Freeze drying and calcining hydrotalcite for improving acid neutralizing capacity

Acid  neutralizing  capacity  (ANC)  is  one  of  the  important  factor  on effectivity  determination  of  antacid  dosage  forms.  Antacid dosage forms have different values depend on their ANC.  The objective of this research was to modified physical and chemical properties of hydrotalcite which can increase its acid neutralization capacity.  Hydrotalcite was treated by freeze drying and calcination at different temperature 100, 200, 300, and 500°C. This hydrotalcite was characterized by X-Ray Diffractometer  (XRD)  and  Scanning  Electron Microscope (SEM); and was determined acid neutralization capacity. The results showed  that  acid  neutralization  capacity  of  hydrotalcite  increased  after  it  was freeze  dried and  calcined  at  200,  300  and  500  °C.  The  result  of  XRD  for  the hydrotalcite  calcined  at  200  °C  have  showed  the  lower  intensity  of  peaks, whereas the calcination at 300 and 500 °C were disappeared and appeared new peaks at different 2θ.Key words: Acid neutralization capacity, hydrotalcite, calcination, XRD, SE

PENGARUH PENGGILINGAN TERHADAP KARAKTERISTIK PADATAN DIDANOSIN

PENGARUH PENGGILINGAN TERHADAP KARAKTERISTIK PADATAN DIDANOSIN. Pemberian energi mekanik pada suatu padatan kristal dapat menyebabkan kerusakan kristal sehingga akan mempengaruhi sifat fisikokimia padatan tersebut. Tujuan penelitian ini adalah untuk mempelajari pengaruh penggilingan terhadap karakteristik padatan didanosin (2',3'-dideoxyinosine atau DDI). Pengilingan padatan DDI dilakukan dengan menggunakan alat Retsch RM 100 mortar grinder selama 15 menit dan 30 menit. Karakterisasi padatan hasil penggilingan dilakukan dengan menggunakan difraksi sinar-X serbuk, Differential Scanning Calorimeter (DSC), Scanning Electron Microscope (SEM) dan Fourier Transform-Infra Red (FT-IR). Indeks kristalinitas relatif DDI hasil penggilingan ditentukan dengan metode difraksi sinar-X serbuk. Uji kelarutan dilakukan dalampelarut air untuk melihat perubahan sifat fisikokimia akibat penggilingan. Difraktogram DDI memiliki beberapa puncak utama dengan intensitas tertinggi ditunjukkan pada sudut 2θ = 6,0º, untuk menghitung indeks kristalinitas relatif. Penggilingan terhadap DDI tidak mengubah letak sudut 2θ, namun menurunkan intensitas puncak dengan indek kristalinitas relatif 40,8 % dan 30,4 %. Termogram DSC DDI menunjukkan ada 2 puncak endotermik yaitu pada suhu 179,5 ºC yang merupakan titik lebur DDI dan 285,0 ºC serta satu puncak eksotermik pada suhu 183 ºC. Titik lebur DDI mengalami sedikit pergeseran menjadi 180,2 ºC setelah digiling selama15 menit dan 176,9 ºC setelah digiling 30 menit. Fotomikrograf SEM menunjukkan terjadi pengecilan ukuran DDI setelah mengalami penggilingan. Spektrum FT-IR menunjukkan tidak adanya pergeseran bilangan gelombang dari gugus-gugus pada DDI setelah mengalami penggilingan. Kelarutan DDI meningkat setelah mengalami penggilingan selama 15 menit dan 30 menit yaitu dari 24,83 ± 0,73 menjadi 30,25 ± 0,18 mg/mL dan 33,76 ± 0,33 mg/mL. Penggilingan ini disamping meningkatkan luas permukaan, juga menyebabkan sebagian kristal berubah menjadi amorf, sehingga kelarutan DDI dalamair meningkat

Pengamatan Visual Tahap-Tahap Pembentukan Kristal Sistem Eutektikum Asetaminofen-Pseudoefedrin Hidroklorida

The aim of this research was to observe the recrystallization process of two component,acetaminophen-pseudoephedrine hydrochloride in ethanol and the thermal profiles.The visual data resulted from polarization microscope observation confirmed withthermograph DSC showed that the crystal habit was represented to the intrinsic characterrepresentative by thermodynamic properties of the binary system.The visualizationprocess proved that in different molar ratios, the binary system formed crystalshabit with different and step by step showed inhibit, to form polycrystalline until atmolar ratio 6:4 formed the fines single crystals mixture which was smaller than beforeco-recrystallization. Acetaminophen was observed as monoclinic hexagonal crystalswhile pseudoephedrine hydrochloride was observed monoclinic/orthorombic forms.Keywords: acetaminophen, crystals habit, ethanol, pseudoephedrine HCl

Pengaruh Disintegran dan Cara Pencampuran Terhadap Sifat Fisika Kimia Telmisartan

Telmisartan (TMS) has a compact structure and is interlocked between crystal units. As a result, the substance has a high electrostatic force, which causes TMS to sintering when compressed into tablets. One method of overcoming sintering on TMS tablets is to add a disintegrant to the compressed tablet. The disintegrants used are derived from starch groups: Starch 1500® (S1500) and sodium starch glycolate (SSG), as well as microcrystalline cellulose (MCC) and croscarmellose sodium (CCS) groups. The purpose of this study was to examine the effects of several disintegrants on the dissolution and physicochemical properties of TMS with various treatments. TMS was varied with each disintegrant at a ratio of 1:9 % b/b. The treatment of TMS binary mixtures with various disintegrants includes physical mixtures, milled mixtures, compressed mixtures, and crushed compressed mixtures. Characterization and evaluation include PXRD and SEM testing as well as dissolution test. The characterization of PXRD and SEM in various treatments showed the effect of physicochemical properties on the TMS binary mixture with various disintegrants. The combination of TMS:CCS with a ratio of (1:9) resulted in the highest dissolution rate in all treatments.The treatment of the milled mixture produced the highest dissolution with DP60 minutes, which was around 55.86±2.47%. The addition of disintegrants to TMS with various treatments may reduce sintering but is not sufficient to meet the requirements for TMS dissolution, which dissolves within 30 minutes in phosphate buffer medium pH 7.5 with Q>75%.Telmisartan (TMS) mempunyai struktur yang padat dan saling mengunci antar unit kristal.Hal ini mengakibatkan zat mempunyai gaya elektrostatik tinggi sehingga ketika dikompresi menjaditablet, TMS mengalami sintering. Salah satu upaya untuk mengatasi sintering pada tablet TMSadalah dengan menambahkan disintegran. Disintegran yang digunakan adalah berasal dari golonganpati: Starch 1500® (S1500) dan sodium starch glikolat (SSG) serta golongan selulosa mikrokristalinselulosa (MCC) dan croscarmellose sodium (CCS). Tujuan penelitian ini adalah melihat pengaruhbeberapa disintegran terhadap sifat fi sikokimia TMS dengan berbagai perlakuan. TMS divariasikandengan masing-masing disintegran dengan perbandingan 1:9% b/b. Perlakuan terhadap campuranbiner TMS dengan berbagai disintegran meliputi campuran fi sik, campuran digiling, campuran yangdikompresi dan campuran dikompresi yang dihancurkan. Karakterisasi dan evaluasi meliputi pengujianPXRD, SEM dan uji disolusi. Karakterisasi PXRD dan SEM pada berbagai perlakuan menunjukkanadanya pengaruh sifat fi sikokimia terhadap campuran biner TMS dengan berbagai macam disintegran.Kombinasi TMS:CCS dengan perbandingan (1:9) menghasilkan laju disolusi tertinggi pada semuaperlakuan Perlakuan campuran yang digiling memberikan disolusi tertinggi dengan DP60 menit yaitusekitar 55,86±2,47%. Penambahan disintegran pada TMS dengan berbagai perlakuan dapat mengurangisintering tetapi masih belum cukup untuk memenuhi persyaratan disolusi TMS yaitu dalam waktu 30menit terdisolusi dalam media dapar fosfat pH 7,5 dengan Q>75%

Optimasi Formula Emulgel Vitamin C dengan Pendekatan Simplex Lattice Design

Vitamin C dalam bidang kosmetik memiliki banyak manfaat termasuk sebagai antioksidan. Akan tetapi sediaan vitamin C mudah teroksidasi dan mengalami perubahan warna sehingga perlu ditambahkan penstabil yang mampu menjaga kestabilan vitamin C selama pemakaian dan penyimpanan. Penelitian ini bertujuan untuk mengetahui pengaruh hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer  dan natrium metabisulfit  terhadap karaktiristik emulgel vitamin C serta menentukan formula emulgel yang optimum melalui pendekatan Design of Experiment (DOE) dengan metode  Simplex Lattice Design. Hasil penelitian menunjukkan bahwa variabel konsentrasi hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer  dan natrium metabisulfit  memberikan pengaruh yang signifikan terhadap viskositas (P0,05). Formulasi optimum dihasilkan dengan penambahan adalah 2,305% hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer  dan 0,194 % natrium metabisulfit  dengan nilai desirability 0,633. Formula ini  memenuhi kriteria sediaan yang cukup baik, namun perlu dilakukan perbaikan aroma untuk meningkatkan penilaian kesukaan

Polimorfisasi dan Solvatomorfi Amoksisilina Trihidrat setelah Proses beku Kering

The polymorphismof amoxicillin has been identified after freeze drying process. Thefreeze dried amoxicillin have some specific physical properties different from their rawmaterial, that was proved by DSC, XRD, and polarize microscope. Exothermal curvefrom DSC thermogram changes to endothermal curve, diffractogram XRD changes todifferent profile, and the crystal shows different habit. All of data showed that freezedrying process improve amoxicillin to different crystal form which has higher meltingoxidation point and lower hydrate. The improvement of the crystal structure mightbe impact to change physical-pharmaceutical properties like dissolution, absorption,and change it antibiotic potency.Keywords: amoxicillin trihydrate, freeze drying, polymorphism

Preparation and Solid State Characterization of Binary Mixtures of Acyclovir – Succinic Acid

Physical interaction of acyclovir – succinic acid (AS) was studied. The aim of this study is to prepare and characterize binary mixture of AS. Methods of cocrystallization was solvent evaporation in equimolar ratio between acyclovir and succinic acid using ethanol and methanol. The cocrystals were characterized by Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), and Fourier Transform Infra Red (FTIR) spectroscopy. Physical characterization showed a new endothermic peak at 175.36 o C according to DSC analysis. The PXRD patterns of AS binary mixture after cocrystallization are different from pure components. Furthermore, specific peaks was found at 2θ = 24,77 o , 35,88 o and 37,99 o (AS in ethanol); 19,99 o and 21,01 o (AS in methanol). In addition, there are a shift in the O-H, N-H and C=O spectrum of FTIR

Solid State Characterization of Acyclovir-Nicotinamide Binary Systemsusing Solvent Evaporation Technique

Objective of the study is to characterize acyclovir-nicotinamide binary systems (AN). Methods ofcocrystallization wassolvent evaporation in equimolar ratio between acyclovir and nicotinamide using ethanoland methanol. The binary systems were characterized by polarization microscope, Differential ScanningCalorimetry (DSC) and Powder X-Ray Diffraction (PXRD). Physical characterization showed that AN binarysystems have unique crystal habit in microscopic. A new endothermic peak appears at 123.69 C. The PXRDpatterns of AN binary systems after cocrystallization are different from pure components which specific peakwasfound on 2θ = 11.27 o (AN in ethanol); 21.05 o (AN in methanol)

SIMULTANEOUS COCRYSTALLIZATION AND MICRONIZATION OF PARACETAMOL-DIPICOLINIC ACID COCRYSTAL BY SUPERCRITICAL ANTISOLVENT (SAS)

Objective: This present study aims to produce cocrystal of paracetamol (PCA)-dipicolinic acid (DPA) using supercritical antisolvent (SAS) cocrystallization process in order to improve tabletability profile of PCA.Methods: The PCA-DPA cocrystal prepared by SAS cocrystallization were compared to those produced using a traditional solvent evaporation. The cocrystals produced were characterized using Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Polarized Light Microscopy (PLM), Fourier Transform Infrared (FTIR) spectroscopy, particle size analysis, Scanning Electron Microscopy (SEM) and High Performance Liquid Chromatography (HPLC). Analysis of flowability, drug content, solubility, dissolution, stability and powder compaction were performed to evaluate the cocrystals.Results: Cocrystal particles with mean diameter of 4.18 µm were produced from SAS process, smaller than those produced by traditional solvent evaporation method (mean diameter of 64.93 μm). The PCA-DPA cocrystal from SAS process showed an enhanced dissolution rate by 2.45 times compared to PCA, higher than cocrystal from traditional solvent evaporation (enhanced dissolution rate by 1.72 times compared to PCA). Tabletability study revealed superior tableting performance of both cocrystals compared to PCA.Conclusion: This study showed the utility of PCA-DPA cocrystal to improve mechanical properties of PCA while also demonstrating that simultaneous micronization and cocrystallization process can be obtained using SAS process.Â