[논문]Effect of Solvents on Physical Properties and Release Characteristics of Monolithic Hydroxypropylmethylcellulose Matrix Granules and Tablets

Cao Qing-Ri; Choi Yun-Woong; Cui Jing-Hao; Lee Beom-Jin

doi:10.1007/bf02977682

Effect of Solvents on Physical Properties and Release Characteristics of Monolithic Hydroxypropylmethylcellulose Matrix Granules and Tablets 원문보기

Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, v.28 no.4, 2005년, pp.493 - 501

Cao Qing-Ri (National Research Laboratory for Bioavailability Control, College of Pharmacy, Kangwon National University, College of Pharmacy, Yanbian University) , Choi Yun-Woong (National Research Laboratory for Bioavailability Control, College of Pharmacy, Kangwon National University, Seoul Pharma Co., LTD.) , Cui Jing-Hao (College of Pharmacy, Yanbian University) , Lee Beom-Jin (National Research Laboratory for Bioavailability Control, College of Pharmacy, Kangwon National University)

Abstract ▼ AI-Helper

Effect of solvents on physical characteristics and release characteristics of monolithic acetaminophen (APAP) hydroxypropylmethylcellulose (HPMC) matrix granules and tablets were examined. Various types and amounts of solvents were employed for granulation and coating. APAP and other excipients were mixed and were then wet-granulated in a high-speed mixer. The dried granules were then directly compressed and film-coated with low viscosity grade HPMC. As the amount of water increased, the size of granules also increased, showing more spherical and regular shape. However, manufacturing problems such as capping and lamination in tableting occurred when water was used alone as a granulating solvent. The physical properties of HPMC matrix granules were not affected by the batch size. The initial release rate as well as the amount of APAP dissolved had a tendency to decrease as the water level increased. Addition of nonaqueous solvent like ethanol to water resulted in good physical properties of granules. When compared to water/ethanol as a coating solvent, the release rate of film-coated HPMC matrix tablets was more sensitive to the conditions of coating and drying in methylene chloride/ethanol. Most of all, monolithic HPMC matrix tablet when granulated in ethanol/water showed dual release with about $50\%$ drug release immediately within few minutes followed by extended release. It was evident that the type and amount of solvents (mainly water and ethanol) were very important for wet granulation and film-coating of monolithic HPMC matrix tablet, because the plastic deforming and fragmenting properties of material were changed by the different strengths of the different solvents.

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제안 방법

After optimizing the effect of solvents for granulation and coatings, release profiles of monolithic HPMC matrix tablet (open symbol) and commercially available bi-lay- ered Tylenol® ER (closed symbol) in four different dissolution media were investigated and compared (Fig. 6). Release profiles of monolithic 너PMC matrix tablets were found to be in good agreement with commercial bi-fay- ered Tylenol® ER.
Particle size distribution of the final dried granules was determined by sieve analysis using a Sifter (Model 35- VSS-300, Kukje Science, Seoul, Korea) equipped with a series of four standard stainless steel sieves (25, 40, 60, and 100 mesh). Approximately 20 g granule samples were sifted for 5 min in triplicate and then the collected particles on each screen were weighed.
The entire granulation process was carried out using a high-speed mixer at impeller speed of 100 rev/min for the production of three different batch sizes of 3000, 50000 or 100000 tablets. The chopper speed was kept constant at 2800 rpm.

대상 데이터

, Osaka, Japan) were obtained from the respective companies. Methylene chloride and ethanol were purchased from Duksan (Seoul, Korea). The commercial bi-layered Tylenol® ER tablet (Janssen Korea, Seo니I, Korea) was purchased as the reference for comparison in the present study.
Two types (Type A and Type B) of coating formulation were used in this study. Coating solution was prepared by continuously dispersing propylene glycol, polyethylene glyco! and low viscosity grade of HPMC (6 cps) in either hydrophobic ethanol/methylene chloride (Type A) or hydrophilic 28% ethanol/5% water (Type B) using a mechanical stirrer for 1 h at room temperature until uniform dispersion was formed.

이론/모형

The surface morphologies of granules were examined by a scanning electron microscope (SEM). In this study, APAP was used as a mod이 drug. ARAP is widely used as a non-prescription, non-narcotic analgesic and antipyretic drug (Walson et al.

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