SYSTEMATIC REVIEW: COCRYSTAL AS EFFORTS TO IMPROVE PHYSICOCHEMICAL AND BIOAVAILABILITY PROPERTIES OF ORAL SOLID DOSAGE FORM

Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability

Detection of Enteropathogenic Bacteria under Fingernails of Canteen Workers at Universitas Padjadjaran, Jatinangor

Background: Food poisoning is a major problem in Indonesia as most people do not clean under their fingernails to remove bacteria. This study was designed to detect enteropathogenic bacteria under the fingernails of canteen workers in Universitas Padjadjaran, Jatinangor.Methods: A cross-sectional study was conducted from October−November 2014 at the Faculty of Medicine’s Microbiology Laboratory to detect enteropathogenic bacteria under the fingernails of canteen workers in Universitas Padjadjaran, Jatinangor. Based on the inclusion and exclusion criteria of the study, 30 canteen workers were selected by random sampling from three canteens. Samples were collected from the fingernails of both the right and left hands by using a cotton swab. Sixty specimens were cultured for identification of the enteropathogenic bacteria by using gram staining method and biochemical tests.Results: The highest percentage of enteropathogenic bacteria found under the fingernails of canteen workers was Klebsiella pneumoniae with a percentage of 45% followed by Enterobacter aerogenes with a percentage of 25.7%, Salmonella paratyphii with a percentage of 9.7%, E. coli with a percentage of 6.4%, and Serratia sp, Proteus mirabillis, Klebsiella oxytoca and Shigella sp. with a percentage of 3.2%.Conclusions: The highest number of bacteria found under the fingernails of the canteen workers is Klebsiella pneumoniae, followed by Enterobacter aerogenes, Salmonella paratyphii and E. coli which has potential to cause gastroenteritis if cross-contamination occurs between the fingernails and the food.[AMJ.2016;3(2):309–13]DOI: 10.15850/amj.v3n2.798

Formulasi Lotion Ekstrak Buah Raspberry(rubus Rosifolius) Dengan Variasi Konsentrasi Trietanolamin Sebagai Emulgator Serta Uji Hedonik Terhadap Lotion

Raspberry (Rubus rosifolius) memiliki aktivitas antioksidan tinggi yang dapat digunakan dalam perawatan kulit. Salah satu kosmetika untuk perawatan kulit adalah lotion, yang merupakan emulsi cair terdiri dari fase minyak dan fase air yang distabilkan oleh emulgator serta dapat melindungi dan menjaga kelembaban kulit. Tujuan penelitian adalah untuk formulasi sediaan lotion dan menguji sifat fisiko lotion serta uji hedonik berkaitan dengan kepuasan dan Kenyamanan responden terhadap sediaan lotion yang telah diformulasi. Formulasi yang digunakan menggunakan bahan-bahan sebagai berikut, fase minyak (lanolin), fase air (aquadest), stiffening agent (setil alkohol, asam stearat), emulgator (trietanolamin), humektan (gliserin), pengawet (metil paraben, propil paraben) dan pemberi aroma (Lavender essential oil). Penelitian menggunakan 3 formulasi lotion dengan konsentrasi ekstrak Raspberry (zat aktif) sebanyak 3% dengan variasi Trietanolamin (TEA), yaitu 2,5%, 3%, dan 3,5% pada formulasi I, II, dan III. Sediaan lotion kemudian diuji sifat fisiknya, yang meliputi uji organoleptis, uji pH, uji daya lekat, uji daya sebar, dan uji viskositas. Kemudian dilakukan uji hedonik 3 formulasi lotion terhadap 30 responden di kalangan civitas Farmasi Universitas Udayana. Berdasarkan hasil pengujian sifat fisik, ketiga formulasi lotion menunjukkan tekstur kental, warna ungu dengan aroma khas Lavender, memiliki nilai pH pada kisaran 5,9-6,5 sertawaktu lekat pada pengujian 2-3 detik. Penggunaan variasi konsentrasi TEA tidak memberikan pengaruh yang signifikan terhadap sifat fisik 3 formulasi lotion yang berbeda. Pada uji hedonik, formulasi lotion II dengan konsentrasi TEA 3% paling memberikan kepuasan dan Kenyamanan bagi responden. Kepuasan responden berkaitan dengan tekstur, warna, dan aroma terkait penampilan sediaan serta memiliki kekentalan, daya sebar, dan daya lekat yang baik sehingga memberikan rasa nyaman saat diaplikasikan pada kulit

ALGORITMA IMAGE PROCESSING PENDUGAAN LUASAN SERANGAN PENYAKIT TUNGRO PADA PADI MELALUI PENDEKATAN FOTO UDARA

Tungro is one cause of crop failure. The calculation of the extent of the attack is very important to determine how big the attack on a land and to predict the results to be gained. Aerial photographs are one of the technologies that can be used to predict the extent of tungro disease. The development of image processing algorithms should be developed to predict the extent of attacks with aerial photographs.The purpose of this research were to develop an application that can be used to predict the extent of tungro disease on rice. To develop the program of estimate attack area use software Adobe Photoshop CS 6 and Matlab R2013a. This research consists of several steps, namely image acquisition, preprocessing, thresholding, image morphology operation, pixel calculation, calculation of the area of attack.The algorithm of this study were : image acquisition, color normalization, mosaicking, resize, scale calculation, land pixel calculation, pixel attack calculation, calculation of attack area and percentage of attack. T test is performed on data of percentage estimation of attack and manual calculation using planimeter. From the T test results obtained that both data is the same. Based on the above, it can be concluded that the algorithm of image processing estimation to estimate the extent of tungro disease attack is image acquisition, color normalization, mosaicking, resize, scale calculation, land pixel calculation, pixel counting attack and percentage of attack calculation.Tungro merupakan salah satu penyebab kegagalan panen. Pendugaan luasan serangan sangat penting dilakukan untuk mengetahui besarnya serangan yang terjadi dan pendugaan hasil yang akan didapat. Foto udara merupakan salah satu teknologi yang dapat dikembangkan untuk menduga luasan serangan penyakit tungro. Tujuan dari penelitian ini adalah mengembangkan algoritma pendugaan luasan serangan penyakit tungro pada padi melalui pendekatan foto udara. Pengembangan algoritma pendugaan luas serangan menggunakan bantuan software Adobe Photoshop CS 6 dan Matlab R2013a. Penelitian ini terdiri dari beberapa tahapan, yaitu akuisisi citra, preprocessing, thresholding, operasi morfologi citra, perhitungan pixel, perhitungan luas serangan. Algoritma pendugaan luas serangan adalah akuisisi citra, normalisasi warna, mosaicking, resize, perhitungan skala, perhitungan pixel lahan, perhitungan pixel serangan dan perhitungan persentase serangan. Perhitungan pixel lahan menggunakan proses thresholding  dan penjumlahan pixel. Perhitungan pixel serangan menggunakan thresholding otsu, operasi morfologi citra dan penjumlahan pixel. Perhitungan persentase serangan menggunakan perbandingan pixel serangan dengan pixel lahan. Uji T dilakukan terhadap data pendugaan persentase serangan dan perhitungan manual dengan menggunakan bantuan planimeter. Dari uji T didapatkan hasil bahwa kedua data memiliki besar yang sama. Berdasarkan hal tersebut maka dapat disimpulkan bahwa algoritma pendugaan image processing untuk menduga luasan serangan penyakit tungro adalah akuisisi citra, normalisasi warna, mosaicking, resize, perhitungan skala, perhitungan pixel lahan, perhitungan pixel serangan dan perhitungan persentase serangan

Review: Sintesis Senyawa Turunan Andrografolid pada Gugus Hidroksil C-14

Andrografolid merupakan suatu diterpenoid lakton yang terkandung dalam tanaman sambiloto (Andrographis paniculata) sebagai senyawa aktif utama. Andrografolid memiliki banyak aktivitas biologis, diantaranya sebagai antiinflamasi, antikanker, hepatoprotektor, antioksidan, antidiabetes, antihiperlipidemia, antibakteri, dan antivirus. Untuk meningkatkan sifat fisikokimia dan mengoptimalkan aktivitas terapeutik dari andrografolid, diperlukan modifikasi struktur andrografolid. Pada review ini akan dibahas mengenai metode yang dapat dilakukan dalam memodifikasi struktur andrografolid terutama pada gugus hidroksil C-14 dan membandingkan potensi dari aktivitas biologisnya setelah dimodifikasi. Terdapat dua metode modifikasi yaitu dengan cara memproteksi gugus hidroksil C-3 dan C-19 terlebih dahulu untuk menghasilkan senyawa 3,19-isopropiliden andrografolid yang kuat terhadap serangan nukleofil dan cara kedua yaitu langsung mereaksikannya dengan klorida asam dengan bantuan amina tersier seperti trietilamin dan piridin. Dari hasil review didapatkan bahwa modifikasi terhadap gugus hidroksil C-14 dapat meningkatkan potensi aktivitas biologis andrografolid dan metode yang paling baik untuk memodifikasi andrografolid pada gugus hidroksil C-14 yaitu dengan cara memproteksi gugus hidroksil C-3 dan C-19 terlebih dahulu serta mereaksikannya dengan klorida asam atau anhidrida asam agar diperoleh rendemen yang lebih banyak

Elucidation of Molecular Interactions Between Drug–Polymer in Amorphous Solid Dispersion by a Computational Approach Using Molecular Dynamics Simulations

Diah Lia Aulifa,1 Adnan Aly Al Shofwan,2 Sandra Megantara,1 Taufik Muhammad Fakih,3 Arif Budiman2 1Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia; 2Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, Indonesia; 3Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Universitas Islam Bandung, Bandung, IndonesiaCorrespondence: Diah Lia Aulifa, Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Jl. Raya Bandung-Sumedang Km. 21, Sumedang, 45363, Indonesia, Email [email protected]: Amorphous drug dispersion is frequently used to enhance the solubility and dissolution of poorly water-soluble drugs, thereby improving their oral bioavailability. The dispersion of these drugs into polymer matrix can inhibit their recrystallization. The inter-molecular interactions between drug and polymer plays a role in the improvement of the dissolution rate, solubility, and physical stability of drug.Aim: This study aims to investigate the formation and interactions of ritonavir (RTV)/poloxamer (PLX) amorphous formulation using a computational approach via molecular dynamics (MD) simulations, which mimicked solvent evaporation and melt-quenching method.Methods: TheRoot Mean Square Deviation (RMSD) value, Root Mean Square Fluctuation (RMSF), Radial Distribution Function (RDF), Radius of Gyration (Rg), Solvent Accessible Surface Area (SASA), and hydrogen bond interactions were analyzed to determine interaction mechanisms between RTV and PLX in amorphous solid dispersion.Results: The pi-alkyl bonds between RTV and PLX were formed after simulations of solvent evaporation, while the hydrogen bond interactions of RTV-PLX was observed during melt method simulations. These results indicate the successful formulation of amorphous solid dispersion (ASD) from RTV and PLX. The RMSD values obtained from the solvent evaporation, melt-cooling-A, melt-cooling-B, and melt-cooling-C methods were 3.33 Å, 1.97 Å, 1.30 Å, and 1.29 Å, respectively, while the average RMSF values were 2.65 Å, 1.04 Å, 1.05 Å, and 1.07 Å, respectively. This indicates that the suppression of translational motion of RTV from the melt method can be stronger than solvent evaporation caused by the intermolecular interactions of RTV-PLX.Conclusion: MD simulations helped in understanding the formation and interaction mechanisms of ASD formulations that were difficult to detect by experimental approaches.Keywords: amorphous solid dispersion, molecular interaction, molecular dynamics simulations, ritonavir, poloxame

Development and validation of simple simultaneous analysis for amlodipine and glibenclamide by nonderivatization high-performance liquid chromatography-fluorescence

Studies have shown that about 65% of diabetics have hypertension. Treatment for diabetic patients with hypertension is usually given a combination of drugs such as amlodipine (AML) and glibenclamide (GLI). The aim of this study was to develop and validate the simple simultaneous analysis method for separation of AML and GLI using high-performance liquid chromatography (HPLC) with fluorescence detector without derivatization. The arrangement of isocratic and gradient methods, mobile phase compositions, and flow rates to develop and validate the simple simultaneous analysis method for separation of AML and GLI by nonderivatization HPLC fluorescence was done. Optimum condition was obtained using an RP 18 (125 mm × 4 mm, i.d., 5 μm) and guard column RP 18 (4 mm × 4 mm, i.d., 5 μm) with mobile phase composition containing acetonitrile and phosphate buffer pH 3.0 using a 20:80 gradient condition at flow rate 1.0 ml/min measured at 361 nm for λ excitation and 442 nm for λ emission for AML and 235 nm for λ excitation and 354 nm for λ emission for GLI. The analysis of AML and GLI demonstrated a valid result with r2 value 0.999, recoveries were 100.04% and 99.14% relative standard deviations were 0.508% and 0,797%, respectively, detection limits were 0.055 and 0.104 μg/ml, and quantification limits were 0.166 and 0.316 μg/ml, respectively. An accurate method of separation for AML and GLI using HPLC with fluorescence detector without derivatization has been validated

Voice processing for COVID-19 scanning and prognostic indicator

COVID-19 pandemic has posed serious risk of contagion to humans. There is a need to find reliable non-contact tests like vocal correlates of COVID-19 infection. Thirty-six Asian ethnic volunteers 16 (8M & 8F) infected subjects and 20 (10M &10F) non-infected controls participated in this study by vocalizing vowels /a/, /e/, /i/, /o/, /u/. Voice correlates of 16 COVID-19 positive patients were compared during infection and after recovery with 20 non-infected controls. Compared to non-infected controls, significantly higher values of energy intensity for /o/ ( = 0.048); formant F1 for /o/ ( = 0.014); and formant F3 for /u/ ( = 0.032) were observed in male patients, while higher values of Jitter (local, abs) for /o/ ( = 0.021) and Jitter (ppq5) for /a/ ( = 0.014) were observed in female patients. However, formant F2 for /u/ ( = 0.018), mean pitch F0 for /e/, /i/ and /o/ ( = 0.033; 0.036; 0.047) decreased for female patients under infection. Compared to recovered conditions, HNR for /e/ ( = 0.014) was higher in male patients under infection, while Jitter (rap) for /a/ ( = 0.041); Jitter (ppq5) for /a/ ( = 0.032); Shimmer (local, dB) for /i/ ( = 0.024); Shimmer (apq5) for /u/ ( = 0.019); and formant F4 for vowel /o/ ( = 0.022) were higher in female patients under infection. However, HNR for /e/ ( = 0.041); and formant F1 for /o/ ( = 0.002) were lower in female patients compared to their recovered conditions. Obtained results support the hypothesis since changes in voice parameters were observed in the infected patients which can be correlated to a combination of acoustic measures like fundamental frequency, formant characteristics, HNR, and voice perturbations like jitter and shimmer for different vowels. Thus, voice analysis can be used for scanning and prognosis of COVID-19 infection. Based on the findings of this study, a mobile application can be developed to analyze human voice in real-time to detect COVID-19 symptoms for remedial measures and necessary action