Reference

An industrial process for the preparation of fexofenadine hydrochloride and a process for the purification of fexofenadine via refluxing in organic solvents

All Rights Reserved. An industrial process for the preparation of fexofenadine hydrochloride and a process for the purification of fexofenadine via refluxing in organic solvents. Jaweed Mukarram, Siddiqui Mohammed; Merwade, Aravind Yekanathsa; Khan, Anjum Reyaz; Solanki, Pawan Vrajlal (Wockhardt Limited, India). PCT Int. Appl. WO 2007007347 A1 18 Jan 2007, 19pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2005-IN241 13 Jul 2005. PRIORITY: IN 2005-MU809 7 Jul 2005. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 45, 63 The invention relates to a manufg. process for the prodn. of anhyd. fexofenadine hydrochloride (I.HCl) having ￡ 1.0% of total impurities and moisture content ￡ 0.5%. Another aspect of the invention is purifn. of fexofenadine base (I), giving a product free of both the meta isomer of I and fexofenadinone. The purifn. process involves refluxing of crude I in (a mixt. of) org. solvents. Manuf. of crude I is also described. For instance, esterification of a,a-dimethylphenylacetic acid (HPLC purity = 98%) followed by Fridel-Crafts acylation with 4-chlorobutanoyl chloride gave the corresponding acylated Me a,a-dimethylphenylacetate intermediate as a mixt. having para and meta isomer (HPLC purity of para isomer = 95%), which was further substituted with azacyclonol, reduced by sodium borohydride, and hydrolyzed to gave the crude I. The exclusive sepn. involved suspensions in methanol/MEK mixt. having specific ratio of ingredients, followed by refluxing the material in methanol/DMF, and final rinsing with hot water, providing I having total impurities ￡ 1.0% and having moisture content in the range of 2.5 to 6.0%. Treatment of I with methanol and 50% aq. 826-55-1 and 153439-40-8 which are cas registry numbers of substances are two of reagents here. HCl to pH 2.4-2.6, followed by refluxing in acetone gave anhyd. I.HCl with moisture content 0.2-0.5%, which meets all the requirements of the International Conference on Harmonization (ICH) guidelines. .

Treatment of allergic rhinitis can improve blood pressure control

All Rights Reserved. Treatment of allergic rhinitis can improve blood pressure control. Magen, E.; Yosefy, C.; Viskoper, R. J.; Mishal, J. (Internal Medicine B' Department, WHO Collaborative Center for Prevention of CVD, Ben-Gurion University of the Negev, Ashkelon, Israel). Journal of Human Hypertension, 20(11), 888-893 (English) 2006 Nature Publishing Group. CODEN: JHHYEN. ISSN: 0950-9240. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Owing to high prevalence of arterial hypertension (AH) and allergic rhinitis (AR), these diseases frequently coexist. The study aimed to assess whether improvement of AR by conventional treatment can improve blood pressure (BP) control in this population. Sixty-eight subjects of both sexes aged 35-60 years with AR and AH were randomized into two groups to receive in addn. to their antihypertensive medications: treatment group (n=34) Fluticasone nasal 50 mg/spray b.i.d. and Fenoxifenadine 180 mg tablets q.d., and control group (n=34) 0.9% NaCl nasal drops b.i.d. Office BP and AR severity (using the Relative Quality of Life Questionnaire (RQLQ)) and high-sensitive C-reactive protein (hs-CRP) were measured at study entry and after 8 wk in both groups, without changing of antihypertensive medications. 80474-14-2 and 153439-40-8 which are cas registry numbers are also used here. In Treatment group an improvement in RQLQ, significant redn. of systolic BP (SBP) (DSBP 7.4±4.3 mm Hg, P=0.006) and redn. of hs-CRP level (DCRP 2.05±1.08; P=0.028) were obsd., whereas diastolic BP (DBP) remained unchanged (DDBP 0.9±1.7 mm Hg, P=0.7). There was a significant correlation between DRQLQ and DSBP (r=0.86; P=0.019) and between DCRP and DSBP (r=0.56; P=0.027). No statistically significant changes of RQLQ, BP and CRP were obsd. in the control group. In patients with coincidence of AH and AR, medications meant to improve AR attenuate low-grade systemic inflammation and can lower SBP, but not DBP. .