Effect of hydroxypropylcellulose and Tween 80 on physicochemical properties and bioavailability of ezetimibe-loaded solid dispersion

2015 ◽  
Vol 130 ◽  
pp. 26-31 ◽  
Author(s):  
Rehmana Rashid ◽  
Dong Wuk Kim ◽  
Fakhar ud Din ◽  
Omer Mustapha ◽  
Abid Mehmood Yousaf ◽  
...  
1990 ◽  
Vol 38 (8) ◽  
pp. 2237-2241 ◽  
Author(s):  
Makiko FUJII ◽  
Katsuhiro HARADA ◽  
Mitsuo MATSUMOTO

Author(s):  
Panithi Raknam ◽  
Sirirat Pinsuwan ◽  
Thanaporn Amnuaikit

Phenylethyl Resorcinol (PR) is a cosmeceutical skin lightening agent and the purpose of this study was to enhance its stability by using liposomal cream formulation which increases local efficacy and safety. Liposome formulation was prepared by modified ethanol injection method, and it contained soy phosphatidyl choline (SPC), cholesterol (CHO), Tween 80 (TW80) and deoxycholic acid (DA) mixed with 2% PR. The physicochemical properties, skin permeation as well as cellular study were evaluated in order to obtain the optimized formulation. The optimized liposome formulation composed of SPC:TW80:DA (84:16:2.5) and exhibited vesicle size, polydispersity index (PDI) and zeta potential of 286.4±8.04 nm, 0.317±0.03 and -39.20±3.85 mV, respectively. Entrapment efficiency (EE) of liposome formulation was 93.55±0.05%. The vesicle was spherical in shape and showed good physicochemical stability for 4 months. The skin permeation study demonstrated that liposome with a negative charge could result in a high PR skin deposition value of 1732.76±216.24 µg/cm2 after 24 h. Cellular study showed that liposome formulation could inhibit melanin content in B16 melanoma cells and enhance cell viability in HaCaT keratinocyte cells. The optimized PR liposome was incorporated in cream and investigated physicochemical properties, stability and skin permeation. Liposomal PR cream showed a good stability and a superior result than PR cream in skin permeation parameters, as well as in tyrosinase inhibition.


2021 ◽  
Vol 16 ◽  
Author(s):  
Hossein Asgarirad ◽  
Ali Farmoudeh ◽  
Shervin AmirKhanloo ◽  
Amirhossein Babaei ◽  
Seyyedeh Saba Hosseini ◽  
...  

Background: Valerian root extract is used in traditional medicine to treat sleep disorders. According to previous studies, sedative effects are related to the presence of valerenic acid. Formulating orodispersible tablets (ODTs) is an effective and cost-benefit technique for accelerating drugs' therapeutic effects. This study aimed to formulate ODTs of valerian root extract and evaluate their properties. Materials and Methods: Valerian root was extracted by percolation in 70% ethanol. The solubility of valerenic acid was investigated in various liquid carriers. The extract was uniformly dispersed in the selected carrier (Tween 80), then mixed with other excipients and compressed into tablets. Fourteen formulations with different amounts of sodium starch glycolate (SSG, as a super disintegrant) and camphor (as a sublimating agent) were prepared. The physicochemical properties of the ODTs, drug release rates, and microbial limit tests (MLTs) were studied. Results: Both SSG and camphor accelerated tablet disintegration rates, and their composition showed a synergistic effect (P<0.05). The infrared spectroscopy revealed no chemical interaction between formulation components. The MLTs confirmed that a limited number of microbial colonies were grown in the liquid medium, and no pathogen growth occurred in the specific culture media. Conclusion: The results revealed that Valerian ODT's physicochemical properties were significantly improved compared to conventional tablets. The technique can be utilized for other poorly water-soluble pharmaceuticals.


2016 ◽  
Vol 89 ◽  
pp. 109-118 ◽  
Author(s):  
Chaturbhuj K. Saurabh ◽  
Sumit Gupta ◽  
Prasad S. Variyar ◽  
Arun Sharma

Author(s):  
Naila Shahrin ◽  
Asma Huq

To develop a novel dosage form of ibuprofen loaded solid dispersion with improved dissolution, formulations were developed using mixture of tween 80 & span 80 with a sugar such as dextrose, icing sugar. Percentage of tween 80 & span 80 was 10% & 5%, 7.5% & 7.5%, 5% & 10% and amount of sugar was fixed (1.2 g). In-vitro dissolution study was conducted in phosphate buffer (pH 7.2) for 1 hour. Release property from formulations of both sugars was investigated. In both cases, enhanced release property was observed where the release was compared with pure ibuprofen powder. Formulations having same amount of tween 80 & span 80 showed maximum release of drug. Formulations of icing sugar showed maximum release of drug within 1 hour time frame than the formulations of dextrose. DOI: http://dx.doi.org/10.3329/ijpls.v1i1.12946 International Journal of Pharmaceutical and Life Sciences Vol.1(1) 2012


Author(s):  
Nguyen Van Khanh ◽  
Ta Thi Thu ◽  
Hoang Anh Tuan

Abstract: The poor solubility of rutin leads to poor bioavailability. The present study is aimed to increase the solubility and bioavailability of rutin using solid dispersion technique. The solid dispersions of rutin were prepared by spray-dried method using β-CD, HPMC E6, HPMC E15, PVP K30, SLS, poloxamer 188 and Tween 80 as carriers. The interaction of rutin with the carriers was evaluated by using methods such as dissolved measurement, Fourier-transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The optimization of formulation was carried out by using Central Composite Face design. Independent variables include PVP K30/rutin ratio, Tween 80/rutin ratio, inlet air temperature, and feed flow rate. Dependent variables are the dissolution and product yield. The optimized preparation conditions for rutin solid dispersions were obtained as PVP K30: rutin at a ratio of 5.77, Tween 80: rutin at a ratio of 0.14, inlet temperature of 110.05, flow rate of 1370.9 ml per hour. The results of this study indicate that the solid dispersion of rutin increases significantly the dissolution of rutin in comparison with rutin. The results of the DSC and XRD studies prove the state transition of rutin from crystalline to amorphous. Keywords Rutin, solid dispersion, spray drying, PVP K30, dissolution. References [1] Beatriz Gullón, Thelmo A. Lú-Chau, María Teresa Moreira, Juan M. Lema, Gemman Eibes, Rutin: A review on extraction, identification and purification methods, biological activities and approaches to enhance its bioavailability, Trends in Food Science & Technology 67 (2017) 220-235. https://doi.org/10.1016/j.tifs.2017.07.008.[2] Carla Aparecida Pedriali, Adjaci Uchoa Fernandes, Leandra de Cássia Bernusso, Bronislaw Polakiewicz, The synthesis of a water-soluble derivative of rutin as an antiradical agent, Química Nova 31(8) (2008) 2147-2151. http://dx.doi.org/10.1590/S0100-40422008000800039.[3] Chiou, Win Loung, Riegelman, Sidney, Pharmaceutical applications of solid dispersion systems, Journal of pharmaceutical sciences 60(9) (1971) 1281-1302. https://doi.org/10.1002/jps.2600600902.[4] Xingwang Zhang, Huijie Xing,Yue Zhao, Zhiguo Ma, Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs, Pharmaceutics 10(3) (2018) 1-33. https://doi.org/10.3390/pharmaceutics10030074.[5] Ladan Akbarpour Nikghalb, Gurinder Singh, Gaurav Singh, Kimia Fazaeli Kahkeshan, Solid Dispersion: Methods and Polymers to increase the solubility of poorly soluble drugs, Journal of Applied Pharmaceutical Science 2(10) (2012) 170-175. https://doi.org/10.7324/JAPS.2012.2103.[6] Amrit Paudel, Zelalem Ayenew Worku, Joke Meeus, Sandra Guns, Guy Van den Mooter, Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations, International Journal of Pharmaceutics 453(1) (2013) 253-284. https://doi.org/10.1016/j.ijpharm.2012.07.015.[7] P.B. Dalvi, A.B. Gerange, R. IngaleP, Solid dispersion: strategy to enhance solubility, Journal of Drug Delivery & Therapeutics 5(2) (2015) 20-28. https://doi.org/10.22270/jddt.v5i2.1060.[8] Chau Le Ngoc Vo, Chulhun Park, Beom Jin Lee, Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. European Journal of Pharmaceutics and Biopharmaceutics 85(3) (2013) 799-813. https://doi.org/10.1016/j.ejpb.2013.09.007.[9] I.V. Koval’skii, I.I. Krasnyuk, I.I. Krasnyuk, O.I. Nikulina, A.V. Belyatskaya, Yu. Ya. Kharitonov, N.B. Fel’dman, S.V. Lutsenko, V.V. Grikh, Studies of the Solubility of Rutin from Solid Dispersions, Pharmaceutical Chemistry Journal 47(11) (2014) 612-615. https://doi.org/10.1007/s11094-014-1020-z.  


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