FORMULATION AND EVALUATION OF LIQUISOLID COMPACTS OF OLANZAPINE

The Main objective of the present study was to enhance the dissolution rate of olanzapine by liquisolid compact method. Olanzapine is practically insoluble in water. Solubility of olanzapine was estimated in different nonvolatile solvents. The study was designed to evaluate the effect of various formulation parameters like Drug concentration and Excipient ratio on angle of repose and % drug release using 32  full factorial design. Quality control tests were done to evaluate each batch of tablets.  Liquisolid compact powder was subjected to angle of repose, Carr’s index, and hausner’s ratio to determine flow property. Hardness, friability, disintegration time, drug content, dissolution rate are determined. Fourier transforms infrared analysis, x-ray diffraction studies also performed. All the formulations showed acceptable flow property and better drug release. The optimized batch was subjected to stability studies for 30 days. The dissolution profile of optimized batch was compared with direct compressed tablet and with marketed preparation. Fourier transform infrared spectroscopy conformed that drug does not interact with excipients which are added in the formulation. X-ray diffraction study proved that olanzapine (crystalline form) converted into amorphous form. From this study it was concluded that liquisolid compact technique improves dissolution rate of olanzapine

Priprava i karakterizacija mukoadhezivnih flastera za bukalnu primjenu propranolol hidroklorida s kitozanom

Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 ± 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.Mukoadhezivni flasteri za bukalnu primjenu s propranolol hidrokloridom pripravljeni su koristeću metodu isparavanja otapala. Kao mukoadhezivni polimer upotrebljen je kitozan u različitim omjerima u odnosu na PVP K-30. Određivana su sljedeća svojstva flastera: masa, ujednačenost količine lijeka, savitljivost, ex vivo mukooadhezivnost, ex vivo vrijeme mukoadhezije, pH na površini, in vitro oslobađanje ljekovite tvari i in vitro permeacija. Iz flastera se ljekovita tvar kontrolirano oslobađala prema kinetici prvog reda tijekom 7 h i nije slijedila Fickov zakon difuzije. Upotreba PVP K-30 produljila je vrijeme oslobađanja. Indeks bubrenja bio je proporcionalan koncentraciji PVP K-30. Snaga bioadhezije optimiranih flastera (F4) bila je 9,6 ± 2,0 g, a ex vivo vrijeme mukoadhezije 272 minute. pH na površini svih flastera bio je između 5,7 i 6,3 pa ne bi trebali iritirati bukalnu šupljinu. Flasteri sa 10 mg propranolola imali su veću bioadhezivnost, a lijek se iz njih polaganije oslobađao nego iz flastera sa 20 mg ljekovite tvari. Dobivena je dobra korelacija između in vitro oslobađanja i in vitro permeacije lijeka (koeficijent korelacije 0,9364). Ispitivanja stabilnosti pokazala su da su i propranolol i flasteri za bukalnu primjenu stabilni u ljudskoj slini

DESIGN AND CHARACTERIZATION OF DONEPEZIL HYDROCHLORIDE SUSTAINED RELEASE MATRIX TABLETS

The ultimate aim of the present study was to develop sustained release (SR) tablets of Donepezil Hydrochloride by employing natural polymers (Guar gum and Xanthan gum) as the matrix material in different proportion by wet granulation method. Initially drug-excipients compatibility studies were carried out using FTIR and DSC which showed no interaction between drug and excipients. Granules of prepared batches were evaluated for bulk density, tapped density, carr’s index, hausner’s ratio, angle of repose. Tablets were evaluated for various physicochemical parameters like hardness, thickness, friability, weight variation test, drug content and in vitro drug release. All the formulation showed compliance with pharmacopoeial standards. 32 full factorial design was applied in which Guar gum (X1) and Xanthan gum (X2) were taken as independent factor and %CDR at 2hr (Y1) and at 12hr (Y2) were taken as response. In-vitro drug release study revealed that as the amount of polymers increased, % CDR decreased. Contour plots as well as response surface plots were constructed to show the effect of X1 and X2 on %CDR and predicted at the concentration of independent variables X1(40mg) and X2(40mg) for maximized response. The kinetic release treatment showed that korsmeyer peppas equation has shown of  r2 0.9517 which was close to one indicating that the dissolution profile fits in Korsmeyer-Peppas model and the mechanism of drug release from these tablets was by non-fickian diffusion mechanism. The optimized batch was kept for stability study at 40 ± 2oC/ 75 ± 5 % RH for a period of 1 month according to ICH guidelines and found to be stable after 1 month of study. Keywords: Sustained release matrix tablet, Donepezil hydrochloride, Guar gum, Xanthan gum, 32 full factorial design

Priprava i in vitro karakterizacija mikrosfera amoksicilina dobivenih metodom sušenja sprejom

The purpose of the present study was to design mucoadhesive chitosan microspheres containing amoxycillin. Chitosan microspheres with a small particle size and good sphericity were prepared by a spray-drying method followed by chemical treatment with a chemical crosslinking agent (glutaraldehyde). Parameters affecting the extent of crosslinking were the crosslinking time and the concentration of the crosslinker agent. Crosslinked spray-dried chitosan microspheres were analyzed for their morphological aspects, particle size, drug entrapment efficiency, swelling percent and in vitro drug release. Batch M4 with a drug polymer ratio of 1:2, dissolved in minimum concentration of acetic acid solution treated with glutraldehyde, was found to be optimal giving controlled drug release for 10 h. It was found that both the increase of glutaraldehyde concentration and crosslinking duration decreased the swelling capacity of chitosan microspheres. This could be directly correlated to drug release from the microspheres.Cilj ovog rada bio je priprava mukoadhezivnih kitozanskih mikrosfera amoksicilina. Mikrosfere male veličine čestica i dobre sferičnosti pripravljene su metodom sušenja sprejom, te obradom s glutaraldehidom kao sredstvom za umrežavanje. Stupanj umrežavanja ovisio je o vremenu umrežavanja i koncentraciji sredstva za umrežavanje. Umreženim kitozanskim mikrosferama određen je oblik, veličina čestica, količina uklopljenog lijeka, postotak bubrenja i in vitro oslobađanje ljekovite tvari. Pripravak M4 s optimalnim svojstvima i kontroliranim oslobađanjem amoksicilina tijekom 10 sati pripravljen je pomoću smjese polimera omjera 1:2 otopljenih u razrijeđenoj octenoj kiselini, te umreženih pomoću glutraldehida. Povećanje koncentracije glutaraldehida i trajanja umrežavanja smanjuje sposobnost bubrenja kitozanskih mikrosfera, što je u izravnoj korelaciji s oslobađanjem lijeka iz mikročestica

FORMULATION OF FUROSEMIDE SOLID DISPERSION WITH MICRO CRYSTALLINE CELLULOSE FOR ACHIEVE RAPID DISSOLUTION

Furosemide, a weekly acidic, loop diuretic drug indicated for treatment of edema and hypertension having high permeability through stomach. It is practically insoluble in gastric fluid (0.006 mg/ mL) and having highly permeability through stomach but due to its solubility limitation it can’t enter into systemic circulation. It was logically decided to design experiment, so as to achieve the set objectives. Attempt was made to prepare solid dispersion of furosemide with Poly ethylene glycol (PEG) 6000 containing microcrystalline cellulose (MCC) as adsorbent which would dissolve completely in less than 30 minutes (target selected by considering minimum gastric empting time). Microcrystalline cellulose converted sticky dispersion in to free flow powder hence increase surface area which responsible for dissolution improvement. Factorial design was applied to optimize formulation. Amount of poly ethylene glycol 6000 and microcrystalline cellulose were selected as an Independent variable while angle of repose and T100% were selected as dependent variable. Attempts for dissolution rate of furosemide improve bioavailability and consequently dose reduction would possible

PHARMA SCIENCE MONITOR AN INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES ANTI-ARTHRITIC AND VASCULAR PROTECTIVE EFFECTS OF FENUGREEK, BOSWELLIA SERRATA AND ACACIA CATECHU ALONE AND IN COMBINATIONS

ABSTRACT Rheumatoid arthritis is a systemic inflammatory disease associated with generation of oxidative stress that produced vascular dysfunction. The present study was undertaken for detection of Anti-Arthritic and Vascular Protective Effects of Fenugreek, Boswellia Serrata and Acacia catechu alone and in Combinations. Arthritis was induced by CFA (6 mg/ml, i.d.) and Parameters were measured includes paw volume, Body weight, RA Factor, Arthritic index, E.S.R., WBC counts. Vascular and endothelial dysfunction study was done by performing CRC of Peroxynitrite and Acetylcholine respectively using Rat thoracic aorta strip pre-contracted with Phenylephrine. The Results of arthritis model, Combination of three drugs exhibited 48.75 % and combination of two drugs such as Methi and Boswellia exhibited 44.58 %, Acacia and Boswellia exhibited 36.25 % and Methi and Acacia exhibited 29.16 % reduction in Paw edema after 21 days respectively. Also Combination of three drugs showed significant reduction in arthritic index, RA factor, ESR, WBC counts and normalization of body weight in Arthritic rats as compare to diseased control or other two drugs combination. In vascular study combination of three drugs showed significant difference in relaxation (P<0.001) Vs. disease control as compare to other two drug combination (P<0.01) or alone drug (P<0.05) in Ach CRC, while in Peroxynitrite CRC combination of three drugs showed significant relaxation (P<0.01) compare to other two drug combination (P<0.01) and alone drug (P<0.05) Vs. disease control. Combination of three drugs showed significant anti-arthritic and vascular protective effect

Formulation and evaluation of mucoadhesive glipizide microspheres

The purpose of this research was to formulate and system-atically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a cross-linking agent. Results of preliminary trials indicate that volume of cross-linking agent, time for cross-linking, polymer-to-drug ratio, and speed of rotation affected characteristics of microspheres. Microspheres were discrete, spherical, and free flowing. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test and also showed a high percentage drug entrapment efficiency. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X1), and stirring speed (X2) on dependent variables percentage mucoadhesion, t80, drug entrapment efficiency, and swelling index. The best batch exhibited a high drug entrapment efficiency of 75% and a swelling index of 1.42; percentage mucoadhesion after 1 hour was 78%. The drug release was also sustained for more than 12 hours. The polymer-to-drug ratio had a more significant effect on the dependent variables. In vivo testing of the mucoadhesive microspheres to albino Wistar rats demonstrated significant hypoglycemic effect of glipizide