Preparation and evaluation of gelling granules to improve oral administration

A self-nanoemulsifying drug delivery system (SNEDDS) was developed to enhance the absorption of heparin after oral administration, in which heparin was compounded with phospholipids to achieve better fat solubility in the form of heparin-phospholipid (HEP-Pc) complex. HEP-Pc complex was prepared using the solvent evaporation method, which increased the solubility of heparin in n-octanol. The successful preparation of HEP-Pc complex was confirmed by differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR) spectroscopy, NMR, and SEM. A heparin lipid microemulsion (HEP-LM) was prepared by high-pressure homogenization and characterized. HEP-LM can enhance the absorption of heparin after oral administration, significantly prolong activated partial thromboplastin time (APTT) and thrombin time (TT) in mice, and reduce fibrinogen (FIB) content. All these outcomes indicate that HEP-LM has great potential as an oral heparin formulation.

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Preparation and evaluation of BSA-based hydrosol nanoparticles cross-linked with genipin for oral administration of poorly water-soluble curcumin

International Journal of Biological Macromolecules ◽

10.1016/j.ijbiomac.2017.06.083 ◽

2017 ◽

Vol 104 ◽

pp. 788-798 ◽

Cited By ~ 15

Author(s):

Narges Shahgholian ◽

Ghadir Rajabzadeh ◽

Bizhan Malaekeh-Nikouei

Keyword(s):

Oral Administration ◽

Water Soluble ◽

Poorly Water Soluble ◽

Preparation And Evaluation

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Preparation and Evaluation of Antidiabetic Agents of Berberine Organic Acid Salts for Enhancing the Bioavailability

Molecules ◽

10.3390/molecules24010103 ◽

2018 ◽

Vol 24 (1) ◽

pp. 103 ◽

Cited By ~ 5

Author(s):

Hong-Xin Cui ◽

Ya-Nan Hu ◽

Jing-Wan Li ◽

Ke Yuan ◽

Ying Guo

Keyword(s):

Oral Administration ◽

Organic Acid ◽

Intestinal Tract ◽

Intestinal Flora ◽

Pharmacological Effects ◽

Antidiabetic Agents ◽

Hypoglycemic Agent ◽

Preparation And Evaluation ◽

Organic Acid Salts ◽

Acid Salts

Berberine has many pharmacological effects, such as antidiabetic, antimicrobial, anti-inflammatory, and antioxidant, but the question remains on how its low oral bioavailability has greatly limited its clinical application. As a safer hypoglycemic agent, we must evaluate the bioavailability of berberine organic acid salts (BOAs) to ensure that the bioavailability of berberine is not negatively affected. It has been proven that the bioavailability of BOAs is higher than that of BH (berberine hydrochloride); especially BF (berberine fumarate) and BS (berberine succinate), which are improved by 1.278-fold and 1.313-fold, respectively. After 1 h of oral administration, berberine mainly acted on the stomach of mice, it also influenced the liver, kidney, lungs, and intestines after 4 h. The accumulation of BF in the lung is more evident than BH. Our analysis shows that these results are closely related to the regulation of organic acids and berberine in the intestinal tract, they also indicate the influence of intestinal flora on berberine metabolism.

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Preparation and Evaluation of Spray-Dried Nano-Hydroxyapatite/Saccharide Complex for Oral Administration

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.782.124 ◽

2018 ◽

Vol 782 ◽

pp. 124-128

Author(s):

Yuya Honda ◽

Yuji Rin ◽

Hideki Aoki ◽

Takayuki Terukina ◽

Yusuke Hattori ◽

...

Keyword(s):

Oral Administration ◽

Phosphoric Acid Solution ◽

Particle Sizes ◽

Composition And Structure ◽

Plate Shape ◽

Rate Test ◽

Main Component ◽

Preparation And Evaluation ◽

Complex Powder ◽

Spray Dried

nanohydroxyapatite (nanoHA) is a main component of bone and dentin. The nanoHA was synthesized by a neutralization reaction of calcium hydroxide suspension and phosphoric acid solution. The sizes of the nanoHA were in the range of 5-80 nm. The composition and structure of the nanoHA was determined by XRD and FTIR as hydroxyapatite containing small amounts of carbonate. The morphology of the nanoHA was observed by TEM as plate shape. Saccharides including dextrin, lactose and glucose were mixed into the nanoHA suspension and dried by a spray dry method to produce a complex powder for oral administration. The particle sizes of the complex were in the range of 10-20 μm. The dispersibility of the complex in water was examined by a precipitation rate test and the order was as follows: glucose > dextrin > lactose complex.

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