Multiple emulsions are of great therapeutic interest especially in the administration of medicines which can be inactivated by digestive enzymes;moreover the researches of formulation not being often easy, a control o...Multiple emulsions are of great therapeutic interest especially in the administration of medicines which can be inactivated by digestive enzymes;moreover the researches of formulation not being often easy, a control of the different phases physicochemical parameters would be of great interest in rapid formulations and at low cost. When formulating emulsions, the preliminary tests, also known as formulation tests, constitute a step which can be long and expensive because of the quantity of reagents that can be used. A rigorous methodology could thus be of great interest, which is at the aim of our study which consists of evaluating the physico-chemical parameters of different phases used to make thus multiple emulsions. In our study, physico-chemical parameters such as conductivity, pH, density, viscosity, and surface tension have been studied by direct measurement using equipment and also by means of suitable mounting. The results showed that the pH and the surface tension have an important role in the prediction of the stability of emulsions, these latter must be of the same order of magnitude. For all phases conductivity does not have too much interest apart from helping to determine the type of the emulsion.展开更多
Biological treatment efficiency of six pharmaceutical compounds (acetazolamide, metronidazole, opipramol, piracetam, salicylamide and tinidazole) was evaluated using lab-scale Sequencing Batch Reactor (SBR). Compa...Biological treatment efficiency of six pharmaceutical compounds (acetazolamide, metronidazole, opipramol, piracetam, salicylamide and tinidazole) was evaluated using lab-scale Sequencing Batch Reactor (SBR). Comparative biological degradation processes of two types of activated sludge from municipal and pharmaceutical industry sewage treatment plants were examined. Three different organic loadings (0.05 g COD/g MLSS.d, 0.1 g COD/g MLSS.d and 0.2 g COD/g MLSS-d) and reaction time on the efficiency of Active Pharmaceutical Ingredient (API) decomposition were examined. Chemical oxygen demand, non-purgeable organic carbon as well as ammonium nitrogen contents were monitored by standard methods. Percentage of API decomposition was analysed by High Performance Liquid Chromatography (HPLC). The overall API removal efficiency was strictly dependent on the type of activated sludge origin. The main biodegradation products were identified using HPLC-MS,1H NMR and 13C NMR methods as e.g. ({4-[3-(5H-dibenzo[b,f]azepin-5-yl]piperazin-l-yl}methanamine) and (2-amino-1,3,4-thiadiazol-5-sulfonamide) for opipramol and acetazolamide respectively.展开更多
Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-co...Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-consuming and cost-intensive.There is still a lack of effective theoretical models to accurately describe and predict the biological solubility of drugs to reduce costs.Therefore,in this study,osaprazole and irbesartan were selected as model drugs,and their solubility in solutions containing surfactants and biorelevant media was measured experimentally.By calculating the parameters of each component using the perturbed-chain statistical associating fluid theory(PC-SAFT)model,combined with pH-dependent and micellar solubilization models,the thermodynamic phase behavior of the two drugs was successfully modeled,and the predicted results were in good agreement with the experimental values.These results demonstrate that the model combination used provides important basic parameters and theoretical guidance for the development and screening of poorly soluble drugs and related formulations.展开更多
The disposal of unwanted and expired medications has been a concern to public health practitioners, and patients alike. The objective of the current investigation was to look closely at the practice of patients and ca...The disposal of unwanted and expired medications has been a concern to public health practitioners, and patients alike. The objective of the current investigation was to look closely at the practice of patients and carers in Nablus-Palestine with regard to disposal of unused or expired medicines. The study was a cross-sectional survey administered via face-to-face structured interviews with randomly selected patients, community pharmacists and physicians from Nablus-Palestine. Two hundred and fifty patients/carers completed a questionnaire regarding medicines disposal current practice, effects on environment, and their views to overcome this problem. Most of the people completing the questionnaire (67%) stated that they throw unwanted medicines in the normal household bins, and about 75% think that this can impose illegal and environmental hazards. Nearly half of the questionnaire showed that main reason for need to dispose medicines was possessing expired ones with almost believe there should be more appropriate way to dispose medicines. About 95% said they have not been directed for safe disposal of medicines with 46% thinking that a national campaign can be very educative in this issue mainly through Ministry of Health (54%) followed by .73% of the sampled patients were in favor of national campaign to direct people to safe disposal of medicines. This pilot study in Nablus clearly highlights the need for appropriate method for safe disposal of medicines in Palestine through guidelines in pharmacies and hospitals. A well organized method for collecting unwanted medicines from people should be encouraged through appropriate teaching of patients and caters about effects of waste medicines on environment as well as being domestic hazard. The data and information is valuable for furthering discussions regarding patients behaviour and also provides a basis for future research into determining what quantities of active pharmaceutical ingredients (APIs) are disposed, enter the environment and what effects it can impose.展开更多
Pulmonary hypertension(PH)is a severe pathophysiological condition characterized by pulmonary artery remodeling and continuous increases in pulmonary artery pressure,which may eventually develop to right heart failure...Pulmonary hypertension(PH)is a severe pathophysiological condition characterized by pulmonary artery remodeling and continuous increases in pulmonary artery pressure,which may eventually develop to right heart failure and death.Although newly discovered and incredible treatment strategies in recent years have improved the prognosis of PH,limited types of effective and economical drugs for PH still makes it as a life-threatening disease.Some drugs from Chinese materia medica(CMM)have been traditionally applied in the treatment of lung diseases.Accumulating evidence suggests active pharmaceutical ingredients(APIs)derived from those medicines brings promising future for the prevention and treatment of PH.In this review,we summarized the pharmacological effects of APIs derived from CMM which are potent in treating PH,so as to provide new thoughts for initial drug discovery and identification of potential therapeutic strategies in alternative medicine for PH.展开更多
We report here a cocrystal with artesunate as the active pharmaceutical ingredient(API)and a pharmaceutical intermediate 4,4?-bipyridine as the cocrystal former(CCF).The analysis of single-crystal X-ray diffraction de...We report here a cocrystal with artesunate as the active pharmaceutical ingredient(API)and a pharmaceutical intermediate 4,4?-bipyridine as the cocrystal former(CCF).The analysis of single-crystal X-ray diffraction demonstrates that the eutectic structural unit consists of two artesunate molecules and one 4,4?-bipyridine molecule with their ratio to be 2:1.The carboxyl group on artesunate acts as a donor,and the acceptor is N on 4,4?-bipyridine,forming an O–H···N hydrogen bond.The appearance of new diffraction peaks in the X-ray powder diffraction pattern also indicates the formation of new phases.The PXRD results indicated a pure phase for the synthesized sample.The cocrystal is slightly soluble in water.Antimicrobial activities showed that the cocrystal displayed effective inhibition of different bacteria.展开更多
文摘Multiple emulsions are of great therapeutic interest especially in the administration of medicines which can be inactivated by digestive enzymes;moreover the researches of formulation not being often easy, a control of the different phases physicochemical parameters would be of great interest in rapid formulations and at low cost. When formulating emulsions, the preliminary tests, also known as formulation tests, constitute a step which can be long and expensive because of the quantity of reagents that can be used. A rigorous methodology could thus be of great interest, which is at the aim of our study which consists of evaluating the physico-chemical parameters of different phases used to make thus multiple emulsions. In our study, physico-chemical parameters such as conductivity, pH, density, viscosity, and surface tension have been studied by direct measurement using equipment and also by means of suitable mounting. The results showed that the pH and the surface tension have an important role in the prediction of the stability of emulsions, these latter must be of the same order of magnitude. For all phases conductivity does not have too much interest apart from helping to determine the type of the emulsion.
文摘Biological treatment efficiency of six pharmaceutical compounds (acetazolamide, metronidazole, opipramol, piracetam, salicylamide and tinidazole) was evaluated using lab-scale Sequencing Batch Reactor (SBR). Comparative biological degradation processes of two types of activated sludge from municipal and pharmaceutical industry sewage treatment plants were examined. Three different organic loadings (0.05 g COD/g MLSS.d, 0.1 g COD/g MLSS.d and 0.2 g COD/g MLSS-d) and reaction time on the efficiency of Active Pharmaceutical Ingredient (API) decomposition were examined. Chemical oxygen demand, non-purgeable organic carbon as well as ammonium nitrogen contents were monitored by standard methods. Percentage of API decomposition was analysed by High Performance Liquid Chromatography (HPLC). The overall API removal efficiency was strictly dependent on the type of activated sludge origin. The main biodegradation products were identified using HPLC-MS,1H NMR and 13C NMR methods as e.g. ({4-[3-(5H-dibenzo[b,f]azepin-5-yl]piperazin-l-yl}methanamine) and (2-amino-1,3,4-thiadiazol-5-sulfonamide) for opipramol and acetazolamide respectively.
基金the financial support from the National Natural Science Foundation of China(22278070,21978047,21776046)。
文摘Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-consuming and cost-intensive.There is still a lack of effective theoretical models to accurately describe and predict the biological solubility of drugs to reduce costs.Therefore,in this study,osaprazole and irbesartan were selected as model drugs,and their solubility in solutions containing surfactants and biorelevant media was measured experimentally.By calculating the parameters of each component using the perturbed-chain statistical associating fluid theory(PC-SAFT)model,combined with pH-dependent and micellar solubilization models,the thermodynamic phase behavior of the two drugs was successfully modeled,and the predicted results were in good agreement with the experimental values.These results demonstrate that the model combination used provides important basic parameters and theoretical guidance for the development and screening of poorly soluble drugs and related formulations.
文摘The disposal of unwanted and expired medications has been a concern to public health practitioners, and patients alike. The objective of the current investigation was to look closely at the practice of patients and carers in Nablus-Palestine with regard to disposal of unused or expired medicines. The study was a cross-sectional survey administered via face-to-face structured interviews with randomly selected patients, community pharmacists and physicians from Nablus-Palestine. Two hundred and fifty patients/carers completed a questionnaire regarding medicines disposal current practice, effects on environment, and their views to overcome this problem. Most of the people completing the questionnaire (67%) stated that they throw unwanted medicines in the normal household bins, and about 75% think that this can impose illegal and environmental hazards. Nearly half of the questionnaire showed that main reason for need to dispose medicines was possessing expired ones with almost believe there should be more appropriate way to dispose medicines. About 95% said they have not been directed for safe disposal of medicines with 46% thinking that a national campaign can be very educative in this issue mainly through Ministry of Health (54%) followed by .73% of the sampled patients were in favor of national campaign to direct people to safe disposal of medicines. This pilot study in Nablus clearly highlights the need for appropriate method for safe disposal of medicines in Palestine through guidelines in pharmacies and hospitals. A well organized method for collecting unwanted medicines from people should be encouraged through appropriate teaching of patients and caters about effects of waste medicines on environment as well as being domestic hazard. The data and information is valuable for furthering discussions regarding patients behaviour and also provides a basis for future research into determining what quantities of active pharmaceutical ingredients (APIs) are disposed, enter the environment and what effects it can impose.
文摘Pulmonary hypertension(PH)is a severe pathophysiological condition characterized by pulmonary artery remodeling and continuous increases in pulmonary artery pressure,which may eventually develop to right heart failure and death.Although newly discovered and incredible treatment strategies in recent years have improved the prognosis of PH,limited types of effective and economical drugs for PH still makes it as a life-threatening disease.Some drugs from Chinese materia medica(CMM)have been traditionally applied in the treatment of lung diseases.Accumulating evidence suggests active pharmaceutical ingredients(APIs)derived from those medicines brings promising future for the prevention and treatment of PH.In this review,we summarized the pharmacological effects of APIs derived from CMM which are potent in treating PH,so as to provide new thoughts for initial drug discovery and identification of potential therapeutic strategies in alternative medicine for PH.
基金supported by the National Natural Science Foundation of China(No.21861005)the Foundation of Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources(CMEMR2018-C15 and CMEMR2016-A11)。
文摘We report here a cocrystal with artesunate as the active pharmaceutical ingredient(API)and a pharmaceutical intermediate 4,4?-bipyridine as the cocrystal former(CCF).The analysis of single-crystal X-ray diffraction demonstrates that the eutectic structural unit consists of two artesunate molecules and one 4,4?-bipyridine molecule with their ratio to be 2:1.The carboxyl group on artesunate acts as a donor,and the acceptor is N on 4,4?-bipyridine,forming an O–H···N hydrogen bond.The appearance of new diffraction peaks in the X-ray powder diffraction pattern also indicates the formation of new phases.The PXRD results indicated a pure phase for the synthesized sample.The cocrystal is slightly soluble in water.Antimicrobial activities showed that the cocrystal displayed effective inhibition of different bacteria.