scholarly journals Preparation and evaluation of an ispaghula based directly compressible matrixing agent for controlled release

2008 ◽  
Vol 58 (3) ◽  
pp. 309-316 ◽  
Author(s):  
Anita Lalwani ◽  
Jolly Parikh

Preparation and evaluation of an ispaghula based directly compressible matrixing agent for controlled releaseThe objective of the present investigation was to prepare and evaluate an ispaghula husk based directly compressible (DC) adjuvant that can be used as matrixing agent using an agglomeration technique. Addition of hydroxypropyl methylcellulose was found necessary to improve cohesion. Lactose (X1), calcium hydrogen phosphate dihydrate (X2) and Avicel PH101 (X3), used along with ispaghula in preparation of agglomerates, were selected as three independent variables in a simplex lattice design affecting compressional and dissolution characteristics of the drug from the DC adjuvant. The agglomerates were evaluated for their flow properties. Tablets were prepared using 70% agglomerates and 30% acetaminophen, a poorly compressible drug, and were subjected toin vitrodrug release study. Amounts of the drug released at the end of 60 min (Y60), 300 min (Y300) and 480 min (Y480) were selected as dependent variables in a simplex lattice design. Batch IH05 that contained lactose and calcium hydrogen phosphate dihydrate in a 1:2 ratio could control the release for 12 hours and thus form the basis for twice a-day-dosing.

2018 ◽  
Vol 14 (1) ◽  
pp. 29 ◽  
Author(s):  
Mercy Arizona ◽  
A. Karim Zulkarnain

Ekstrak temu mangga (Curcuma mangga Val.) memiliki aktivitas sebagai tabir surya secara spektrofotometri. Penelitian ini bertujuan untuk mengetahui formula optimum lotion o/w, sifat dan stabilitas fisik formula optimum lotion o/w, serta aktivitas tabir surya formula optimum lotion o/w ekstrak temu mangga  (Curcuma mangga Val.) secara spektrofotometri. Formula optimum diperoleh dengan metode Simplex Lattice Design (SLD). Respon yang digunakan untuk menentukan formula optimum adalah daya lekat dan viskositas. Stabilitas fisik lotion o/w pada suhu ruang meliputi uji daya sebar, daya lekat, dan viskositas, serta uji freeze thaw cycling. Aktivitas tabir surya lotion o/w ditentukan secara spektrofotometri untuk menentukan Sun Protecting Factor (SPF), % transmisi eritema, dan % transmisi pigmentasi. Data dianalisis dengan One Way ANOVA dan uji t. Hasil penelitian menunjukkan bahwa formula optimum lotion o/w pada kombinasi 5% trietanolamin (TEA)-stearat dan 5% setil alkohol. Lotion o/w ekstrak temu mangga memiliki memiliki daya sebar 63,21±2,69 cm2, daya lekat 2,32±0,15 detik, dan viskositas sebesar 133,5±8,05 dPas. Hasil analisis statistika menunjukkan bahwa lotion o/w smemiliki stabilitas yang baik. Lotion o/w mempunyai aktivitas sebagai tabir surya pada konsentrasi lotion o/w 12,5% yang ditunjukkan dengan nilai SPF sebesar 12,82±0,16 dan tidak efektif dalam perlindungan terhadap eritema dan pigmentasi.


2019 ◽  
Vol 10 (8) ◽  
pp. 515-525
Author(s):  
Shivaji Phadke ◽  
Tanvi Kanekar ◽  
Suhas Gumaste ◽  
Vaishnavi Parikh

Aim: Simplex lattice design was applied to predict extent of drug release from extended release diclofenac sodium tablets. Methods: The effects of composition on dissolution rate were evaluated by varying the levels of hydroxypropyl methylcellulose, dicalcium phosphate and cornstarch via three component design. Results: The rate of drug release was primarily dictated by the proportion of hydroxypropyl methylcellulose and was also affected by the proportion of dicalcium phosphate and the method of processing (direct compression/wet granulation). Polynomial equations constructed for directly compressed and wet-granulated formulations could successfully predict the extent of drug release at an arbitrary time point of 3 h. Conclusion: Simplex lattice design is a viable tool to predict the drug release patterns of extended release formulations.


2018 ◽  
Vol 5 (2) ◽  
pp. 80
Author(s):  
Dwi Nurahmanto ◽  
Nurul Shalikha ◽  
Lidya Ameliana

<p align="center"><strong>Abstrak</strong></p><p align="center"> </p><p>Piroksikam merupakan anti inflamasi non steroid (AINS) turunan oksikam yang berkhasiat sebagai analgesik dan antiinflamasi digunakan untuk pengobatan <em>rheumatoid arthritis</em> dan <em>osteoarthritis</em>. Piroksikam menyebabkan masalah pada saluran cerna dan <em>first pass metabolism</em> yang dapat dihindari dengan cara pemberian transdermal <em>patch.</em> Salah satu komponen <em>patch</em> yaitu polimer yang berfungsi untuk mengontrol kecepatan pelepasan obat dari sediaan. Penelitian ini dilakukan untuk menentukan komposisi terbaik dari kombinasi polimer hidroksipropil metilselulosa (HPMC) dan Carbopol terhadap <em>% moisture content</em> (MC) dan <em>flux</em> pelepasan sediaan transdermal <em>patch </em>dispersi padat piroksikam dengan rancangan formula <em>Simplex Lattice Design</em>. Piroksikam dibuat dalam bentuk dispersi padat dengan pembawa PEG 4000 untuk meningkatkan kelarutannya. Rancangan formula <em>patch</em> dispersi padat piroksikam dibuat dengan menggunakan tiga polimer Etil selulosa:HPMC:carbopol dimana yang divariasikan adalah perbandingan HPMC : Carbopol yaitu 1 : 0 ; 0,5 : 0,5 ; 0 : 1. Hasil uji menunjukkan ketiga formula memenuhi persyaratan keseragaman kadar dengan rentang keseragaman 3,735 – 97,349 %. Hasil juga menunjukkan formula 3 menghasilkan patch yang lebih tebal, pH permukaan patch lebih rendah, nilai % moisture content lebih besar dan nilai flux lebih tinggi dibandingkan formula 2 dan formula 3, Formula 3 mempunyai nilai % moisture content yang memenuhi persyaratan sebesar 6,613% dan nilai <em>flux</em> pelepasa yang paling bagus sebesar 32,562 µg/cm<sup>2</sup>.menit<sup>1/2</sup>. Hasil penelitian juga menunjukkan formula 1 memiliki keseragaman bobot lebih baik dibandingkan formula 2 dan formula 3. Dapat disimpulkan bahwa komposisi optimum dari kombinasi polimer HPMC dan Carbopol pada sediaan <em>patch</em> dispersi padat piroksikam yaitu formula dengan komposisi polimer HPMC sebanyak 0 mg dan Carbopol sebanyak 75 mg.</p><p> </p><p><strong>Kata kunci</strong><em>:</em><em>     </em>Dispersi padat, <em>patch </em>piroksikam, HPMC, Carbopol</p><p align="center"> </p><p align="center"><strong><em>Optimization of Hydroxypropyl Methylcellulose K-4M</em></strong><strong> <em>and  Carbopol® 940 in</em></strong><strong><em> </em></strong><strong><em>Solid Dispersion Piroxicam Patch</em></strong><strong><em></em></strong></p><p align="center"> </p><p align="center"><strong><em>Abstract</em></strong></p><p><strong> </strong></p><p><em>Piroxicam is a non-steroidal anti-inflammatory (NSA) oxysmic derivative as an analgesic and anti-inflammatory agent used for the treatment of rheumatoid arthritis and osteoarthritis. Piroxicam causes problems in the gastrointestinal tract and first pass metabolism that can be avoided by giving transdermal patches. One of the patch components is a polymer that serves to control the speed of drug release from the preparation. The present study was conducted to determine the best composition of the combination of hydroxypropyl methylcellulose (HPMC) and Carbopol polymers against% moisture content (MC) and fluxes release of the pyroxicam dispersion transdermal patch dispersion with the design of the Simplex Lattice Design formula. Piroxicam is prepared in the form of a solid dispersion with a PEG 4000 carrier to increase its solubility. The design of a pyroxicam solid dispersion patch formulation was prepared using three ethyl cellulose polymers: HPMC: carbopol wherein the HPMC ratio is computed: Carbopol is 1: 0; 0.5: 0.5; 0: 1. The test results show the three formulas meet the requirements of uniformity of the content with a uniformity range of 3.735 - 97.349%. the results also show formula 3 resulting in thicker patches, lower patch pH surfaces, greater moisture content values and higher flux values than formula 2 and formula 3, Formula 3 has a moisture content value of 6.613% the finest fl ux flux of 32,562 μg / cm2.menit1 / 2. The results also show that formula 1 has better weight uniformity than formula 2 and formula 3. It can be concluded that the optimum composition of HPMC and Carbopol polymer combinations in the preparation of piroxicam solid dispersion patch is a formula with HPMC polymer composition as 0 mg and Carbopol as much as 75 mg..</em></p><p><strong><em> </em></strong></p><p><strong><em>Key</em></strong><strong><em> </em></strong><strong><em>words</em></strong><em>: </em><em>     </em><em>solid dispersion, piroxicam patch, HPMC, Carbopol</em></p>


2017 ◽  
Vol 5 (2) ◽  
pp. 80
Author(s):  
Dwi Nurahmanto ◽  
Nurul Shalikha ◽  
Lidya Ameliana

<p align="center"><strong>Abstrak</strong></p><p align="center"> </p><p>Piroksikam merupakan anti inflamasi non steroid (AINS) turunan oksikam yang berkhasiat sebagai analgesik dan antiinflamasi digunakan untuk pengobatan <em>rheumatoid arthritis</em> dan <em>osteoarthritis</em>. Piroksikam menyebabkan masalah pada saluran cerna dan <em>first pass metabolism</em> yang dapat dihindari dengan cara pemberian transdermal <em>patch.</em> Salah satu komponen <em>patch</em> yaitu polimer yang berfungsi untuk mengontrol kecepatan pelepasan obat dari sediaan. Penelitian ini dilakukan untuk menentukan komposisi terbaik dari kombinasi polimer hidroksipropil metilselulosa (HPMC) dan Carbopol terhadap <em>% moisture content</em> (MC) dan <em>flux</em> pelepasan sediaan transdermal <em>patch </em>dispersi padat piroksikam dengan rancangan formula <em>Simplex Lattice Design</em>. Piroksikam dibuat dalam bentuk dispersi padat dengan pembawa PEG 4000 untuk meningkatkan kelarutannya. Rancangan formula <em>patch</em> dispersi padat piroksikam dibuat dengan menggunakan tiga polimer Etil selulosa:HPMC:carbopol dimana yang divariasikan adalah perbandingan HPMC : Carbopol yaitu 1 : 0 ; 0,5 : 0,5 ; 0 : 1. Hasil uji menunjukkan ketiga formula memenuhi persyaratan keseragaman kadar dengan rentang keseragaman 3,735 – 97,349 %. Hasil juga menunjukkan formula 3 menghasilkan patch yang lebih tebal, pH permukaan patch lebih rendah, nilai % moisture content lebih besar dan nilai flux lebih tinggi dibandingkan formula 2 dan formula 3, Formula 3 mempunyai nilai % moisture content yang memenuhi persyaratan sebesar 6,613% dan nilai <em>flux</em> pelepasa yang paling bagus sebesar 32,562 µg/cm<sup>2</sup>.menit<sup>1/2</sup>. Hasil penelitian juga menunjukkan formula 1 memiliki keseragaman bobot lebih baik dibandingkan formula 2 dan formula 3. Dapat disimpulkan bahwa komposisi optimum dari kombinasi polimer HPMC dan Carbopol pada sediaan <em>patch</em> dispersi padat piroksikam yaitu formula dengan komposisi polimer HPMC sebanyak 0 mg dan Carbopol sebanyak 75 mg.</p><p> </p><p><strong>Kata kunci</strong><em>:</em><em>     </em>Dispersi padat, <em>patch </em>piroksikam, HPMC, Carbopol</p><p align="center"> </p><p align="center"><strong><em>Optimization of Hydroxypropyl Methylcellulose K-4M</em></strong><strong> <em>and  Carbopol® 940 in</em></strong><strong><em> </em></strong><strong><em>Solid Dispersion Piroxicam Patch</em></strong><strong><em></em></strong></p><p align="center"> </p><p align="center"><strong><em>Abstract</em></strong></p><p><strong> </strong></p><p><em>Piroxicam is a non-steroidal anti-inflammatory (NSA) oxysmic derivative as an analgesic and anti-inflammatory agent used for the treatment of rheumatoid arthritis and osteoarthritis. Piroxicam causes problems in the gastrointestinal tract and first pass metabolism that can be avoided by giving transdermal patches. One of the patch components is a polymer that serves to control the speed of drug release from the preparation. The present study was conducted to determine the best composition of the combination of hydroxypropyl methylcellulose (HPMC) and Carbopol polymers against% moisture content (MC) and fluxes release of the pyroxicam dispersion transdermal patch dispersion with the design of the Simplex Lattice Design formula. Piroxicam is prepared in the form of a solid dispersion with a PEG 4000 carrier to increase its solubility. The design of a pyroxicam solid dispersion patch formulation was prepared using three ethyl cellulose polymers: HPMC: carbopol wherein the HPMC ratio is computed: Carbopol is 1: 0; 0.5: 0.5; 0: 1. The test results show the three formulas meet the requirements of uniformity of the content with a uniformity range of 3.735 - 97.349%. the results also show formula 3 resulting in thicker patches, lower patch pH surfaces, greater moisture content values and higher flux values than formula 2 and formula 3, Formula 3 has a moisture content value of 6.613% the finest fl ux flux of 32,562 μg / cm2.menit1 / 2. The results also show that formula 1 has better weight uniformity than formula 2 and formula 3. It can be concluded that the optimum composition of HPMC and Carbopol polymer combinations in the preparation of piroxicam solid dispersion patch is a formula with HPMC polymer composition as 0 mg and Carbopol as much as 75 mg..</em></p><p><strong><em> </em></strong></p><p><strong><em>Key</em></strong><strong><em> </em></strong><strong><em>words</em></strong><em>: </em><em>     </em><em>solid dispersion, piroxicam patch, HPMC, Carbopol</em></p>


2021 ◽  
Vol 2 (1) ◽  
pp. 34-42
Author(s):  
Sesilia Putri Nandita ◽  
Ilham Kuncahyo ◽  
Reslely Harjanti

Furosemide is a potent diuretic drug that has low bioavailability. Furosemide can be formulated into nanoemulsion preparations using the SNEDDS method to increase its bioavailability as SNEDDS can form stable nanoemulsions with droplet sizes 200 nm. This study aims to identify the optimum formula for variations in the concentration of surfactant Tween 80 and cosurfactant PEG 400 based on the characterization tests of emulsification time, percent transmittance, and drug loading. The independent variables used in this study were Tween 80 and PEG 400. Seven furosemide SNEDDS formulas from the Simplex Lattice Design (SLD) method were tested for characterization in the form of emulsification time, percent transmittance, and drug loading. The characterization results were optimized using Simplex Lattice Design. The optimum formula was re-characterized, including emulsification time, percent transmittance, drug loading, particle size, zeta potential, and in vitro dissolution. The results were then compared with theoretical values and analyzed using the One-Sample T-test method. Optimization results showed Tween of 61.4922% and PEG 400 of 18.5078% with the characterization of emulsification time 15.25 seconds, percentage transmittance 94.20%, drug loading 50 100.2 ppm, particle size 12.18 nm. Furthermore, the zeta potential was -17.6 mV, and the in vitro dissolution rate reached 106.71% within 15 minutes.


2019 ◽  
Vol 3 (2) ◽  
pp. 109
Author(s):  
Uqwatul Alma Wizsa

A mixture experiment is a special case of response surface methodology in which the value of the components are proportions. In case there are constraints on the proportions, the experimental region can be not a simplex. The classical designs such as a simplex-lattice design or a simplex-centroid design, in some cases, cannot fit to the problem. In this case, optimal design come up as a solution. A D-optimal design is seeking a design in which minimizing the covariance of the model parameter.  Some model parameters are important and some of them are less important. As the priority of the parameters, the prior information of parameters is needed in advance. This brings to a Bayesian D-optimal design. This research was focus on a baking experiment in which consisted of three ingredients with lower bounds on the proportion of the ingredients. The assumption model was a quadratic model. Due to the priority of the model parameters, the Bayesian D-optimal design was used to solve the problem. A point-exchange algorithm was developed to find the optimal design. Nineteen candidates is used to choose twelve design points. It found that the potential term is feasible to the actual model and design points represent overall points in the design area.


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