scholarly journals Probabilistic methods for drug dissolution. Part 2. Modelling a soluble binary drug delivery system dissolving in vitro

2006 ◽  
Vol 14 (7) ◽  
pp. 857-873 ◽  
Author(s):  
Ana Barat ◽  
Heather J. Ruskin ◽  
Martin Crane
Author(s):  
Zainab Ali Hussein

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes ,the oral bioavailability is  approximately 6%, therefore aim  its  prepare and evaluate bromocriptine mesylate  as liquid self nano emulsifying drug delivery system to enhance its solubility , dissolution and stability . Solubility study was made in different vehicles to select the best excipients for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios of surfactant and co-surfactant, four formulations were prepared using various concentrations of castor oil, tween 80 and ethanol. All prepared formulations were evaluated for particle size distribution, polydispersity index, drug content, thermodynamic stability, dispersibility and emulsification time, robustness to dilution and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p < 0.05) than plain drug powder. from the study, it was concluded that self-nanoemulsifying drug delivery system is a promising approach to improve solubility, dissolution, and stability of bromocriptine mesylate.


Author(s):  
Suresh Gande ◽  
S. Srikanth Reddy ◽  
Bhikshapathi D. V. R. N.

Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.


Author(s):  
Fahad F. Salim ◽  
Nawal A. Rajab

Piroxicam (PIR) is a nonsteroidal anti-inflammatory drug of oxicam category, used in gout, arthritis, as well as other inflammatory conditions (topically and orally). PIR is practically insoluble in water, therefore the aim is prepare and evaluate piroxicam as liquid self-nanoemulsifying drug delivery system to enhance its dispersibility and stability. The Dispersibilty and Stability study have been conducted in Oil, Surfactant and Co-surfactant for choosing the best materials to dissolve piroxicam. The pseudo ternary phase diagrams have been set at 1:1, 2:1, 3:1 as well as 4:1 ratio of surfactants and co-surfactants, also there are 4 formulations were prepared by using various concentrations of transcutol HP, cremophore EL and triacetin oil. All the constructed prepared formulas have been assessed for in vitro drug dissolution, thermodynamic stability, polydispersity index, robustness to dilution, particle size distribution, drug content, and the dispersibility and emulsification time.From the presented research concluded that the self-nanoemulsifying drug delivery system is the convenient method for improving Dispersibilty and Stability of piroxicam.  Keywords: Pseudo-ternary phase diagram, Dissolution rate, SNEDDS, Piroxicam.


Author(s):  
Ali N. Wannas ◽  
Nidhal K. Maraie

Objective: This study aimed to prepare tablets containing solid supersaturable self-emulsifying drug delivery system (S-SEDD) of cilostazol for oral use. Method: To improve drug dissolution and so bioavailability for cilostazol (calss II drug) as well as reducing the amount of additives (except for drug =50 mg), liquid S-SEDD of cilostazol were prepared. In this study the liquid supersaturable formula was converted into a solid supersaturable self-emulsifying form using different amounts of two different types of the adsorbents (avicel 101 and aerosil 200). Accordingly; six-formulas (SS1-SS6) were prepared and evaluated applying pre-compression evaluation and the best formula was SS3 formula having an amorphous homogenous free-flowing property and used to prepare tablets using direct compression method. Consequently; six tablet formulas (T1-T6) containing different types and amounts of additives were prepared and evaluated applying post-compression parameters and in-vitro drug release. Result: The best tablet formula was T2 formula which showed high dissolution profile under sink and non-sink condition in comparison to conventional marketed tablet indicating that it kept its supersaturable self-emulsification in-vitro with faster drug release which may lead to improve drug absorption and bioavailability with a fast onset of action. Conclusion: This work succeeded in converting the prepared cilostazol liquid S-SEDD to solid SEDD which is compressed into an immediate release tablets that disintegrate and spontaneously emulsified to form supersaturable system in the GIT which improved drug solubility, release and consequently may enhance its absorption and bioavailability leading to reducing dose size and drug/excipient size effects.


Author(s):  
Vikrant P Wankhade ◽  
Nivedita S Kale ◽  
K.K Tapar

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.


2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 


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