Preformulation Study of Glimepiride: An Insight for Formulation  and Development of Parenteral Formulation

Patel, Chirag; Suthar, Disha; Patel, Hetal; Movaliya, Vinit; Parejiya, Punit B.

doi:10.9734/jpri/2022/v34i15b35718

Cited by 3 publications

(5 citation statements)

References 5 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The absorption maxima was obtained to be 224.0 nm and was used to measuring the absorbance of glimepiride in solutions throughout the study. In previous studies the absorption maxima have been reported to be 225 nm 50 , 228 nm 57 and 236 nm 58 .…”

Section: Uv Absorption Spectra Of Glimepiridementioning

confidence: 82%

Formulation and Characterization of Blend Microspheres of Anti Diabetic Drug Glimepiride

2023

IJFMR

View full text Add to dashboard Cite

The objective of the present investigation was to prepare polymeric blend microspheres of glimepiride for improving its half-life using chitosan and gelatin as the two polymers for preparing the blend. The blend microspheres of chitosan and gelatin were prepared by using different ratios of both the polymers as well as cross-linking agent, glutaraldehyde (GA), by emulsion cross-linking method. The optimum formulation was one which exhibited the lowest particles size and it was used to load glimepiride (20% by weight) of the polymers. The glimepiride loaded blend microspheres were evaluated for yield, drug polymer interaction, entrapment efficiency, surface study and in vitro release. The particle size of the blend microspheres was found to be in the range of 126.8 µm to 371.3 µm. The lowest particle size (126.8 ± 6.11 µm) was obtained in AF5 containing 50% of gelatin and 50% of chitosan. The FTIR spectra of the physical mixture of glimepiride, gelatin and chitosan displayed all the characteristic peaks of glimepiride, thus indicating that no incompatibility was present between the drug and the polymer. The SEM image of the drug loaded blend microsphere revealed spherical particles of irregular size with smooth surface. The average particles size of the glimepiride loaded blend microspheres was obtained to be 131.4 ± 9.7 µm with a yield of 91.6% by weight of the drug and polymers used for formulation of the microspheres. It was found that 82.4 ± 6.8% of glimepiride was found to be entrapped in the particles. The results of the in vitro release studies of the glimepiride loaded blend microsphere revealed that 71.49 ± 0.74 % glimepiride was released from the particles at the end of 12th hour of study.

show abstract

Section: Uv Absorption Spectra Of Glimepiridementioning

confidence: 82%

Formulation and Characterization of Blend Microspheres of Anti Diabetic Drug Glimepiride

2023

IJFMR

View full text Add to dashboard Cite

show abstract

“…This indicated that glimepiride is a crystalline material that melts sharply upon heating. Table 3 presents data on thermal transitions, melting points, and thermal degradations of drug, PVP K-90, PVA, and Soluplus ® [ 27 ]. The physical mixture of glimepiride and its excipients exhibited a noticeable shift in the melting point, indicating enhanced thermal stability and preventing drug degradation at 205 °C, as evident from the thermogram illustrated in above Figure 9 b.…”

Section: Resultsmentioning

confidence: 99%

“…Two mg GM was mixed with each of the components (PVA, PVP, and Soluplus ® ) at an appropriate ratio, equivalent to that used in the formulation. The spectra of the pure GM, Soluplus ® , PVA, and PVP K-90 and their physical mixture were analyzed by scanning across a frequency span ranging from 4000–400 cm −1 [ 27 ].…”

Section: Methodsmentioning

confidence: 99%

Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles

et al. 2023

View full text Add to dashboard Cite

Glimepiride (GM) is a hydrophobic drug that dissolves slowly and yields inconsistent clinical responses after oral administration. Transdermal drug delivery (TDD) is an appropriate alternative to oral administration. Microneedles (MNs) offer a promising delivery system that penetrates the skin, while polymeric micelles can enhance the solubility; hence, the combination of both results in high drug bioavailability. This study aims to improve glimepiride’s solubility, dissolution rate, and bioavailability by incorporating nanomicelles into MNs for TDD. The nanomicelles formulated with 10% Soluplus® (SP) and 40% GM had a mean particle size of 82.6 ± 0.54, PDI of 0.1 ± 0.01, −16.2 ± 0.18 zeta potential, and achieved a 250-fold increase in solubility. The fabricated pyramid shaped GM-dissolving MNs were thermally stable and had no formulation incompatibility, as confirmed by thermal and FTIR analysis. The in vitro dissolution profile revealed that the GM release from nanomicelles and nanomicelle-loaded DMN was concentration-independent following non-Fickian transport mechanism. Improved pharmacokinetic parameters were obtained with dose of 240 µg as compared to 1 mg of GM oral tablet, in healthy human volunteers. The observed Cmax, Tmax and MRT were 1.56 μg/mL ± 0.06, 4 h, and 40.04 h ± 3.37, respectively. The safety profile assessment indicated that microneedles are safe with no adverse effects on skin or health. This study provides an alternative delivery system for the administration of glimepiride, resulting in improved bioavailability, enhanced patient compliance, and reduced dosing frequency.

show abstract

“…The moisture uptake measurement is done by Karl Fischer titration, Thermogravimetric analysis (TGA), and gas chromatography techniques. As per European Pharmacopoeia, four separate grades of hygroscopicity are defined when a drug substance is stored at 80% relative humidity and a temperature of 25°C for 24 h. The four classes of hygroscopicity are described here as per the above-mentioned storage conditions [48,49].…”

Section: Hygroscopicity and Deliquescencementioning

confidence: 99%

“…The active metabolite hydrocortisone is produced when prednisolone and cortisone are reduced. Azo dyes are used as colouring additives in drug products or food items and this can be degraded by liver and intestinal flora to create amines [48].…”

Section: Reductionmentioning

confidence: 99%

Preformulation Studies: A Versatile Tool in Formulation Design

Ahirwar¹,

Shukla²

2023

Drug Formulation Design

View full text Add to dashboard Cite

The physicochemical properties of pharmacological molecules have a tremendous effect on safety and efficacy. Poor physicochemical properties can often make it hard to set up a reliable structure-activity relationship (SAR) with no prominent efficacy in preclinical and clinical models. This can lead to more variability in capability and higher drug development costs in the entire development process, and in the worst case, even to stop the clinical trials in the later period. Understanding the basic physicochemical properties makes it possible to separate and untangle investigational observations hence poor molecular properties can be changed or fixed during the design phase. This makes it more likely that the molecule will make it through the long and difficult development process. The decline in innovator pharmacotherapeutics number registrations decline each year and the industry is under even more pressure than in the past to speed up the drug development process. This reduces the length of time required for development and introduces innovative pharmaceutical products. To do this, it is imperative to proceed with an organised approach and act appropriately the first time. The current chapter aims to focus on the important physicochemical properties of the selected molecule, along with how those properties are evaluated and implicated in both discovery enablement and final dosage form development.

show abstract

Preformulation Study of Glimepiride: An Insight for Formulation and Development of Parenteral Formulation

Cited by 3 publications

References 5 publications

Formulation and Characterization of Blend Microspheres of Anti Diabetic Drug Glimepiride

Formulation and Characterization of Blend Microspheres of Anti Diabetic Drug Glimepiride

Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles

Preformulation Studies: A Versatile Tool in Formulation Design

Contact Info

Product

Resources

About