scholarly journals Penggunaan D-Optimal Mixture Design untuk Optimasi dan Formulasi Self-Nano Emulsifying Drug Delivery System (SNEEDS) Asam Mefenamat

2020 ◽  
Vol 7 (3) ◽  
pp. 180
Author(s):  
Yandi Syukri ◽  
Bambang Hernawan Nugroho ◽  
Istanti Istanti

Penelitian ini bertujuan untuk melakukan optimasi formulasi asam mefenamat yang sukar larut dalam air dalam bentuk sediaan Self-Nano Emulsifying Drug Delivery System (SNEDDS) menggunakan D-optimal mixture design. Skrining awal dilakukan untuk menentukan fase minyak, surfaktan dan ko-surfaktan yang akan digunakan untuk pembuatan diagram fase terner. D-optimal mixture design digunakan untuk mengoptimasi SNEDDS asam mefenamat dengan memilih komposisi SNEDDS sebagai faktor independent dan karakterisasi SNEDDS sebagai respons. Karakterisasi SNEDDS pada formula optimal meliputi transmitan, ukuran partikel, polidispersity index (PDI) dan zeta potensial. Asam oleat, Tween 80, dan polietilenglikol (PEG) 400 merupakan fase minyak, surfaktan, dan ko-surfaktan yang terpilih karena memiliki kemampuan paling tinggi dalam melarutkan asam mefenamat. Hasil optimasi menunjukkan bahwa formula optimal diperoleh pada komposisi 10% asam oleat, 80% Tween 80 dan 10% PEG 400. SNEDDS asam mefenamat tersebut menghasilkan nanoemulsi dengan transmitan 88,5%, ukuran partikel 190,03 ± 1,18 nm, PDI 0,469 ± 0,03, dan zeta potensial -44,1 ± 1,69 mV. Studi ini menyimpulkan bahwa D-optimal mixture design dapat digunakan untuk mengoptimasi dan formulasi SNEDDS asam mefenamat yang sukar larut dalam air.

2015 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Yandi Syukri ◽  
Agung Endro Nugroho ◽  
Ronny Martien ◽  
Endang Lukitaningsih

Penelitian ini bertujuan untuk mengembangkan analisis kuantitatif untuk penentuan kadar isolat andrographolide dari tanaman sambiloto (Andrographis paniculata) dan pelarut yang berbeda untuk studi awal untuk pembuatan Self Nanoemulsifying Drug Delivery System (SNEDDS) menggunakan KCKT. Pemisahan menggunakan kolom Sunfire C18 dengan campuran isokratik metanol dan air dengan perbandingan 6: 4, v / v sebagai fase gerak. Metode untuk menentukan isolat andrographolide menunjukkan presisi yang memadai, dengan RSD lebih kecil dari 1%. Akurasi dianalisis dengan menambahkan andrografolid standar, dan didapatkan nilai perolehan kembali yang baik untuk semua konsentrasi yang digunakan. Metode HPLC yang dikembangkan dalam penelitian ini menunjukkan spesifisitas dan selektivitas dengan linearitas dalam rentang kerja dan presisi dan akurasi yang baik, sehingga sangat cocok untuk menentukan kandungan isolat andrografolida. Dibandingkan dengan standar, kemurnian isolat andrografolida adalah 95,74 ± 0,29%. Penelitian awal untuk menentukan kelarutan tertinggi isolat andrographolid adalah dalam fasa minyak Capryol-90 1,226 ± 0,009 mg mL-1, surfaktan tween 80 2,965 ± 0.014 mg mL-1 dan co-surfaktan PEG 400 6,074 ± 0,101 mg mL-1. Dapat disimpulkan, metode ini cocok digunakan untuk penentuan kelarutan dari isolat andrographolide untuk pembuatan SNEDDS.


2019 ◽  
Vol 1 (2) ◽  
pp. 37-46
Author(s):  
Muhamad Handoyo Sahumena ◽  
Suryani Suryani ◽  
Neni Rahmadani

Mefenamic acid is a non-steroidal anti-inflammatory drug (NSAID) which has analgesic, anti-inflammatory and antipyretic effects. Mefenamic acid works by inhibiting prostaglandin synthesis as an inflammatory mediator. Mefenamic acid has low drug solubility and a long process of dissolution in the body which greatly affects the speed of absorption and bioavailability of the drug. In this study, mefenamic acid nanoemulsion formulation was carried out through a Self-Nanoemulsifying Drug Delivery System (SNEDDS) delivery system. SNEDDS is a drug delivery method through isotropic oil extraction, surfactants, cosurfactans and drug that form oil in water (m/a) emulsions which when in contact with the water phase in the digestive tract wiil from a nanoemulsion that occurs spontaneously so that the drug dissolves with a particle size small so as to increase the effective surface area for absorption. The purpose of the study was to determine the ratio of surfactant and cosurfactant composition to the optimum formula of SNEDDS of mefenamic acid with VCO as an oil phase. The SNEDDS formula was obtained by mixing the surfactants tween 80 and span 80, cosurfactant PEG 400 and VCO as the oil phase using the characterization of determining the optimum formula, namely emulsion formation, transmittance and emulsification time. The composition of the optimum formula of SNEDDS of mefenamic acid is 1 mL VCO; 1 mL PEG 400; 6 mL tween 80; 1 mL span 80. Optimum formula showed clear emulsion results, with transmittance values of 89,04% and emulsification time under 1 minute. In this study produced the optimum formula SNEDDS the met the criteria based on droplet size parameters of 153,5 nm, potential zeta value of 8,2 mV and showed good stability.


2017 ◽  
Vol 14 (2) ◽  
pp. 99-109
Author(s):  
Ilham Kuncahyo ◽  
Pudiastuti RSP

Kurkumin terbukti memiliki aktivitas sebagai anti-tumor, anti-inflamasi, anti-virus, anti-oksidasi dan anti HIV. Penggunaan kurkumin dalam proses pengobatan jangka panjang memberikan toksisitas yang rendah sehingga secara klinis akan sangat menguntungkan untuk dikembangkan. Kandungan aktif kurkumin yang berasal dari ekstrak tanaman curcuma longa ini mempunyai bioavaiblitas yang sangat rendah. Hal ini berkaitan karena kelarutan kurkumin yang jelek dalam air (11 ng/ml, pH 5,0) sehingga sedikit diserap di saluran pencernaan. Permasalahan ini dapat diatasi dengan membuat sediaan kurkumin dalam bentuk Self Mikroemulsi Drug Delivery System (SMEDDS) Penelitian awal dilakukan skrining terhadap kelarutan kurkumin dengan pembawa berbagai jenis minyak, surfaktan dan kosurfaktan. Hasil skrining dilanjutkan dengan pemilihan formula optimum SMEDDS kurkumin dengan menggunakan metode Simpelx Lattice Design (SLD). Tiga variabel akan memberikan 14 formula SMEDDS kurkumin yang masing-masing formula dilakukan pengujian terhadap karakteristiknya sebagai titik kritis meliputi : % transmitan, waktu emulsifikasi dan drug loading. Hasil masing-masing pengujian dianalisis datanya dengan Design Exspert versi 7 dan dilanjutnya validasi formula optimum dengan uji T dengan taraf kepercayaan 95%. Hasil penelitian menunjukkan bahwa skrining awal terhadap kurkumin didapatkan kelarutan yang terbesar pada jenis minyak zaitun, surfaktan Tween 80 dan kosurfaktan PEG 400. Ketiga jenis bahan ini dilakukan optimasi dengan SLD memberikan formula optimum komposisi SMEDDS kurkumin dengan komposisi 0,026 minyak zaitun ; 0,0913 Tween 80 dan 0,061 PEG 400.


2020 ◽  
Vol 1 (2) ◽  
pp. 27-34
Author(s):  
Septiana Indratmoko ◽  
Asep Nurrahman ◽  
Axl Aprizal Herawan

Kandungan flavonoid dan tanin pada daun kersen dapat  menghambat pertumbuhan bakteri Staphylococcus aureus. Penelitian ini bertujuan untuk mengetahui pengaruh formulasi nanoemulsi daun kersen (Mutingia calabura.L) terhadap karakteristik nanoemulsi menggunakan teknik Self Nano Emulsifying Drug Delivery System (SNEDDS) dan  pengaruhnya sebagai antibakteri Staphylococcus aureus. Ekstrak etanol daun kersen diformulasi dengan surfaktan, kosurfaktan dan minyak terpilih. Kemudian nanoemulsi ekstrak daun kersen diuji ukuran partikel, potensial zeta, drug loading dan stabilitas nanoemulsi. Nanoemulsi ekstrak etanol daun kersen dapat dihasilkan dengan formula Tween 80, PEG 400 dan VCO perbandingan 6:1:1. Ukuran partikel nanoemulsi 12,4 nm, potensial zeta 30,8 mV, drug loading yaitu 125 mg/ml dan stabil. Nanoemulsi ekstrak daun kersen dapat memberikan aktivitas antibakteri lebih baik daripada ekstrak daun kersen.


INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (06) ◽  
pp. 16-26
Author(s):  
V Suthar ◽  
◽  
M Gokel ◽  
S Butani ◽  
A Solanki

The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.


2014 ◽  
Vol 2014 ◽  
pp. 1-6
Author(s):  
Sajal Kumar Jha ◽  
Roopa Karki ◽  
Venkatesh Dinnekere Puttegowda ◽  
Amitava Ghosh

Ranitidine microemulsion was investigated for its pharmacodynamic and pharmacokinetic evaluation to find out the suitability of microemulsion as a potential drug delivery system in the treatment of ulcer. The bioavailability of ranitidine after oral administration is about 50% and is absorbed via the small intestine; this may be due to low intestinal permeability. Hence the aim of present investigation was to maximize the therapeutic efficacy of ranitidine by developing microemulsion to increase the intestinal permeability as well as bioavailability. A ground nut oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed for oral delivery of ranitidine and characterized for physicochemical parameters. In pharmacodynamic studies, significant (P<0.05) variation in parameters estimated was found between the treated and control groups. Ranitidine microemulsion exhibited higher absorption and Cmax (863.20 ng·h/mL) than the standard (442.20 ng/mL). It was found that AUC0–24 hr obtained from the optimized ranitidine test formulation (5426.5 ng·h/mL) was significantly higher than the standard ranitidine (3920.4 ng·h/mL). The bioavailability of optimized formulation was about 1.4-fold higher than that of standard drug. This enhanced bioavailability of ranitidine microemulsion may be used as an effective and alternative drug delivery system for the antiulcer therapy.


1970 ◽  
Vol 7 (1) ◽  
pp. 38-40
Author(s):  
Ankur Gupta ◽  
Arpna Indurkhya ◽  
S.C Chaturvedi ◽  
Ajit Varma

Spironolactone is aldosterone antagonist drug belonging to the category of potassium sparing diuretics administered orally that has absolute bioavailability of only 68% due to the poor aqueous solubility. The main aim of the present work was to develop a self emulsifying drug delivery system (SEDDS) to enhance the oral absorption of spironolactone. The solubility of spironolactone in various oils, surfactants, and co surfactants was determined. Pseudo ternary phase diagrams were constructed using castor oil, Tween 80, and polyethylene glycol 400, and distilled water to identify the efficient self-micro emulsion region. Prepared self emulsifying drug delivery system was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro drug release. The results showed that 96.16% drug was released from the SEDDS formulation in 3 hrs. This demonstrated an enhancement in the drug release and thereby, absorption of the drug through the membrane, this was significantly higher than that of the plain drug suspension. Thus, the above findings support that the utility of SEDDS to enhance solubility and dissolution of poorly water soluble compounds which may result in improved Therapeutic performance.


2020 ◽  
Vol 11 (2) ◽  
pp. 1294-1301
Author(s):  
Geethanjali K ◽  
Vaiyana Rajesh C

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was         90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.


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.


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