Patent Document:

nasal spray or nasal drops or eye drops with 0 . 1 % azelastine hydrochloride as active ingredient the following are dissolved , in the following order , into 9 . 00 kg of water : 10 g of azelastine hydrochloride , 5 g of edetic acid disodium salt . 2 h 2 o , 68 g of sodium chloride , 1 . 25 g of alkyl - benzyldimethylammonium chloride ( benzalkonium chloride ), 4 . 38 g of citric acid , 64 . 8 g of sodium monohydrogen - phosphate . 12 h 2 o as well as 10 g of hydroxypropylmethyl cellulose .) 1 the solution obtained is diluted to 10 . 05 kg = 10 liters with water . the solution is filtered through a membrane filter of pore size 0 . 2 μm after careful mixing , the first 500 ml of filtrate being discarded . the filtrate has a ph value of 6 . 8 ± 0 . 3 . this is filled into plastic bottles which are closed with a conventional spray insert or into plastic or glass bottles which are closed with a conventional pump sprayer . in the latter case , pumps with nasal spray inserts are , for example used , which spray about 0 . 14 ml of solution per actuation . in this manner , 0 . 14 mg of azelastine hydrochloride are sprayed into the nose per actuation in the form of the solution . if the above obtained filtrate is filled into the bottles with dropper pipettes conventionally used for nasal drops or eye drops , the solution can be dripped into the nose or eye using a dropper pipette . 5 kg of polyoxyethylene stearate 2 , 8 kg of cetylstearyl alcohol ( lanette 0 ), 20 kg of white vaseline , 15 kg of liquid paraffin and 0 . 5 kg of silicon oil are melted together in a heatable vessel . 126 g of p - hydroxybenzoic acid methyl ester and 53 g of p - hydroxybenzoic acid propyl ester are dissolved in the melt ( temperature of the melt 80 ° c .). subsequently , a solution heated to 70 ° c . of 0 . 1 kg of azelastine hydrochloride , 140 g of p - hydroxybenzoic acid methyl ester and 60 g of p - hydroxybenzoic acid propyl ester in 51 . 021 kg of purified water are emulsified with the aid of a high speed stirrer and the emulsion obtained is stirred until cold and repeatedly homogenized at regular time intervals . the ointment is filled into tubes which have a tubular extension beyond the thread and are thus particularly suitable for applying the ointment into the nose . dosage aerosol giving off 0 . 5 mg of azelastine hydrochloride per stroke about 8 . 0 kg of a mixture of 70 parts by weight of difluorodichloromethane and 30 parts by weight of 1 , 2dichlorotetrafluoroethane are cooled to about - 55 ° c . in an appropriate cooling vessel . a mixture of 0 . 086 kg of precooled sorbitantrioleate and 0 . 8600 kg of precooled trichlorofluoromethane are dissolved with stirring into this mixture at - 55 ° c . 0 . 0688 kg of micronized azelastine hydrochloride and 0 . 0688 kg of micronized lactose are then incorporated in portions into the solution thereby obtained with intensive stirring . the total weight of the suspension thereby obtained is made up to 9 . 547 kg through addition of more of the mixture of 70 parts by weight of difluorodichloromethane and 30 parts by weight of 1 , 2 - dichlorotetrafluoroethane cooled to about - 55 ° c . following closure of the cooling vessel the suspension is again cooled to about - 55 ° c . under intensive stirring . it is then ready to be filled . with continued stirring the suspension is filled into the conventional suitable aluminum monobloc tins . the monobloc tins are closed immediately after the suspension has been filled using conventional dosage valves which release 0 . 05 ml of suspension per valve actuation . actuation of the valve thus releases 0 . 5 mg of azelastine hydrochloride . presentation is effected in conjunction with a conventional applicator which permits introduction of the active substance into the nose of the patient . 140 g of polyvinylalcohol ( trade name for example : mowiol 26 - 88 / hoechst ag , frankfurt 80 ) are stirred into 4 liters of cold water for injection purposes , the suspension is heated to 90 ° c . and left at this temperature for 45 minutes . after cooling , the solution obtained is mixed with the following solutions : 5 g of azelastine hydrochloride in 1 liter of water for injection purposes , 0 . 2 g of phenyl mercuric nitrate in 2 liters of water for injection purposes , 70 g of sodium chloride in 1 liter of water for injection purposes . the mixture is adjusted to a ph value of 6 . 8 through addition of 0 . 1 n sodium hydroxide solution , mixed with a solution of 15 g of sodium dihydrogen phosphate . 2 h 2 o and 21 g of disodium hydrogen phosphate . 2 h 2 o in 1 liter of water for injection purposes and filled up to 10 liters with water for injection purposes . following careful mixing the solution is filtered through a membrane filter of pore size 0 . 2 μm with glass fiber pre - filter and filled into sterile eye drop bottles under aseptic conditions after discarding a first 500 ml of filtrate .

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