دورية أكاديمية
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Oral Bioavailability Enhancement of Poorly Soluble Drug by Amorphous Solid Dispersion Using Sucrose Acetate Isobutyrate.

التفاصيل البيبلوغرافية
العنوان: Oral Bioavailability Enhancement of Poorly Soluble Drug by Amorphous Solid Dispersion Using Sucrose Acetate Isobutyrate.
المؤلفون: Mohamed EM; Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, Texas, 77843-1114, U.S.A.; Department of Pharmaceutics, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514, Egypt., Dharani S; Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, Texas, 77843-1114, U.S.A., Khuroo T; Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, Texas, 77843-1114, U.S.A., Nutan MTH; Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, Kingsville, Texas, 78363, U.S.A., Cook P; Eastman Chemical Company, Kingsport, Tennessee, 37662, U.S.A., Arunagiri R; Eastman Chemical Company, Kingsport, Tennessee, 37662, U.S.A., Khan MA; Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, Texas, 77843-1114, U.S.A., Rahman Z; Irma Lerma Rangel School of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, Texas, 77843-1114, U.S.A.. rahman@tamu.edu.
المصدر: AAPS PharmSciTech [AAPS PharmSciTech] 2024 Sep 05; Vol. 25 (7), pp. 202. Date of Electronic Publication: 2024 Sep 05.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Springer Country of Publication: United States NLM ID: 100960111 Publication Model: Electronic Cited Medium: Internet ISSN: 1530-9932 (Electronic) Linking ISSN: 15309932 NLM ISO Abbreviation: AAPS PharmSciTech Subsets: MEDLINE
أسماء مطبوعة: Publication: New York : Springer
Original Publication: Arlington, VA : American Association of Pharmaceutical Scientists, c2000-
مواضيع طبية MeSH: Biological Availability* , Solubility* , Sucrose*/analogs & derivatives , Sucrose*/chemistry , Excipients*/chemistry, Administration, Oral ; Animals ; Male ; Hypromellose Derivatives/chemistry ; Chemistry, Pharmaceutical/methods ; Drug Stability ; X-Ray Diffraction/methods
مستخلص: The focus of the present work was to develop amorphous solid dispersion (ASD) formulation of aprepitant (APT) using sucrose acetate isobutyrate (SAIB) excipient, evaluate for physicochemical attributes, stability, and bioavailability, and compared with hydroxypropyl methylcellulose (HPMC) based formulation. Various formulations of APT were prepared by solvent evaporation method and characterized for physiochemical and in-vivo performance attributes such as dissolution, drug phase, stability, and bioavailability. X-ray powder diffraction indicated crystalline drug conversion into amorphous phase. Dissolution varied as a function of drug:SAIB:excipient proportion. The dissolution was more than 80% in the optimized formulation (F10) and comparable to HPMC based formulation (F13). Stability of F10 and F13 formulations stored at 25 C/60% and 40°C/75% RH for three months were comparable. Both ASD formulations (F10 and F13) were bioequivalent as indicated by the pharmacokinetic parameters C max and AUC 0-∞ . C max and AUC 0-∞ of F10 and F13 formulations were 2.52 ± 0.39, and 2.74 ± 0.32 μg/ml, and 26.59 ± 0.39, and 24.79 ± 6.02 μg/ml.h, respectively. Furthermore, the bioavailability of ASD formulation was more than twofold of the formulation containing crystalline phase of the drug. In conclusion, stability and oral bioavailability of SAIB based ASD formulation is comparable to HPMC-based formulation of poorly soluble drugs.
(© 2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.)
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فهرسة مساهمة: Keywords: amorphous solid dispersion; aprepitants; pharmacokinetic; stability; sucrose acetate isobutyrate
المشرفين على المادة: 57-50-1 (Sucrose)
0 (Excipients)
H5KI1C3YTV (sucrose acetate isobutyrate)
3NXW29V3WO (Hypromellose Derivatives)
تواريخ الأحداث: Date Created: 20240905 Date Completed: 20240905 Latest Revision: 20240905
رمز التحديث: 20240906
DOI: 10.1208/s12249-024-02924-5
PMID: 39237685
قاعدة البيانات: MEDLINE
الوصف
تدمد:1530-9932
DOI:10.1208/s12249-024-02924-5