Volume 9, Issue 4, Oct-Dec 2017

Volume 9

October-December 2017

Comprehensive study of pharmaceutical process validation of solid dosage forms: Quality assurance point of view

Komal M Jadhav, Jameel Ahmed S Mulla, Rajendra C Doijad

Abstract:
The purpose and interest of this overview on pharmaceutical process validation of immediate release tablets, is to highlight the critical process parameters to be validate during the activity of validation of solid dosage form. It is the most common dosage form for orally administration of drug. The Process validation should confirm that the control strategy is sufficient to support the process design and the quality of the product. This validation review covers the solid dosage form of process validation. The process is developed in such a way that the required parameters are achieved and it ensures that the output of the process will consistently meet the required parameters during routine production, the process is validated. A manufacturer can assure through careful design of the device, processes, process controls and process variable that all manufactured units will meet specifications and have uniform quality. This review provides info on objectives and advantages of method validation, varieties of method validation, major phases in validation and regulative aspects. Guidelines and strategy for process validation of solid dosage form validation and regulatory aspects. Guidelines and strategy for process validation of solid dosage form are also discussed.

Keywords: Pharmaceutical Process Validation, Process Validation Stages, Validation Acceptance Criteria.

Stability study of microemulsion and their use in formulation of pellets with enhanced solubility and dissolution efficiency of nevirapine

Pradum Pundlikrao Ige, Puja Mahendrsing Rajput

Abstract:
This investigation explores use of Oleic acid, Tween 80 and Transcutol HP in self emulsifying pellets of nevirapine with enhanced solubility and dissolution efficiency. Liquid SEDDS was prepared and characterized by self emulsification time, precipitation, thermodynamic stability, globule size, PDI, zeta potential. Self emulsifying pellets were characterized by surface topography, flow properties, disintegration time, in vitro drug release and stability. Optimized SEP6 had disintegration time (7 ± 2 min) and % dissolution efficiency about 86.22 ± 1.25 for 1 h. In conclusion, self emulsifying pellets of nevirapine could be demonstrated as new approach to enhance its solubility and dissolution efficiency.

Keywords: Nevirapine, Lipophilicity, Self Emulsifying Pellets, Dissolution Efficiency.

Preparation and characterization of voriconazole solid lipid nanospheres

Somayeh Brahimi, Tayebeh Toliyat

Abstract:
Voriconazole is an antifungal drug used for treatment of various conditions caused by yeast or fungi. Voriconazole is changed form of flouconazole and it is improved potency and spectrum. In this study, we prepared voriconazole as solid lipid nanoparticles (SLN) using the melting method. Stearic acid, palmitic acid and glyceryl monostearate were selected as lipid carriers based on drug solubility and partitioning behaviour. Poloxamer and soya lecithin were the choice for surfactant. The particle sizes of the SLNs determined by zeta sizer. The in vitro release study of SLNs exhibited a sustained-release property of the drug. The effect of various lipids on capture volume, particle size and drug release of these particles were studied. The results show that the presence of glyceryl monostearate as lipid phase has significant effects on the size of particles. In Vitro release performed in phosphate buffer (pH=7.4) by using dialysis bags. It can be assumed that drug release from SLNs is following biphasic model and the first phase is followed the first order equation.

Keywords: Voriconazole, Solid Lipid Nanospheres, Physicochemical Characterization, In Vitro Release Study.

Preparation and evaluation of mefenamic acid loaded microspheres using eudragit by solvent evaporation technique

A Krishna Sailaja, Tanzia Khan

Abstract:
The aim of the present investigation is to prepare mefenamic acid loaded Eudragit microsphere by solvent evaporation technique. Total seven formulations were prepared by altering drug to polymer. The obtained microspheres were evaluated for drug content, entrapment efficiency, loading capacity and surface morphology. In vitro dissolution profile of all the seven formulation was compared. Among all the formulations F3 formulation was found to be the best formulation with a product yield pf 83%, drug content of 87%. The entrapment efficiency and loading capacity was observed as 93% and 79% respectively. In a time period of 12 hrs 98.5% of drug was released from F3 formulation.

Keywords: Mefenamic Acid, Eudragit, Microsphere, Solvent Evaporation Technique.

Formulation and evaluation of immediate release pellets by using coprocessed polymer

Raju O Sonawane, Rajesh R Mogre, Pradum P Ige , Prashant J Chaudhari

Abstract:
The present study was intended towards the formulation and evaluation of immediate release pellets of irbesartan (Irbesartan as model drug has low solubility). Pellets were prepared by the extrusion-spheronization method using co-processed excipient to improve the disintegration time and faster drug release from the pellets. Immediate release pellets were prepared by using co-processed excipient consisting silicon dioxide and calcium stearate. The prepared pellets were evaluated by the flow parameters, friability, disintegration time, FTIR, DSC, SEM and in-vitro dissolution study. It was found that pellet prepared by using co-processed excipient were mechanically stable, good flowability and sphericity. FTIR and DSC study shows that there is no drug excipient interaction; SEM Images shows that co-processed excipient gives spherical pellets. Formulation containing 40% co-processed excipient and 20% MCC shows higher drug release and faster disintegration. Hence, study concludes that co-processed excipient which shows improved disintegration time and faster drug release may be suitable for immediate release pellets.

Keywords: Pellet, Extrusion-spheronization, Irbesartan, Silicon dioxide, Calcium stearate, Disintegration, In-Vitro Dissolution Study.

Solid dispersions based on poloxamer 188 improve the dissolution rate of trandolapril, a poorly water-soluble ace inhibitor

Kenechukwu F C, Ofokansi K C, Momoh M A, Ogbonna J D N, Nnadi C O, Akpa P A

Abstract:
The purpose of this study was to formulate and evaluate trandolapril/poloxamer 188 solid dispersions (SDs) for improved delivery of trandolapril, a poorly water-soluble antihypertensive prodrug. Poloxamer 188 was employed as a hydrophilic carrier at various trandolapril: poloxamer 188 ratios to prepare trandolapril-loaded SDs by fusion method. Characterization based on surface morphology, particle size, entrapment efficiency and moisture sorption properties were carried out on the SDs. Compatibility study was carried out using Fourier transform infrared (FT-IR) spectroscopy while the in vitro dissolution of trandolapril from the SDs was performed in phosphate buffered saline (PBS, pH 7.4). The results showed that discrete and irregularly-shaped SDs of average particle size in the range 2.16 ± 0.78 to 2.94 ± 0.25 µm, which were stable over 3 months, were obtained. The moisture sorption studies indicated the amorphous/ microcrystalline state of trandolapril in the SDs, which also exhibited good entrapment efficiency (EE%) and marked increase in the dissolution rate of trandolapril from the SDs when compared to pure trandolapril (unformulated trandolapril). Spectroscopic studies indicate that there was no strong chemical interaction between the drug and poloxamer 188 which, when incorporated inside SD, had prominent effect in improvement of trandolapril dissolution. As we increased poloxamer 188 concentration in SD formulation, the dissolution rate of the drug (trandolapril) increased, which may be due to the formation of microcrystals, increased wettability and dispersibility in the formulations. The present finding has shown that trandolapril/poloxamer 188 SDs is a potential carrier system for dissolution and bioavailability enhancement of the poorly water-soluble anti-hypertensive prodrug, trandolapril.

Keywords: Solid Dispersions (SDs), Drug Dissolution, Trandolapril, Moisture Sorption, Poloxamer 188.

Indian Journal of

Novel Drug Delivery ISSN 0975-5500

Indian Journal of Novel Drug Delivery ISSN 0975-5500