Objective: The objective of this study was to formulate once daily sustained oral release floating tablet of prochlorperazine maleate, this floating tablet has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility. Methods:The prochlorperazine maleate floating tablets were formulated by using hydrophilic swellable polymer and gas generating agent. In this study, 15 formulas were prepared with many variables in order to achieve an optimum dissolution and floating behaviour for the floating tablet.The all prepared formulas were tested for bulk density, tap density, angle of repose, Carr's Index, thickness, weight variation, hardness, friability, drug content, in vitro dissolution test, in vitro buoyancy, and swelling index.Results: Formula (F2) that contain 55% (w/w) hydroxypropyl methylcellulose k4M (HPMCK4M), 5 % (w/w) sodium bicarbonate (NaHCO3 Conclusion: It can be concluded that that the selected formula (F2) can be a promising formula for the preparation of gastro retentive floating drug delivery systems of prochlorperazine maleate.) have acceptable flow properties and compressibility index and good physical properties with floating lag time (16±0.57) seconds and total floating time (32±0.29) h with 100% release of prochlorperazine maleate at the end of 24 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F2) showed no chemical interaction between the drug and the excipients that used in the formula.
The aim of this study was to formulate granisetron (GSN) in a new dosage form using natural substances and to improve pediatric patient compliance to achieve maximum drug efficacy. GSN is a 5HT3 receptor antagonist that used as prophylaxis for prevention of nausea and vomiting before radiotherapy and chemotherapy. This dosage form was selected because of sharing both the advantages of liquid and solid dosage forms. In this study, two types of natural jellifying agents have been used in different concentrations. The natural jellifying agents which have been used were gelatin and caragennan (CRG). The effect of jellifying agent and their concentrations have been investigated. Six formulations of (GSN) oral jellies were prepared by heat and congealing method and the prepared jellies were evaluated by measuring their pH, content uniformity, drug-polymer compatibility, syneresis, physical stability, general appearance and production yield. Among the prepared formulations, formulation F1 with 4.5% gelatin was considered the best one, since it gave the highest drug release 99.4% in 15 min with acceptance results for all other evaluation test.
In the present investigation an attempt was made to prepare colon targeted enteric coated tablet containing different prednisolone solid dispersion formulations, to prevent ulcerative colitis, improve the patient compliance and reduce the side effects of drug in the gastro intestinal tract (GIT). Solid dispersion is one of the most widely used approaches to enhance the solubility as well as dissolution rate of poorly water soluble drugs. Solid dispersions (SDs) of Prednisolone with D-mannitol, PEG 4000 and Kollicoat IR were prepared and evaluated to deliver Prednisolone to the colon in a pre-solubilized form. The selected formula using drug compatible excipients was compressed into fast disintegrating tablets and then coated with Eudragit S100 (pH-responsive polymer), several variables related to both solid dispersion preparation (carrier type and drug to the carrier ratio) and tablet coating (coat level) were studied to show their effects on drug solubility and dissolution. Different analytical techniques like differential scanning caloremitry (DSC), powder x-ray diffraction (PXRD) and scanning electron microscopy (SEM) were studied to prove the change of drug particle from crystal to amorphous form in SDs. The 1:3 Prednisolone/Kollicoat IR SDs showed the greatest improvement in the dissolution rate. The coating level was critical for determining the duration of the lag phase. Best result was given by the 16% coat (Eudragit S100/ Dibutyl phthalate/ talc). This coating level showed an acceptable lag time for the proposed colonic targeting (5 h) as the selected tablet resisted pre-colonic pH values, followed by an immediate release stage in pH 7.4. The suggested covered (coated) tablets may provide a colonic delivery system for prednisolone with enhanced solubility and bioavailability.
Lozenges are formulations of solid dosage form which tend to liquefy in mouth or pharynx. They could be consisting of one or more drugs in a flavored and sweetened base. They are recommended to treat local mouth or pharynx irritation or infection, or they may be used also for systemic combi- nation of two drugs (Acyclovir and Lidocaine) by pressed coated tablet lozenges. Thus, the lozenges will have both antiviral and local anesthetic effects suitable for the treatment of virus that infects oral cavity. In this study, nine formulations of acyclovir compressed tablet lozenges were prepared to investigate the effects of type and concentration of binders (gelatin, acacia, and tragacanth) on physical appearance, weight variation, hardness, thickness, friability, dissolving , drug content and in vitro released of drug. Compressed tablet lozenges formula F4 contening (Acacia 10%) as binder was successfully prepared and has been selected as optimum formula since it released 98% of drug after 45 min, as compared to other formulas.
In this study, solid dispersion using hydrophilic carriers (polyethylene glycols) and fast dissolving sugars (sorbitol and lactose) has been employed to enhance dissolution and hence the bioavailability of ibuprofen.Solid dispersions of different weight ratios (drug: carrier: fast dissolving sugars) have been prepared using fusion method.Microscopic images showed disappearance of specific features of ibuprofen, carriers and sugars in the solid dispersions.Release study of ibuprofen from prepared systems was performed in phosphate buffer pH 6.8; faster drug release was obtained from solid dispersions with high polyethylene glycol ratio and/ or from solid dispersions to which fast dissolving sugars has been added duringtheir preparations.The study also explored hydrogen bond interactions between polyethylene glycols and ibuprofen in the solid dispersions. FTIR spectroscopy confirmed intermolecular interaction at (2:1) drug to carrier mole ratio. This interaction was considered the most important factor in enhancing the dissolution of ibuprofen via solid dispersions.
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