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1.
The effect of complexation of irbesartan (IRB), a practically water-insoluble drug, with cyclodextrins in presence of different
concentrations of water-soluble polymers (PEG 4000 and PVP K-90) on the dissolution rate of the drug has been investigated.
Phase solubility studies were carried out to evaluate the solubilizing power of βCD in association with water-soluble polymers
towards IRB and to determine the apparent stability constant (K
S) of the complexes. Improvement in K
S value for ternary complexes (IRB–βCD–polymers) clearly proved the benefit on the addition of water-soluble polymer to increase
complexation efficiency. The dissolution rate of the drug from ternary systems containing PEG 4000 and PVP K-90 was higher
as compared to the binary system. An optimum increase in the dissolution rate of the drug was observed at a polymer concentration
of 5% w/w for PVP K-90 and 10% w/w for PEG 4000. DSC, FTIR, SEM, and XRD studies were carried out to characterize the complexes. 相似文献
2.
Complexation of celecoxib with hydroxypropyl β-cyclodextrin (HPβCD) in the presence and absence of 3 hydrophilic polymers—polyvinyl
pyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG)—was investigated with an objective
of evaluating the effect of hydrophilic polymers on the complexation and solubilizing efficiencies of HPβCD and on the dissolution
rate of celecoxib from the HPβCD complexes. The phase solubility studies indicated the formation of celecoxib-HPβCD inclusion
complexes at a 1∶1M ratio in solution in both the presence and the absence of hydrophilic polymers. The complexes formed were
quite stable. Addition of hydrophilic polymers markedly enhanced the complexation and solubilizing efficiencies of HPβCD.
Solid inclusion complexes of celecoxib-HPβCD were prepared in 1∶1 and 1∶2 ratios by the kneading method, with and without
the addition of hydrophilic polymers. The solubility and dissolution rate of celecoxib were significantly improved by complexation
with HPβCD. The celecoxib-HPβCD (1∶2) inclusion complex yielded a 36.57-fold increase in the dissolution rate of celecoxib.
The addition of hydrophilic polymers also markedly enhanced the dissolution rate of celecoxib from HPβCD complexes: a 72.60-,
61.25-, and 39.15-fold increase was observed with PVP, HPMC, and PEG, respectively. Differential scanning calorimetry and
X-ray diffractometry indicated stronger drug amorphization and entrapment in HPβCD because of the combined action of HPβCD
and the hydrophilic polymers.
Published: September 29, 2006 相似文献
3.
The purpose of the present investigation was to increase the solubility and dissolution rate of rofecoxib by the preparation
of its solid dispersion with polyvinyl pyrrolidone K30 (PVP K30) using solvent evaporation method. Drug-polymer interactions
were investigated using differential scanning calorimetry (DSC), x-ray diffraction (XRD), and Fourier transform infrared spectroscopy
(FTIR). For the preparation of rofecoxib mouth dissolve tablets, its 1∶9 solid dispersion with PVP K30 was used with various
disintegrants and sublimable materials. In an attempt to construct a statistical model for the prediction of disintegration
time and percentage friability, a 32 randomized full and reduced factorial design was used to optimize the influence of the amounts of superdisintegrant and subliming
agent. The obtained results showed that dispersion of the drug in the polymer considerably enhanced the dissolution rate.
The drug-to-carrier ratio was the controlling factor for dissolution improvement. FTIR spectra revealed no chemical incompatibility
between the drug and PVP K30. As indicated from XRD and DSC data, rofecoxib was in the amorphous form, which explains the
better dissolution rate of the drug from its solid dispersions. Concerning the optimization study, the multiple regression
analysis revealed that an optimum concentration of camphor and a higher percentage of crospovidone are required for obtaining
rapidly disintegrating tablets. In conclusion, this investigation demonstrated the potential of experimental design in understanding
the effect of the formulation variables on the quality of mouth dissolve tablets containing solid dispersion of a hydrophobic
drug. 相似文献
4.
Peng Hou Jian Ni Sali Cao Haimin Lei Zhengjun Cai Tao Zhang Fang Yu Qingzhong Tan 《AAPS PharmSciTech》2013,14(2):629-638
Ensuring sufficient drug solubility is a crucial problem in pharmaceutical-related research. For water-insoluble drugs, various formulation approaches are employed to enhance the solubility and bioavailability of lead compounds. The goal of this study was to enhance the dissolution and absorption of a new antitumor lead compound, T-OA. Early-stage preparation discovery concept was employed in this study. Based on this concept, a solid dispersion system was chosen as the method of improving drug solubility and bioavailability. Solid dispersions of T-OA in polyvinylpyrrolidone (PVP) K30 were prepared by the solvent evaporation method. Dissolution testing determined that the ideal drug-to-PVP ratio was 1:5. X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were employed to confirm the formation of solid dispersions. Scanning electron microscopy demonstrated that T-OA was converted into an amorphous form. Both in vitro dissolution testing and the in vivo studies demonstrated that the solubility and bioavailability of T-OA were significantly improved when formulated in a solid dispersion with PVP. The dissolution rate of the T-OA/PVP solid dispersion was greatly enhanced relative to the pure drug, and the relative bioavailability of T-OA solid dispersions was found to be 392.0%, which is 4-fold higher than the pure drug. 相似文献
5.
The studies reported in this work are aimed to elucidate the ternary inclusion complex formation of gemfibrozil (GFZ), a poorly
water-soluble drug, with β-cyclodextrin (β-CD) with the aid of auxiliary substances like different grades of povidone(s) (viz.
PVP K-29/32, PVP K-40, Plasdone S-630, and Polyplasdone XL), organic base (viz. triethanolamine), and metal ion (viz. MgCl2·6H2O), by investigating their interactions in solution and solid state. Phase solubility studies were carried out to evaluate
the solubilizing power of β-cyclodextrin, in association with various auxiliary substances, to determine the apparent stability
constant (K
C) and complexation efficiency (CE) of complexes. Improvement in K
C values for ternary complexes clearly proves the benefit of the addition of auxiliary substances to promote CE. Of all the
approaches used, the use of polymer Plasdone S-630 was found to be the most promising approach in terms of optimum CE and
K
C. GFZ–β-CD (1:1) binary and ternary systems were prepared by kneading and lyophilization methods. The ternary systems clearly
signified superiority over binary systems in terms of CE, solubility, K
C, and reduction in the formulation bulk. Optimized ternary system of GFZ–β-CD–Plasdone S-630 prepared by using lyophilization
method indicated a significant improvement in intrinsic dissolution rate when compared with ternary kneaded system. Differential
scanning calorimetry, X-ray diffraction, Fourier transform infrared, scanning electron microscopy, and proton nuclear magnetic
resonance were carried out to characterize the binary and optimized ternary complex. The results suggested the formation of
new solid phases, eliciting strong evidences of ternary inclusion complex formation between GFZ, β-CD, and Plasdone S-630,
particularly for lyophilized products. 相似文献
6.
Suhail B. Noolkar Namdeo R. Jadhav Santosh A. Bhende Suresh G. Killedar 《AAPS PharmSciTech》2013,14(2):569-577
The effect of ternary solid dispersions of poor water-soluble NSAID meloxicam with moringa coagulant (obtained by salt extraction of moringa seeds) and polyvinylpyrrolidone on the in vitro dissolution properties has been investigated. Binary (meloxicam–moringa and meloxicam–polyvinylpyrrolidone (PVP)) and ternary (meloxicam–moringa–PVP) systems were prepared by physical kneading and ball milling and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry. The in vitro dissolution behavior of meloxicam from the different products was evaluated by means of United States Pharmacopeia type II dissolution apparatus. The results of solid-state studies indicated the presence of strong interactions between meloxicam, moringa, and PVP which were of totally amorphous nature. All ternary combinations were significantly more effective than the corresponding binary systems in improving the dissolution rate of meloxicam. The best performance in this respect was given by the ternary combination employing meloxicam–moringa–PVP ratio of [1:(3:1)] prepared by ball milling, with about six times increase in percent dissolution rate, whereas meloxicam–moringa (1:3) and meloxicam–PVP (1:4) prepared by ball milling improved dissolution of meloxicam by almost 3- and 2.5-folds, respectively. The achieved excellent dissolution enhancement of meloxicam in the ternary systems was attributed to the combined effects of impartation of hydrophilic characteristic by PVP, as well as to the synergistic interaction between moringa and PVP. 相似文献
7.
This article investigates enhancement of the dissolution profile of valdecoxib using solid dispersion with PVP. The article
also describes the preparation of fast-dissolving tablets of valdecoxib by using a high amount of superdisintegrants. A phase
solubility method was used to evaluate the effect of various water-soluble polymers on aqueous solubility of valdecoxib. Polyvinyl
pyrrolidone (PVP K-30) was selected and solid dispersions were prepared by the method of kneading. Dissolution studies, using
the USP paddle method were performed for solid dispersions of valdecoxib. Infrared (IR) spectroscopy, differential scanning
calorimetry (DSC), and x-ray diffractometry (XRD) were performed to identify the physicochemical interaction between drug
and carrier, hence its effect on dissolution. Tablets were formulated containing solid dispersion products and compared with
commercial products. IR spectroscopy, XRD, and DSC showed no change in the crystal structure of valdecoxib. Dissolution of
valdecoxib improved significantly in solid dispersion products (<85% in 5 minutes). Tablets containing solid dispersion exhibited
better dissolution profile than commercial tablets. Thus, the solid dispersion technique can be successfully used for improvement
of dissolution of valdecoxib.
Published: August 18, 2006 相似文献
8.
The objective of this work is physicochemical characterization of nimesulide-cyclodextrin binary systems both in solution
and solid state and to improve the dissolution properties of nimesulide (N) via complexation with α-, β, and γ-cyclodextrins
(CDs). Detection of inclusion complexation was done in solution by means of phase solubility analysis, mass spectrometry,
and 1H nuclear magnetic resonance (1H-NMR) spectroscopic studies, and in solid state using differential scanning calorimetry (DSC), powder x-ray diffractometry
(X-RD), scanning electron microscopy (SEM), and in vitro dissolution studies. Phase solubility, mass spectrometry and 1H-NMR studies in solution revealed 1∶1 M complexation of N with all CDs. A true inclusion of N with β-CD at 1∶2 M in solid
state was confirmed by DSC, powder X-RD and SEM studies. Dissolution properties of N-CD binary systems were superior when
compared to pure N. 相似文献
9.
Bibi F. Choonara Yahya E. Choonara Pradeep Kumar Lisa C. du Toit Lomas K. Tomar Charu Tyagi Viness Pillay 《AAPS PharmSciTech》2015,16(4):771-786
A menthol-based solid dispersion was designed to improve the intrinsic solubility of the poorly soluble sulfamethoxazole- a class II drug molecule of Biopharmaceutics Classification System (BCS) displaying widespread antibacterial activity. Solid dispersions of menthol and sulfamethoxazole were compressed with hydroxypropyl methylcellulose (HPMC) into suitable sulfamethoxazole-loaded matrix tablets for oral drug delivery. The sulfamethoxazole-loaded solid dispersions and compressed tablets were characterized for their physicochemical and physicomechanical properties such as changes in crystallinity, melting point, molecular transitions, and textural analysis for critical analysis of their effects on the solubility and dissolution of sulfamethoxazole. The formulations were further evaluated for swelling, degradation, solubility, and in vitro drug release behavior. In vitro drug release from the sulfamethoxazole-loaded matrix tablets displayed a minimum and maximum fractional release of 0.714 and 0.970, respectively. The tablets further displayed different release rate profiles over the study periods of 12, 16, 48, and 56 h which were attributed to the varying concentrations of menthol within each formulation. Menthol was determined as a suitable hydrophilic carrier for sulfamethoxazole since it functioned as a solubilizing and release-retarding agent for improving the solubility and dissolution of sulfamethoxazole as well as controlling the rate at which it was released.KEY WORDS: crystallinity, menthol, oral solubility and dissolution, solid dispersion, sulfamethoxazole 相似文献
10.
The purpose of this research was to perform a granulometrical and flow properties study of a morphine polymeric complex and
determine the influence of 3 variables—particle size of complex, pH value, and ionic strength of the dissolution medium—on
the dissolution behavior. The morphine-Eudragit L complex was produced in aqueous medium from morphine hydrochloride saturated
solution and Eudragit L 30D diluted until 12% wt/vol and partially neutralized (40%). To determine the rheological behavior
of the complex, several rheological tests were developed: bulk and tapped densities, Hausner ratio, angle of repose, and flow
rate. The results corresponding to the technological study suggest that the 100- to 250-μm fraction can be considered as free
flowing powder. In relation to the dissolution behavior of the complex, the results indicate that the ionic strength has been
detected as the most influencing factor when values below physiological conditions are used. In conclusion, no technological
problems for the production of further solid dosage forms are expected. Furthermore, no changes in the dissolution profiles
of the complex have been detected when ionic strength values are inside the physiological range. 相似文献
11.
Complexation of celecoxib with hydroxypropyl beta-cyclodextrin (HPbetaCD) in the presence and absence of 3 hydrophilic polymers-polyvinyl pyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG)-was investigated with an objective of evaluating the effect of hydrophilic polymers on the complexation and solubilizing efficiencies of HPbetaCD and on the dissolution rate of celecoxib from the HPbetaCD complexes. The phase solubility studies indicated the formation of celecoxib-HPbetaCD inclusion complexes at a 1:1M ratio in solution in both the presence and the absence of hydrophilic polymers. The complexes formed were quite stable. Addition of hydrophilic polymers markedly enhanced the complexation and solubilizing efficiencies of HPbetaCD. Solid inclusion complexes of celecoxib-HPbetaCD were prepared in 1:1 and 1:2 ratios by the kneading method, with and without the addition of hydrophilic polymers. The solubility and dissolution rate of celecoxib were significantly improved by complexation with HPbetaCD. The celecoxib-HPbetaCD (1:2) inclusion complex yielded a 36.57-fold increase in the dissolution rate of celecoxib. The addition of hydrophilic polymers also markedly enhanced the dissolution rate of celecoxib from HPbetaCD complexes: a 72.60-, 61.25-, and 39.15-fold increase was observed with PVP, HPMC, and PEG, respectively. Differential scanning calorimetry and X-ray diffractometry indicated stronger drug amorphization and entrapment in HPbetaCD because of the combined action of HPbetaCD and the hydrophilic polymers. 相似文献
12.
The objective of this work was to develop tablet formulations of nimesulide-β-cyclodextrin (NI-β-CD) and meloxicam-γ-cyclodextrin
(ME-γ-CD) binary systems. In the case of nimesulide, 3 types of binary systems—physical mixtures, kneaded systems, and coevaporated
systems—were studied. In the case of meloxicam, 2 types of binary systems—physical mixtures and kneaded systems—were investigated.
Both drug-CD binary systems were prepared at 1∶1 and 1∶2 molar ratio (1∶1M and 1∶2M) and used in formulation studies. The
tablet formulations containing drug-CD binary systems prepared by the wet granulation and direct compression methods showed
superior dissolution properties when compared with the formulations of the corresponding pure drug formulations. Overall,
the dissolution properties of tablet formulations prepared by the direct compression method were superior to those of tablets
prepared by the wet granulation method. Selected tablet formulations showed good stability with regard to drug content, disintegration
time, hardness, and in vitro dissolution properties over 6 months at 40°C±2°C and 75% relative humidity.
Published: May 11, 2007 相似文献
13.
The aim of the current study was to design oral fast-release polymeric tablets of prednisone and to optimize the drug dissolution profile by modifying the carrier concentration. Solid dispersions were prepared by the solvent evaporation method at different drug:polymer ratios (wt/wt). The physical state and drug:carrier interactions were analyzed by X-ray diffraction, infrared spectroscopy, and scanning electron microscopy. The dissolution rate of prednisone from solid dispersions was markedly enhanced by increasing the polymer concentration. The tablets were prepared from solid dispersion systems using polyethylene glycol (PEG) 6000 as a carrier at low and high concentration. The results showed that PEG 6000-based tablets exhibited a significantly higher prednisone dissolution (80% within 30 minutes) than did conventional tablets prepared without PEG 6000 (<25% within 30 minutes). In addition, the good disintegration and very good dissolution performance of the developed tablets without the addition of superdisintegrant highlighted the suitability of these formulated dosage forms. The stability studies performed in normal and accelerated conditions during 12 months showed that prednisone exhibited high stability in PEG 6000 solid dispersion powders and tablets. The X-ray diffraction showed that the degree of crystallinity of prednisone in solid dispersions decreased when the ratio of the polymer increased, suggesting that the drug is present inside the samples in different physical states. The Fourier transform infrared spectroscopic studies showed the stability of prednisone and the absence of well-defined drug:polymer interactions. Scanning electron microscopy images showed a novel morphology of the dispersed systems in comparison with the pure components. 相似文献
14.
Guedes FL de Oliveira BG Hernandes MZ De Simone CA Veiga FJ de Lima Mdo C Pitta IR Galdino SL Neto PJ 《AAPS PharmSciTech》2011,12(1):401-410
Solid dispersions have been used as a strategy to improve the solubility, dissolution rate, and bioavailability of poor water-soluble
drugs. The increase of the dissolution rate presented by (5Z)-3-(4-chloro-benzyl)-5-(4-nitro-benzylidene)-imidazolidine-2,4-dione (LPSF/FZ4) from the solid dispersions is related to
the existence of intermolecular interactions of hydrogen bond type (>N–H...O<) between the amide group (>N–H) of the LPSF/FZ4 and the ether group (–O–) of the polyethyleneglycol polymer, or the carbonyl
(C=O) of the polyvinylpyrrolidone polymer (PVP). The intensity of these interactions is directly reflected in the morphology
acquired by LPSF/FZ4 in these systems, where a new solid phase, in the form of amorphous aggregates of irregular size, was
identified through scanning electron microscopy and confirmed in the characterizations achieved using X-ray diffraction and
thermal analysis of DSC. The solid dispersions with the polymer PVP, in higher concentrations, were revealed to be the best
option to be used in the formulations of LPSF/FZ4 in both theoretical and experimental studies. 相似文献
15.
Masanori Ochi Keisuke Kimura Atsushi Kanda Takaki Kawachi Akitoshi Matsuda Kayo Yuminoki Naofumi Hashimoto 《AAPS PharmSciTech》2016,17(4):932-939
The aim of the present study was to develop amorphous solid dispersion (ASD) of meloxicam (MEL) for providing rapid onset of action. ASDs of MEL with polyvinylpyrrolidone (PVP) K-30 (MEL/PVP), HPC-SSL (MEL/HPC), and Eudragit EPO (MEL/EPO) were prepared. The physicochemical properties were characterized by focusing on morphology, crystallinity, dissolution properties, stability, and the interaction of MEL with coexisting polymers. MEL/EPO was physicochemically stable after storage at 40°C/75% RH for 30 days. In contrast, recrystallization of MEL was observed in MEL/PVP and MEL/HPC at 40°C/50% RH for 30 days. Infrared spectroscopic studies and 1H NMR analyses of MEL/EPO revealed that Eudragit EPO interacted with MEL and reduced intermolecular binding between MEL molecules. Intermolecular interaction of drug molecules is necessary for the formation of crystalline. Thus, the interaction of MEL with Eudragit EPO and interruption of the formation of supramolecular interaction between MEL molecules might lead to the inhibition of crystal growth of MEL. Of all the MEL solid dispersions prepared, MEL/EPO showed the largest improvement in dissolution behavior. Oral administration of MEL/EPO to rats showed rapid and enhanced MEL exposure with a 2.4-fold increase in bioavailability compared with crystalline MEL. Based on these findings, MEL/EPO was physicochemically stable and provided a rapid onset of action and enhanced bioavailability after oral administration. 相似文献
16.
Farouk Semcheddine Nida El Islem Guissi XueYin Liu ZuoMin Wu Bo Wang 《AAPS PharmSciTech》2015,16(3):704-715
The aims of this study were to enhance the solubility and dissolution rate of nimodipine (ND) by preparing the inclusion complexes of ND with sulfobutylether-b-cyclodextrin (SBE-β-CD) and 2-hydroxypropyl-b-cyclodextrin (HP-β-CD) and to study the effect of the preparation method on the in vitro dissolution profile in different media (0.1 N HCl pH 1.2, phosphate buffer pH 7.4, and distilled water). Thus, the inclusion complexes were prepared by kneading, coprecipitation, and freeze-drying methods. Phase solubility studies were conducted to characterize the complexes in the liquid state. The inclusion complexes in the solid state were investigated with differential scanning calorimetry (DSC), X-ray diffractometry (X-RD), and Fourier transform infrared spectroscopy (FT-IR). Stable complexes of ND/SBE-β-CD and ND/HP-β-CD were formed in distilled water in a 1:1 stoichiometric inclusion complex as indicated by an AL-type diagram. The apparent stability constants (Ks) were 1334.4 and 464.1 M−1 for ND/SBE-β-CD and ND/HP-β-CD, respectively. The water-solubility of ND was significantly increased in an average of 22- and 8-fold for SBE-β-CD and HP-β-CD, respectively. DSC results showed the formation of true inclusion complexes between the drug and both SBE-β-CD and HP-β-CD prepared by the kneading method. In contrast, crystalline drug was detectable in all other products. The dissolution studies showed that all the products exhibited higher dissolution rate than those of the physical mixtures and ND alone, in all mediums. However, the kneading complexes displayed the maximum dissolution rate in comparison with drug and other complexes, confirming the influence of the preparation method on the physicochemical properties of the products. 相似文献
17.
Effects of tromethamine (Tris), polyvinylpyrrolidone (PVP-K25), and low molecular weight chitosan (LM-CH) on dissolution and therapeutic efficacy of glimepiride (Gmp) were investigated using physical mixtures (PMs), coground mixtures, coprecipitates (Coppts) or kneaded mixtures (KMs), and compared with drug alone. Fourier transform infrared spectroscopy, differential scanning colorimetry, and X-ray diffractometry were performed to identify any physicochemical interaction with Gmp. Surface morphology was examined via scanning electron microscopy. The results of Gmp in vitro dissolution revealed that it was greatly enhanced by Coppt with Tris or PVP-K25 and KM with LM-CH at a drug to carrier ratio of 1:8. Gmp amorphization by PVP-K25 and LM-CH was a major factor in increasing Gmp dissolution. Being basic, Tris might increase the pH of the microdiffusion layer around Gmp particles improving its dissolution. Formation of water-soluble complexes suggested by solubility study may also explain the enhanced dissolution. Capsules were prepared from Coppts and KM 1:8 drug to carrier binary systems and also with Tris PMs. In vivo, the hypoglycemic efficacy of Gmp capsules in rabbits increased by 1.63-, 1.50-, and 1.46-fold for 1:8 Coppts with Tris or PVP-K25 and KM with LM-CH respectively, compared with Gmp alone. Surprisingly, the response to Tris PM 1:20 capsules was 1.52-fold revealing statistically insignificant difference to that of Tris Coppt 1:8 (1.63 fold). As a conclusion, dissolution enhancement and hypoglycemic potentiation by 1:20 PM of Gmp/Tris, being simple and easy to prepare, may enable development of a reduced-dose and fast-release oral dosage form of Gmp. 相似文献
18.
The objective of this work was to study dissolution enhancement efficiency and solid dispersion formation ability of hydrophilic
swellable polymers such as sodium carboxymethyl cellulose (Na-CMC), sodium starch glycolate (SSG), pregelatinized starch (PGS),
and hydroxypropylmethyl cellulose (HPMC) with carbamazepine using 32 full factorial design for each of the polymers. Solid dispersions of carbamazepine were prepared using solvent evaporation
method with around 70% solvent recovery. The independent variables were the amount of polymer and organic solvent. The dependent
variables assessed were percentage drug dissolved at various time points and dispersion efficiency (ie, in terms of particle
size of solid dispersion). Solid dispersions were evaluated for percentage drug dissolved, wettability, differential scanning
calorimetry, scanning electron microscopy, and angle of repose. Multiple linear regression of results obtained led to equations,
which generated contour plots to relate the dependent variables. Similarity factor and mean dissolution time were used to
compare dissolution patterns obtained in distilled water and simulated gastric fluid United States Pharmacopeia (USP) XXVI
of pH 1.2. Maximum drug dissolution was obtained with polymer order Na-CMC>SSG>PGS>HPMC. Particle size of drug was reduced
≈ 10–15, 3–5, 5–7, and 10–25 times in Na-CMC, SSG, PGS, and HPMC solid dispersions, respectively; whereas wettability of solid
dispersions was found in the order of Na-CMC>HPMC>PGS>SSG. Angle of repose was found to be in the range of 29° to 35° for
all solid dispersions, which shows good flowability characteristics. HPMC showed increase in drug dissolution up to an optimized
level; however, furthers increase in its concentration decreased drug dissolution.
Published: April 6, 2007 相似文献
19.
Conclusions Results from the present study conclude that PR in combination with PVP and with incorporation of dibutyl phthalate (30% wt/wt)
produces smooth flexible films with improved tensile strength and percentage elongation. The release rate of drug from films
and permeation across skin increases with increase in drug and PVP loading but is independent of film thickness. Patches containing
PR:PVP (7:3) show promise for pharmacokinetic and pharmacodynamic performance evaluation in a suitable animal model. In view
of the overall results reported in the present study, it may be proposed that PR can be used in the design of a matrix type
transdermal drug delivery system to prolong the drug release.
Published: December 27, 2005 相似文献
20.
Shilpi Sinha Mushir Ali Sanjula Baboota Alka Ahuja Anil Kumar Javed Ali 《AAPS PharmSciTech》2010,11(2):518-527
Ritonavir is an antiretroviral drug characterized by low solubility and high permeability which corresponds to BCS class II
drug. The purpose of the study was to develop solid dispersion by different methods and investigate them for in vitro and in vivo performance for enhancing dissolution and bioavailability, respectively. Since the drug possesses food-related absorption,
the effect of biorelevant media (FaSSIF and FeSSIF state) on dissolution behavior was also studied. The solid dispersion was
prepared using Gelucire as carrier in 1:4 ratio by different methods and were characterized for differential scanning calorimetry
(DSC), X-ray diffractometry, scanning electron microscopy, and FT-IR. Oral bioavailability of 10 mg of ritonavir in solid
dispersion prepared by solvent evaporation (SE1) and melt method (MM1) was compared with pure drug after oral administration
of solid dispersion and pure drug to Albino Wistar rats of either sex. The results suggested formation of eutectic solid dispersion.
In vitro dissolution studies was performed in 0.1 N HCl and biorelevant media showed enhanced dissolution rate as compared to pure
drug in both FeSSIF media and 0.1 N HCl. The apparent rate of absorption of ritonavir from SE1 (C
max 20221.37 ng/ml, t
max 0.5 h) was higher than that of MM1 (C
max 2,462.2, t
max 1 h) and pure drug (C
max 1,354.8 ng/ml, t
max 0.5 h). On the basis of the result obtained, it was concluded that solid dispersion is a good approach to enhance solubility
and bioavailability of poorly water-soluble ritonavir. 相似文献