Preparation of Buccal Patch Composed of Carbopol, Poloxamer and Hydroxypropyl Methylcellulose

Chun, Myung-Kwan,Kwak, Byoung-Tae,Choi, Hoo-Kyun The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.11

A polymeric film composed of Carbopol, Poloxamer and hydroxypropyl methylcellulose was prepared to develop a buccal patch and the effects of composition of the film on adhesion time, swelling ratio, and dissolution of the film were studied. The effects of plasticizers or penetration enhancers on the release of triamcinolone acetonide (TAA) were also studied. The hydrogen bonding between Carbopol and Poloxamer played important role in reducing swelling ratio and dissolution rate of polymer film and increasing adhesion time. The swelling ratio of the composite film was significantly reduced and the adhesion time was increased when compared with Carbopol film. As the ratio of Poloxamer to hydroxypropyl methylcellulose increased from 0/66 to 33/33, the release rate of TAA decreased. However, no further significant decrease of release rate was observed beyond the ratio of 33/33. The release rate of TAA in the polymeric film containing polyethylene glycol 400, a plasticizer, showed the highest release rate followed by triethyl citrate, and castor oil. The release rate of TAA from the polymeric film containing permeation enhancers was slower than that from the control without enhancers. Therefore, these observations indicated that a preparation of a buccal patch is feasible with the polymeric film composed of Cabopol, Poloxamer and hydropropyl methylcellulose.

실란처리된 하이드록시프로필 메틸셀룰로오스/상전이된 칼슘포스페이트 복합체 골시멘트의 제조 및 특성평가

정나현,김동현,조훈상,윤석영,Jeong, Nahyun,Kim, Dong-Hyun,Cho, Hoon-Sang,Yoon, Seog-Young 한국결정성장학회 2016 한국결정성장학회지 Vol.26 No.6

Silanized-hydroxypropyl methylcellulose (Si-HPMC)/phase transformed calcium phosphate (PTCP) composites are prepared to purpose application of injectable bone cements with enhanced biocompatibility. The crystal structure and chemical state of the synthesized PTCP and Si-HPMC as solid and liquid phase of the composite cements were measured by XRD and FT-IR. The handling and mechanical properties of cements were measured by injectability tests and three-point bending tests. The in-vitro mechanical properties, XRD, and SEM results of bone cements were showed that enhanced hardening behavior was an inherent function of bone cements after in-vitro test. The cytotoxicity result of bone cements also was showed enhanced biocompatibility. Therefore, these injectable cements had potential be used as calcium phosphate cements for biomedical applications. 실란처리된 하이드록시프로필 메틸셀룰로오스/상전이된 칼슘포스페이트 복합체 시멘트는 향상된 생체적합성을 가지는 주입이 가능한 골시멘트로서 제조 되었다. 복합체 시멘트의 고체상과 액체상으로서 상전이된 칼슘포스페이트와 실란처리된 하이드록시프로필 메틸셀룰로오스의 결정구조 및 화학적 상태는 XRD 및 FT-IR에 의해 측정 되었고, 시멘트의 조작성 및 기계적 물성은 주입성 및 3점 굽힘 시험에 의해 측정하였다. 체외에서 진행된 골시멘트의 기계적 물성, XRD 및 SEM 결과는 골시멘트의 고유 기능으로서의 향상된 경화거동을 보였다. 또한 골시멘트의 세포독성 결과 향상된 생체적합성을 보였다. 따라서 이러한 주입이 가능한 시멘트는 생체의학 응용에 대한 칼슘포스페이트 시멘트로서 사용이 가능하리라 판단되어진다.

Hydroxypropyl methylcellulose를 활용한 비타민 C 지속성 정제의 용출 특성 분석

차자현(Ja Hyun Cha),홍준기(Jun Kee Hong),이성완(Sung Wan Lee),차재욱(Jae Uk Cha),고원화(Won Hwa Ko),백현호(Hyon Ho Baek),박현진(Hyun Jin Park) 한국식품과학회 2012 한국식품과학회지 Vol.44 No.3

본 연구에서는 널리 사용되는 수용성 비타민인 비타민 C의 지속성 특성을 발현시키기 위해 HPMC를 사용하여 정제를 제조하였다. 먼저 비타민 C 지속성 정제의 효과적인 용출실험을 진행하기 위해서 용출 용매에 비타민 C의 산화를 방지할 수 있는 항산화제를 첨가함으로써 수분에 의한 비타민 C의 분해를 방지하였다. 비타민 C 지속성 정제의 용출 거동을 확인하기 위해「대한약전 9개정」과「경구용의약품의 용출규격 설정 가이드라인」의 용출시험법과「건강기능식품이 기준 및 규격 고시전문(제2009-153호)」에 근거하여 함량시험과 시간별 용출률을 분석하였다. 분석된 용출 거동은 zero-order release model과 Korsmeyer-Peppas model에 의해 겔 내에서의 활성 성분의 확산과 겔층의 소실로 인한 이의 유리 메카니즘이 분석되었다(37,38). 비타민 C 지속성 정제에 사용된 지속성 HPMC의 사용량이 증가할수록 위장관 운동의 영향에 관계없는 zero-order release의 용출 거동에 가까워짐을 확인하였다. 이는 정제에 사용된 HPMC의 사용량이 높을수록 물을 흡수하여 초기에 겔을 형성하는 속도가 빨라져 용출 속도가 감소함을 보여준다. 점도에 따른 차이는 비타민 C의 높은 수용성 성질 때문에 차이를 보이지 않았으나, 난용성 유효 성분을 적용한 처방에서는 수화능과 겔 형성능에 따라 점도별로 차이가 날것으로 사료된다. 이는 Korsmeyer-Peppas model에 의한 메커니즘분석에서 비타민 C의 겔 내 활성 성분의 확산이 겔 층의 소실로 인한 유리보다 다소 우세한 것으로 설명될 수 있다. 이러한 결과를 바탕으로 비타민 C는 수분에 대한 안정성이 부족함에도 지속성 정제로의 개발 및 용출분석이 가능하며, 지속성 고분자로 사용된 HPMC의 사용량에 따라 용출 거동을 조절할 수 있어 1일 2회 내지 1일 1회 요법의 비타민 C 지속성 정제의 제제화와 안정적인 용출분석을 수행할 수 있다. 건강기능식품에 고시된 비타민 C의 정량법인 HPLC법 및 본 연구를 통해 차이가 없음이 확인된 UV spectrophotometer를 사용한 평가방법을 통해 보다 편리하게 수행할 수 있다. The objective of this study was to develop oral matrix tablets for the sustained release of vitamin C. In this study hydroxypropyl methylcellulose (HPMC) has been utilized as an excipient, as it is one of the most widely used polymers, for use during long periods of time in formations. The vitamin C tablet formulation depends on the molecular weight and concentration of sustained-delivery in HPMC. Anti-oxidants have been added as a dissolution medium in order to prevent vitamin C degradation in water. The dissolution test was carried out in a distilled water medium, and the release model equation was applied to analyze the vitamin C release pattern. The results demonstrated that the release and lasting power of vitamin C tablets, containing HPMC, lasted for more than 12 h.

Hydroxypropyl Methylcellulose-graft-Poly(ethyl acrylate-co-methyl methacrylate) Particles by Resin-fortified Emulsion Polymerization

백현호,이정민,조지은,조진훈,김중현,정인우 한국고분자학회 2010 Macromolecular Research Vol.18 No.1

This article describes the preparation and characterization of hydroxypropyl methylcellulose-graftpoly(ethylacrylate-co-methyl methacrylate) particles [HPMC-g-poly(EA-co-MMA) NPs]. The particles were prepared by resin-fortified emulsion polymerization using ceric ammonium nitrate (CAN). In this study, a series of HPMC-g-poly(EA-co-MMA) NPs were synthesized by varying the CAN : HPMC and HPMC : (EA/MMA) ratios to determine the effects of these variables on the physical properties of HPMC-g-poly(EA-co-MMA) as well as the dissolution behavior of an aspirin tablet, as a model drug. The drug dissolution profiles of the coated tablets were affected significantly by the HPMC : (EA/MMA) molar ratio.

발사르탄 고체 분산체를 함유하는 위체류 매트릭스 부유 정제의 개발 및 평가

조영호(Young Ho Cho),이종화(Jong-Hwa Lee),이계원(Gye Won Lee) 한국생물공학회 2016 KSBB Journal Vol.31 No.4

Valsartan, a drug for the treatment of cardiovascular disease, exhibited low bioavailability which was caused by, at least in part, limited solubility at low pH. Present investigation deals with the preparation and characterization of gastro-retentive drug delivery system (GRDDS) using valsartan solid dispersion. We prepared solid dispersion using surfactants (Poloxamer 407) and alkalizer (Na₂CO₃) which may to be useful for improving solubility of valsartan at low pH and evaluated by saturated solubility of valsartan in distilled water. Valsartan gastro-retentive (GR) tablets containing solid dispersion prepared and evaluated by weight variation, floating time and dissolution rate. Compression at lower pressures resulted in the tablets floating over simulated gastric fluid (pH 1.2) for more than 17 h. In vitro release of valsartan from GR tablet was dependent on the amount of poloxamer 407 and hydroxypropyl methylcellulose. On the basis of evaluation parameter, formulation E-3 was selected as a final formulation. Therefore, it can be concluded that the GR tablets containing solid dispersion may be exploited successfully for the delivery of poorly drug such as valsartan.

Amphiphilic adhesive mechanism of Hydroxypropyl methylcellulose

임찬웅,송영훈,서정현,황동수,이동욱 한국공업화학회 2020 한국공업화학회 연구논문 초록집 Vol.2020 No.-

Hydroxypropyl methylcellulose (HPMC), a FDA approved water-soluble cellulose derivative, has played as a binder in a variety of applications in construction products, paints, and drug delivery. In spite of these many applications of HPMC as a binder, its adhesion mechanism is not well understood. In this study, we measured adhesion characteristics of HPMC in different hydrophobicity, water content, and temperature. The adhesion of HPMC were not affected by surface hydrophobicity in both bulk compression test and nano-mechanical test by surface forces apparatus, but strongly influenced by temperature and water content. The results indicate water content and temperature are critical variable for the adhesion of HPMC to inorganic surfaces. As adhesive and coating technologies have shifted towards environmentally friendly systems, these results provide a starting point for the fabrication of HPMC-based composites for a variety of future applications.

Antihyperglycemic and Antioxidative Effects of Hydroxyethyl Methylcellulose (HEMC) and Hydroxypropyl Methylcellulose (HPMC) in Mice Fed with a High Fat Diet

Ban, Su Jeong,Rico, Catherine W.,Um, In Chul,Kang, Mi Young Molecular Diversity Preservation International (MD 2012 INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES Vol.13 No.3

<P>The effect of dietary feeding of hydroxyethyl methylcellulose (HEMC) and hydroxypropyl methylcellulose (HPMC) on the glucose metabolism and antioxidative status in mice under high fat diet conditions was investigated. The mice were randomly divided and given experimental diets for six weeks: normal control (NC group), high fat (HF group), and high fat supplemented with either HEMC (HF+HEMC group) or HPMC (HF+HPMC group). At the end of the experimental period, the HF group exhibited markedly higher blood glucose and insulin levels as well as a higher erythrocyte lipid peroxidation rate relative to the control group. However, diet supplementation of HEMC and HPMC was found to counteract the high fat-induced hyperglycemia and oxidative stress via regulation of antioxidant and hepatic glucose-regulating enzyme activities. These findings illustrate that HEMC and HPMC were similarly effective in improving the glucose metabolism and antioxidant defense system in high fat-fed mice and they may be beneficial as functional biomaterials in the development of therapeutic agents against high fat dietinduced hyperglycemia and oxidative stress.</P>

Synthesis and Characterization of HPMC Derivatives as Novel Duodenum-Specific Coating Agents

Yuan Huang,ling-li Zheng,Jun Liu,Zhi-rong Zhang 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.3

HPMC (Hydroxypropyl methylcellulose) was chemically modified, using maleic anhydrides, to obtain pH-sensitive HPMCAM (Hydroxypropyl methylcellulose acetate maleate) polymers for use as novel duodenum-specific coating agents. The pharmaceutical properties of HPMCAM, such as film forming, acid values, pH-sensitive values, water vapor permeability, tensile strength and Tg, were investigated, and found to show good film forming properties. The pHsensitive values were 3.0 to 3.7. In vitro results demonstrate that HPMCAM could completely suppress drug release within 2h in a simulated gastric fluid (pH 1.2) and rapidly release the drug in a simulated pathological duodenal fluid (pH 3.4). These results indicate that HPMCAM might be a useful material for a duodenum-specific drug delivery system.

Utilization of foam structured hydroxypropyl methylcellulose for oleogels and their application as a solid fat replacer in muffins

Oh, Im Kyung,Lee, Suyong IRL Press 2018 Food hydrocolloids Vol.77 No.-

<P><B>Abstract</B></P> <P>Hydroxypropyl methylcellulose (HPMC) was utilized to structure sunflower oil into solid-like oleogels by generating foaming-templates and the feasibility of HPMC oleogels as a shortening replacer in muffins was evaluated in terms of physical, rheological, and tomographical properties. Sunflower oil was successfully converted into a solid form with the assistance of foam-structured HPMC. The resultant oleogels and their blends with shortening rheologically behaved as elastic gels. The replacement of shortening with HPMC oleogels produced muffin batters with lower viscosity and less shear-thinning behavior. The viscoelastic measurements also showed greater contribution of HPMC oleogels to the viscous nature of muffin batters. While the specific gravity of batter had a tendency to increase with increasing replacement levels of shortening, the specific volume of baked muffins was not significantly reduced at shortening replacement levels of up to 50%. Furthermore, the X-ray micro-computed tomographic analysis demonstrated that air cells were much larger in size and inhomogeneously distributed in the muffins prepared with HPMC-oleogels. The shortening replacement with HPMC oleogels at up to 50% by weight did not negatively contribute to the soft and chewy texture of the muffins. These results demonstrated that HPMC oleogels could be effective in replacing shortening at up to 50% without significant deterioration in the quality attributes of muffins.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Foam structured HPMC was successfully used to structure sunflower oil into oleogel. </LI> <LI> HPMC oleogel as a fat replacer reduced viscosity/viscoelasticity of muffin batters. </LI> <LI> Lower pore size uniformity and larger pore size were observed in HPMC oleogel-muffins. </LI> <LI> Shortening replacement with HPMC oleogel at up to 50% did not affect muffin qualities. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Examination of thermo-gelation behavior of HPMC and HEMC aqueous solutions using rheology

Yoo, Young Jin,Um, In Chul 한국유변학회 2013 Korea-Australia rheology journal Vol.25 No.2

In this study, the thermo-gelation behavior of hydroxypropyl methylcellulose (HPMC) and hydroxyethyl methylcellulose (HEMC) were examined by rheology. Temperature sweep shear viscosity measurements revealed a significant decrease in the shear viscosity of HPMC and HEMC at the aggregation temperature ($T_{agr}$), which depended on the substitution type (HPMC or HEMC) and degree of substitution. In the dynamic test, G' decreased slightly at $T_{agr}$ and increased significantly at the gelation temperature ($T_{gel}$). The shear viscosity and shear storage modulus (G') can be utilized complementarily to examine $T_{agr}$ and $T_{gel}$. $T_{agr}$ could be detected clearly by the shear viscosity measurement but could not be observed in the G' measurement. On the other hand, $T_{gel}$ could not be detected in the shear viscosity measurement although it can be clearly recognized in G' measurement. Conclusively, the two rheological measurements could be utilized complementarily in detection of $T_{agr}$ and $T_{gel}$. In the meanwhile, HPMC with more hydrophobic residues (methoxy and hydroxypropyl residues) showed smaller $T_{agr}$ and $T_{gel}$ than HEMC, which has hydroxyethyl and methoxy groups. $T_{agr}$ and $T_{gel}$ decreased with increasing number of hydrophobic groups. Molecular weight almost did not affect $T_{agr}$ and $T_{gel}$ of HPMC solution.