Abstract：
:The objective of the present investigation was to reduce the bitterness with improved dissolution, in acidic medium (pH 1.2), of mefloquine hydrochloride (MFL). Microparticles were prepared by coacervation method using Eudragit E (EE) as polymer and sodium hydroxide as precipitant. A 3(2) full factorial design was used for optimization wherein the drug concentration (A) and polymer concentration (B) were selected as independent variables and the bitterness score, particle size and dissolution at various pH were selected as the dependent variables. The desirability function approach has been employed in order to find the best compromise between the different experimental responses. The model is further cross validated for bias. The optimized microparticles were characterized by FT-IR, DSC, XRPD and SEM. Bitterness score was evaluated by human gustatory sensation test. Multiple linear regression analysis revealed that the reduced bitterness of MFL can be obtained by controlling the dissolution of microparticles at pH 6.8 and increasing the EE concentration. The increase in polymer concentration leads to reduction in dissolution of microparticles at pH > 5 due to its insolubility. However the dissolution studies at pH 1.2 demonstrated enhanced dissolution of MFL from microparticles might be due to the high porosity of the microparticles, hydrophilic nature of the EE, and improved wettability, provided by the dissolved EE. The bitterness score of microparticles was decreased to zero compared to 3+ of pure ARM. In conclusion the bitterness of MFL was reduced with improved dissolution at acidic pH.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Shah PP,Mashru RC,Rane YM,Thakkar Adoi
10.1208/s12249-008-9052-xsubject
Has Abstractpub_date
2008-01-01 00:00:00pages
377-89issue
2issn
1530-9932journal_volume
9pub_type
杂志文章abstract：:Our objective was to prepare nanoparticulate system using a simple yet attractive innovated method as an ophthalmic delivery system for fluocinolone acetonide to improve its ocular bioavailability. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were prepared by adopting thin film hydration method using PLGA/poloxa...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,随机对照试验
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abstract：:The purpose of this research was to evaluate in vitro transnasal sustained-release ability of sorbitan monostearate (SMS) organogels in isopropyl myristate (IM). Organogels were prepared containing SMS (2.5%-20%) and water (5%-25%) in IM and analyzed microscopically for phase behavior. The effect of Tween surfactants ...
journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,随机对照试验
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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