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Hong Cattle Colon Shu

Posted on:2005-05-26Degree:MasterType:Thesis
Country:ChinaCandidate:W H DuFull Text:PDF
GTID:2191360122498642Subject:Pharmacy
Abstract/Summary:PDF Full Text Request
Ulcerative colitis (UC) is high incidence disease and lack of effective therapy with either Chinese herbs or chemical drugs. Based on the current concept of Chinese medicine and modern medicine, we designed a formula composed of herbs with the entity of antipyretic detoxication, invigoration of blood circulation and wound-healing referred to as Xiang-Niu colon-specific tabelts, which can be applied intracolonically with best therapeutic effects of anti- inflammation, detoxication and myogenesis. Here we extended our studies as the following 4 sections: processing of raw medicinal herbs, tablet moulding, quality analysis and pharmacological research.Radix arnebiae was optimally processed with 7-fold volume of 95% ethanol at a penetration velocity of 3 ml/kg ?min, based on L933 orthogonal design with different concentration, volume and penetration velocity of ethanol. It resulted in extraction rate of 93.2%.Radix Angelicae sinensis got a different extraction rates depended on ethanol concentration. That was 5.7%, 42.6% and 63% under 95%, 75% and 50% ethanol concentration. In contrast, Radix Angelicae sinensis got an extraction rate of 56% by ultrasonic water extraction and 65.2 - 71.8% by water boiling extraction.In tablets moulding section , These tablets were made by adding Radix Angelicae sinensis power(sieved, 200mu) into extracted solution ,we selected to use 5% Carbopol 934 and 3% PVP XL-10 (1:1 inside and outside) based on single factors of tablets hardness and disintegration time. The resulted tablet hardness was 58.1 ?.1N and collapse time 20.8?1.2min. Tablet coating consisted of Eudragit (S, L ) and EC with a ratio of 4 : 1 optimalized by single factors design.Tablet coating conditions were as the following, 35?elevation angle of coating pot, 15 rpm centrifuge speed, 30癈 coating temperature. Tablet weight increased 8% by coating and tablets forwarded to be dried 2h under 40?.In quality analysis , tablets were extracted, isolated, and developed by thin layer chromatography and components of Calculus boris, borneolum syntheticum, Radix Angelicae sinensis could be detected.The shikonin content of tabelts was 2.32mg ,RSD 3. 24% detected by violet spectrometer and the standard curve was A=0.024164C+0.00138, v=0.99999. Ferulic acid content of tabelts quantified by HPLC was 84.1μ.g, RSD 1. 48% with a linear equation of A=6178097.8X-13.8, r=0.99999 . Muscone of tabelts quantified by GC was 42.. 1 μg ,RSD2.4% with a linear equation of Y=0. 05039X-0. 0041, r=0.9998.In the last pharmacology section, no significant effect of tabelt granules was observed on the normal secretion and evacuation of gastrointestine. Tablet granules significantly increased the pain threshold in mice with an increase of 49.2% (6.1 ?2.7 s, P<0.05).Finally, the pharmacological effect of tablet granules on UC was observed on TNBS/ethanol induced mouse model. Modeled mice in group A, B, C, D, E and F were respectively administered with CMC-Na (0.5%), CMC-Na (0.5%), salicylazosulfapyridine (SASP)(250mg/kg.d) and tablet granules (300mg/kg.d, 150 mg/kg.d and 75 mg/kg.d) 6hrs after UC modeling. Mice were sacrificed 7d after drug usage and colons were dissected out for further analysis of their weight, MPO activity and histological staining. The ratios of Colon to body weight were 2.55?.24 , 4.28?.47, 3.28?0.17, 3.23?0.25, 3.15?0.20, 3.78?0.45 and MPO activity 0.1155?.0171 , 0.6517?.0639, 0.2577?.0272, 0.2591?.0217, 0.2470?.0209, 0.4991?.0217U/mg respectively in Group A, B, C ,D ,E and F. HE staining of colon sections showed that inflammation cells deeply infiltrated into smooth muscle layer in group B mice, and only fewer inflammation cells scattered superficially in mucous layer in both group C and D, compared with group A. The results showed that the tablets had significant therapeutic effect on UC in modeled mice.
Keywords/Search Tags:colitis, orthogonal design, extraction technics, granulation, compressibility, coating, quality analysis
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