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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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The high insolubility of some precipitates can result in an unfavorable relative supersaturation. This can lead to colloidal particles with a large surface-to-mass ratio, where adsorption is promoted. For instance, in the precipitation of silver chloride, silver ions are adsorbed on the surface of the colloidal particles, forming a primary layer. This layer attracts ions of opposite charge (such as nitrate ions), forming a diffuse secondary layer of adsorbed ions. This electric double layer...
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Polymers Enhance Chlortetracycline Hydrochloride Solubility.

Chao Zhang1,2, Bing Li2, Yubin Bai2

  • 1College of Veterinary Medicine, Gansu Agricultural University, Anning District, Lanzhou 730070, China.

International Journal of Molecular Sciences
|October 16, 2024
PubMed
Summary

Chlortetracycline hydrochloride (CTC) solid dispersions were developed using polymers to enhance solubility and stability. Gelatin-based solid dispersions showed improved dissolution and particle characteristics, offering potential for drug delivery.

Keywords:
characterizationchlortetracycline hydrochloridegelatinhydroxypropyl-β-cyclodextrinpovidone K30solid dispersionsolubility

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Chlortetracycline hydrochloride (CTC) is a broad-spectrum antibiotic with limited clinical use due to poor solubility, stability, and bioavailability.
  • Developing effective drug delivery systems is crucial for improving the therapeutic efficacy of poorly soluble compounds like CTC.

Purpose of the Study:

  • To enhance the solubility, dissolution rate, and stability of chlortetracycline hydrochloride (CTC).
  • To develop novel solid polymer dispersions of CTC using various hydrophilic polymers and characterize their properties.

Main Methods:

  • Solid dispersions of CTC were prepared using a medium grinding method with hydrophilic polymers like povidone K30 (PVPK30), hydroxypropyl-β-cyclodextrin (HP-β-CD), and gelatin.
  • Characterization involved scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FT-IR), and particle size distribution (PSD).
  • In vitro dissolution studies were conducted to evaluate the drug release profiles.

Main Results:

  • Optimized solid dispersions significantly increased CTC solubility: PVPK30 (6.25-fold), HP-β-CD (7.7-fold), and gelatin (3.75-fold) compared to pure CTC.
  • Gelatin-based solid dispersions exhibited a higher initial dissolution rate and smaller, more uniform particle sizes.
  • Characterization techniques confirmed successful formation of solid dispersions and improved physical properties.

Conclusions:

  • Solid polymer dispersions effectively improved the solubility, dissolution rates, and stability of chlortetracycline hydrochloride.
  • The developed solid dispersions, particularly the gelatin-based formulation, show promise as advanced drug delivery systems for CTC.
  • Further investigation into these solid dispersions could lead to improved clinical applications of chlortetracycline hydrochloride.