• Journal of Pharmaceutical Investigation
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• v.33 no.1
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• pp.67-71
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• 2003

Drug excipients are material used in the formulation of pharmacologically active drugs. They have a variety of roles including dilutents/fillers/bulking agents, binders/adhesives, propellant, disintegrants, lubricants/dlidants, colors, flavors, coating agents, polising agents, fragrance, sweeteening agent, polymers and waxes. Excipient should be inert or inactive and does not interfere with the test. Nowadays within industry there has been a recent surge of interest in novel excipient for novel dosage forms. The purpose of the review is to introduce the administration systems of drug excipient about kinds, matters to be attended to change of excipients.

• Journal of Pharmaceutical Investigation
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• v.12 no.3
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• pp.74-87
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• 1982

To evaluate the pharmaceutical aspects of solvent deposition method where drug is solvent deposited on the surface of excipients, a study has been made on dissolution characteristics of indomethacin solvent deposited on lactose and potato starch. In a solvent deposition system, the drug-to-excipient ratio and kind of excipient effect much on dissolution rates of indomethacin. The experimental results are as follows: 1) Lactose was shown to be superior to potato starch as excipients in indomethacin solvent deposited. 2) Total amount of indomethacin dissolved from solvent deposition systems at 30 minutes were enhanced about 5 to 23 times compared with that of pure indomethacin. 3) Increased dissotion amount of indomethacin from the solvent deposition systems were observed to be alike in the systems where the drug-to-excipient weight ratios were 1 : 5, 1 : 7 and 1 : 10.

• Analytical Science and Technology
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• v.34 no.2
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• pp.46-55
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• 2021

Evaluation of drug-excipient compatibility is one of the basic steps in the preformulation of pharmaceutical dosage forms. Some reactive excipients have been known so far which may cause stability problems for drug molecules in pharmaceutical dosage forms. The aim of this study was to evaluate drugexcipient compatibility of gliclazide with some common pharmaceutical excipients, known for their ability to incorporate in drug-excipient interactions. Binary mixtures were prepared using lactose, magnesium stearate, polyvinylpyrrolidone, sodium starch glycolate, polyethylene glycol 2000 and dicalcium phosphate. Based on the results; gliclazide was incompatible with all tested excipients; but not with dicalcium phosphate. DSC (Differential Scanning Calorimetry) results were in accordance with HPLC (High Pressure liquid chromatography) data and were more predictive than FTIR (Fourier Transform Infrared Spectroscopy). Drug and reactive excipients incompatibility was fully discussed and documented. It is advisable to avoid incompatible excipients or carefully monitor the drug stability when incorporating such excipients in final formulation designs.

• Journal of Pharmaceutical Investigation
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• v.15 no.3
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• pp.100-112
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• 1985

Dissolution characteristics of flurbiprofen solvent deposited on ${\alpha}-cyclodextrin$, ${\beta}-cyclodextrin$, lactose and corn starch were studied to evaluate the pharmaceutical aspects of solvent deposition method where drug was solvent deposited on the surface of excipients. In a solvent deposition system, the drug to excipient ratio and kind of excipient affect much on dissolution rates of flurbiprofen. The solvent deposition system formation was confirmed by scanning electron microscope. By increasing the amounts of matrix, it was possible to enhance the dissolution rate of flurbiprofen solvent deposition system. The amount of flurbiprofen dissolved from ${\beta}-cyclodextrin$ deposition system (1:10) at 60 minutes was enhanced 6.5 times in water and 28 times in simulated gastric juice compared with flurbiprofen alone. Flurbiprofen solvent deposited system (1:10) enhanced dissolution rate greater than inclusion complex and dispersion system.

• Journal of Pharmaceutical Investigation
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• v.25 no.1
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• pp.19-29
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• 1995

The study was carried out to develop useful formulation for omeprazole(OMP) through OMP-ethylendiamine complex(OMPED), and the pharmaceutical properties of formula were tested to find out the difference in vivo behaviors of formulations between the free and complexed OMP. Oral and suppository dosage forms were also formulated and the dissolution profiles and pharmacokinetic parameters were measured to observe the difference in bioavailability between the free and complex form, and the correlation between dissolution rate and bioavailability was evaluated. The results are summarized as follows; In the case of formulation for oral administration, the release of OMP from enteric OMPED pellets was found satisfactory to the requirement standard and no decomposition of OMP in the pellets was found in acidic solution. Therefore the enteric OMPED pellets are anticipated to be a stable formulation. The release of OMP from OMPED tablet with chitosan as excipient and coated with cellulose acetate phthalate was found to be significantly retarded. The results of bioavailability test for OMP and OMPED tablets with lactose-excipient showed that the AUC value of OMP tablet was $116.89\;{\mu}g\;{\cdot}\;min/ml$, that of OMPED tablet was $161.10\;{\mu}g\;{\cdot}\;min/ml$, respectively. The reason why was thought that OMP decomposes more readily in body than OMPED, and the AUC of the tablet with chitosan-excipient and coated with cellulose acetate phthalate was most enhanced. In the case of bioavailability for suppositories with OMP, $OMP-{\beta}\;-cyclodextrin$ complex and OMPED, the AUC of OMPED suppository was most increased. From the above results, it is thought that the more stable and bioavailable oral or rectal dosage forms could be developed by using the OMPED as a potential OMP complex.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.21 no.3
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• pp.215-222
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• 2020

Metformin is a recommended first-line therapy drug for type 2 diabetes patients. However, compared to other oral antidiabetic drugs (OAD), metformin has a large unit dosage, with bioavailability of 40-60%. This limiting bioavailability is because metformin is absorbed only in the upper gastrointestinal tract as a BCS class 3 drug. Hence, we propose that applying the Gastroretentive Drug Delivery System (GRDDS) and extending drug release time in the stomach will result in improved bioavailability. We selected the swelling type delivery system, as it is considered the most stable gastroretention technology compared to other GRDDSs. We modified the swelling excipient by using a natural swelling excipient to form a swelling tablet made of carrageenan and hydroxypropyl methylcellulose (HPMC). Our results indicate that the swelling complex tablet made of carrageenan and HPMC has a good swelling ability and shows required sustained release in a dissolution pattern. In addition, the carrageenan complex has a better swelling ability than the marketed metformin tablet, as determined by the ratio, (swelling ability)/(excipient weight). Taken together, our results indicate that the carrageenan complex can be developed as a good swelling excipient. Further optimizations are required for the commercialization of the carrageenan complex.

• Journal of Pharmaceutical Investigation
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• v.36 no.1
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• pp.11-17
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• 2006

The objective of this study was to confirm the effect of the type of dissolution media and paddle speed on nifedipine (ND) release profile from osmotic granule and the storage stability. Osmotic granule was manufactured by fluidized bed coating method. At each coating step, morphology of osmotic granule was differed. The size of osmotic granule was $750\;{\mu}m$ at 3 wt% membrane thickness. ND release was changed in diverse dissolution media, paddle speed. ND release is governed by not only osmotic pressure but diffusion from osmotic granule. ND release from osmotic granule decreased as storage period increased. These may be caused by liquid excipient which has low molecular weight. Storage stability of osmotic granule could be improved by removing liquid excipient from semipermeable membrane.

• YAKHAK HOEJI
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• v.31 no.3
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• pp.189-196
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• 1987

This study was carried out to investigate the effect of surfactant on the dissolution of relatively hydrophilic drugs, such as sulfanilamide (SF) and sulfacetamide (SFA) granules prepared by wet granulation. The additive incorporated in the granules is starch or microcrystalline cellulose(MCC) as an excipient, PVP as a binder, and polysorbate 80 (P-80) as a surfactant. The dissolution characteristics of SF and SFA granules in distilled water were as follows: The values of T$_{75%}$ were 4.60 and 2.50min, respectively for SF and SFA granules. Incorporation of 0.1% P-80 in SF granule ratarded the dissolution of SF as compared with control, but addition of 0.1% P-80 to SFA granule improved the dissolution of SFA in comparison with control. In SF and SFA granules formulated with either starch or PVP, the release of the drug was increased as compared with control. In SF granule, the dissolution of the drug was further reduced by the inclusion of P-80 in the granule containing starch or PVP. Incorporation of P-80 in SFA granule with starch or PVP affected little on the dissolution of the drug. Addition of a nonswelling excipient, MCC decreased the dissolution rate of SF and SFA granules. as compared with each control. The presence of P-80 in these granules made the dissolution rate slower in comparison with the granules containing only MCC.

• Environmental Engineering Research
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• v.23 no.3
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• pp.258-264
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• 2018

The objectives of this research were to 1) isolate and identify thermophilic bacteria for food waste treatment; 2) investigate the capability of food waste treatment using Bacillus species; and 3) develop air-dried Bacillus starters for food waste treatment. Five Bacillus species were isolated from food wastes and identified as Bacillus licheniformis (B. licheniformis) G1, Bacillus circulans C2, Bacillus subtilis (B. subtilis) E1, Bacillus vanillea F1, and Bacillus atrophaeus G2 based on 16S rDNA sequencing. Each identified Bacillus and the mixture of Bacillus species were cultivated in the standard food waste at $45^{\circ}C$ for 8 d. Changes in cell count, solid contents, and pH of the food waste were monitored during cultivation. Air-dried Bacillus cell powders were prepared using wheat flour and lactomil as excipients, and the cell count and survival rate were determined. The cell count of B. licheniformis G1 exhibited the highest number among the tested Bacillus (${\sim}10^8CFU/mL$). The greatest reduction in solid contents of food waste was achieved by B. subtilis E1 (22.6%). The mixture of B. licheniformis G1 and B. subtilis E1 exhibited a synergistic effect on the reduction of solid contents. Lactomil was determined as better excipient than wheat flour based on the greatest survival rate of 95%.

• Asian-Australasian Journal of Animal Sciences
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• v.12 no.7
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• pp.1096-1103
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• 1999

A study was conducted to clarify the impact of recombinant porcine somatotropin (pST) on the efficiency of absorbed nitrogen use for protein deposition in growing pigs. Three levels of dietary crude protein (9.0, 11.5, 14.0% CP) were used. Each had either a sub-optimum or near optimum lysine: CP concentration (Low-lysine, 3.8 g/100 g CP and High-lysine, 5.5 g/100g CP) in order to achieve different metabolic efficiencies for nitrogen deposition (ca. 45 vs. 60%). Twelve crossbred female pigs $(59{\pm}4kg\;BW)$ were placed in metabolism cages and fitted with bladder catheters. Each pig received an excipient injection daily for the first 10-d, a pST (5 mg/d) injection for the second 10-d, and then excipient for the last 10-d. Pigs were randomly assigned to one of six dietary treatments (2 pigs/diet) and fed 4 times per d at $92g/kg\;BW^{0.75}$ $(3{\times}maintenance)$. Means for the excipient period were compared to means for the pST period. Urinary nitrogen (N) output declined in pST-treated pigs (p<0.01) irrespective of dietary protein content or lysine level. Nitrogen retention increased by an average of 11% (p<0.01) with pST treatment (726 vs. $803mg\;N/kg^{0.75}\;BW/d$). Forty-eight percent of the absorbed N was retained with Low-lysine diets, but this increased to 53% with pST injection (+11%, p<0.01). Pigs fed High-lysine diets retained 62% of absorbed N which increased to 69% with pST (+11% p<0.01). the addition of lysine improved N use by 27% (High vs. Low, p<0.01), but the effect of lysine and pST was additive (+40%). Therefore, pST improves N retention and the efficiency of apparently absorbed N use in growing pigs (>60kg). It does so with diets having the potential for either low or high efficiencies of N use (48% and 62%). More work is needed to determine if the partial efficiency of N use improves in direct proportion to pST dose since the improvement in protein deposition is a function of pST dose.