Alzheimer’s disease is a neurological disorder marked by the accumulation of amyloid beta(Aβ)aggregates,resulting from mutations in the amyloid precursor protein.The enzymeβ-secretase,also known asβ-site amyloid p...Alzheimer’s disease is a neurological disorder marked by the accumulation of amyloid beta(Aβ)aggregates,resulting from mutations in the amyloid precursor protein.The enzymeβ-secretase,also known asβ-site amyloid precursor protein cleaving enzyme 1(BACE1),plays a crucial role in generating Aβpeptides.With no targeted therapy available for Alzheimer’s disease,inhibiting BACE1 aspartic protease has emerged as a primary treatment target.Since 1999,compounds demonstrating potential binding to the BACE1 receptor have advanced to human trials.Structural optimization of synthetically derived compounds,coupled with computational approaches,has offered valuable insights for developing highly selective leads with drug-like properties.This review highlights pivotal studies on the design and development of BACE1 inhibitors as anti-Alzheimer’s disease agents.It summarizes computational methods employed in facilitating drug discovery for potential BACE1 inhibitors and provides an update on their clinical status,indicating future directions for novel BACE1 inhibitors.The promising clinical results of Elenbecestat(E-2609)catalyze the development of effective,selective BACE1 inhibitors in the future.展开更多
In this paper,we reviewed the various advanced technologies and methods that could help patients for measuring ad herence of patients.There exist intelligent technologies that are available for measuring medication ad...In this paper,we reviewed the various advanced technologies and methods that could help patients for measuring ad herence of patients.There exist intelligent technologies that are available for measuring medication adherence,including medication event monitoring system(MEMS@),smart blister packs,radio frequency identifcation(RFID)embedded smart drawers,and wisely aware RFID dosage(WARD)system,Utilization of these advanced technologies and systems have aided in enhancing the adherence to a greater extent.For example,MEMS@refers to the electronic cap that counts the number of bottles opened,but it can be employed only with bottles.Smart blisters are pharmaceutical packagings that possess the capability of monitoring when a pill or tablet is taken out of its packing.All those intelligent technologies can help in active monitoring of patients regarding adherence and capable of eradicating various medication errors due to which adherence is affected.展开更多
The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inser...The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac.The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose(HPMC,3% to 5%),chitosan(3% to 5%),poly vinyle alcohol(PVA,3% to 5%),methyl cellulose(MC,3% to 5%) as drug reservoir and ethyl cellulose(EC) polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time,achieving controlled release and greater therapeutic efficiency.The prepared ocular insert were then evaluated for physical appearances tensile strength,elongation at break(%),weight variation,uniformity of thickness,moisture absorption(%),pH,folding endurance,Fourier Transform Infrared spectroscopy,differential scanning calorimetry.Physicochemical characterization and in vitro transcorneal permeation studies reveals that,the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content,98.54% and 96.24%,respectively,over an extended period of 24 h.Hence these formulations were selected as best optimized formulations.It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system.Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release,proving a promising controlled release delivery system.展开更多
文摘Alzheimer’s disease is a neurological disorder marked by the accumulation of amyloid beta(Aβ)aggregates,resulting from mutations in the amyloid precursor protein.The enzymeβ-secretase,also known asβ-site amyloid precursor protein cleaving enzyme 1(BACE1),plays a crucial role in generating Aβpeptides.With no targeted therapy available for Alzheimer’s disease,inhibiting BACE1 aspartic protease has emerged as a primary treatment target.Since 1999,compounds demonstrating potential binding to the BACE1 receptor have advanced to human trials.Structural optimization of synthetically derived compounds,coupled with computational approaches,has offered valuable insights for developing highly selective leads with drug-like properties.This review highlights pivotal studies on the design and development of BACE1 inhibitors as anti-Alzheimer’s disease agents.It summarizes computational methods employed in facilitating drug discovery for potential BACE1 inhibitors and provides an update on their clinical status,indicating future directions for novel BACE1 inhibitors.The promising clinical results of Elenbecestat(E-2609)catalyze the development of effective,selective BACE1 inhibitors in the future.
文摘In this paper,we reviewed the various advanced technologies and methods that could help patients for measuring ad herence of patients.There exist intelligent technologies that are available for measuring medication adherence,including medication event monitoring system(MEMS@),smart blister packs,radio frequency identifcation(RFID)embedded smart drawers,and wisely aware RFID dosage(WARD)system,Utilization of these advanced technologies and systems have aided in enhancing the adherence to a greater extent.For example,MEMS@refers to the electronic cap that counts the number of bottles opened,but it can be employed only with bottles.Smart blisters are pharmaceutical packagings that possess the capability of monitoring when a pill or tablet is taken out of its packing.All those intelligent technologies can help in active monitoring of patients regarding adherence and capable of eradicating various medication errors due to which adherence is affected.
文摘The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac.The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose(HPMC,3% to 5%),chitosan(3% to 5%),poly vinyle alcohol(PVA,3% to 5%),methyl cellulose(MC,3% to 5%) as drug reservoir and ethyl cellulose(EC) polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time,achieving controlled release and greater therapeutic efficiency.The prepared ocular insert were then evaluated for physical appearances tensile strength,elongation at break(%),weight variation,uniformity of thickness,moisture absorption(%),pH,folding endurance,Fourier Transform Infrared spectroscopy,differential scanning calorimetry.Physicochemical characterization and in vitro transcorneal permeation studies reveals that,the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content,98.54% and 96.24%,respectively,over an extended period of 24 h.Hence these formulations were selected as best optimized formulations.It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system.Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release,proving a promising controlled release delivery system.