Formulation and Development of Gastroretentive Drug Delivery System of Efavirenz

Rao, Monica Rp; Karanjkar, Pooja B.

doi:10.25004/ijpsdr.2019.110513

Cited by 2 publications

(1 citation statement)

References 12 publications

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“…Improvements in the solubility of EFV have been reported in some studies through the preparation of co-crystals, the addition of superdisintegrant excipients, surfactants or cosolvency, amorphization, and the application of some technologies such as nanoemulsions, nanosuspensions, nanoparticles, and complex inclusion (10,(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29)(30)(31). Some solid dispersion techniques are also used, including comminution to reduce particle size (22,(32)(33)(34)(35)(36)(37)(38). Apart from these methods, the use of other metastable forms that are theoretically more soluble is not well known.…”

Section: Introductionmentioning

confidence: 99%

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

Wardhana¹,

Aisyah²,

Sopyan³

et al. 2021

Dissolution Technol.

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Efavirenz (EFV) was approved by the United States Food and Drug Administration in 1998 with no polymorphic forms, but further research defined 23 different forms, including amorphous and solvated forms. This study aims to determine the ability of dissolved EFV polymorphs in in vitro media kinetic release models of pKa values. The polymorph types were obtained through various organic solvents such as acetonitrile, n-hexane, and methanol, i.e., form I, II, and III. The characteristics were distinguished by polarisation microscopy, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), and Raman spectroscopy. The solubility and dissolution of each polymorph were examined by adding 0.25% sodium lauryl sulphate (SLS) to the comparative dissolution media (water, HCl at pH 1.2, phosphate buffer at pH 4.6 and 6.8). The different microscopic shapes provided a unique fingerprint in the FTIR and the Raman spectra. The thermal behaviour examination provided a DSC thermogram with a specific melting point for each polymorph. The results of the solubility and dissolution tests reported that the highest peak was reached by form II, followed by forms III and I. These followed the pKa values of each polymorph, namely 10.12, 10.63, and 10.37 for form I, II, and III, respectively. The dissolution profile shows that pH conditions affect the release kinetics of form I compared to the metastable forms. The kinetic model of form I is pH-dependent; the acidic medium provided a slower release rate. Unlike the metastable forms, drug loading remained constant but still followed Higuchi's kinetic release model, even in acidic medium.

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Section: Introductionmentioning

confidence: 99%

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

Wardhana¹,

Aisyah²,

Sopyan³

et al. 2021

Dissolution Technol.

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Novel Swellable/Expandable Gastroretentive Floating Films of Gliclazide Folded in Capsule Shell for the Effective Management of Diabetes Mellitus: Formulation Development, Optimization and In Vitro Evaluation

Sharma

2021

CDTH

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Background: Gliclazide (GLZ) belongs to the second-generation of sulphonylureas, is a drug of choice for the management of type II DM. It belongs to BCS Class II. The major site of drug absorption for GLZ is the stomach; it displayed variation in the drug absorption rate and bioavailability due to the shorter gastric retention time. Floating mechanism performance gets affected when the gastric fluid level not sufficiently higher, which ultimately obstructs the floating behavior, which is the major limitation of reported formulations. This limitation can get over by folded the film into the capsule shell that dissolved in gastric fluid and film swell/expands to dimensions higher than pylorus sphincter (12mm), thus prevents its evacuation. Objective: To explore the floating mechanism in the designing of films along with a tendency to expand by swelling and unfolding by utilizing a mixture of hydrophilic and hydrophobic polymer to achieve the controlled drug delivery and prolonged gastric retention of drug. Methods: The gastroretentive floating films were formulated by the solvent casting technique using 32 full factorial design and subjected to in vitro evaluation parameters, drug-excipient compatibility, X-ray diffraction and accelerated stability study. Results: The pre-formulation study established the purity and identification of drug. FTIR study confirmed no drug excipient interaction. F3, F6, and F9 were optimized based on in vitro floating characteristics, swelling/expanding ability, and unfolding time study. All developed formulations were unfolded within 14-22 min after capsule disintegration. The F3 was selected as final formulation as its ability to control the release of drug for 24 hrs followed by Zero-order kinetics having super case 2 transport. XRD confirmed the amorphousness of drug within formulation. The stability study results revealed that formulation was quite stable at extreme storage condition. Conclusion: The developed novel formulation has a good potential for the effective management and treatment of Diabetes Mellitus.

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Formulation and Development of Gastroretentive Drug Delivery System of Efavirenz

Cited by 2 publications

References 12 publications

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

Novel Swellable/Expandable Gastroretentive Floating Films of Gliclazide Folded in Capsule Shell for the Effective Management of Diabetes Mellitus: Formulation Development, Optimization and In Vitro Evaluation

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