Rats, Inbred Lew
Rats, Inbred Strains
title Anti-inflammatory effect of topically applied pranoprofen-gel
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