Abstract: The present invention relates to an improved process for O-demethylating methoxy substituted morphinan-6-one derivatives using AlCl3 as a demethylating agent in a reaction-inert solvent having a water content ranging from 0.1% wt to 0.8% wt.

Abstract: Process for the preparation of N-methylnaltrexone bromide, wherein a compound of the general formula (I): wherein X? represents an anion other than the bromide anion, and R represents hydrogen or a leaving group, is dissolved or dispersed in a suitable polar solvent, the solution or dispersion is mixed with a compound containing bromide anions, and the resulting reaction mixture is stirred until N-methylnaltrexone bromide has formed and crystallized, wherein, in the case where R represents a leaving group, that group is removed during or after the reaction.

Abstract: A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, ?,?-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a selected noroxymorphone compound in a reaction which converts the hydroxyl groups present in the mixture to leaving groups of the formula —OR2 in which R2 is the introduced radical of the leaving group, (b) these leaving groups are optionally detached again, then (c) the resulting mixture is subjected to a selective hydrogenation, so that a saturated bond is formed in the ?,?-position of the unsaturated noroxymorphone compounds and any remaining leaving groups are each converted to a hydroxyl group and then optionally (d) the pure noroxymorphone compound is isolated; processing of the noroxymorphone purified in this way to naltrexone or naloxone or a salt of these compounds or a quaternary derivative of these compounds; pharmaceutical formulations c

Abstract: The present invention concerns an injection device with a housing adapted to receive a syringe having a discharge nozzle, the housing having an indicator opening. There is a trigger and a forward drive arranged to act upon the syringe on actuation of the trigger to advance the syringe from a retracted position to an extended position thereby discharging the contents of the syringe through the discharge nozzle. A support member is in contacting juxtaposition with the housing and a return drive is supported by the support member and arranged to act upon the syringe after the contents of the syringe has been discharged so that the syringe can be withdrawn from the extended position to the retracted position. Advantageously, the support member is arranged in the housing so that the second drive does not obscure an inspection of the contents of the syringe through the indicator opening. Hence, it can be clearly determined whether the contents of the syringe have been expelled from the syringe.

Abstract: The invention relates to a method for producing N-phenyl-N-(4-piperidinyl)amide salts, particularly pharmaceutically tolerable addition salts of the compound Remifentanil, in that a compound of the formula (III) is reacted with an acrylic acid alkyl ester of the formula CH2?CH—C(O)—OR: where independently of each other R denotes low-molecular alkyl, preferably (C1-4)alkyl, preferably methyl or ethyl, R1 denotes low-molecular alkyl, preferably (C1-4)alkyl, preferably methyl or ethyl; and HX denotes an inorganic or organic acid, wherein the components are optionally reacted in the presence of a catalyst, preferably at a higher temperature, thereby obtaining the salt of the compound of formula (I).

Abstract: Solvent-free crystalline polymorphic form of naltrexone, characterized in that it has the XRD data listed in Table 1, and a method for the preparation of this polymorphic form; and a method for converting this polymorphic form of naltrexone into a known polymorphic form of naltrexone.

Abstract: The invention relates to non-hydrated fexofenadine hydrochloride which can be obtained from a fexofenadine base and hydrogen chloride, according to the reaction conditions, either in the form of a novel polymorph (“form A”), in an amorphous form, or in the form of a mixture of different polymorphs. Said novel polymorph (“form A”) can be used as a therapeutic active ingredient and can be processed to form a pharmaceutical containing the same and a pharmaceutically acceptable carrier. Said pharmaceutical is suitable for use as an antihistaminic agent, an antiallergic agent and/or a bronchodilating agent.

Abstract: Process for the preparation of N-methylnaltrexone bromide, wherein a compound of the general formula (I): wherein X? represents an anion other than the bromide anion, and R represents hydrogen or a leaving group, is dissolved or dispersed in a suitable polar solvent, the solution or dispersion is mixed with a compound containing bromide anions, and the resulting reaction mixture is stirred until N-methylnaltrexone bromide has formed and crystallised, wherein, in the case where R represents a leaving group, that group is removed during or after the reaction.

Abstract: An injection device 110 is described having a housing 112 and a housing closure means 130. The injection device 110 houses a syringe 114 having a needle 118 which is sealed by a boot 120. The housing closure means 130 is arranged so that the boot 120 can be connected to the housing closure means 130 simply, but cannot be removed from the housing closure means 130. The housing 112 and housing closure means 130 are arranged so that upon rotation of the housing closure means 130, the housing closure means 130 is moved axially away from the housing 112 and the boot 120 is removed from the syringe 114. The injection device is simple to use and manufacture.

Abstract: The invention concerns an injection device with a housing adapted to receive a syringe having a discharge nozzle and a plunger. There is a trigger and a drive arranged to act upon the plunger on actuation of the trigger to advance the syringe from a retracted position to an extended position through an opening in the housing. A locking mechanism is arranged in and moveable relative to the housing. The locking mechanism is engaged with the plunger when the syringe is not in its extended position and disengaged from the plunger when the syringe is in its extended position. This means that movement of the plunger relative to the syringe is prevented when, in use, the syringe is advanced from a retracted position to an extended position. Hence the contents of the syringe are not expelled from the syringe during advancement from the retracted position to the extended position. The contents are only expelled when the syringe reaches the extended position.

Abstract: An injection device 110 is described having a housing 112 that receives a syringe 114 having a needle 118, wherein the syringe is supported in a syringe carrier 150. The syringe 114 and syringe carrier 150 are biased by a return spring 126 from an extended position in which the needle 118 extends from the housing 112 through an exit aperture 128 to a retracted position in which it does not. A drive spring 130 acts via a drive to advance the syringe 114 from its retracted position to its extended position and discharge its contents through the needle 118 and a return spring 126, brought into play when the drive has reached a nominal return position, restores the syringe 114 to its retracted position. The injection device is less prone to failure than prior art devices and is safer should failure occur.

Abstract: An injection device (210) is described. A housing (212) receives a syringe and includes a return spring (226) for biasing the syringe from an extended position in which its needle (218) extends from the housing (212) to a retracted position in which the it does not. A drive spring (230) acts on a first drive element (232) and a second drive element (234) acts upon the syringe to advance it from its retracted position to its extended position and discharge its contents through the needle. The first drive element (232) is capable of movement relative to the second (234) once a nominal decoupling position has been reached. A release mechanism is activated when the first drive element (234) is further advanced to a nominal release position, to release the syringe (214) from the action of the drive spring (230), whereupon the return spring (226) restores the syringe (214) to its retracted position. A locking mechanism (337, 375) confines the returned syringe in its retracted position.

Abstract: This invention relates to an oral pharmaceutical preparation, suitable for dosing every 24 hours, comprising a substrate, which substrate comprises a pharmaceutically effective amount of tramadol or a salt thereof and a pharmaceutically effective amount of topiramate and wherein said substrate may be coated with a controlled release coating; said preparation having a specific dissolution rate in vitro.

Abstract: N-ethyl-N-[3-(3-cyanopyrazolo[1,5-a]pyrimidine-7-yl)phenyl]acetamide (Zaleplon) can be produced by condensing 3-(N-acetyl-N-ethyl-amino)-?-oxo-phenylpropanal sodium salt with 3-amino-4-cyanopyrazole. Said sodium salt can be produced by first treating 3-acetylamino-acetophenone with an alkali metal hydroxide, in particular with powdered potassium hydroxide and then with an ethylating reagent, in particular ethyl bromide and the N-(3-acetylphenyl)-N-ethyl-acetamide that is obtained is reacted with a formic acid alkyl ester in the presence of an alkali metal alkanolate, in particular in the presence of sodium ethanolate. Zaleplon is the active ingredient of the soporific licensed under the trade name Sonata®.

Abstract: The present invention refers to a method for making iron(III)gluconate complex, preferably alkali iron(III)gluconate complex. The method includes the following steps: (i) mixing a water soluble iron(III)salt in aqueous solution, simultaneously or in any desired sequence, with a member selected from gluconic acid, a water soluble salt of gluconic acid and combinations thereof, and a member selected from an alkali hydroxide, an alkali carbonate, an alkali hydrogen carbonate and combinations thereof, so that the reaction mixture has an acid value (pH-value) within the range of from 7.0 to 12, provided that when alkali hydroxide is used, gluconic acid or a water soluble salt of gluconic acid is provided at the beginning of the reaction or is added to the reaction mixture simultaneously with the alkali hydroxide; (ii) heating the reaction mixture until the iron(III)gluconate complex has formed; and (iii) adding an organic solvent which is miscible with water until the iron(III)gluconate complex is precipitated.

Abstract: A compound of the general formula (1), in which: Y denotes hydrogen, a halogen or a C1-4 alkyl group; X1 and X2 denote, independently of each other, hydrogen, a halogen, a C1-4 alkoxy, C1-6 alkyl, CF3, CH3S CH3SO2 or NO2 group; and R1 and R2 denote independently of each other, hydrogen or a C1-5 alkyl group, with the proviso that R1 and R2 do not both denote hydrogen, or a salt thereof, and is prepared by a multi-step process, the last step of which comprises reducing a compound of the general formula (6), in which Y, X1, X2, R1 and R2 are as defined above with an appropriate reducing agent, such as Zn, and, if desired, converting the compound of formula (1) thus obtained, into a salt. The products of this process are known to have useful pharmacological properties, e.g. as anxiolytics.

Abstract: The invention relates to a method for producing compounds which contain at least one molecule valproic acid salt and at least one molecule valproic acid. The valproic acid salt represents alkali or alkaline earth salt. Valproic acid is directly converted with the calculated amount of the corresponding alkali carbonate or earth alkaline carbonate and/or the calculated amount of the corresponding alkali bicarbonate or earth alkaline bicarbonate without adding a solvent and at a temperature that is higher than the melting temperature of valproic acid.

Abstract: The present invention relates to a liposome based formulation of erythropoietin comprising: (a) an effective amount of an erythropoietin; (b) a lipidic phase comprising: (i) lecithin or hydrogenated lecithin; (ii) optionally, a charged electropositive or electronegative lipid compound; and (iii) cholesterol or a derivative thereof selected from cholesterol esters, polyethylene glycol derivatives of cholesterol (PEG-cholesterols), and organic acid derivatives of cholesterols; and (c) a phosphate buffer. The liposome based parenteral dosage form of the invention is prepared by means of an ethanol injection technique. The composition avoids the need for use of human serum albumin and exhibits superior stability.

Abstract: A liposome-based formulation with good skin penetration of the effective substance, particularly calcitriol, is described. This formulation is well suited for the treatment of psoriasis.

Abstract: A medicated suppository for use in the vaginal or rectal cavity comprising a medicament, a mixture of triglycerides of fatty acids, a gel forming agent and a gel dispersing agent is described.