Objective: To formulate orally disintegrating taste masked tablets of drotaverine hydrochloride (HCl) by sublimation technique. Methods:Initially superdisintegrant was selected and its concentration was optimized by pre-compression and post-compression parametric evaluation. Camphor and menthol were used as sublimating agents alone and in combination to mask the taste of drotaverine hydrochloride. Prepared tablets were evaluated for physicochemical evaluation, in vitro dissolution studies and fourier transformation-infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry studies. Results:The optimised formulation DCM2 prepared with a mixture of camphor and menthol was characterised by fourier transformation-infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry studies and found no incompatibility and no major shifts were noticed. Conclusion:The results demonstrated that the prepared drotaverine HCl orally disintegrating tablets showed better taste masking. The present sublimation technique can be effectively used for taste masking and also for orally disintegrating tablets.
Colon Targeted Oral Drug Delivery System has gained much importance in recent times in delivering drug substance for the local action against colonic cancers, infections, Ulcerative Colitis (UC) and Crohn's disease and for systemic action of protein peptides and non-peptide drugs include Cardiovascular and Antiasthamatics etc. This article gives an overview about the anatomy, physiology of colon and factors that are having influence on the formulation. Various approaches for colon targeting are specified and micro sponges are at forefront having unique, versatile and novel approach. Micro sponges are highly cross linked porous polymeric microspheres with many interconnected voids loaded with API that are released in a controlled manner. Micro sponges are designed to deliver efficiently at minimum dose with reduced side effects, enhancing the stability and solubility of active pharmaceutical ingredients. Further, the novel techniques in preparation, compiling the present research information with novel applications of drug delivery with micro sponges are highlighted.
Objective: The objective of this study is to formulate orally disintegrating taste masked tablets of drotaverine HCl using solid mixture technique.Methods: Taste masked drug-polymer solid mixtures of drotaverine HCl were prepared by using hydroxypropyl methylcellulose (HPMC) 3 cps and rxcipient ® FM1000/calcium silicate (rxcipient) as carriers employing kneading method using varying drug-polymer ratios of 1:1, 1:5, 1:7.5, and 1:9. Prepared drug-polymer mixtures evaluated for taste masking, and the ratio of drug-polymer is optimized. The granules and tablets prepared with optimized drug-polymer ratio were evaluated for pre-and post-compression parameters, in vitro dissolution studies, Fourier-transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD) studies. Results:The drug:polymer ratios 1:7.5 with rxcipient and 1:9 with HPMC were optimized based on taste evaluation. The pre-compression results showed that all the formulae have good flow properties. The post-compression evaluations showed that all the formulae met the specifications of orally disintegrating tablets. From all the prepared taste masked drotaverine HCl tablets, R10 formulation consisting of 4% croscarmellose sodium and H9 formulation consisting of 3% croscarmellose sodium, 3% sodium starch glycolate, and 2% microcrystalline cellulose shown more than 99% drug release in 60 min, and both the formulations showed better taste masking and were meting oral disintegrating tablet (ODT) parameters. The optimized formulation was characterized by FTIR, DSC, and XRD studies and found no incompatibility. Conclusion:The results demonstrated that the prepared drotaverine HCl ODT showed better taste masking and meeting the parameters of ODT formulations R10 and H9. The present solid mixture technique can be effectively used for taste masking.
Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.
The aim of the present research work was to formulate fast dissolving tablets of ranitidine HCl by direct compression method and to evaluate fenugreek seeds mucilage as a natural superdisintegrating agent. The fast dissolving tablets were prepared by using fenugreek seed mucilage powder, crospovidone, croscarmellose sodium, sodium starch glycolate as superdisintegrants (2 and 4% w/w) and microcrystalline cellulose (34 and 36% w/w) as a directly compressible vehicle. All the prepared tablets were evaluated for hardness, friability, drug content uniformity, weight variation, disintegrating time, wetting time and in vitro drug release studies. All the prepared fast dissolving tablets formulations were within the Pharmacopoeial standards limits. Based on in vitro drug release studies (>90 % within 30 min), the two formulations were tested for the short term stability (40 ˚C/75% RH for 3 months) and drug excipient interaction (IR spectroscopy). From all the prepared formulations, the formulation FR8 prepared with 6% w/w fenugreek seeds mucilage and 34% w/w of MCC was optimised as the best formulation (>90 % within 30 min) compared to conventional commercial tablets formulation (>75 % within 30 min). There is no significant on drug content and in vitro drug release (p < 0.05) (Accelerated stability studies).
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