METOPROLOL SUCCINATE SUSTAINED RELEASE MATRIX TABLETS- FORMULATION DEVELOPMENT AND INVITRO EVALUATION

Objective: Metoprolol succinate is a Beta 1 selective antagonist used as an Anti hypertensive, Anti angina, Anti arrhythmic. The aim of present investigation was to develop matrix tablets of Metoprolol succinate using different polymers. Methods: Metoprolol succinate matrix tablets were prepared by direct compression and wet granulation method using different polymers. All the formulations were evaluated for weight variation, thickness, hardness, friability and dissolution. Results: It has been studied that a matrix tablet containing hydroxyl propyl methyl cellulose polymers for oral controlled delivery of Metoprolol succinate has been formulated with greater significance; hence it was decided to check the in-vitro drug-polymer study in formulating a sustained release tablet for Metoprolol succinate. All the formulations are prepared by using polymers include HPMC K15M, HPMC K100M, Ghatti gum, Sodium CMC, Pectin. All the formulation is subjected to invitro dissolution studies. Conclusion: Among all these formulations F-11 is optimized. This formulation containing 50mg of drug, 150mg of HPMC K15M, 3mg of Mg stearate, 3mg of talc, and 69mg of MCC. As the result of this study it may conclude that the formulation meet the needed theoretical drug release profile and has the sustain action i.e., retarding the drug release so the release is for a long time and thus more bio availability

Priprava i in vitro vrednovanje bukoadhezivnih tableta karvedilola

Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 ± 0.4%) with the Higuchi model release profile and permeated 21.5 ± 2.9% of the drug (flux 8.35 ± 0.291 µg h1cm2) permeation coefficient 1.34 ± 0.05 cm h1) through porcine buccal membrane. BC3 formulation showed 1.62 ± 0.15 N of peak detachment force and 0.24 ± 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.Varirajući koncentracije bukoadhezivnih polimera HPMC K4M, HPMC K15M i Carbopol 934 pripravljeno je 15 tableta karvedilola. Pripravci iz serije BC ili BD izrađeni su iz karvedilola i HPMC K4 M ili HPMC K 15M u omjerima 1:1, 1:2, 1:3, 1:4 i 1:5, a pripravci iz BE serije iz karvedilola i Carbopol 934 u omjerima 1:0.25, 1:0.50, 1:0.75, 1:1.00 i 1:1.50. In vitro je ispitivana brzina oslobađanja ljekovite tvari, bioadhezija, apsorpcija vlage i permeacija kroz bukalnu membranu svinje. Iz pripravka BC3 postignuto je maksimalno oslobađanje (88,7 + 0,4 %) koje je slijedilo Higuchijev model i maksimalna permeacija 21,5 + 2,9 % (fluks 8,35 ± 0,291 µg h-1 cm-2; permeacijski koeficijent 1,34 ± 0,05 cm h-1). Sila odvajanja za taj pripravak bila je 1,62 ± 0,15 N, a adhezija 0,24 ± 0,11 mJ. FTIR ispitivanja su pokazala da nije bilo interakcija između ljekovite tvari i polimera, a XRD ispitivanja da je ljekovita tvar u kristaliničnoj formi u polimernom matriksu. Pripravljene bukalne tablete su dovoljno bioadhezivne, a permeacija iz njih je zadovoljavajuća

FORMULATION AND IN VIVO EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL IN WISTAR RATS

Objective: The aim was to formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of ramipril, an antihypertensive drug to improve the solubility and bioavailability. Methods: Based on solubility studies oil phase (Sefsol 218), surfactant (Acrysol EL135), and cosurfactant (Transcutol P), respectively, were selected to prepare SNEDDS. Ramipril SNEDDS optimized employing box-Behnken design through the study of factors. All formulations were evaluated for particle size, zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), drug content, and in vitro drug release. The optimized formulation was characterized for Fourier transform infrared (FTIR), scanning electron microscopy (SEM), stability studies, and pharmacokinetic study. Results: The mean particle size, PDI, ZP, EE, content uniformity, and in vitro drug release profile of optimized ramipril-loaded SNEDDS (RF14) were found to be 75.3±2.21nm, 0.126±0.05, −24.4±5.78mV, 98.74±1.97%, 99.52±1.67%, and 98.65±1.73%, respectively. FTIR studies revealed that there is no incompatibility between drug and excipients, SEM images exhibited nanoparticles to be more porous and in spherical shape. Stability studies indicated formulation was stable for 6 months. In vivo studies were conducted for optimized formulation RF14, the Tmax was found to be 0.5±0.62 and 0.5±0.95 h for the optimized and commercial formulations respectively, while Cmax was 25.16±1.73 ng/mL was significant (p<0.05) as compared to the ramipril pure drug 8.02±0.086 ng/mL. AUC0-t of the SNEDDS formulation was higher 355.49±1.76ng h/ml compared to pure drug 116.57±1.64 ng h/ml indicated higher amount of drug concentration in blood proving better systemic absorption of ramipril from SNEDDS formulation as compared to the pure drug. Conclusion: It is concluded from the results that ramipril was successfully formulated into SNEDDS with higher concentration with fast action

DESIGN AND IN-VITRO EVALUATION OF CONTROLLED RELEASE TRI-LAYER VENLAFAXINE HCL TRANSDERMAL PATCH

 Objectives: The purpose of this study was to design a suitable transdermal therapeutic system for venlafaxine hydrochloride (VFH) with the objectiveto prolong the release to be used for controlled release drug delivery.Methods: Transdermal patches of VFH with a hydroxypropyl methylcellulose drug reservoir were prepared by the solvent evaporation technique.In this investigation, the Eudragit RSPO membrane in different concentrations was cast to achieve controlled release of the drug. The absence ofphysiochemical interactions between VFH and the polymers was confirmed by Fourier transform infrared spectroscopy. The physicochemicalparameters and in-vitro drug release studies of formulations were performed and data of optimized formulation were fitted to various kinetic models.Results: The results indicated that suitable tri-layered transdermal patches of VFH with controlled drug release could be prepared. All the formulationsexhibited satisfactory physicochemical characteristics. Among the formulations prepared, formulation F2 showed optimized controlled release for24 hrs (96.42%) with the flux of 28.28 μg/cm2/hr and permeability coefficient of 1.1315×10−3 cm/hr. Drug release from optimized patch followedKorsmeyer-Peppas model and was mediated by Fickian diffusion mechanism.Conclusion: Hence, the development of adhesive type tri-layered transdermal patches for VFH might be a promising one to control the drug releasefor 24 hrs with reduced side-effects.Keywords: Venlafaxine hydrochloride, Tri-layered transdermal patch, Plasticizer, In-vitro drug release study, In-vitro permeation study

Thermo-physical characterization of Pharmacoatr 603, Pharmacoatr 615 and Mowiolr 4-98

Chemical EngineeringApplied Science