Priprava i vrednovanje matriksnog agensa na bazi ispagule za kontrolirano oslobađanje

The 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 hydroxylpropyl methylcellulose was found necessary to improve cohesion. Lactose (X1), calcium hydrogen phosphate diydrate (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 to the in vitro drug 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.Cilj rada bio je priprava i vrednovanje pomoćne tvari za izravnu kompresiju dobivene iz ljuski ispagule, primjenjive u izradi pripravaka metodom aglomeracije. Dodatak hidroksipropil metilceluloze bio je neophodan za povećanje kohezije. U pripravi aglomerata s ispagulom upotrebljeni su laktoza (X1), kalcijev hidrogenfosfat dihidrat (X2) i Avicel PH101 (X3). U eksperimentalnom dizajnu (simplex lattice design) te tri tvari izabrane su kao nezavisne varijable. Proučavan je njihov utjecaj na kompresibilnost i oslobađanje ljekovite tvari iz pripravka dobivenih izravnom kompresijom te svojstva tečnosti aglomerata. Tako dobiveni aglomerati upotrebljeni su za pripravu tableta teško kompresibilne tvari acetaminofena (omjer aglomerata i ljekovite tvari 7:3). Količine oslobođene tvari in vitro pri kraju 60 min (Y60), 300 min (Y300) i 480 min (Y480) bils su zavisne varijable. Iz pripravka IH05 koji sadrži laktozu i kalcijev hidrogenfosfat dihidrat u omjeru 1:2 kontrolirano se oslobađa ljekovita tvar tijekom 12 sati, što je dobar temelj za doziranje dva puta dnevno

PREPARATION, CHARACTERIZATION, AND OPTIMIZATION OF MEBENDAZOLE SPHERICAL AGGLOMERATES USING MODIFIED EVAPORATIVE PRECIPITATION IN AQUEOUS SOLUTION (EPAS)

Objective: Mebendazole is a popular benzimidazole class anthelmintic drug useful in the treatment of main infections of threadworms as well as other less common worm infections like whipworm, roundworm, and hookworm in adults and children over 2 y of age. It is poorly soluble in water resulting in poor absorption from the intestinal tract leading to a decrease in bioavailability. Moreover, Mebendazole has poor flowability due to the needle-shaped crystals. This work was carried out with the aim of increasing the flowability and solubility of Mebendazole. Methods: A 32 full factorial design was used to investigate the effect of the concentration of Mebendazole and the quantity of water as an external phase using evaporative precipitation into an aqueous solution. The prepared agglomerates were characterized for particle size distribution, shape, Hausner ratio, Carr’s index and % dissolved in 60 min (C60).   Results: The prepared agglomerates were found to be monodispersed. They also showed a decrease in the Hausner ration and Carr’s index, indicating improved flowability. Increase in C60 indicated that the agglomerates were found to have increased water solubility. Conclusion: Scanning Electron Microscopy showed that the agglomerates were spherical in shape. Fourier Transformed Infra-Red studies showed no chemical change in the prepared spherical agglomerates. Differential Scanning Calorimetry and X-ray diffraction studies showed an increase in amorphous characteristics of prepared spherical agglomerates. This method may be used for drugs with similar characteristics as Mebendazole

Development and Validation of UV- Spectrophotometric Method for estimation of Vancomycin Hydrochloride

UV-spectrophotometry refers to absorption spectroscopy or reflectance spectroscopy in the ultraviolet-visible spectral region. This method of analysis is gaining importance as it is rapid, simple, precise, less time consuming and highly accurate. The objective of the present investigation was to develop an accurate, rapid and robust method for determination of Vancomycin hydrochloride in pharmaceutical preparations by using UV spectrophotometric method. Vancomycin hydrochloride shows maximum absorbance at a wavelength of 281 nm, which is used for this study. The method provides a linear response from a quantitation range of 20 µg/ml to 100 µg/ml in phosphate buffer pH 6.8 with regression equation y = 0.0038x + 0.0045 and r2 0.9994. Interday precision and accuracy was found to be below 0.2 and above 99.00% respectively for the developed method. Thus the developed method may be suitably applied for regular quality control of Vancomycin hydrochloride in bulk and pharmaceutical preparations. Keywords: Vancomycin hydrochloride, spectroscopic method, validation

Improving the Isotretinoin Photostability by Incorporating in Microemulsion Matrix

The present paper demonstrates the increased photostability of isotretinoin when loaded in microemulsion. The photodegradation of isotretinoin, in methanol and microemulsion formulation was studied under direct sun light. The photodegradation process was monitored by UV spectrophotometry. In methanol solution, isotretinoin undergoes complete photodegradation just within a few minutes of light exposure. Isotretinoin incorporated in microemulsion formulation showed an increased stability in comparison to the methanol solutions. In particular for isotretinoin, a residual concentration of 75% was still present after a light irradiance versus a residual value of just 16% measured at the same time in methanol solution. Further, degradation kinetic parameters of isotretinoin-loaded microemulsion formulation were demonstrated increase isotretinoin half-life about five-times in comparison with a methanol solution under a direct sun light

<span style="font-size:11.0pt;line-height:115%; font-family:"Calibri","sans-serif";mso-ascii-theme-font:minor-latin;mso-fareast-font-family: "Times New Roman";mso-fareast-theme-font:minor-fareast;mso-hansi-theme-font: minor-latin;mso-bidi-font-family:"Times New Roman";mso-ansi-language:EN-US; mso-fareast-language:EN-US;mso-bidi-language:AR-SA">Formulation and <i>in vitro </i>characterization of niosomes containing 5-fluorouracil</span>

192-194<span style="font-size:11.0pt;line-height:115%; font-family:" calibri","sans-serif";mso-ascii-theme-font:minor-latin;mso-fareast-font-family:="" "times="" new="" roman";mso-fareast-theme-font:minor-fareast;mso-hansi-theme-font:="" minor-latin;mso-bidi-font-family:"times="" roman";mso-ansi-language:en-us;="" mso-fareast-language:en-us;mso-bidi-language:ar-sa"="">The present work describes preparation and in vitro characterization of niosomes containing 5fluorouracil (5-FU) using non-ionic surfactant series of sorbitan esters (Spans) by thin film hydration method. Niosomes prepared from Span 40 and Span 60 exhibit higher entrapment of 5-FU as compared to niosomes prepared from Span 80 and Span 85. Cholesterol increases the entrapment of 5-FU into niosomes. Dicetyl phosphate reduces the size of niosomes. The leakage of 5-FU from niosomes reduces on freeze drying.</span

Formulation and optimization of piroxicam proniosomes by 3-factor, 3-level box-behnken design

The aim of this study was to investigate the combined influence of 3 independent variables in the preparation of piroxicam proniosomes by the slurry method. A 3-factor, 3-level Box-Behnken design was used to derive a second-order polynomial equation and construct contour plots to predict responses. The independent variables selected were molar ratio of Span 60:cholesterol (X1), surfactant loading (X2), and amount of drug (X3). Fifteen batches were prepared by the slurry method and evaluated for percentage drug entrapment (PDE) and vesicle size. The transformed values of the independent variables and the PDE (dependent variable) were subjected to multiple regression to establish a full-model second-order polynomial equation. F was calculated to confirm the omission of insignificant terms from the full-model equation to derive a reduced-model polynomial equation to predict the PDE of proniosome-derived niosomes. Contour plots were constructed to show the effects of X1, X2 and X3 on the PDE. A model was validated for accurate prediction of the PDE by performing checkpoint analysis. The computer optimization process and contour plots predicted the levels of independent variables X1, X2, and X3 (0, −0.158 and -0.158 respectively), for maximized response of PDE with constraints on vesicle size. The Box-Behnken design demonstrated the role of the derived equation and contour plots in predicting the values of dependent variables for the preparation and optimization of piroxicam proniosomes

Effect of heating temperature and time on pharmaceutical characteristics of albumin microspheres containing 5-fluorouracil

In this study, we found that both heating temperature and heating time affect mean particle size, particle size distribution, and drug entrapment efficiency of albumin microspheres. The change in heating temperature may affect the particle size of the product, especially when heating is carried out at a lower temperature (90°C–120°C). Hence the temperature should be selected on the basis of desired size range. Given that it is desirable for a maximum amount of the drug used in the preparation to become entrapped in microspheres, heating temperature and heating time for denaturation of albumin should be selected cautiously, as both have a significant effect on drug entrapment efficiency. In the present case, the highest entrapment was found in batches prepared by heating at 90°C for 5 minutes. However, the extent of stabilization at the selected temperature and the time of heating should also be taken into consideration, as they may affect the release of drugs to target tissue

Poly(D,L-Lactide-Co-Glycolide) microspheres containing 5-fluorouracil: Optimization of process parameters

The objective of this research was to optimize the processing parameters for poly(D,L-lactide-coglycolide) (PLGA) microspheres of 5-fluorouracil (5-FU) and to mathematically relate the process parameters and properties of microspheres. Microspheres were prepared by a water-in-oil-in-water emulsion solvent evaporation technique. A 32 factorial design was employed to study the effect of the volume of the internal phase of the primary emulsion and the volume of the external phase of the secondary emulsion on yield, particle size, and encapsulation efficiency of microspheres. An increase in the volume of the internal phase of the primary emulsion resulted in a decrease in yield and encapsulation efficiency and an increase in particle size of microspheres. When the volume of the external phase of the secondary emulsion was increased, a decrease in yield, particle size, and encapsulation efficiency was observed. Microspheres with good batch-to-batch reproducibility could be produced. Scanning electron microscopic study indicated that microspheres existed as aggregates