Patents lie at the interface between technology and law. This review provides a summary of four high profile cases from 2022 in which patents in the pharmaceutical or medical space were litigated in the UK Courts. The first case concerns Astellas’ patent for Betmiga® (mirabegron) for overactive bladder. The second case involves a patent to Bristol-Meyers Squibb for Eliquis® (apixaban) for thromboembolic disorders. The third case concerns Novartis’ patent for Exjade® (deferasirox) for use in the treatment of conditions involving excess iron in the blood caused by haemochromatosis, etc. In the final case, Novartis defended its patent for Gilenya® (fingolimod) as a disease modifying therapy for relapsing remitting multiple sclerosis. The article aims to focus on the technology behind the patents and to provide an insight into how science interacts with law in the context of patent enforcement and infringement.
{"title":"Case Law: A Review of Selected Pharmaceutical Patents Litigated in the UK Courts during 2022","authors":"Sarah-Jane Crawford, H. O'Brien, J. A. Stones","doi":"10.5920/bjpharm.1346","DOIUrl":"https://doi.org/10.5920/bjpharm.1346","url":null,"abstract":"Patents lie at the interface between technology and law. This review provides a summary of four high profile cases from 2022 in which patents in the pharmaceutical or medical space were litigated in the UK Courts. The first case concerns Astellas’ patent for Betmiga® (mirabegron) for overactive bladder. The second case involves a patent to Bristol-Meyers Squibb for Eliquis® (apixaban) for thromboembolic disorders. The third case concerns Novartis’ patent for Exjade® (deferasirox) for use in the treatment of conditions involving excess iron in the blood caused by haemochromatosis, etc. In the final case, Novartis defended its patent for Gilenya® (fingolimod) as a disease modifying therapy for relapsing remitting multiple sclerosis. The article aims to focus on the technology behind the patents and to provide an insight into how science interacts with law in the context of patent enforcement and infringement.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"98 24","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139131835","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
It isessential to understand excipients’ critical material attributes. A QbDstrategy that includes historical data analysis and experimental work has beenused in functional excipients such as Hypromellose (HPMC) to develop thisunderstanding. The use of multivariate analysis helped to identify excipientvariability and the support it could provide to improve the final product robustness.
{"title":"Ensuring Pharmaceutical Product Success through Excipient QbD Efforts","authors":"M. S. Qadir","doi":"10.5920/bjpharm.1243","DOIUrl":"https://doi.org/10.5920/bjpharm.1243","url":null,"abstract":"It isessential to understand excipients’ critical material attributes. A QbDstrategy that includes historical data analysis and experimental work has beenused in functional excipients such as Hypromellose (HPMC) to develop thisunderstanding. The use of multivariate analysis helped to identify excipientvariability and the support it could provide to improve the final product robustness.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89676840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A. Kaya, Niusha Ansari-Fard, D. Alves, B. Arafat, H. Chichger, Mohammad Najlah
Diethyldithiocarbamate zinc (Zn(DDC)2), has shown promising antineoplastic effects against a wide variety of cancers. However, this application was hindered by its poor water solubility. Therefore, complexation with cyclodextrin was used to enhance the solubility. Five different concentrations of 2-hydroxyl beta-cyclodextrin (HP) and ether beta-cyclodextrin (SBE) were used. CD-Zn(DDC)2 solutions were freez-dried for further characterisation using DSC, TGA and FT-IR. The phase solubility study showed a significant water-solubility enchantment of Zn(DDC)2, and the characterisation studies confirmed the formation of inclusion complexes CD-Zn(DDC)2. Overall, CDs have improved Zn(DDC)2 solubility significantly and showed a promising anticancer activity against lung cancer cells. Hence, CD-Zn(DDC)2 complexes have a great potential for further studies against cancer.
{"title":"Solubility Enhancement for Dietheyldithiocarbamate-Zinc for Lung Cancer Treatment","authors":"A. Kaya, Niusha Ansari-Fard, D. Alves, B. Arafat, H. Chichger, Mohammad Najlah","doi":"10.5920/bjpharm.1147","DOIUrl":"https://doi.org/10.5920/bjpharm.1147","url":null,"abstract":"Diethyldithiocarbamate zinc (Zn(DDC)2), has shown promising antineoplastic effects against a wide variety of cancers. However, this application was hindered by its poor water solubility. Therefore, complexation with cyclodextrin was used to enhance the solubility. Five different concentrations of 2-hydroxyl beta-cyclodextrin (HP) and ether beta-cyclodextrin (SBE) were used. CD-Zn(DDC)2 solutions were freez-dried for further characterisation using DSC, TGA and FT-IR. The phase solubility study showed a significant water-solubility enchantment of Zn(DDC)2, and the characterisation studies confirmed the formation of inclusion complexes CD-Zn(DDC)2. Overall, CDs have improved Zn(DDC)2 solubility significantly and showed a promising anticancer activity against lung cancer cells. Hence, CD-Zn(DDC)2 complexes have a great potential for further studies against cancer. ","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87425494","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The influence of HPMCviscosity and the degree of substitution hydroxypropyl level (DSHP) on therelease rate of gliclazide was examined. The increase in the HPMC viscosity ledto a significant decrease in the release rate. The second parameter, DSHP,showed a surprisingly high impact on the release rate with higher hydroxypropyllevels leading to a faster drug release. The results demonstrated the need forcontrol on both parameters for formulators of gliclazide tablets in order toensure a consistent drug release performance.
{"title":"Impact of Critical Material Attributes of HPMC on the Release of Gliclazide from Hydrophilic Matrix Tablets","authors":"M. S. Qadir, Carsten Huettermann","doi":"10.5920/bjpharm.1244","DOIUrl":"https://doi.org/10.5920/bjpharm.1244","url":null,"abstract":"The influence of HPMCviscosity and the degree of substitution hydroxypropyl level (DSHP) on therelease rate of gliclazide was examined. The increase in the HPMC viscosity ledto a significant decrease in the release rate. The second parameter, DSHP,showed a surprisingly high impact on the release rate with higher hydroxypropyllevels leading to a faster drug release. The results demonstrated the need forcontrol on both parameters for formulators of gliclazide tablets in order toensure a consistent drug release performance.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73030700","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
O. Akin-Ajani, Olamide I. Agbomeji, Oluwatoyin A. Odeku, U. Ahmadu
Poir starches from three cultivars (Lagos, Giwa, and Sule) were evaluated asexo-disintegrants (5 and 10%w/w) in paracetamol tablet formulations to determine whether the similarity in their physicochemical and material properties translates to performance in tablet formulation. The tablets were prepared by wet granulation and were evaluated for compressional properties (Heckel equation), mechanical strength (crushing strength and friability), and drug release (disintegration and dissolution times). Plastic deformation occurred in all tablets with rank order for the onset of plastic deformation Lagos>Giwa>Sule. An increase in the concentration of disintegrants in the tablets led to a decrease in mean yield pressure, total relative precompression density, and relative density at low pressure, but an increase in relative density at zero pressure. The crushing strength and disintegration times of the tablets were dependent on the disintegrants' concentration. All tablets passed the disintegration test (≤15min) with tablets containing the Sule cultivar producing the fastest disintegration (p<0.05). Tablets containing 10% of the Sule cultivar had the fastest release of paracetamol (t80=32.1min), though it failed the compendial standard for immediate release tablets (t80≤30min). Starches from the three cultivars despite their similar physicochemical and material properties exhibited different disintegrant properties and could find different applications as excipients in tablet formulations.
{"title":"Comparative Evaluation of the Disintegrant Properties of Starches from Three Cultivars of Dioscorea rotundata (Poir)","authors":"O. Akin-Ajani, Olamide I. Agbomeji, Oluwatoyin A. Odeku, U. Ahmadu","doi":"10.5920/bjpharm.880","DOIUrl":"https://doi.org/10.5920/bjpharm.880","url":null,"abstract":"Poir starches from three cultivars (Lagos, Giwa, and Sule) were evaluated asexo-disintegrants (5 and 10%w/w) in paracetamol tablet formulations to determine whether the similarity in their physicochemical and material properties translates to performance in tablet formulation. The tablets were prepared by wet granulation and were evaluated for compressional properties (Heckel equation), mechanical strength (crushing strength and friability), and drug release (disintegration and dissolution times). Plastic deformation occurred in all tablets with rank order for the onset of plastic deformation Lagos>Giwa>Sule. An increase in the concentration of disintegrants in the tablets led to a decrease in mean yield pressure, total relative precompression density, and relative density at low pressure, but an increase in relative density at zero pressure. The crushing strength and disintegration times of the tablets were dependent on the disintegrants' concentration. All tablets passed the disintegration test (≤15min) with tablets containing the Sule cultivar producing the fastest disintegration (p<0.05). Tablets containing 10% of the Sule cultivar had the fastest release of paracetamol (t80=32.1min), though it failed the compendial standard for immediate release tablets (t80≤30min). Starches from the three cultivars despite their similar physicochemical and material properties exhibited different disintegrant properties and could find different applications as excipients in tablet formulations.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"56 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83047037","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zoe Chu1,2, Christopher Windows-Yule¹, Ian Gabbott², Gavin Reynolds², Rachael Shinebaum² and Andy Ingram¹1. School of Chemical Engineering, University of Birmingham, Edgbaston, B15 2TT2. Oral Product Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield, UKEmail: zhc906@student.bham.ac.ukIntroductionA tablet consists of the active pharmaceutical ingredients (API), and the other components, excipients. A tablet needs to withstand coating, packing and shipping stresses whilst maintaining the dissolution time; therefore, the tensile strength is of great importance. Currently, there is a lack of understanding on why excipients improve the bulk powder properties and the bonding mechanisms of the powder during compression. This makes tablet formulation development an inefficient trial-and-error process that is required for every new API (1). Literature has shown that the surface energy of the powders contributes a significant amount towards the tablet tensile strength. Hydrophobic powders have a lower surface energy (2) and are seen to disrupt this tablet strength (3,4).Experimental Aim and MethodThe aim was to investigate the impact of the hydrophobicity of excipient powders on tabletability of microcrystalline cellulose. This was done by mixing powders of varying hydrophobicity with MCC at varying mass fractions. There was focus on a lower mass fraction (0.02-0.1 m/m) with increasing increments of 0.02 m/m of added additive as well as gaining a global picture (0.2-1 m/m) with increments of 0.2 m/m.ResultsIt was found that at low mass fractions (0.02-0.4 m/m) of additive added the hydrophobic powders disrupted the tablet strength more compared to hydrophilic powders which could be attributed to the levels of surface energy of the additive. In contrast, at higher mass fractions (0.6-0.8 m/m), the surface energy is not as important and it is hypothesised that the deformation mechanisms of the additives governs the tablet strength.1. Reynolds GK, Campbell JI, Roberts RJ. A compressibility based model for predicting the tensile strength of directly compressed pharmaceutical powder mixtures. Int J Pharm [Internet]. 2017;531(1):215–24. Available from: http://dx.doi.org/10.1016/j.ijpharm.2017.08.0752. Sunkara D, Capece M. Influence of Material Properties on the Effectiveness of Glidants Used to Improve the Flowability of Cohesive Pharmaceutical Powders. AAPS PharmSciTech. 2018;19(4):1920–30. 3. Zuurman K, Maarschalk KVDV, Bolhuis GK. Effect of magnesium stearate on bonding and porosity expansion of tablets produced from materials with different consolidation properties. 1999;179:107–15. 4. Mishra SM, Rohera BD. Mechanics of tablet formation: a comparative evaluation of percolation theory with classical concepts. Pharm Dev Technol [Internet]. 2019;24(8):954–66. Available from: https://doi.org/10.1080/10837450.2019.1599913
{"title":"Effect of Hydrophobic Powders on the Tensile Strength of the Tablet","authors":"Zoe Chu","doi":"10.5920/bjpharm.1162","DOIUrl":"https://doi.org/10.5920/bjpharm.1162","url":null,"abstract":"Zoe Chu1,2, Christopher Windows-Yule¹, Ian Gabbott², Gavin Reynolds², Rachael Shinebaum² and Andy Ingram¹1. School of Chemical Engineering, University of Birmingham, Edgbaston, B15 2TT2. Oral Product Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield, UKEmail: zhc906@student.bham.ac.ukIntroductionA tablet consists of the active pharmaceutical ingredients (API), and the other components, excipients. A tablet needs to withstand coating, packing and shipping stresses whilst maintaining the dissolution time; therefore, the tensile strength is of great importance. Currently, there is a lack of understanding on why excipients improve the bulk powder properties and the bonding mechanisms of the powder during compression. This makes tablet formulation development an inefficient trial-and-error process that is required for every new API (1). Literature has shown that the surface energy of the powders contributes a significant amount towards the tablet tensile strength. Hydrophobic powders have a lower surface energy (2) and are seen to disrupt this tablet strength (3,4).Experimental Aim and MethodThe aim was to investigate the impact of the hydrophobicity of excipient powders on tabletability of microcrystalline cellulose. This was done by mixing powders of varying hydrophobicity with MCC at varying mass fractions. There was focus on a lower mass fraction (0.02-0.1 m/m) with increasing increments of 0.02 m/m of added additive as well as gaining a global picture (0.2-1 m/m) with increments of 0.2 m/m.ResultsIt was found that at low mass fractions (0.02-0.4 m/m) of additive added the hydrophobic powders disrupted the tablet strength more compared to hydrophilic powders which could be attributed to the levels of surface energy of the additive. In contrast, at higher mass fractions (0.6-0.8 m/m), the surface energy is not as important and it is hypothesised that the deformation mechanisms of the additives governs the tablet strength.1. Reynolds GK, Campbell JI, Roberts RJ. A compressibility based model for predicting the tensile strength of directly compressed pharmaceutical powder mixtures. Int J Pharm [Internet]. 2017;531(1):215–24. Available from: http://dx.doi.org/10.1016/j.ijpharm.2017.08.0752. Sunkara D, Capece M. Influence of Material Properties on the Effectiveness of Glidants Used to Improve the Flowability of Cohesive Pharmaceutical Powders. AAPS PharmSciTech. 2018;19(4):1920–30. 3. Zuurman K, Maarschalk KVDV, Bolhuis GK. Effect of magnesium stearate on bonding and porosity expansion of tablets produced from materials with different consolidation properties. 1999;179:107–15. 4. Mishra SM, Rohera BD. Mechanics of tablet formation: a comparative evaluation of percolation theory with classical concepts. Pharm Dev Technol [Internet]. 2019;24(8):954–66. Available from: https://doi.org/10.1080/10837450.2019.1599913","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"59 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89488333","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bayan Abu Ras, Youssef Haggag, M. Isreb, M. El Tanani
This study investigate the effect of processparameters on the size, distribution, zeta potential and loading efficiency for the co-delivery of liposomalformulation of Ran-RCC1 inhibitory peptide (RANIP) and doxorubicin (DOX) tobreast cancer. The results showthat drug concentration, pH and ultrasound intensity are all critical factors tocontrol the attributes of the liposomes.
{"title":"Effect of Process Parameters on the critical attributes of the Liposomal formulations","authors":"Bayan Abu Ras, Youssef Haggag, M. Isreb, M. El Tanani","doi":"10.5920/bjpharm.1172","DOIUrl":"https://doi.org/10.5920/bjpharm.1172","url":null,"abstract":"This study investigate the effect of processparameters on the size, distribution, zeta potential and loading efficiency for the co-delivery of liposomalformulation of Ran-RCC1 inhibitory peptide (RANIP) and doxorubicin (DOX) tobreast cancer. The results showthat drug concentration, pH and ultrasound intensity are all critical factors tocontrol the attributes of the liposomes.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77072129","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Implantable drug delivery systems are presented as a potential alternative to current treatments of chronic conditions. The aim of this work was to formulate a subcutaneous implantable device made with prefabricated poly(caprolactone) (PCL) cylinders, loaded with olanzapine (OLZ) as a model drug and cyclodextrin in a mass ratio of 1:1. The final formulation was characterized using optical microscopy, infrared spectroscopy, thermal analysis, and X-ray diffraction. The proposed device was successfully fabricated and demonstrated ability to control drug release for 60 days. With continued development, these novel implants could be an alternative to currently available treatments for schizophrenia.
{"title":"Formulation of an implantable device from mini tablets-in-PCL cylinders for sustained delivery of a hydrophobic drug","authors":"Camila J Picco, Peter E. McKenna, E. Larrañeta","doi":"10.5920/bjpharm.1153","DOIUrl":"https://doi.org/10.5920/bjpharm.1153","url":null,"abstract":"Implantable drug delivery systems are presented as a potential alternative to current treatments of chronic conditions. The aim of this work was to formulate a subcutaneous implantable device made with prefabricated poly(caprolactone) (PCL) cylinders, loaded with olanzapine (OLZ) as a model drug and cyclodextrin in a mass ratio of 1:1. The final formulation was characterized using optical microscopy, infrared spectroscopy, thermal analysis, and X-ray diffraction. The proposed device was successfully fabricated and demonstrated ability to control drug release for 60 days. With continued development, these novel implants could be an alternative to currently available treatments for schizophrenia.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87942426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Shilpkala Gade, E. Larrañeta, R. Donnelly, R. Vanrell, C. A. ALVAREZ LORENZO, R. Thakur
Age-related macular degeneration (AMD) is a potentially blinding posterior segment disease; inflammatory responses and subretinal drusen formation lead to leaky blood vessels. The current treatment method involves intravitreal injections of anti-VEGF agents, which is highly invasive and requires frequent injections administered by trained personnel. Periocular injections such as trans-/intra-scleral injections would provide a minimally invasive treatment option. The sclera is the outermost protective layer occupying 5/6th of the ocular globe. Owing to its avascular nature and self-healing ability, sclera could be the potential space for the delivery of depot forming long-acting formulations. This project focuses on the development of chitosan grafted poly(n-isopropylacrylamide) (Cs-g-PNIPAAm) gel for the sustained intrascleral delivery of small molecular weight, multiple tyrosine kinase inhibitor Sunitinib malate.
{"title":"Development and characterization of injectable depot forming thermoresponsive hydrogel for the sustained intrascleral delivery of Sunitinib Hollow microneedles for intrascleral drug delivery","authors":"Shilpkala Gade, E. Larrañeta, R. Donnelly, R. Vanrell, C. A. ALVAREZ LORENZO, R. Thakur","doi":"10.5920/bjpharm.1175","DOIUrl":"https://doi.org/10.5920/bjpharm.1175","url":null,"abstract":"Age-related macular degeneration (AMD) is a potentially blinding posterior segment disease; inflammatory responses and subretinal drusen formation lead to leaky blood vessels. The current treatment method involves intravitreal injections of anti-VEGF agents, which is highly invasive and requires frequent injections administered by trained personnel. Periocular injections such as trans-/intra-scleral injections would provide a minimally invasive treatment option. The sclera is the outermost protective layer occupying 5/6th of the ocular globe. Owing to its avascular nature and self-healing ability, sclera could be the potential space for the delivery of depot forming long-acting formulations. This project focuses on the development of chitosan grafted poly(n-isopropylacrylamide) (Cs-g-PNIPAAm) gel for the sustained intrascleral delivery of small molecular weight, multiple tyrosine kinase inhibitor Sunitinib malate.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81432122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zoe McKinnon, Hannah Batchelor, I. Khadra, Gavin W. Halbert
Adequatedrug solubility in the gastrointestinal tract is essential for systemic therapyof orally administered medications. To carry out research on the solubility ofpoorly soluble drugs in vitro, simulated intestinal fluid (SIF) is usedin place of human intestinal fluid (HIF). However, typical SIF reflects averagecompositions of HIF rather than the full range of compositions previouslyreported. This study examines a new suite of SIF media (based on variabilityobserved in HIF) to explore the range of solubility of four poorly soluble drugs(Naproxen, Indomethacin, Phenytoin and Tadalafil) in the fasted state.
{"title":"Solubility measurement of poorly soluble drugs in fasted state simulated intestinal fluid","authors":"Zoe McKinnon, Hannah Batchelor, I. Khadra, Gavin W. Halbert","doi":"10.5920/bjpharm.1075","DOIUrl":"https://doi.org/10.5920/bjpharm.1075","url":null,"abstract":"Adequatedrug solubility in the gastrointestinal tract is essential for systemic therapyof orally administered medications. To carry out research on the solubility ofpoorly soluble drugs in vitro, simulated intestinal fluid (SIF) is usedin place of human intestinal fluid (HIF). However, typical SIF reflects averagecompositions of HIF rather than the full range of compositions previouslyreported. This study examines a new suite of SIF media (based on variabilityobserved in HIF) to explore the range of solubility of four poorly soluble drugs(Naproxen, Indomethacin, Phenytoin and Tadalafil) in the fasted state.","PeriodicalId":9253,"journal":{"name":"British Journal of Pharmacy","volume":"119 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79415204","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：