SummaryWhat is known and objective: Migraine headache is a relatively common, debilitating condition that costs our healthcare system over 78 billion dollars per year. Riboflavin has been advocated as a safe, effective prophylactic therapy for the prevention of migraines. The purpose of this study was to provide a systematic review of the current role of riboflavin in the prophylaxis of migraine headache. Methods What is new and conclusion:Riboflavin is well tolerated, inexpensive and has demonstrated efficacy in the reduction of adult patient's migraine headache frequency.Additional data are needed, however, to resolve questions involving pharmacokinetic issues and pharmacogenomic implications of therapy. K E Y W O R D Smigraine, pharmacogenomics, pharmacokinetics, riboflavin | WHAT IS KNOWN AND OBJECTIVEMigraine headache is a common, often disabling neurologic condition characterized by painful headaches associated with nausea, vomiting, and hypersensitivity to visual, auditory, and olfactory stimuli. The worldwide prevalence of migraine headache is about 10%; however, it is slightly higher in the United States at 12%.1,2 Women experience migraine headache at a greater rate (15%-17%) as compared to men. 1,3Epidemiologic data suggest that while 38% of patients with migraine headache need prophylactic therapy, only 3%-13% currently take prophylactic treatment. 4 Prophylactic therapy should be considered in situations where the patient feels that the recurring migraine headaches interfere with their daily routines and responsibilities despite acute treatment. 1-4The goals of treatment for patients requiring prophylactic therapy are to decrease the frequency, duration and severity of attacks,
Abstract:The purpose of this study is to confirm the impact of polar functional groups on inter and intra-molecular hydrogen bonding in haloperidol (HP) and droperidol (DP) and, hence, their effects on dissolution using a new approach. To confirm our theory, a new molecule: deshydroxy-haloperidol (DHP) was designed and its synthesis was requested from a contract laboratory. The molecule was then studied and compared to DP and HP. Unlike DHP, both the HP and DP molecules have hydrogen donor groups, therefore, DHP was used to confirm the relative effects of the hydrogen donor group on solubility and crystal packing. The solid dispersions of the three structurally related molecules: HP, DP, and DHP were prepared using PVPK30, and characterized using XRPD and IR. A comparative dissolution study was carried out in aqueous medium. The absence of a hydrogen bonding donor group in DHP resulted in an unexpected increase in its aqueous solubility and dissolution rate from solid dispersion, which is attributed to weaker crystal pack. The increased dissolution rate of HP and DP from solid dispersions is attributed to drug-polymer hydrogen bonding that interferes with the drug-drug intermolecular hydrogen bonding and provides thermodynamic stability of the dispersed drug molecules. The drug-drug intermolecular hydrogen bond is the driving force for precipitation and crystal packing.
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