Method Development And Validation Of Donepezil Hydrochloride By Using Uv Spectrophotometric Method

Abstract: Simple, specific, accurate and cost economic UV spectrophotometric methods weredeveloped and validated for determination of Donepezil Hydrochloride. Instead of usingorganic solvents, mixture of Acetonitrile and water was used during method development andvalidation. Donepezil hydrochloride standard solution was scanned in the UV range (400-200nm) in a 1cm quartz cell in a double beam UV spectrophotometer. The standard solution ofDonepezil Hydrochloride showed maximum absorption at wavelength 231 nm. The methodobeys Beer’s law in the concentration range from 4-20µg/ml. The correlation coefficient wasfound to be 0.9983and regression of the curve was found Y=0.0376x+0.0185 with excellentrecovery 99.66-100.83%. Limit of detection and limit of quantification were found to be0.197µg/ml and 0.6µg/ml respectively. The ruggedness and robustness were performed. Themethod was validated for several parameters like accuracy, precision as per ICH guidelines.Statistical analysis proved that the methods are repeatable and specific for determination ofthe drug. These methods can be adopted in the routine assay analysis of DonepezilHydrochloride in API and pharmaceutical dosage form.

Efficacy of nursing intervention combined with donepezil in the treatment of senile dementia / 中国生化药物杂志

Objective To investigate and analyze the efficacy of nursing intervention combined with donepezil in the treatment of senile dementia. Methods 100 patients with Alzheimer's disease from February 2015 to August 2016 in our hospital were randomly divided into the control group and the experimental group, with 50 cases in each group. The patients in control group were treated with donepezil hydrochloride, and the experimental group was given nursing intervention measures, reasonable nursing program, comfortable medical environment, targeted safety nursing and psychological nursing were given. The clinical efficacy of the two groups was compared. Results After treatment, the effective rate of the experimental group was 94.0%, which was significantly higher than that of the control group, and the effective rate was 76.0%, the differences were statistically significant(P<0.05). After treatment, the scores of MMSE and ADL in the experimental group were (22.30±3.12) and (62.33±11.45) significantly better than that of the control group, the differences were statistically significant(P<0.05). The incidence of adverse reactions in the two groups was 10% and 12%, respectively, and there was no statistical significance. Conclusion The clinical efficacy of nursing intervention combined with donepezil in the treatment of senile dementia is ideal, can significantly improve the cognitive ability of patients, and has high security.

Efficacy of nursing intervention combined with donepezil in the treatment of senile dementia / 中国生化药物杂志

Objective To investigate and analyze the efficacy of nursing intervention combined with donepezil in the treatment of senile dementia. Methods 100 patients with Alzheimer's disease from February 2015 to August 2016 in our hospital were randomly divided into the control group and the experimental group, with 50 cases in each group. The patients in control group were treated with donepezil hydrochloride, and the experimental group was given nursing intervention measures, reasonable nursing program, comfortable medical environment, targeted safety nursing and psychological nursing were given. The clinical efficacy of the two groups was compared. Results After treatment, the effective rate of the experimental group was 94.0%, which was significantly higher than that of the control group, and the effective rate was 76.0%, the differences were statistically significant(P<0.05). After treatment, the scores of MMSE and ADL in the experimental group were (22.30±3.12) and (62.33±11.45) significantly better than that of the control group, the differences were statistically significant(P<0.05). The incidence of adverse reactions in the two groups was 10% and 12%, respectively, and there was no statistical significance. Conclusion The clinical efficacy of nursing intervention combined with donepezil in the treatment of senile dementia is ideal, can significantly improve the cognitive ability of patients, and has high security.

Effect of levothyroxine combined with donepezil hydrochloride in adult rats with hypothyroidism and its mechanism / 重庆医学

Objective To investigate the effect and potential mechanism of levothyroxine combined with donepezil hydrochloride in adulthood hypothyroidism rats.Methods A total of 60 male SD rats was divided by random number table into group A,group B,group C and group D,15 rats in each group.The rats in group B,group,C and group D were treated with PLT to prepare hypothyroidism model,and group A was used as the control group.After successful preparation of the model,rats in group C and group D were injected intraperitoneally with levothyroxine(6 g/100 g) every day,and then group D was given another 0.005％ donepezil in drinking water.After 2 weeks,the learning and memory behavior of rats was observed by Morris water maze;the levels of serum T3 and T4 were measured by radioimmunoassay;the expression of syntaxin-1 in hippocampus was detected by immunohistochemistry and Western blot.Results The escape latency and swimming distance of rats were prolonged significantly in group B but shorted significantly in group C and group D,and swimming speed was significantly slowed in group B but significantly strengthened in group C and group D;the levels of T3 and T4 were obviously decreased in group B but increased significantly in group C and group D,especially in group D.The results of immunohistochemistry and Western blot showed that the expression level of syntaxin-1 in hippocampus of rats was lower in group B compared to control group but increased significantly in both group C and group D.Conclusion Levothyroxine combined with donepezil hydrochloride can improve the learning and memory ability in adult rats with hypothyroidism,and its mechanism is related to the increase of expression of synaptotagmin-1 in hippocampus.

Clinical Study on Congrong Yishen Granules Combined with Donepezil Hydrochloride Tablets in the Treat-ment of Parkinson Disease with Dementia / 中国药房

OBJECTIVE:To observe the effects and safety of Congrong yishen granule combined with Donepezil hydrochloride tablet on mental state and quality of life in patients with Parkinson disease with dementia(PDD). METHODS:A total of 60 PDD patients were randomized into control group and treatment group,with 30 cases in each group. Both groups were given drugs for Parkinson disease. Control group was additionally given Donepezil hydrochloride tablet 5 mg,qd;treatment group was additionally given Congrong yishen granules 2 g,bid,on the basis of control group. The treatment lasted for 6 months in both groups. MMSE, MoCA,ADAS-Cog,ADL-R and TCM symptom score were observed in 2 groups before and after treatment. The occurrence of ADR were compared between 2 groups. RESULTS:Before treatment,there was no statistical significance in MMSE,MoCA, ADAS-Cog,ADL-R or TCM symptom score between 2 groups (P>0.05). After treatment,MMSE and MoCA score of 2 groups were increased significantly,while ADAS-Cog,ADL-R and TCM symptom score were decreased significantly;the treatment group were better than the control group,with statistical significance (P<0.05). No obvious ADR was found in 2 groups. CONCLU-SIONS:Congrong yishen granule combined with donepezil hydrochloride tablet can significantly improve mental state and cogni-tive ability of PDD patients,and relieve clinical symptoms with good safety.

The security of epilepsy patients use both donepezil and transcranial magnetic stimulation / 中国医师杂志

Epilepsy is a complications of brain injury or stroke,and is a common diseases in reha-bilitation or neurology department.Transcranial magnetic stimulation as a classical treatment means for stroke or brain injury,but also can promote the recovery of epilepsy.However,there is no clear clinical re-port for safety of epilepsy patients use both donepezil and transcranial magnetic stimulation .The article re-views the literature.Clinicians maybe provided some help.

The clinical efficacy of nicergoline combined with donepezil hydrochloride in the treatment of mild vascular dementia and its influence on cognitive function / 中国基层医药

Objective To investigate the clinical efficacy of nicergoline combined with donepezil hydrochlo-ride in the treatment of mild vascular dementia and its influence on cognitive function.Methods 66 patients with mild vascular dementia from neurology were divided into two groups by random numbers,33 cases in each group.On the based of the routine symptomatic treatment,the control group were given nicergoline,the observation group were treated with nicergoline combined with aricept.Four weeks was a course,both groups were continuously treated for 3 courses.Results The MMSE scores of the observation group after treatment was (36.7 ±5.7)points,which was significantly increased compared with before treatment(t =10.137,P <0.05)and the control group(t =11.236,P <0.05);The ADL score was(35.8 ±16.2)points,which was significantly lower compared with before treatment(t =10.825,P <0.05)and the control group(t =11.415,P <0.05);The total effective rate of the observation group was 78.9%,which was higher than 54.5% of the control group(χ2 =9.24,P <0.05).Conclusion Nicergoline com-bined with donepezil hydrochloride in the treatment of mild vascular dementia can significantly improve cognitive func-tion scores,and it is a significant effect,safe and reliable method.

Comparison of the Effects of a Brand-name Drug and Its Generic Drug on the Quality of Life of Alzheimer's Disease Patients

OBJECTIVE: The pharmacological effects of generic (GE) donepezil are the same as Aricept, its brand-name counterpart. However, little is known as to whether these two drugs provide the same quality of life (QOL). The study subjects were patients with Alzheimer's disease who were taking donepezil hydrochloride tablets, and were selected by visiting either the local pharmacies or the patients' homes. We chose the brand-name drug Aricept and its GE form donepezil to investigate, from a long-term caregiver's perspective, the influence of both drugs on the patients' QOL. METHODS: An EuroQol-5 Dimension (EQ-5D) was used to assess the QOL of patients with Alzheimer's disease, before and after various Aricept and/or donepezil regimens. Patients were divided into four groups: first time users of Aricept (n=43), first time users of GE donepezil (n=45), users refilling previous prescriptions of Aricept (n=51), and users switching from Aricept to GE donepezil (n=51). RESULTS: The average change in the EQ-5D utility indices rose significantly in the patients starting a new regimen of Aricept and its GE drug. The patients continuing an existing regimen of Aricept showed no significant differences, even after Aricept was switched to a GE drug. CONCLUSION: The QOL of patients starting a new regimen of Aricept and its GE drug improved. The QOL was maintained upon switching to the GE drug form.

Effect of synthetic super disintegrants and natural polymers in the preparation of donepezil hydrochloride fast disintegration films.

The main aim of the present research was to develop a fast dissolving oral polymeric film with good mechanical properties, faster disintegration and dissolution when placed on tongue. Donepezil hydrochloride (DPH) is prescribed in the treatment of mild to moderate Alzheimer’s disease (AD). The polymers selected for preparing films were sodium alginate (SA), poly vinyl alcohol (PVA) and guar gum (GG). Three batches of films were prepared by solvent casting method with sodium alginate, sodium alginate & PVA and with the combination of sodium alginate & guar gum. From these three batches, three optimized film formulations S3, SP7 and SG8 were selected based on disintegration time. To these three selected film formulations, superdisintegrants sodium starch glycolate (SSG), cross carmellose sodium (CCS) and cross povidone (CP) were added at a concentration of 4% w/w of polymer to improve the disintegration time. The films prepared with or without superdisintegrants were compared for fast releasing properties. Based on DT and in vitro dissolution data, S3CP was selected as the best formulation among the all formulations.

A clinical randomized case-control study of donepezil in the treatment of aphasia after stroke / 中华行为医学与脑科学杂志

Objective To explore the efficacy and safety of the donepezil hydrochloride in the treatment of post-stroke aphasia.Methods 60 patients with post-stroke aphasia were divided randomly into donepezil hydrochloride group (30 cases) and control group (30 cases).Trail group patients were received 5 mg per time,and once a day for oral administration of 2 weeks.From the third week they were received 10 mg per time,once a day,for continuous 10 weeks,and finally implemented four weeks washout period.The control group patients were received conventional treatment of neurology.The language function of patients were assessed with the Western Aphasia Battery (WAB) and the adverse reactions after treatment were evaluated by Treatment Emergent Symptom Scale (TESS).Assessments were implemented at the three time points,the start of trail,12 weeks,a washout period of 4 weeks.Results After 12 weeks of treatment,the AQ,PQ,CQ scores of WAB in the experimental group were (91.35±8.14),(32.74±8.12),(91.53±7.89).After 4-week washout period,they were (94.69±5.21),(33.70±4.94),(93.33±5.59) respectively.After the trail for 12 and 16 weeks,the score of each WAB item in the trail group was significantly higher than that before treatment.Compared with the control group,there was significant difference between the two groups(P＜0.01).The trail group had no significant adverse reactions.Conclusion Donepezil hydrochloride in the early treatment of post-stroke aphasia is safe,effective and the therapeutic effect is stable.

Effect of synthetic super disintegrants and natural polymers in the preparation of donepezil hydrochloride fast disintegration films.

The main aim of the present research was to develop a fast dissolving oral polymeric film with good mechanical properties, faster disintegration and dissolution when placed on tongue. Donepezil hydrochloride (DPH) is prescribed in the treatment of mild to moderate Alzheimer’s disease (AD). The polymers selected for preparing films were sodium alginate (SA), poly vinyl alcohol (PVA) and guar gum (GG). Three batches of films were prepared by solvent casting method with sodium alginate, sodium alginate & PVA and with the combination of sodium alginate & guar gum. From these three batches, three optimized film formulations S3, SP7 and SG8 were selected based on disintegration time. To these three selected film formulations, superdisintegrants sodium starch glycolate (SSG), cross carmellose sodium (CCS) and cross povidone (CP) were added at a concentration of 4% w/w of polymer to improve the disintegration time. The films prepared with or without superdisintegrants were compared for fast releasing properties. Based on DT and in vitro dissolution data, S3CP was selected as the best formulation among the all formulations.

Effect of donepezil hydrochloride on the Calpain Ⅰ-Cdk5 pathway expression in the hippocampus of mice with vascular dementia / 中华行为医学与脑科学杂志

Objective To investigate the effect of donepezil hydrochloride on the expression of Calpain Ⅰ-Cdk5/p25 pathway in the hippocampal CA1 area by cerebral ischemia and reperfusion in mice.Methods Mice were divided into model group,sham-operated group and donepezil-treated group.The expression of Calpain Ⅰ in hippocampal CA1 area was measured by immunohistochemistry staining respectively at 4,6 and 8 weeks post cerebral ischemia and reperfusion.Western blot was used to evaluate Cdk5 and p25 protein expression.Results The abilities of learning and memory performance was damaged significantly at 4,6 and 8 weeks after surgery compared to sham-operated group (P＜ 0.05).The expression of Calpain Ⅰ of model group were (0.098 ± 0.009),(0.129 ±0.01),(0.116 ± 0.01),which were higher than that of sham-operated group (0.03 ± 0.003),(0.031 ± 0.003),(0.029 ±0.003) and there was significant difference (P ＜ 0.05).The expression of Cdk5 in model group was (0.54 ± 0.05),(0.73 ± 0.07),(0.7 ± 0.06),which were higher than that of sham-operated group (0.23 ±0.02),(0.31 ± 0.02),(0.33 ± 0.02) and there was significant difference (P ＜ 0.05).The expression of p25 in model group was (0.44 ± 0.04),(0.51 ± 0.04),(0.55 ± 0.06),which were higher than that of sham-operated group(0.19 ± 0.02),(0.24 ± 0.02),(0.2 ± 0.02) and there was significant difference (P ＜ 0.05).The expression of Calpain Ⅰ of donepezil-treated group was (0.041 ± 0.004),(0.054 ± 0.004),(0.046 ± 0.003),which were lower than that of model group.The expression of Cdk5 was (0.28 ± 0.02),(0.33 ± 0.03),(0.38 ± 0.02),and expression of p25 was (0.26 ± 0.02),(0.25 ± 0.03),(0.21 ± 0.02),which were lower than that of model group respectively(P ＜ 0.05).Conclusion Donepezil hydrochloride probably improve the learning and memory abilities by reducing the expression of Calpain Ⅰ and Cdk5/p25.

The Effect of Donepezil on Language Functions in Children with Autism Spectrum Disorders / 신경정신의학

OBJECTIVES: Recent studies in autistic brain samples have shown diminished acetylcholine and nicotinic receptor activity. We hypothesized that acetylcholinergic enhancement may pharmacologically improve some autistic characteristics. Donepezil hydrochloride, a cholinesterase inhibitor, was studied in few studies which showed improvement in the expressive and receptive speech of autistic children. We therefore undertook an open label trial to evaluate this effect on speech function in Korean autistic children. METHODS: Twenty-one patients (18 males, 3 females, average age 77.9+/-23.7 months), with a diagnosis of autism spectrum disorder enrolled in a 12-week open label trial of donepezil hydrochloride. Changes were evaluated by PLS (Preschool language scale). Testing was administered at baseline and at 12-week follow-up. RESULTS: Test administered at baseline and at 12-week follow-up showed gains in both expressive and receptive speech functions. CONCLUSION: Donepezil hydrochloride, a cholinesterase inhibitor, appears to improve expressive and receptive speech functions of autistic children.

Therapeutic effect of Donepezil hydrochloride on Alzheimer's disease rats / 吉林大学学报(医学版)

Objective To explore the mechanism of therapeutic effect of Donepezil hydrochloride on Alzheimer's disease(AD) rats.Methods According to weight,36 rats were divided into normal group,model group and Donepezil hydrochloride group.AD rat model was set up by injecting D-galactose into abdominal cavity for seven weeks,learning and memory function of rats was determined by using Morris water maze and Step-down test.The section of rat cerebral cortex and hippocampus were stained with haematoxylin eosin(HE),and the effect of Donepezil hydrochloride was observed by detecting the MDA content and SOD activity in cerebral tissue.Results Compared with model group,latency and distance of Donepezil hydrochloride rats shortened on the fourth day and the fifth day,starting angle of Donepezil hydrochloride rats shortened on the fourth day and the fifth day in the Morris water maze test,error times of Donepezil hydrochloride rats decreased on the first day and the second day in Step-down test;MDA content in cerebral tissue of Donepezil hydrochloride rat was deceased(P

Effect of donepezil hydrochloride on learning and memory function of normal under age rats / 吉林大学学报(医学版)

0.05).Conclusion Donepezil hydrochloride do not improve the learning and memory function of normal under age rats.

Formula Optimization of Piribedil Hydrochloride Oral-Disintegrating Tablets / 中国药房

OBJECTIVE:To optimize the formula of piribedil hydrochloride orally disintegrating tablets and to investigate their related indexes.METHODS:Taking the contents of crospovidone(PVP XL)(disintegrating agent),amylum pregelatinisatum(loading agent) and Gum Acacia(glidant) as factors,the disintegrating time(td),the wet time(t) and the suspend stability(?A) as the evaluate indexes to carry on the orthogonal experimental to optimize the formula.The dissolution curve of the optimized formula was drawn.RESULTS:The optimized formula for the piribedil hydrochloride orally disintegrating tablets were as follows:the contents of crospovidone(PVP XL),amylum pregelatinisatum and Gum Acacia were 15%,20%,and 15% respectively.The prepared orally disintegrating tablets disintegrated completely within 30s and dissolved basically within 2min.CONCLUSION:The prepared preparation can meet the related standards specified of China Pharmacopeia.

Determination of Related Substances in Donepezil Hydrochloride Tablets by HPLC / 中国药房

OBJECTIVE:To establish an HPLC method for the determination of related substances in Donepezil hydrochloride tablets.METHODS:The separation was performed on AlltimaTM C18 column with mobile phase consisted of 0.01 mol?L-1 dipotassium hydrogen phosphate(3% triethylamine,pH=4.3)-methanol(60 :40) and flow rate of 1.0 mL?min-1.The detection wavelength was set at 271 nm and the column temperature was maintained at 35 ℃.The content of related substance was calculated by self-control with main component.RESULTS:Related substances were completely separated from the main constituent and the impurities were separated well from each other.The determination limit was 0.05 ng and the contents of related substances were 0.42%.CONCLUSION:The method is specific,sensitive and reproducible for the determination of related substances in Donepezil hydrochloride tablets.

Clinical research of donepezil hydrochloride in treatment of vascular dementia / 中国康复理论与实践

@#ObjectiveTo assess the clinical efficacy and safety of donepezil in treating the mild to moderate cognitive impairment of vascular dementia.Methods60 patients with vascular dementia were randomly divided into therapy group (donepezil 5 mg/d for 4 weeks, and then increased to 10 mg/d) and control group (piracetan 800 mg,3/d). All patients were assessed with Mini Mental State Examination (MMSE), Wechsler Adult Intelligence Revised in China (WAIS-RC), Activities of daily living (ADL), and Clinical Global Impression (CGI), before and 12 weeks after treatment. ResultsMMSE scores improved significantly in both groups after the treatment. The therapy group produced significantly better scores than the control groups on the MMSE(P<0.05). WAIS-RC scores improved significantly in the therapy groups(P<0.01), but there was no significant difference for control groups(P>0.05), before and after treatment. Severity Improvement(SI) score of ADL and CGI in the both groups decreased. The total efficiencies of donepezil and piracetan groups were 86% and 56% respectively. There was no significant difference in adverse effects between two groups. ConclusionDonepezil can improve the cognitive function of patients with vascular dementia, which seems better than that of piracetan, and it is fairly safe for vascular dementia patients to take donepezil 10 mg a day.