Development and characterization of fast-dissolving tablet formulations of glyburide based on solid self-microemulsifying systems

Cirri, Marzia; Roghi, Alessandra; Valleri, Maurizio; Mura, Paola

doi:10.1016/j.ejpb.2016.04.008

Cited by 25 publications

(11 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…For developing tablet dosage forms, choice of components and compaction procedure is important. In particular, the role of disintegrating agents is crucial in the formulation of solidified SMEDDS preparations that can rapidly disintegrate and spontaneously emulsify in gastric or intestinal fluid [ 4 , 6 ]. Solidified tablets containing croscarmellose sodium or Kollidon ® CL-SF as a disintegrant showed maximum drug release of over 90% within 30 min, whereas tablets without disintegrant resulted in poor drug release of less than 5% after 2 h [ 2 , 6 ].…”

Section: Introductionmentioning

confidence: 99%

Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability

et al. 2017

View full text Add to dashboard Cite

In order to improve the dissolution and oral bioavailability of valsartan (VST), and reduce the required volume for treatment, we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) composed of VST (80 mg), Capmul® MCM (13.2 mg), Tween® 80 (59.2 mg), Transcutol® P (59.2 mg), and Poloxamer 407 (13.2 mg). In the present study, by using Florite® PS-10 (119.1 mg) and Vivapur® 105 (105.6 mg) as solid carriers, VST-loaded solidified SuSMEDDS (S-SuSMEDDS) granules were successfully developed, which possessed good flow properties and rapid drug dissolution. By introducing croscarmellose sodium (31 mg) as a superdisintegrant, S-SuSMEDDS tablets were also successfully formulated, which showed fast disintegration and high dissolution efficiency. Preparation of granules and tablets was successfully optimized using D-optimal mixture design and 3-level factorial design, respectively, resulting in percentage prediction errors of <10%. In pharmacokinetic studies in rats, the relative bioavailability of the optimized granules was 107% and 222% of values obtained for SuSMEDDS and Diovan® powder, respectively. Therefore, we conclude that novel S-SuSMEDDS formulations offer great potential for developing solid dosage forms of a liquefied formulation such as SuSMEDDS, while improving oral absorption of drugs with poor water solubility.

show abstract

Section: Introductionmentioning

confidence: 99%

Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability

et al. 2017

View full text Add to dashboard Cite

show abstract

“…Dissolution test was performed under the same experimental conditions (900 mL of pH 7.4 buffer solution) used in our previous studies aimed at the development of GLY fast-dissolving tablets [ 12 , 15 , 16 , 20 ], in order to obtain comparable results. Moreover, these conditions of medium volume and pH are those indicated by FDA and USP (test 5, Revision Bulletin 2010, 1st Supplement USP 34-NF 29) for the dissolution test of GLY (micronized) tablets.…”

Section: Resultsmentioning

confidence: 99%

“…A comparison between the drug dissolution properties from the new liquisolid tablets and those from the previously developed GLY fast-dissolving tablets based on other different formulation approaches, showed that the new technology was actually more effective in enhancing the GLY dissolution properties than the formation of binary or ternary solid dispersions [ 15 , 16 ], cyclodextrin complexation [ 12 ] or simple adsorption on mesoporous silicas [ 46 ]. The performance of the new GLY liquisolid tablets resulted comparable only to that of fast-dissolving tablets based on solid-self-microemulsifying systems (SMEDDS) [ 20 ]. However, the new liquisolid-tablets presented the strong advantage of a simpler and faster formulation development and of a lower production cost.…”

Section: Resultsmentioning

confidence: 99%

“…Despite the fact that several strategies have been investigated in an effort to improve the dissolution performance of GLY, including complexation with cyclodextrins [ 11 , 12 , 13 ], solid dispersions in hydrophilic carriers [ 14 , 15 , 16 ], micellar solubilization [ 17 ], and formulation of self-micro-emulsifying drug delivery systems (SMEDDS) [ 18 , 19 , 20 ], at present, there are no commercial GLY products arising from such approaches. As a result, the development of effective GLY tablets with optimized dissolution behavior and ease of manufacture with industrial scale-up feasibility still remains a challenge and would be an important and useful result.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development and Characterization of Liquisolid Tablets Based on Mesoporous Clays or Silicas for Improving Glyburide Dissolution

et al. 2020

Self Cite

View full text Add to dashboard Cite

The aim of this work was to evaluate the effectiveness of mesoporous clays or silicas to develop fast-dissolving glyburide tablets based on a liquisolid approach. Selected clay (Neusilin®US2) and silica (Aeroperl®300) allowed preparation of innovative drug liquisolid systems containing dimethylacetamide or 2-pyrrolidone as drug solvents, without using coating materials which are necessary in conventional systems. The obtained liquisolid powders were characterized for solid-state properties, flowability, compressibility, morphology, granulometry, and then used for directly compressed tablet preparation. The developed liquisolid tablets provided a marked drug dissolution increase, reaching 98% dissolved drug after 60 min, compared to 40% and 50% obtained from a reference tablet containing the plain drug, and a commercial tablet. The improved glyburide dissolution was attributed to its increased wetting properties and surface area, due to its amorphization/solubilization within the liquisolid matrix, as confirmed by DSC and PXRD studies. Mesoporous clay and silica, owing to their excellent adsorbent, flow, and compressibility properties, avoided use of coating materials and considerably improved liquid-loading capacity, reducing the carrier amount necessary to obtain freely flowing powders. Neusilin®US2 showed a superior performance than Aeroperl®300 in terms of the tablet’s technological properties. Finally, simplicity and cost-effectiveness of the proposed approach make it particularly advantageous for industrial scale-up.

show abstract

“…A fixed quantity of isotropic admixture is diluted with double purified water to yield a clear emulsion [19,20]. The resulting emulsions can be inspected outwardly for their relative polluting influence and their transmittance can be evaluated in UV-visible spectrophotometer with the help of double purified water as the blank [21][22][23].…”

Section: Composition Of Smedsmentioning

confidence: 99%

Review of formulation and evaluation of self-micro emulsifying drug delivery system (SMEDDS)

Bahadur¹,

Yadu²,

Baghel³

et al. 2020

ScienceRise: Pharmaceutical Science

View full text Add to dashboard Cite

Approximately half of the new drug applicants that reach formulation have poor water solubility. Oral delivery has been the main route of drug administration for the chronic treatment of numerous diseases. In different cases, in oral conveyance, 50 % of the medication compound is hampered because of the high lipid soluble or fat soluble of the medication itself. Around 40 % of new drug applicants show low solubility in water, which prompts poor oral bioavailability, high Intra and Intersubject changeability, and deficiency of dose proportionality Aim of review. The main aim of this review article is to gather the information related to design and evaluation of SMEDDS. These information can be utilized to enhance the bioavailability of the poorly aqueous soluble drug for various types of orally administered drugs. In this review article, various literature are reviewed and summerised in single paper to serve as reference guide to various research scholars and researchers working on self-micro-emulsifying drug delivery systems. Materials and Methods. To prepare this manuscript various keywords were searched in different search engine such as Google, Yahoo and Bing etc. This review article reviews the recent work done in the field of SMEDDS. It comprises review of literatures available in public domain and formulation of SMEDDS and its characterization is summarized in this article. Result. The various strategies to developed poor aqueous soluble drug for improvement of bioavailability for example, salt development and molecular size reduction of the compound might be one technique to enhance the dissolution rate of the drug. In any case, these methods have their limitations. SMEDDS is one of the novel applications for the delivery of low water soluble and low bioavailability of drug. SMEDDS is a method to improve the aqueous solubility of the medication; SMEDDS are described as isotropic blenders of oils, surfactants, and co-surfactant. Upon slightly stir followed by dilution with distilled water, for example, gastrointestinal liquids, these techniques can define clear o/w micro emulsion. SMEDDS is first choice and key technology for developing the lipophilic drug and other different factors that chance to affect the oral bioavailability. Conclusions. This review paper attempts to describe the preparation of SMEDDS and furthermore discusses the development of pseudo ternary phase diagram for SMEDDS. It describes the mechanism and method of preparation involved in SMEDDS. The capability of oral absorption of drug compound from the SMEDDS relies upon numerous formulation−related parameters, for example, surfactant concentration, oil/surfactant ratio, and hydrophobicity of emulsion, globule size and charge, in vitro, in vivo all of which basically characterized the ability of self-emulsification. SMEDDS are administered as unit dosage form and it also protect the degradation of drug.

show abstract

Development and characterization of fast-dissolving tablet formulations of glyburide based on solid self-microemulsifying systems

Cited by 25 publications

References 32 publications

Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability

Solid formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability

Development and Characterization of Liquisolid Tablets Based on Mesoporous Clays or Silicas for Improving Glyburide Dissolution

Review of formulation and evaluation of self-micro emulsifying drug delivery system (SMEDDS)

Contact Info

Product

Resources

About