Improvement of Dissolution Properties Through Acyclovir - Succinic Acid Cocrystal Using Solvent Evaporation Technique

The objective of this research was to prepared acyclovir cocrystals with succinic acid as coformer using three different solvents (ethanol, acetic acid glacial, and 0.1N HCl) to influence the characters and improve the dissolution rate of acyclovir. Cocrystallization of acyclovir with succinic acid as coformer was successfully prepared by solvent evaporation technique using three different solvents (ethanol, acetic acid glacial, and 0.1N HCl). The screening indicated that acyclovir formed novel cocrystals with succinic acid in the three different solvents. PXRD profile show that there is three peaks in ethanol cocrystal in angle 2θ 5.9134o ; 9.1645o and 13.4044o . For acetic acid glacial and 0.1N HCl cocrystal there is one peak in angle 2θ 5.9263o and 2θ 9.6011o . In analysis diffractogram DSC formed ethanol cocrystal with melting point 175.84oC. The melting point of acetic acid glacial cocrystal is 178.41oC and 0.1N HCl cocrystal is 156.75oC. The dissolution rate of the cocrystals measured by the effisiency disolution (ED45) that considerable faster than that pure acyclovir and the physical mixtures. On the result of FTIR analysis there is changes of the wavenumber that indicated that there is cocrystal formed. And for SEM analysis, morphology of cocrystals was different than the original materials. In dissolution test, ethanol and acetic acid glacial cocrystals have better efficiency dissolution (ED45) (92.96 %) than the acyclovir ED45 (84.48 %). But 0.1N HCl cocrystal has lower ED45 than acyclovir that is 48.19 %. The results obtained in this research indicated the acyclovir cocrystals have formed with succinic acid as coformer using three different solvents. The physical properties was different from the three cocrystals. Dissolution rate of acyclovir cocrystals using ethanol and acetic acid glacial solvents was increase, whereas using 0.1N HCl was decrease rather than pure acyclovir

Determination Of Curcumin In Capsule Containing Curcuma xanthorrhiza Roxb. Extracts By High Performance Liquid Chromatography

Curcumin, the major yellow pigment of Curcuma sp. has several interesting biological activities, such as anticarcinogenecity, antiinflamatory, and antioxidant. Curcumin naturally occurs as major compound in Curcuminoid substance beside its derivatives, i.e. Bisdemethoxycurcumin (BDC) and Demethoxycurcumin (DC). Quantitative analysis of Curcumin is difficult to carry out unless prior to completely resolved Curcumin from BDC and DC. A good resolution, reproducible, and accurate method for determination Curcumin in pharmaceutical product (capsule formed) by HPLC has been carry out. Using C18 colurnn and mixture of Acetonitrile: Acetic Acid glacial 1% (45:55 v/v) as eluent, BDC, DC, and Curcumin were retained with retention time of 10.79, 12.29, and 13.91 minutes, respectively. Curcumin was simultaneously separated from BDC or DC. The resolution factor (Rs) between Curcumin and DC was 1.73. Good linear relationship (r = 0.9997, Vxo = 0.99%) between peak area and concentrations was found at range of the Curcumin concentration used, i.e. 23.56-62.83 µg/mL. Curcumin recoveries were (93.60-118.17)% with the coefficient of variation (CV) 6.99%. Curcumin content in each capsule sample was found to be (8.89±0.06) mg. It showed that samples contained higher amount of Curcumin than that claimed on its label, 5 mg.

SYNTHESIS AND CONFORMATION OF p-(AMINO)BUTOXYCALIX[4]ARENE

Derivatization of 5,11,17,23-tetra-t-butyl-25,26,27,28-tetrahydroxycalix[4]-arene to 5,11,17,23-tetra-amino-25,26,27,28-tetrabutoxycalix[4]arene compound via etherification, ipso nitration, and reduction reactions, respectively has been conducted. The etherification reaction was carried out by refluxed the mixture of 5,11,17,23-tetra-t-butyl-25,26,27,28-tetrahydroxy-calix[4]arene, 1-bromobutane, NaI, and NaH in solvent mixture of THF-DMF (10:1 v/v) and nitrogen atmosphere for 4 hours to resulted 5,11,17,23-tetra-t-butyl-25,26,27,28-tetrabutoxycalix[4]-arene 84% in yield; ipso nitration reaction was carried out by stirred the mixture of 5,11,17,23-tetra-t-butyl-25,26,27,28-tetrabutoxycalix[4]arene and HNO3 100% in solvent mixture of dichloromethane-acetic acid glacial (1:1 v/v) for 2 hours and than refluxed for 1 hour to resulted 5,11,17,23-tetra-nitro-25,26,27,28-tetra-butoxycalix[4]arene 50% in yield; and reduction reaction was carried out by refluxed the mixture of 5,11,17,23-tetra-nitro-25,26,27,28-tetrabutoxycalix[4]arene and SnCl2/HCl reductor in ethanol solvent for 6 hours to resulted 5,11,17,23-tetra-amino-25,26,27,28-tetrabutoxycalix[4]arene 67% in yield. In the etherification reaction, the conformation of calix[4]arene compound was converted from cone to partial cone; but in the followed reactions, i.e. nitration and reduction reactions, the conformation of calix[4]arene compounds were remain in partial cone. Keywords: aminobutoxycalixarene, conformation, etherification, ipso nitration, reduction