Study on Enteric Vacant Capsules Based on Hydroxypropyl Methylcellulose Phthalate-55S

The formulation and preparation technology of enteric cellulose hollow capsules were studied, and its properties were evaluated. The enteric cellulose hollow capsules were prepared with hydroxypropyl methylcellulose phthalate~55S (Hp55S) as film~forming material, agar as molding agent and hydroxypropyl methylcellulose (HPMC) as disintegration regulator. The preparation process was as follows: (1) At room temperature, 9~16 phr of Hp55S was dissolved in 30~50 phr of dilute ammonia solution with pH of 10~11 to obtain transparent Hp55S glue solution; (2) Put 1.2~1.6 parts of agar into 50~70 parts of water, heat and boil to obtain agar solution. 1~7 phr of HPMC, 0.12~0.16 phr of KCl and 0.1~0.2 phr of Tween~80 were poured into agar solution to disperse evenly, and then the temperature of gel solution was reduced to 50~55 oC to obtain agar/HPMC mixed gel solution; (3) The Hp55S solution was heated to 50~55 oC and then poured into agar/HPMC solution to obtain composite cellulose solution. The temperature of the solution was kept at 50~55 oC. (4) Enteric cellulose hollow capsules were prepared by dipping in glue, shaping, drying, trimming and assembling. The results showed that the enteric cellulose hollow capsules met the quality requirements of “enteric coated hollow capsules” in Chinese Pharmacopoeia. Compared with the traditional formula and preparation process of enteric coated hollow capsules, it avoids the use of organic solvents and multiple molding process. The enteric cellulose hollow capsule greatly reduces the preparation cost from the formula to the process, which is green, safe and environmental friendly, and has good application value.

FORMULATION AND EVALUATION OF NOVEL CHROMENE DERIVATIVE AS AN ANTI INFLAMMATORY AGENT USED FOR IBD

Objective: To formulate and evaluate an extended-release (ER) tablet of a new molecule, 2-amino-4-(4-bromophenyl)-7-hydroxy-4H-chromene-3- carbonitrile using a combination of two polymers (hydroxypropyl methyl cellulose [HPMC] K100 and HPMC phthalate) which control the rate and degree of the drug release through 12 hrs period and protect the drug release from acidic pH.Methods: Five batches of tablets (4HC1, 4HC2, 4HC3, 4HC4, 4HC5) were produced by direct compression method. Morphological evaluation of the powder blend was carried out by differential scanning calorimetry and Powered X-ray diffractometry. The evaluation studies such as flow properties, hardness, friability, drug content, and release study were conducted according to pharmacopoeial standards.Results: The physicochemical characteristics of all the granules and tablets were generally satisfactory. The drug release followed zero order, Higuchi model kinetics with diffusion and dissolution mediated mechanism. Tablets were evaluated for physicochemical parameters and promising. Stability studies indicated the dosage form is stable for 3 months at accelerated conditions.Conclusion: From the results received from all test, it was concluded that formulation 4HC4 are the most suitable choice for developing 12 hrs ERtablets. This finding reveals that a particular concentration of HPMC K100 was capable of producing ER.Keywords: Chromene derivative, Extended-release, Hydroxypropyl methylcellulose phthalate, Hydroxypropyl methylcellulose K100.