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Abstrak :
Kaptopril merupakan obat antihipertensi oral yang memiliki permasalahan terkait bioavailabilitas dan frekuensi pemberian sehingga dapat menurunkan kepatuhan pasien. Penghantaran kaptopril secara transdermal dapat mengatasi permasalahan tersebut. Namun, kaptopril bersifat hidrofilik sehingga hydrogel-forming microneedle (HFMN) dapat digunakan untuk meningkatkan permeasinya ke dalam kulit. Tujuan penelitian ini adalah memformulasikan dan mengevaluasi HFMN terintegrasi film yang mengandung kaptopril untuk penghantaran transdermal. HFMN dibuat dari poli(vinil alkohol) (PVA), poli(vinilpirolidon) (PVP) K-29/32, dan asam sitrat lalu dievaluasi fisik, kemampuan mengembang, permeabilitas, insersi, dan kekuatan mekaniknya. Film yang mengandung kaptopril dibuat dari PVP K-29/32, PVP K-90, dan PVA dengan variasi konsentrasi, serta gliserol, lalu dievaluasi fisik, kekuatan tarik, kadar kaptopril, dan kemampuannya melarut secara ex vivo. Untuk uji permeasi in vitro, dipilih formula film yang optimal untuk diintegrasikan dengan HFMN. HFMN yang dihasilkan mampu mengembang dalam kulit tikus hingga 47,18±2,87% setelah 1 jam, dapat memfasilitasi difusi kaptopril sebesar 30,78±2,01% setelah 24 jam, dan mampu menembus lapisan parafilm hingga kedalaman 500 µm dengan pengurangan tinggi jarum sebesar 6,70±0,27%. Berdasarkan evaluasi, formula terpilih dari film yang mengandung kaptopril adalah F3 (PVP K-29/32 20%), F5 (PVP K-90 15%), dan F6 (PVP K-90 20%). Pada uji permeasi in vitro, jumlah kaptopril yang terpermeasi melewati kulit tikus setelah 24 jam dari HFMN terintegrasi F3, F5, dan adalah 9,90±0,31, 9,92±0,50, dan 9,60±0,42 mg (p>0,05). F3 dipilih sebagai formula terbaik karena dapat melarut paling cepat dan memiliki persentase kaptopril terpermeasi tertinggi setelah 24 jam (52,35±1,66%). Penelitian ini menunjukkan kaptopril dapat dihantarkan secara in vitro dengan HFMN terintegrasi film. ......Captopril, an oral antihypertensive drug, has problems related to its bioavailability and frequent administration which may reduce patient compliance. Transdermal delivery of captopril may overcome these issues. However, captopril is hydrophilic, thus hydrogel-forming microneedles (HFMN) can enhance its skin permeation. This study aimed to formulate and evaluate HFMN integrated with captopril-containing film for transdermal delivery. HFMN was prepared from poly(vinyl alcohol) (PVA), poly(vinylpyrrolidone) (PVP) K-29/32, and citric acid, then evaluated for its physical, swelling, permeability, insertion, and mechanical strength properties. Captopril-containing films were made from PVP K-29/32, PVP K-90, and PVA with various concentrations, and glycerol, then assessed for their physical characteristics, tensile strength, captopril content, and ex vivo dissolution. For the in vitro permeation study, the optimal captopril-containing film formulation was chosen to be integrated with HFMN. The resulting HFMN can be swelled in rat skin by 47.18±2.87% after 1h, facilitating captopril diffusion by 30.78±2.01% after 24h, and penetrated parafilm layers to a depth of 500µm with 6.70±0.27% of needle height reduction. The selected captopril-containing film formulations were F3 (PVP K-29/32 20%), F5 (PVP K-90 15%), and F6 (PVP K-90 20%). In the in vitro permeation study, the amount of captopril that permeated through rat skin after 24h from HFMN integrated with F3, F5, and F6 was 9.90±0.31, 9.92±0.50, and 9.60±0.42 mg (p>0.05). F3 was chosen as the best formulation because it dissolves the fastest and has the highest percentage of permeated captopril after 24h (52,35±1,66%). This study demonstrated that captopril can be delivered in vitro using film-integrated HFMN.

Abstrak :
[ABSTRAK
Penggunaan angiotensin converting enzyme inhibitor (ACEi) sebagai antihipertensi dapat menyebabkan efek samping berupa batuk kering. Penelitian ini bertujuan untuk menilai risiko penggunaan ACEi, yaitu kaptopril sebagai standar dibandingkan ACEi lain terhadap kejadian batuk kering pada pasien hipertensi di RSUD Cengkareng Jakarta Barat dan RSUD Tarakan Jakarta Pusat. Desain penelitian ini adalah kohort prospektif. Kriteria inklusi adalah pasien hipertensi rawat jalan yang mendapatkan terapi obat golongan ACEi selama ≤ 3 bulan dan bersedia untuk diikutsertakan sebagai sampel dalam penelitian di RSUD Cengkareng Jakarta Barat dan RSUD Tarakan tahun 2014. Sampel terdiri dari 54 pasien yang mendapat kaptopril dan 54 pasien yang mendapat obat ACEi bukan kaptopril yang diambil secara consecutive sampling pada bulan Januari-Juli 2014. Alat pengumpul data menggunakan wawancara terstruktur dan rekam medis pasien. Kejadian batuk kering akibat ACEi dievaluasi dengan menggunakan Algoritma Naranjo dan analisis data menggunakan uji Chi Square. Kejadian batuk kering terjadi pada 19,44% sampel. Faktor usia, jenis kelamin, suku bangsa, komorbiditas, body mass index (BMI), dosis obat, dan lama penggunaan tidak berhubungan bermakna dengan kejadian batuk kering akibat penggunaan ACEi. Tidak ada perbedaan risiko penggunaan ACEi kelompok kaptopril dibanding bukan kaptopril terhadap kejadian batuk kering.

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ABSTRACT
Use of angiotensin converting enzyme inhibitors (ACEi) as an antihypertensive agent can cause side effects such as dry cough. This study aimed to evaluate the risk of ACEi administration with captopril as the standard against another ACEi on dry cough incidence in hypertensive patients from various tribes at RSUD Cengkareng West Jakarta and RSUD Tarakan Central Jakarta. The design of this study is prospective cohort. The inclusion criteria were patients who received ACEi as hypertension therapy for ≤ 3 months gathered from outpatient polyclinics and those willing to participate as sample in this study at RSUD Cengkareng West Jakarta and RSUD Tarakan Central Jakarta. Sample consist of 54 patients who received captopril and 54 patients received non captopril ACEi, taken by consecutive sampling from January-July 2014. The data was collected using structured interviews and from medical record. Dry cough incidence due to ACEi was evaluated using Naranjo Algorithm and the data was analyzed using Chi Square test. Dry cough incidence was found in 19,44% of sample. No significant relationship of age, gender, tribe, comorbidity, body mass index (BMI), dosage, and duration of use with dry cough incidence due to the use of ACEi. Furthermore there is no difference in risk between the use of captopril group and non captopril ACEi group on dry cough incidence.;Use of angiotensin converting enzyme inhibitors (ACEi) as an antihypertensive agent can cause side effects such as dry cough. This study aimed to evaluate the risk of ACEi administration with captopril as the standard against another ACEi on dry cough incidence in hypertensive patients from various tribes at RSUD Cengkareng West Jakarta and RSUD Tarakan Central Jakarta. The design of this study is prospective cohort. The inclusion criteria were patients who received ACEi as hypertension therapy for ≤ 3 months gathered from outpatient polyclinics and those willing to participate as sample in this study at RSUD Cengkareng West Jakarta and RSUD Tarakan Central Jakarta. Sample consist of 54 patients who received captopril and 54 patients received non captopril ACEi, taken by consecutive sampling from January-July 2014. The data was collected using structured interviews and from medical record. Dry cough incidence due to ACEi was evaluated using Naranjo Algorithm and the data was analyzed using Chi Square test. Dry cough incidence was found in 19,44% of sample. No significant relationship of age, gender, tribe, comorbidity, body mass index (BMI), dosage, and duration of use with dry cough incidence due to the use of ACEi. Furthermore there is no difference in risk between the use of captopril group and non captopril ACEi group on dry cough incidence., Use of angiotensin converting enzyme inhibitors (ACEi) as an antihypertensive agent can cause side effects such as dry cough. This study aimed to evaluate the risk of ACEi administration with captopril as the standard against another ACEi on dry cough incidence in hypertensive patients from various tribes at RSUD Cengkareng West Jakarta and RSUD Tarakan Central Jakarta. The design of this study is prospective cohort. The inclusion criteria were patients who received ACEi as hypertension therapy for ≤ 3 months gathered from outpatient polyclinics and those willing to participate as sample in this study at RSUD Cengkareng West Jakarta and RSUD Tarakan Central Jakarta. Sample consist of 54 patients who received captopril and 54 patients received non captopril ACEi, taken by consecutive sampling from January-July 2014. The data was collected using structured interviews and from medical record. Dry cough incidence due to ACEi was evaluated using Naranjo Algorithm and the data was analyzed using Chi Square test. Dry cough incidence was found in 19,44% of sample. No significant relationship of age, gender, tribe, comorbidity, body mass index (BMI), dosage, and duration of use with dry cough incidence due to the use of ACEi. Furthermore there is no difference in risk between the use of captopril group and non captopril ACEi group on dry cough incidence.]

Abstrak :
Hidrogel kitosan termodifikasi interpenetrating polymer network berhasil disintesis yaitu kitosan, kitosan terikat-silang, kitosan-poly N-vinyl-2-pyrrolidone semi-IPN dan kitosan-N-vinyl-2-pyrrolidone full-IPN. Hidrogel kitosan termodifikasi interpenetrating polymer network diloadingkan captopril. Metode loading obat ke dalam matriks hidrogel yaitu in situ and post loading. Konsentrasi obat yang terloading ke dalam matriks hidrogel divariasikan yaitu 12.5 mg; 25 mg; 37.5 mg and 50 mg. Loading obat dengan metode in situ loading dilakukan dengan menambahkan obat sebelum penambahan agen pengikat silang, sedangkan post loading dilakukan dengan mengimersikan hidrogel ke dalam larutan obat. hidrogel yang terloading obat disebut mikrokapsul. Efisiensi enkapsulasi ditentukan dengan mengimeriskan mikrokapsul ke dalam larutan buffer pH 7,4. Hidrogel dikarakterisasi dilakukan dengan penentuan derajat ikat-silang , rasio swelling , spketrofotometer FTIR dan mikroskop stereo. Derajat ikat-silang dari kitosan, kitosan terikat-silang, kitosan-poly N-vinyl-2-pyrrolidone semi-IPN dan kitosan-N-vinyl-2-pyrrolidone full-IPN adalah 51.62 , 54.65 , 70.15 dan 77.23 . rasio swelling dari kitosan, kitosan terikat-silang, kitosan-poly N-vinyl-2-pyrrolidone semi-IPN dan kitosan-N-vinyl-2-pyrrolidone full-IPN adalah 4412.88 , 2118.01 , 1748.65 dan 441,38 selama 1 jam. Konsentrasi optimum loading obat 12.5 mg and 25 mg. Hidrogel terloading obat disebut mikrokapsul. Pelepasan mikrokapsul captopril in situ and post loading selama 12 jam menunjukkan pelepasan lambat. Profil pelepasan obat pada pH 1,2 dari matriks hidrogel kitosan dan kitosan terikat-silang in situ loading secara difusi dan degradasi, sedangkan semi-IPN and full-IPN in situ loading secara difusi, pada pH 7,4 pelepasan obat mikrokapsul in situ loading secara difusi. Profil pelepasan obat dari mikrokaspul post loading pada pH 1,2 dan 7,4 terjadi secara difusi diikuti erosi matriks hidrogel.

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Preparation chitosan interpenetrating polymer network modified hydrogels have been successfuly. It were chitosan, chitosan crosslinked, semi IPN chitosan poly N vinyl 2 pyrrolidone and full IPN chitosan N vinyl 2 pyrrolidone. These hydrogels were loaded by captropil. Captopril was loaded within hydrogel matrix using both in situ and post loading method. Concentration variation of drug loaded were 12.5 mg 25 mg 37.5 mg and 50 mg. At in situ loading, drug was loaded during synthesis of hydrogel before the addition of crosslinking agent, while at post loading method hydrogels were immersed into a drug solution. This hydrogels loaded captopril called microcapsul. Encapsulation efficiency was evaluated in pH 7.4 solution. Hydrogels characterization including crosslinking degree , swelling ratio , FTIR spectrophotometer and stereo microscope. Crosslinking degree of chitosan, chitosan crosslinked, semi IPN and full IPN hydrogels were found to be 51.62 , 54.65 , 70.15 and 77.23 respectively. Swelling ratio of chitosan, chitosan crosslinked, semi IPN and full IPN hydrogels were 4412.88 , 2118.01 , 1748.65 and 441,38 for 1 hour, respectively. The optimum drug concenration was 12.5 mg and 25 mg. Hydrogels loading drug called microcapsule. Release of captopril microcapsules by in situ and post loading shown that slow release for 12 hour. Profile of release drug from chitosan and chitosan crosslinked hydrogels by in situ loading at pH 1,2 through difussion and degradation, while semi IPN and full IPN hydrogels by in situ loading at pH 1,2 through difussion. At pH 7,4 of profile of release drug from microcapsules through difussion. Profile of release drug at pH 1,2 and 7,4 from microcapsules by post loading through difussion followed erotion.

Abstrak :
Using enzymatic sensor to determine the level of captopril is an alternative method that is being widely developed. In research , made in captopril sensor using Screen Printed Electrode (SPE), because of its advantage of being practical and simple. Cu electrodeposition on SPE is being done by potential -0,480 V vs Ag½AgCl with variation of time deposition of 5, 30 and 60 second. This research finds that the optimum deposition time is 60 second by taking into loading amount of 6,92 x 10-6 gr.cm-2. Cu/SPE is then applied to the Flow Injection Analysis (FIA) system. The optimum result of sensor appears in the FIA system with at the flow rate of 0,5 mL/minute and KOH Concentration of 1 M. Cu/SPE Sensor in FIA system has LOD of 6,530 x 10-6 M and sensitivity of 308,80 μA.mM-1.cm-2. Cu/SPE sensor has good repeatability with value linearity of 0,9113 and %RSD of 1,75%. Selectivity test on the captopril to the glucose and lactose may produce better sensor. The application of Cu/SPE sensor has value %recovery of 96,29%.

Abstrak :
ABSTRAK

Salah satu efek samping obat antihipertensi kaptopril adalah batuk kering. Penelitian ini bertujuan untuk mengevaluasi efek samping batuk kering pada pasien rawat jalan yang mendapatkan obat antihipertensi kaptopril di Rumah Sakit Umum Universitas Kristen Indonesia. Metode penelitian yang digunakan adalah deskriptif analitik. Pengambilan data dilakukan secara prospektif dengan menggunakan data sekunder dari resep pasien dan data primer dari wawancara pasien dengan menggunakan kuesioner yang telah diuji validitas dan reliabilitasnya. Pengumpulan data dilakukan dari Maret-Mei 2014 secara total sampling. Penilaian kausalitas reaksi obat yang tidak dikehendaki (ROTD) batuk kering menggunakan algoritma Naranjo. Total pasien yang memenuhi kriteria sebagai subyek penelitian adalah 31 pasien dari jumlah total 128 pasien yang menggunakan obat kaptopril. Sebanyak 7 pasien (22,6%) mengalami efek samping batuk kering. Berdasarkan analisis algoritma Naranjo, 1 dari 7 ROTD yang terjadi dikategorikan pasti (definite) dan 6 kejadian dikategorikan besar kemungkinan (probable). Hasil analisis secara statistik memperlihatkan bahwa usia, jenis kelamin, suku, lama penggunaan obat, dan merek obat kaptopril tidak memiliki hubungan bermakna dengan efek samping batuk kering. Prevalensi efek samping batuk kering pada penelitian ini tergolong tinggi.

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ABSTRACT

One of the side effects of antihypertensive drugs captopril is a dry cough. This study aimed to evaluate the side effects of dry cough in outpatients receiving antihypertensive drugs captopril in RSU UKI. The method used in this study was descriptive analytical. Data was collected prospectively using secondary data from the patient's prescription and primary data from patient interviews using a questionnaire that had been tested for validity and reliability. Data collection was conducted from March to May 2014 by total sampling. The causality evaluation on the adverse drug reaction (ADR) of dry cough using Naranjo algorithm. Total patients who participated in this study were 31 patients from a total of 128 patients using the drug captopril. As much as 7 patients (22.6%) experienced side effect dry cough. Based on Naranjo algorithm analysis, 1 of the 7 ADR which occured was catagorized as definite and six were catagorized as probable. Results of statistical analysis showed that age, sex, ethnicity, duration of medication, and brand of Captopril does not have a significant correlation with the dry cough side effect. The prevalence of dry cough side effects in this study is high.

Abstrak :
Captopril merupakan obat antihipertensi dan digunakan dalam pengobatan gagal jantung kongestif. Captopril memiliki waktu paruh biologis pendek dan bioavailabilitas rendah, sehingga captopril harus diminum berulang kali untuk mendapatkan efek terapi yang diharapkan. Mikrokapsul digunakan sebagai alat bantu penghantar obat yang dapat menutupi kekurangan captopril. Penyalut yang digunakan pembuatan mikrokapsul pada penelitian ini adalah polimer yang biodegradable, polipaduan poli(D-asam laktat) (PDLA) dengan polikaprolakton (PCL) menggunakan variasi komposisi massa yang berbeda untuk mengetahui pengaruhnya terhadap efisiensi enkapsulasi serta persen pelepasan obat, Span 80 sebagai surfaktan dan diklorometana sebagai pelarut serta menggunakan metode penguapan pelarut. Selanjutnya dikarakterisasi menggunakan FTIR PSA, dan mikroskop optik pada mikrokapsul captopril, kemudian dilakukan uji efisiensi, dan uji disolusi. Hasil dari persen padatan mikrokapsul berkisar antara 98,52% ±0,95 sampai 97,51% ±0,95. Hasil dari pengukuran PSA didapatkan rata-rata ukuran terbesar dan terkecil berturut-turut adalah  0,546 µm ±0,242 mikrokapsul dengan komposisi polimer PDLA:PCL 40:60 (b/b%), dan 0,446 µm ±0,123 pada mikrokapsul PDLA:PCL 10:90 (b/b%). Hasil dari mikroskop optik terlihat bahwa bentuk dari mikrokapsul berbentuk bulat, dan permukaannya terdapat satu lubang. Efisiensi enkapsulasi yang didapatkan yaitu berkisar antara 17,21% ±4,37 hingga 35,62% ±0,47. Pada uji disolusi, mikrokapsul dapat menahan obat di dalam penyalut dan melepasnya secara perlahan, dengan persen pelepasan tertinggi pada mikrokapsul PDLA:PCL 10:90 (b/b%) yaitu sebesar 97,02% dan paling rendah terdapat pada mikrokapsul PDLA:PCL 40:60 (b/b%) sebesar 53,19%. ......Captopril is an antihypertensive drug and is used for the treatment of congestive heart failure. Captopril has a short biological half-life and low bioavailability, and thus captopril must be taken repeatedly to get the desired therapeutic effect. Microcapsules are used as a drug delivery system that can cover the lack of captopril. In this research polymer used for making microcapsules is biodegradable polymers such as PDLA and PCL by variating mass composition to determine effect on encapsulation efficiency and percentage drug release, using and using solvent evaporation methods and span 80 as surfactant. on Characterization of captopril microcapsules was carried out using FTIR, PSA, UV-VIS and optical microscope. The yield percent of microcapsules ranged from 98.52%-97.51%. The results of the PSA measurements obtained the largest particle size was 0.546 µm for microcapsule of PDLA/PCL 40:60 (%w/w) and the smallest size was 0.446 µm for microcapsule of PDLA:PCL 10:90 (w/w%). The results of the optical microscope showed that the microcapsules had spherical shape, and the surface has hole. The efficiency encapsulation obtained was ranged between 17.21% ±4.37 to 35.62% ±0.47. In dissolution tests, microcapsules could withstand the drug release. The highest percentage drug release was 97.02% for microcapsule of PDLA:PCL 10:90 (w/w%) and the lowest percentage drug release was 53.19% for microcapsule of PDLA:PCL 40:60 (w/w%).

Abstrak :

Pendahuluan: Tujuan dari penelitian ini adalah untuk mempelajari hasil kombinasi pada terapi hipertensi antara terapi konvensional dan terapi herbal, masing-masing antara captopril dan Apium graveolens. Tren tekanan darah dan status oksidatif malondialdehyde dan katalase pada jaringan jantung diamati. Metode: Penelitian ini merupakan studi lanjutan dari penelitian sebelumnya tentang farmakokinetik dan farmakodinamik terapi kombinasi captopril dan Apium graveolens. Data diperoleh dengan menggunakan jaringan jantung tikus Sprague-Dawley yang telah diberikan NaCl 4% secara oral sekali sehari selama 46 hari. Data dibagi menjadi lima kelompok dengan dua kelompok kontrol; kelompok normal dan kelompok negatif dan tiga kelompok perlakuan; Kelompok perlakuan kaptopril 1,25 mg, kaptopril 1,25 mg dengan ekstrak seledri, dan captopril 2,5 mg dengan ekstrak seledri. Pengukuran tingkat katalase dan malondialdehid diamati menggunakan nilai absorbansi dan uji asam thiobarbituric (TBA) pada nilai protein melalui standar Bovine Serum Albumin. Ini dihitung dengan Paket Statistik untuk Ilmu Sosial (SPSS). Hasil: Kecenderungan perubahan tekanan darah yang diamati pada hari ke-46 menunjukkan hasil serupa pada hari terakhir antara terapi kombinasi dan terapi kaptopril pada hipertensi. Pada pengukuran malondialdehid dan katalase, tidak ada perbedaan yang signifikan dalam terapi kombinasi dan terapi konvensional pada tingkat stres oksidatif. Kesimpulan: Tidak ada pengurangan yang cukup pada tingkat katalase dan malondialdehid pada jaringan jantung antara semua kelompok yang diamati. Dengan demikian terapi kombinasi relatif aman pada jaringan jantung tikus dalam penelitian ini dan memiliki hasil yang serupa pada hasil akhir tren penurunan tekanan darah.

 

Kata Kunci:

Hypertension, Rat’s Heart, Apium graveolens, Captopril, Catalase, Malondialdehyde

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Introduction: The aim of this research is to study the combination outcome on hypertension therapy between conventional therapy and herbal therapy, respectively between captopril and Apium graveolens. Blood pressure trend and the oxidative level status  of malondialdehyde and catalase on cardiac’s tissue is being observed. Method: The study is a continuation study from previous research on pharmacokinetic and pharmacodynamic of captopril and Apium graveolens combination therapy.  The data obtain using Sprague-Dawley rat’s cardiac tissue that has been given NaCl 4 %  orally once daily for 46th days. The data is divided into five groups with two control group; normal group and negative group and three treatment group; captopril 1,25mg treatment group, captopril 1,25mg with celery extract, and captopril 2,5mg with celery extract. Catalase and malondialdehyde level measurement is observed using the absorbance value and the thiobarbituric acid assay (TBA) on protein value through the bovine serum albumin standard. The is calculated with Statistical Package for the Social Sciences (SPSS). Results: The trend on Blood pressure changes observed in 46th days show similiar outome on the last day between the combination therapy and captopril therapy on hypertension. On malondialdehyde and catalase measurement, is no valueable differences in combination therapy and conventional therapy on oxidative stress level. Conclusion: There is no sufficient reduction on catalase and malondialdehyde level on the cardiac tissue between all group observed. Thus the combination therapy is relatively safe on the rat’s cardiac tissue in this research and has similiar outcome on blood pressure decrement trend.

 

Abstrak :
Dalam penelitian ini, dilakukan pembuatan mikrokapsul sebagai sistem penghantar obat terkontrol dari captopril yang tersalut oleh polipaduan poli(D-asam laktat) dan polikaprolakton dengan menggunakan surfaktan campuran Tween 80-Span 80 melalui metode penguapan pelarut. Berdasarkan optimasi yang dilakukan, didapatkan konsentrasi optimum surfaktan campuran berada pada konsentrasi 0,0741 M yang menghasilkan persen efisiensi enkapsulasi sebesar 28,245% dengan ukuran mikrokapsul sebesar 0,482 µm. Setelah didapatkan konsentrasi optimum dari surfaktan, dilakukan optimasi perbandingan komposisi polipaduan (PDLA:PCL). Komposisi optimum untuk menghasilkan persen enkapsulasi yang terbaik berada pada komposisi 2:8 (% b/b) dengan persen efisiensi enkapsulasi sebesar 24,0983%. Uji disolusi dilakukan pada masing-masing komposisi dan diperoleh pelepasan obat terbaik pada perbandingan komposisi 4:6 (% b/b) dengan persen pelepasan sebesar 100%. Hasil karakterisasi FTIR menunjukan bahwa interaksi yang terjadi baik antara polimer dengan polimer, maupun polimer dengan obat adalah interaksi fisika berupa ikatan hidrogen, gaya dipol-dipol, dan gaya Van Der Waals.

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In this study, captopril drug delivery system was made from microcapsules coated by poly (D-lactic acid) and polycaprolactone using a mixture of Tween 80 and Span 80 surfactants through solvent evaporation method. Based on the optimization result, the optimum mixture surfactant concentration was 0.0741 M, resulting in a percent encapsulation efficiency of 28.245% with a microcapsule size of 0.482 µm. After obtaining the optimum surfactant concentration, optimization of the ratio of polyblend composition (PDLA: PCL) was carried out. The optimum composition that obtained to produce the best percent encapsulation was 24.0983% with a composition ratio of 2:8 (% w/w). Dissolution test was carried out for each composition and the best release at composition ratio of 4: 6 (% w/w) with 100% release percentage. The results of FTIR characterization shows that the interactions that occur between polymers and polymers, and polymers with drugs are physical interactions such as hydrogen bonds, dipole-dipole forces, and Van Der Waals forces.

Abstrak :
Kaptopril merupakan obat golongan angiotensin-converting enzyme inhibitors (ACEi) yang umum digunakan pada pengobatan hipertensi. Kaptopril dapat diformulasikan menjadi sediaan transdermal untuk mengatasi permasalahan bioavailabilitas dan meningkatkan kepatuhan pasien pada sediaan oral. Kaptopril memiliki log P = 0,34 yang menyebabkannya bersifat terlalu hidrofilik sehingga diperlukan upaya untuk mengatasinya dengan microneedles. Tujuan penelitian ini adalah memformulasikan kaptopril menjadi sediaan dissolving microneedles (DMNs) menggunakan polimer kombinasi poli(vinil alkohol) (PVA) dan poli(vinil pirolidon) (PVP) K-29/32 dan mengevaluasinya. Terdapat sembilan formula dengan konsentrasi polimer yang berbeda-beda. Evaluasi yang dilakukan meliputi evaluasi mikroskopis optik, penetapan kehilangan massa selama proses pengeringan, sifat mekanis, simulasi insersi ke dalam kulit, pelarutan secara ex vivo, penetapan kadar menggunakan kromatografi cair kinerja tinggi, dan uji permeasi in vitro menggunakan sel difusi Franz dengan membran uji berupa kulit tikus betina galur Sprague-Dawley. Berdasarkan hasil evaluasi, seluruh formula memiliki jarum lancip berbentuk piramida dengan tinggi yang optimal (~600 µm.); memiliki persentase penurunan tinggi jarum <10%; dan mampu menembus lapisan parafilm ke-3 sedalam 375 µm. Berdasarkan uji pelarutan ex vivo, jarum pada MN-6 dapat melarut sempurna dalam 9,2 ± 1,4 menit. Dari sembilan formula, MN-6 (PVA 5%˗PVP K-29/32 35%) dan MN-9 (PVA 7,5%˗PVP K-29/32 35%) dipilih sebagai formula optimal yang memenuhi karakteristik ideal sediaan DMNs. Berdasarkan hasil uji permeasi in vitro, diperoleh jumlah kumulatif kaptopril yang terpermeasi ke kompartemen reseptor setelah 24 jam untuk MN-6 dan MN-9 secara berturut-turut adalah 7,49±0,17 mg dan 7,20±0,25 mg (p > 0,05). Hasil penelitian ini menunjukkan bahwa DMNs berpotensi untuk dijadikan alternatif penghantaran kaptopril secara transdermal. ......Captopril (CAP) is an angiotensin-converting enzyme inhibitor (ACEi) commonly used in hypertension treatment. CAP can be given transdermally to overcome its bioavailability problems and improve patient compliance in oral administration. CAP has log P = 0.34, which causes too hydrophilic; thus, it must be enhanced with microneedles. This study aimed to formulate CAP-loaded dissolving microneedles (DMNs) using a combination polymer of poly(vinyl alcohol) (PVA) and poly(vinyl pyrrolidone) (PVP) K-29/32 and evaluate it. There were nine formulas with different polymer concentrations. The evaluations consist of microscopic evaluation, determination of loss on drying, mechanical strength, penetration into the skin, ex vivo dissolution, determination of theoretical drug content, determination of drug content using high-performance liquid chromatography, and in vitro permeation study using Franz diffusion cells with Sprague-Dawley female rats. Based on the evaluation, all DMNs produced pyramid-shaped needles with optimal height (~600 µm); the percentage of height reduction was <10%; and they could penetrate the 3rd parafilm layer as deep as 375 µm. At the ex vivo dissolution test, MN-6’s needles dissolved completely after 9.2 ± 1.4 minutes. From nine formulas, MN-6 (PVA 5%˗PVP K-29/32 35%) and MN-9 (PVA 7.5%˗PVP K-29/32 35%) were selected as optimal formulas. Based on the in vitro permeation study, the cumulative amounts of CAP permeated into the receptor compartment after 24 hours for MN-6 and MN-9 were 7.49±0.17 mg dan 7.20±0.25 mg, respectively (p > 0.05). The results of this study indicate that transdermal delivery systems, such as DMNs, may serve as a promising system for CAP.

Abstrak :
Captopril adalah obat antihipertensi dan digunakan dalam pengobatan gagal jantung kongestif. Kaptopril memiliki waktu paruh biologis yang pendek dan bioavailabilitas yang rendah, sehingga kaptopril harus diminum berulang kali untuk mencapai efek terapeutik yang diinginkan. Mikrokapsul digunakan sebagai alat bantu penghantaran obat yang dapat menutupi kekurangan kaptopril. Pelapis yang digunakan dalam pembuatan mikrokapsul pada penelitian ini adalah polimer biodegradable, polialloy poli(D-asam laktat) (PDLA) dengan polikaprolakton (PCL) menggunakan variasi komposisi massa yang berbeda untuk mengetahui pengaruhnya terhadap efisiensi enkapsulasi dan persen pelepasan obat, Span 80 sebagai surfaktan dan diklorometana sebagai pelarut dan menggunakan metode penguapan pelarut. Selanjutnya dikarakterisasi menggunakan FTIR PSA, dan mikroskop optik pada mikrokapsul kaptopril, kemudian dilakukan uji efisiensi, dan uji disolusi. Rendemen persen padatan mikrokapsul berkisar antara 98,52% ±0,95 sampai 97,51% ±0,95. Hasil pengukuran PSA menunjukkan bahwa ukuran rata-rata terbesar dan terkecil adalah mikrokapsul 0,546 m ± 0,242 dengan komposisi polimer PDLA: PCL 40:60 (b/b%), dan 0,446 m ± 0,123 pada mikrokapsul PDLA: PCL 10:90. (b/b%). Hasil mikroskop optik menunjukkan bahwa bentuk mikrokapsul berbentuk bulat, dan permukaannya memiliki satu lubang. Efisiensi enkapsulasi yang diperoleh berkisar antara 17,21% ±4,37 hingga 35,62% ±0,47. Pada uji disolusi, mikrokapsul dapat menahan obat dalam pelapis dan melepaskannya secara perlahan, dengan persen pelepasan tertinggi pada mikrokapsul PDLA: PCL 10:90 (b/w%) yaitu 97,02% dan terendah pada PDLA: PCL 40 mikrokapsul. :60 (b/b%) sebesar 53,19%.

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Captopril is an antihypertensive drug and is used in the treatment of congestive heart failure. Captopril has a short biological half-life and low bioavailability, so captopril must be taken repeatedly to achieve the desired therapeutic effect. Microcapsules are used as drug delivery aids that can cover the lack of captopril. The coating used in the manufacture of microcapsules in this study was a biodegradable polymer, polyalloy poly(D-lactic acid) (PDLA) with polycaprolactone (PCL) using different mass composition variations to determine its effect on encapsulation efficiency and percent drug release, Span 80 as a surfactant. and dichloromethane as solvent and using solvent evaporation method. Furthermore, it was characterized using FTIR PSA, and optical microscopy on captopril microcapsules, then performed efficiency tests, and dissolution tests. The percent yield of microcapsule solids ranged from 98.52% ±0.95 to 97.51% ±0.95. PSA measurement results showed that the largest and smallest average sizes were 0.546 m ± 0.242 microcapsules with PDLA polymer composition: PCL 40:60 (w/w%), and 0.446 m ± 0.123 in PDLA: PCL 10:90 microcapsules. (w/w%). The results of the optical microscope showed that the shape of the microcapsules was spherical, and the surface had one hole. The encapsulation efficiency obtained ranged from 17.21% ±4.37 to 35.62% ±0.47. In the dissolution test, the microcapsules were able to hold the drug in the coating and release it slowly, with the highest percent release in PDLA microcapsules: PCL 10:90 (w/w%) ie 97.02% and the lowest in PDLA: PCL 40 microcapsules. :60 (w/w%) by 53.19%.