語系:
繁體中文
English
說明(常見問題)
回圖書館首頁
手機版館藏查詢
登入
回首頁
切換:
標籤
|
MARC模式
|
ISBD
Enhancing the pharmaceutical behavio...
~
Spong, Barbara Rodriguez.
FindBook
Google Book
Amazon
博客來
Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases.
紀錄類型:
書目-電子資源 : Monograph/item
正題名/作者:
Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases./
作者:
Spong, Barbara Rodriguez.
面頁冊數:
223 p.
附註:
Source: Dissertation Abstracts International, Volume: 66-02, Section: B, page: 0841.
Contained By:
Dissertation Abstracts International66-02B.
標題:
Health Sciences, Pharmacy. -
電子資源:
http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3163937
ISBN:
0496986023
Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases.
Spong, Barbara Rodriguez.
Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases.
- 223 p.
Source: Dissertation Abstracts International, Volume: 66-02, Section: B, page: 0841.
Thesis (Ph.D.)--University of Michigan, 2005.
This dissertation focuses on understanding the role of molecular recognition, kinetic, and thermodynamic events in forming solid-state supramolecular assemblies. Poorly water soluble drugs present one of the greater challenges during development and stand to benefit from changes in crystal structure that enhance oral bioavailability. Single-component systems of ritonavir (crystalline, mesophase, and amorphous) and multiple-component systems of carbamazepine (binary cocrystals) have been studied with the specific objectives of (1) determining the potential for pH-induced precipitation of ritonavir single-component phases, identifying crystallization pathways from aqueous solution and from the amorphous phase, and characterizing the solid-state properties of phases formed; (2) identifying methods for forming carbamazepine cocrystal from solution and evaluating pharmaceutical behavior relative to the single component crystals (solubility, dissolution, hygroscopicity, physical and chemical stability); and (3) determining the solubility product of carbamazepine cocrystals in organic solvents and relating it to the crystallization in solutions of non-stoichiometric composition. Metastable solid phases of ritonavir were prepared by precipitation from aqueous solution and from the amorphous state exposed to moisture. Some of these phases appear to be lyotropic mesophases, since solvent is required for formation and a higher degree of long-range order is evident relative to amorphous ritonavir. Transformation pathways in suspension are consistent with measured dissolution rates and solubilities: amorphous > mesophase > Form I > Form II. Cocrystals of carbamazepine with nicotinamide and saccharin (CBZ:NCT (1:1) and CBZ:SAC (1:1)) crystallized from organic solvents by solvothermal methods exhibit enhanced physical stability following prolonged exposure to relative humidities ≥75% at 22°C and improved chemical stability following photo-irradiation. Aqueous intrinsic dissolution rates and solubilities of CBZ:NCT and CBZ:SAC show a 1.75 and 2.3-fold increase compared with the dihydrate of carbamazepine (CBZ(D)) at 25°C. Although the cocrystals undergo a solvent-mediated transformation in water to CBZ(D), solution concentrations remain elevated by 1.5 and 2 times the solubility of CBZ(D) for at least 48h. The solubility of cocrystals in ethanol, 2-propanol, and ethyl acetate can be described by the solubility product theory. Conditions for the crystallization of a desired solid-state form (cocrystal or single-component crystal) can be defined from the supersaturation and solution composition of cocrystal components.
ISBN: 0496986023Subjects--Topical Terms:
1017737
Health Sciences, Pharmacy.
Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases.
LDR
:03652nmm 2200289 4500
001
1815660
005
20060710080757.5
008
130610s2005 eng d
020
$a
0496986023
035
$a
(UnM)AAI3163937
035
$a
AAI3163937
040
$a
UnM
$c
UnM
100
1
$a
Spong, Barbara Rodriguez.
$3
1905075
245
1 0
$a
Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases.
300
$a
223 p.
500
$a
Source: Dissertation Abstracts International, Volume: 66-02, Section: B, page: 0841.
500
$a
Chairs: Nair Rodriguez-Hornedo; David Fleisher.
502
$a
Thesis (Ph.D.)--University of Michigan, 2005.
520
$a
This dissertation focuses on understanding the role of molecular recognition, kinetic, and thermodynamic events in forming solid-state supramolecular assemblies. Poorly water soluble drugs present one of the greater challenges during development and stand to benefit from changes in crystal structure that enhance oral bioavailability. Single-component systems of ritonavir (crystalline, mesophase, and amorphous) and multiple-component systems of carbamazepine (binary cocrystals) have been studied with the specific objectives of (1) determining the potential for pH-induced precipitation of ritonavir single-component phases, identifying crystallization pathways from aqueous solution and from the amorphous phase, and characterizing the solid-state properties of phases formed; (2) identifying methods for forming carbamazepine cocrystal from solution and evaluating pharmaceutical behavior relative to the single component crystals (solubility, dissolution, hygroscopicity, physical and chemical stability); and (3) determining the solubility product of carbamazepine cocrystals in organic solvents and relating it to the crystallization in solutions of non-stoichiometric composition. Metastable solid phases of ritonavir were prepared by precipitation from aqueous solution and from the amorphous state exposed to moisture. Some of these phases appear to be lyotropic mesophases, since solvent is required for formation and a higher degree of long-range order is evident relative to amorphous ritonavir. Transformation pathways in suspension are consistent with measured dissolution rates and solubilities: amorphous > mesophase > Form I > Form II. Cocrystals of carbamazepine with nicotinamide and saccharin (CBZ:NCT (1:1) and CBZ:SAC (1:1)) crystallized from organic solvents by solvothermal methods exhibit enhanced physical stability following prolonged exposure to relative humidities ≥75% at 22°C and improved chemical stability following photo-irradiation. Aqueous intrinsic dissolution rates and solubilities of CBZ:NCT and CBZ:SAC show a 1.75 and 2.3-fold increase compared with the dihydrate of carbamazepine (CBZ(D)) at 25°C. Although the cocrystals undergo a solvent-mediated transformation in water to CBZ(D), solution concentrations remain elevated by 1.5 and 2 times the solubility of CBZ(D) for at least 48h. The solubility of cocrystals in ethanol, 2-propanol, and ethyl acetate can be described by the solubility product theory. Conditions for the crystallization of a desired solid-state form (cocrystal or single-component crystal) can be defined from the supersaturation and solution composition of cocrystal components.
590
$a
School code: 0127.
650
4
$a
Health Sciences, Pharmacy.
$3
1017737
650
4
$a
Health Sciences, Pharmacology.
$3
1017717
690
$a
0572
690
$a
0419
710
2 0
$a
University of Michigan.
$3
777416
773
0
$t
Dissertation Abstracts International
$g
66-02B.
790
1 0
$a
Rodriguez-Hornedo, Nair,
$e
advisor
790
1 0
$a
Fleisher, David,
$e
advisor
790
$a
0127
791
$a
Ph.D.
792
$a
2005
856
4 0
$u
http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3163937
筆 0 讀者評論
館藏地:
全部
電子資源
出版年:
卷號:
館藏
1 筆 • 頁數 1 •
1
條碼號
典藏地名稱
館藏流通類別
資料類型
索書號
使用類型
借閱狀態
預約狀態
備註欄
附件
W9206523
電子資源
11.線上閱覽_V
電子書
EB
一般使用(Normal)
在架
0
1 筆 • 頁數 1 •
1
多媒體
評論
新增評論
分享你的心得
Export
取書館
處理中
...
變更密碼
登入