Hyoscyamine sulphate

A comparison of the activities of these three alkaloids lias been made by Graliam and Gunn using their antagonism to the effects of carbamjd-choline chloride on isolated mammalian intestine. The relative activities found were, atropine sulphate 1 I-hyoscyamine sulphate 2-4 hyoscine hydro bromide 1-5. The results of previous authors are discussed and reasons suggested for some of the differences found. 

Emepronium Bromide Norethisterone Etidocaine Hydrochloride Pyridoxine Hydrochloride Dihydroergotamine Tartrate Hyoscyamine Sulphate Benzilonium Bromide Rimiterol... 

Hyoscyamine Sulphate elixir Hyoscyamine Sulfate injection Hyoscyamine Sulphate oral solution Hyoscyamine Sulphate tablets Glass, 1.8 M X 2mm I.D. 3% liquid G3/S1AB Nitrogen 225 FID Hydrobromide USP (24, pp. 851, 852 and 853)... 

The following identification tests are reported in the BP (2) under hyoscyamine sulphate. 

A. The infra-red absorption spectrum, concordant with the spectrum of standard hyoscyamine sulphate. 

For Belladonnae folium (Tl) 1.8 ml scopolamine hydrobromide solution is added to 8 ml hyoscyamine sulphate solution 20 pi is used for TLC. 

For Hyoscyami folium (T2) 4.2ml scopolamine hydrobroinide solution is added to 3.8ml hyoscyamine sulphate solution 20pl is used for TLC. 

Solvent. Hyoscine Hydrobromide C17H21NO4.HBr.3H2O. Hyoscyamine Hydrobromide CiTHasNOs-HBr. Hyoscyamine Sulphate [Pg.151]

Hyoscyamine hydrobromide, Ci HagOaN HBr, Mol. Wt. 370 3 and hyoscyamine sulphate, (Ci H2303N)2,H2S04, Mol. Wt. 676-8, again follow the conventional alkaloid base determination as indicated under Homa-tropine hydrobromide. 1 mi 0 02N 0-007402 g C... 

Atropine-, hyoscine- and hyoscyamine-based drugs are developed on a large scale and they also have a variety of clinical purposes. Atropinol, for example, is based on atropine. This drug contains atropine sulphate. Another example is Buscopan, based on hyoscine. Hyoscyamine is used in transdermal plasters. Bella sanol also contains hyoscyamine. The therapeutic use is similar to that of atropine. At least 50 different products from these alkaloids have been developed and introduced on the pharmaceutical market. 

Fig. 6 Concentration-time profile of antidotal atropine and its enantiomers S- and / -hyoscyamine in plasma of an in vivo swine study. Swine were topically exposed to the nerve agent VR (302 pg/ kg, t0) followed by administration of atropine sulphate (30 pg/kg) and the reactivating oxime HI 6 (12.8 mg/kg) via three i.m. injections into the rear leg at 30 (I), 180 (II) and 330 min (III). Blood samples were collected at distinct time points to generate EDTA plasma. Maximum concentrations were found 4 min after drug administration each. No differences of S- and R-Hyo concentrations were evident underlining similar elimination kinetics for both enantiomers. Data are mean and SD from duplicate measurement using the enantioselective LC-MS/MS approach of John et al. [47,49]. Black circles, total hyo grey circles, S-hyo grey triangles, R-hyo...

This is recrystallised from water until it has the melting point of pure 1-hyoscyamine oxalate (176°). The base is then obtained by dissolving the oxalate in water, making alkaline with ammonia and extracting with chloroform. After removing the solvent, the neutral sulphate is prepared and crystallised from alcohol or moist acetone. 

The crude alkaloid, together with that regenerated from the mother liquors after the removal of /-hyoscyamine oxalate, is racemised by dissolving 52 parts in 520 volumes of 95% alcohol containing 4.16 parts of sodium hydroxide 71 (loc. cit.). The solution is allowed to stand, at room temperature, until it shows no optical activity, after which it is neutralised with oxalic acid, the alcohol is removed, and the oxalate recrystallised from water until a melting point of 196°-197° is obtained. From this the base is regenerated and converted into the sulphate, as described above in the case of hyoscyamine. 

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