Design and optimization of a stomach-specific drug delivery system of repaglinide: Application of simplex lattice design

2010 ◽  
Vol 17 (1) ◽  
pp. 55-65 ◽  
Author(s):  
Subhash S. Vaghani ◽  
Sneha G. Patel ◽  
Rishad Ramjan Jivani ◽  
N. P. Jivani ◽  
Madhabhai M. Patel ◽  
...  
2018 ◽  
Vol 3 (4) ◽  
pp. 164
Author(s):  
Mardiyanto Mardiyanto ◽  
Najma Annuria Fithri ◽  
Martina Tandry

Mefenamic acid as pain relief drug belongs to the biopharmaceutics classification system (BCS) class II which is practically insoluble in water causing extremely low dissolution in gastrointestinal tract. The self nanoemulsifying drug delivery system (SNEDDS) is a new innovation pharmaceutical dosage form that has effectively known to increase solubilization of hydrophobic drug in polar solvent. In this study the capryol-90 was selected as oil phase in SNEDDS as it showed maximal solubility of mefenamic acid (20 mg/mL). Combination of polysorbate-80 and PEG-400 as a generally regarded as safe (GRAS) excipient were used as surfactant and co-surfactant in SNEDDS due to its high HLB property that can increase mefenamic acid solubility in water. The ternary phase diagram of capryol-90, polysorbate-80, and PEG-400 was constructed in advance to obtain the component concentration of spontaneous nanoemulsion region. Model simplex-lattice-design cooperated in Design-Expert®10 was used to define SNEDDS mefenamic acid formula. Optimized mefenamic acid SNEDDS formula consisted of 20% capryol-90, 31.62% polysorbate-80, and 48.38% PEG-400. Characterization study of Optimized mefenamic acid SNEDDS formula showed improvement of drug content (102.820 ± 4.950)%, emulsification time (421.015 ± 1.290) second, and viscosity (0.927 ± 0.017) mm2/s 30oC. One way ANOVA statistical analysis result of optimal formula SNEDDS (105.210 ± 4.425)% of drug content, commercial generic caplet (0.917 ± 0.094)%, and mefenamic acid powder capsule (10.446 ± 0,333)% gave significant value (sig*) below than 0.05. Optimal formula proved that SNEDDS can significantly increase mefenamic acid dissolution of pH 7.4 (ileum fluid). The optimal formula of mefenamic acid SNEDDS successfully formed an uniformity droplet size (PDI 0.18) with mean size 241.9 nm and  the surface charge has a value of -16.5 mV respectively.


Author(s):  
NISHANT OZA ◽  
SWATI SAGAR ◽  
AKRUTI KHODAKIYA

Objective: The aim of the present work was to enhance the solubility of rosuvastatin calcium by self-nano emulsifying drug delivery system (SNEDDS) using mixtures of oil, cosolvent, surfactant and cosurfactant. Methods: Based on solubility study and emulsification efficiency, Preliminary investigations of various oils, surfactants and cosurfactants were carried out for the selection of the proper SNEDDS ingredients. Pseudo-ternary phase diagrams were constructed to identify the efficient self-emulsification region. A series of SNEDDS formulations were prepared using labrasol: cremophor EL with a combination of peceol: ethyl oleate by using the simplex lattice design. Prepared formulation evaluated for refractive index, turbidimetric, droplet size, zeta potential and polydispersity index, self-emulsification, stability tests, viscosity and in vitro diffusion studies. Results: The best formula for SNEDDS in the current study were:  15% oil (peceol: ethyloleatein 1:1 ratio), 50% Labrasol and 35% Cremophor EL. All the SNEDDS batches globule size was found to be varied from 22.90±1.50 nm to 43.90±1.40 nm. and no significant variations in globule size were observed after 3 mo stability studies. All the batches % transparency was found to be varied from 95.40±1.40% to 99.50±1.10% and drug diffused in 10 min varied from 63.65±1.51% to 93.72±1.46 %. Conclusion: The data suggest the use of rosuvastatin calcium SNEDDS to offer the potential for delivery and it increases the aqueous solubility and bioavailability of the drug.


Author(s):  
Maya Uzia Beandrade

<p>Jinten hitam (<em>Nigella sativa</em>) mengandung senyawa timokuinon yang berefek sebagai imunostimulan. Ekstrak jinten hitam dikembangkan menjadi SNEDDS (<em>Self-nanoemulsifying Drug Delivery System</em>) karena masalah kelarutan. Penelitian dilakukan untuk mengetahui karakteristik SNEDDS ekstrak jinten hitam yang meliputi viskositas, ukuran tetesan nanoemulsi, <em>extract loading</em>, dan stabilitas. Pengujian aktivitas imunostimulan SNEDDS meliputi rasio sel makrofag dan indeks fagositosis.</p><p>SNEDDS ekstrak jinten hitam dioptimasi dengan metode <em>Simplex Lattice Design</em> menggunakan <em>Design Expert 7.1.5., </em>selanjutnya SNEDDS optimal diuji ukuran tetesan nanoemulsi dan zeta potensial, viskositas, serta uji stabilitas. Uji aktivitas imunostimulan dilakukan dengan metode <em>biolatex assay</em> terhadap tikus <em>Sprague Dawley</em> sebanyak 5 tikus/kelompok selama 15 hari dengan pemberian satu kali sehari yaitu kontrol positif (ekstrak meniran 7,2 mg/tikus), kelompok perlakuan yaitu ekstrak jinten hitam dengan dosis 200 mg/kgBB serta SNEDDS ekstrak jinten hitam (200 mg/kgBB), kelompok plasebo berupa formula SNEDDS tanpa ekstrak jinten hitam, dan kontrol normal, selanjutnya dihitung rasio dan indeks fagositosis makrofag.</p>SNEDDS ekstrak jinten hitam optimal mengandung 15% minyak ikan hiu cucut botol, 67,344% surfaktan (10,102% croduret 50 ss dan 57,242% tween 80), 17,656% PEG 400 sebagai ko-surfaktan dengan hasil ukuran tetesan nanoemulsi 16,3 nm, PI sebesar 0,202, zeta potensial -43,5 mV, dan viskositas antara 234,69 – 255,71 cP. Hasil <em>extract loading</em> sistem SNEDDS mencapai 600 mg ekstrak/g sistem. SNEDDS stabil setelah penyimpanan selama 90 hari pada suhu kamar dan uji <em>freeze-thawing</em>. SNEDDS ekstrak jinten hitam dengan dosis 200 mg/kgBB dapat meningkatkan rasio sel makrofag dan indeks fagositosis dibandingkan dengan ekstrak jinten tanpa formulasi (P&lt;0,05).


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