Quantification, mechanism, and mitigation of active ingredient phase transformation in tablets
| العنوان: | Quantification, mechanism, and mitigation of active ingredient phase transformation in tablets |
|---|---|
| المؤلفون: | Vishard Ragoonanan, Raj Suryanarayanan, Naveen K. Thakral |
| المصدر: | Molecular pharmaceutics. 10(8) |
| سنة النشر: | 2013 |
| مصطلحات موضوعية: | Active ingredient, Calcium Phosphates, Materials science, Colloidal silica, Thiamine Hydrochloride, Inorganic chemistry, Pharmaceutical Science, medicine.disease, Phase Transition, Reaction rate, chemistry.chemical_compound, Film coating, Ethyl cellulose, chemistry, X-Ray Diffraction, Drug Discovery, medicine, Molecular Medicine, Dehydration, Thiamine, Hydrate, Nuclear chemistry, Tablets |
| الوصف: | Model tablet formulations containing thiamine hydrochloride [as a nonstoichiometric hydrate (NSH)] and dicalcium phosphate dihydrate (DCPD) were prepared. In intact tablets, the water released by dehydration of DCPD mediated the transition of NSH to thiamine hydrochloride hemihydrate (HH). The use of an X-ray microdiffractometer with an area detector enabled us to rapidly and simultaneously monitor both the phase transformations. The spatial information, gained by monitoring the tablet from the surface to the core (depth profiling), revealed that both DCPD dehydration and HH formation progressed from the surface to the tablet core as a function of storage time. Film coating of the tablets with ethyl cellulose caused a decrease in both the reaction rates. There was a pronounced lag time, but once initiated, the transformations occurred simultaneously throughout the tablet. Thus the difference in the phase transformation behavior between the uncoated and the coated tablets could not have been discerned without the depth profiling. Incorporation of hydrophilic colloidal silica as a formulation component further slowed down the transformations. By acting as a water scavenger it maintained a very "dry" environment in the tablet matrix. Finally, by coating the NSH particles with hydrophobic colloidal silica, the formation of HH was further substantially decelerated. The microdiffractometric technique not only enabled direct analyses of tablets but also provided the critical spatial information. This helped in the selection of excipients with appropriate functionality to prevent the in situ phase transformations. |
| تدمد: | 1543-8392 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b760e97db3b753d05cd9f3e55ac8b58a https://pubmed.ncbi.nlm.nih.gov/23869937 |
| رقم الانضمام: | edsair.doi.dedup.....b760e97db3b753d05cd9f3e55ac8b58a |
| قاعدة البيانات: | OpenAIRE |
| ResultId |
1 |
|---|---|
| Header |
edsair OpenAIRE edsair.doi.dedup.....b760e97db3b753d05cd9f3e55ac8b58a 774 3 unknown 773.971801757813 |
| PLink |
https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&scope=site&db=edsair&AN=edsair.doi.dedup.....b760e97db3b753d05cd9f3e55ac8b58a&custid=s6537998&authtype=sso |
| FullText |
Array
(
[Availability] => 0
)
Array ( [0] => Array ( [Url] => https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b760e97db3b753d05cd9f3e55ac8b58a# [Name] => EDS - OpenAIRE [Category] => fullText [Text] => View record in OpenAIRE [MouseOverText] => View record in OpenAIRE ) ) |
| Items |
Array
(
[Name] => Title
[Label] => Title
[Group] => Ti
[Data] => Quantification, mechanism, and mitigation of active ingredient phase transformation in tablets
)
Array ( [Name] => Author [Label] => Authors [Group] => Au [Data] => <searchLink fieldCode="AR" term="%22Vishard+Ragoonanan%22">Vishard Ragoonanan</searchLink><br /><searchLink fieldCode="AR" term="%22Raj+Suryanarayanan%22">Raj Suryanarayanan</searchLink><br /><searchLink fieldCode="AR" term="%22Naveen+K%2E+Thakral%22">Naveen K. Thakral</searchLink> ) Array ( [Name] => TitleSource [Label] => Source [Group] => Src [Data] => <i>Molecular pharmaceutics</i>. 10(8) ) Array ( [Name] => DatePubCY [Label] => Publication Year [Group] => Date [Data] => 2013 ) Array ( [Name] => Subject [Label] => Subject Terms [Group] => Su [Data] => <searchLink fieldCode="DE" term="%22Active+ingredient%22">Active ingredient</searchLink><br /><searchLink fieldCode="DE" term="%22Calcium+Phosphates%22">Calcium Phosphates</searchLink><br /><searchLink fieldCode="DE" term="%22Materials+science%22">Materials science</searchLink><br /><searchLink fieldCode="DE" term="%22Colloidal+silica%22">Colloidal silica</searchLink><br /><searchLink fieldCode="DE" term="%22Thiamine+Hydrochloride%22">Thiamine Hydrochloride</searchLink><br /><searchLink fieldCode="DE" term="%22Inorganic+chemistry%22">Inorganic chemistry</searchLink><br /><searchLink fieldCode="DE" term="%22Pharmaceutical+Science%22">Pharmaceutical Science</searchLink><br /><searchLink fieldCode="DE" term="%22medicine%2Edisease%22">medicine.disease</searchLink><br /><searchLink fieldCode="DE" term="%22Phase+Transition%22">Phase Transition</searchLink><br /><searchLink fieldCode="DE" term="%22Reaction+rate%22">Reaction rate</searchLink><br /><searchLink fieldCode="DE" term="%22chemistry%2Echemical%5Fcompound%22">chemistry.chemical_compound</searchLink><br /><searchLink fieldCode="DE" term="%22Film+coating%22">Film coating</searchLink><br /><searchLink fieldCode="DE" term="%22Ethyl+cellulose%22">Ethyl cellulose</searchLink><br /><searchLink fieldCode="DE" term="%22chemistry%22">chemistry</searchLink><br /><searchLink fieldCode="DE" term="%22X-Ray+Diffraction%22">X-Ray Diffraction</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+Discovery%22">Drug Discovery</searchLink><br /><searchLink fieldCode="DE" term="%22medicine%22">medicine</searchLink><br /><searchLink fieldCode="DE" term="%22Molecular+Medicine%22">Molecular Medicine</searchLink><br /><searchLink fieldCode="DE" term="%22Dehydration%22">Dehydration</searchLink><br /><searchLink fieldCode="DE" term="%22Thiamine%22">Thiamine</searchLink><br /><searchLink fieldCode="DE" term="%22Hydrate%22">Hydrate</searchLink><br /><searchLink fieldCode="DE" term="%22Nuclear+chemistry%22">Nuclear chemistry</searchLink><br /><searchLink fieldCode="DE" term="%22Tablets%22">Tablets</searchLink> ) Array ( [Name] => Abstract [Label] => Description [Group] => Ab [Data] => Model tablet formulations containing thiamine hydrochloride [as a nonstoichiometric hydrate (NSH)] and dicalcium phosphate dihydrate (DCPD) were prepared. In intact tablets, the water released by dehydration of DCPD mediated the transition of NSH to thiamine hydrochloride hemihydrate (HH). The use of an X-ray microdiffractometer with an area detector enabled us to rapidly and simultaneously monitor both the phase transformations. The spatial information, gained by monitoring the tablet from the surface to the core (depth profiling), revealed that both DCPD dehydration and HH formation progressed from the surface to the tablet core as a function of storage time. Film coating of the tablets with ethyl cellulose caused a decrease in both the reaction rates. There was a pronounced lag time, but once initiated, the transformations occurred simultaneously throughout the tablet. Thus the difference in the phase transformation behavior between the uncoated and the coated tablets could not have been discerned without the depth profiling. Incorporation of hydrophilic colloidal silica as a formulation component further slowed down the transformations. By acting as a water scavenger it maintained a very "dry" environment in the tablet matrix. Finally, by coating the NSH particles with hydrophobic colloidal silica, the formation of HH was further substantially decelerated. The microdiffractometric technique not only enabled direct analyses of tablets but also provided the critical spatial information. This helped in the selection of excipients with appropriate functionality to prevent the in situ phase transformations. ) Array ( [Name] => ISSN [Label] => ISSN [Group] => ISSN [Data] => 1543-8392 ) Array ( [Name] => URL [Label] => Access URL [Group] => URL [Data] => <link linkTarget="URL" linkTerm="https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b760e97db3b753d05cd9f3e55ac8b58a" linkWindow="_blank">https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b760e97db3b753d05cd9f3e55ac8b58a</link><br /><link linkTarget="URL" linkTerm="https://pubmed.ncbi.nlm.nih.gov/23869937" linkWindow="_blank">https://pubmed.ncbi.nlm.nih.gov/23869937</link> ) Array ( [Name] => AN [Label] => Accession Number [Group] => ID [Data] => edsair.doi.dedup.....b760e97db3b753d05cd9f3e55ac8b58a ) |
| RecordInfo |
Array
(
[BibEntity] => Array
(
[Languages] => Array
(
[0] => Array
(
[Text] => Undetermined
)
)
[Subjects] => Array
(
[0] => Array
(
[SubjectFull] => Active ingredient
[Type] => general
)
[1] => Array
(
[SubjectFull] => Calcium Phosphates
[Type] => general
)
[2] => Array
(
[SubjectFull] => Materials science
[Type] => general
)
[3] => Array
(
[SubjectFull] => Colloidal silica
[Type] => general
)
[4] => Array
(
[SubjectFull] => Thiamine Hydrochloride
[Type] => general
)
[5] => Array
(
[SubjectFull] => Inorganic chemistry
[Type] => general
)
[6] => Array
(
[SubjectFull] => Pharmaceutical Science
[Type] => general
)
[7] => Array
(
[SubjectFull] => medicine.disease
[Type] => general
)
[8] => Array
(
[SubjectFull] => Phase Transition
[Type] => general
)
[9] => Array
(
[SubjectFull] => Reaction rate
[Type] => general
)
[10] => Array
(
[SubjectFull] => chemistry.chemical_compound
[Type] => general
)
[11] => Array
(
[SubjectFull] => Film coating
[Type] => general
)
[12] => Array
(
[SubjectFull] => Ethyl cellulose
[Type] => general
)
[13] => Array
(
[SubjectFull] => chemistry
[Type] => general
)
[14] => Array
(
[SubjectFull] => X-Ray Diffraction
[Type] => general
)
[15] => Array
(
[SubjectFull] => Drug Discovery
[Type] => general
)
[16] => Array
(
[SubjectFull] => medicine
[Type] => general
)
[17] => Array
(
[SubjectFull] => Molecular Medicine
[Type] => general
)
[18] => Array
(
[SubjectFull] => Dehydration
[Type] => general
)
[19] => Array
(
[SubjectFull] => Thiamine
[Type] => general
)
[20] => Array
(
[SubjectFull] => Hydrate
[Type] => general
)
[21] => Array
(
[SubjectFull] => Nuclear chemistry
[Type] => general
)
[22] => Array
(
[SubjectFull] => Tablets
[Type] => general
)
)
[Titles] => Array
(
[0] => Array
(
[TitleFull] => Quantification, mechanism, and mitigation of active ingredient phase transformation in tablets
[Type] => main
)
)
)
[BibRelationships] => Array
(
[HasContributorRelationships] => Array
(
[0] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Vishard Ragoonanan
)
)
)
[1] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Raj Suryanarayanan
)
)
)
[2] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Naveen K. Thakral
)
)
)
)
[IsPartOfRelationships] => Array
(
[0] => Array
(
[BibEntity] => Array
(
[Dates] => Array
(
[0] => Array
(
[D] => 23
[M] => 07
[Type] => published
[Y] => 2013
)
)
[Identifiers] => Array
(
[0] => Array
(
[Type] => issn-print
[Value] => 15438392
)
[1] => Array
(
[Type] => issn-locals
[Value] => edsair
)
)
[Numbering] => Array
(
[0] => Array
(
[Type] => volume
[Value] => 10
)
[1] => Array
(
[Type] => issue
[Value] => 8
)
)
[Titles] => Array
(
[0] => Array
(
[TitleFull] => Molecular pharmaceutics
[Type] => main
)
)
)
)
)
)
)
|
| IllustrationInfo |