A simple and inexpensive enteric-coated capsule for delivery of acid-labile macromolecules to the small intestine

Enteric coated dosage form bypasses the stomach and releases the drug into the small intestine. Advantages of enteric coated pellets in comparison with enteric coated tablets are a) Pellets provide rapid onset of action and faster drug release due to the smaller size than tablets and b) Pellets exhibit less residence time of acid-labile drugs in the stomach compared to tablets. Dosage form coat can be damaged by longer resistance time in the stomach. The present review summarizes the current state of enteric coated pellets where core pellets are prepared by extrusion-spheronization technique and the enteric coating is applied in a fluidized bed processor. Two approaches are involved in the preparation of core pellets. In the first approach, a mixture of drug and excipient(s)/co-processed excipient is passed through extruders to prepare core pellets. In the second approach, excipient core pellets are prepared by extrusion technique and the drug is layered onto it before the enteric coating. The excipients present in the core pellets decide immediate or extended release of drug in the intestine. The coprocessed excipient pellets provide less batch variability and provide a platform for layering of many drugs before enteric coating. Some patents included enteric coating pellets [CN105456223 (A), CN105596310 (A), CN105616371 (A), CN105663095 (A), CN101611766B, CN106511862 (A), CN106668018 (A), CN106727381 (A), CN106924222 (A), TW200624127 (A), US 2017/0165248A1, US 2017/0224720A1] are discussed.

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A Cyclodextrin-Based Controlled Release System in the Simulation of In Vitro Small Intestine

Molecules ◽

10.3390/molecules25051212 ◽

2020 ◽

Vol 25 (5) ◽

pp. 1212

Author(s):

Danni Zheng ◽

Liuxi Xia ◽

Hangyan Ji ◽

Zhengyu Jin ◽

Yuxiang Bai

Keyword(s):

Complex System ◽

Small Intestine ◽

Controlled Release ◽

Glucose Production ◽

Scanning Calorimetry ◽

Release System ◽

In Vitro Simulation ◽

Controlled Release System ◽

Enteric Coated

A novel cyclodextrin (CD)-based controlled release system was developed in the small intestine to control the rate of drug release, on the premise of enteric-coated tablets. The system was designed based on the enzymes exogenous β-cyclodextrin glycosyltransferase (β-CGTase) and endogenous maltase-glucoamylase (MG), wherein MG is secreted in the small intestine and substituted by a congenerous amyloglucosidase (AG). The vanillin-/curcumin-β-CD complexes were prepared and detected by Fourier transform infrared (FT-IR), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC), and host CD degradation was measured based on the glucose yield. The combination of β-CGTase and AG was also functional in the CD complex system. The variations in the concentrations of added β-CGTase, with AG constantly in excess, could effectively alter the rate of host CD degradation and guest release by monitoring glucose production and color disappearance, thus, demonstrating that guest release in the CD complex system could be precisely controlled by changing the amount of β-CGTase used. Thus, the in vitro simulation of the system indicated that a novel controlled release system, based on endogenous MG, could be established in the small intestine. The CD-based controlled release system can be potentially applied in drug delivery and absorption in the small intestine.

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Safety and Efficacy of Didanosine Enteric-Coated Capsule in Patients with HIV-1 Infection

Clinical Medicine Therapeutics ◽

10.4137/cmt.s3049 ◽

2009 ◽

Vol 1 ◽

pp. CMT.S3049

Author(s):

Alejandro Arenas-Pinto

Keyword(s):

Close Monitoring ◽

Resistance Mutations ◽

Potent Inducer ◽

Resource Limited ◽

Enteric Coated Capsule ◽

Gastrointestinal Intolerance ◽

Previously Treated Patients ◽

Previously Treated ◽

Low Threshold ◽

Enteric Coated

Didanosine (ddl) has been used to treat HIV infection, in combination with other anti-retroviral drugs, for over 15 years. However, the use of the original formulation of ddI was limited by serious gastro-intestinal adverse effects, which were mainly attributable to the buffer used to protect ddI from the effect of gastric pH. Didanosine enteric-coated capsule (ddI-EC), a more recently introduced formulation, is less likely to cause gastrointestinal intolerance and its absorption might not be compromised by food intake. In this review we discuss efficacy of ddI-EC-containing anti-retroviral combinations (cART) both in naïve and previously treated patients. Because of its favorable resistance profile, ddI-EC has been shown to be potentially efficacious in rescuing patients in virological failure, even if they have nucleoside reverse transcriptase inhibitors (NRTI)-associated resistance mutations. However, ddI has been shown as a potent inducer of mitochondrial dysfunction. Peripheral neuropathy, severe hyperlactatemia and pancreatitis have all been described in patients exposed to ddI. Close monitoring of patients on ddI-EC-containing cART and low threshold for treatment modifications are required to prevent major complications. In the context of once daily cART, ddI-EC is a valid option, particularly when other agents are not available, or when other medical conditions preclude the use of drugs such as tenofovir or abacavir. The role of ddI-EC in second line cART may be even more important in resource-limited settings where additional options are lacking.

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Bioequivalence study of two enteric coated capsule formulations of omeprazole in healthy volunteers

Ethiopian Pharmaceutical Journal ◽

10.4314/epj.v23i1.35091 ◽

2006 ◽

Vol 23 (1) ◽

Author(s):

Nayyar Parvez ◽

Tausif Monif ◽

Nilanjan Saha ◽

Pyare Lal Sharma

Keyword(s):

Healthy Volunteers ◽

Bioequivalence Study ◽

Enteric Coated Capsule ◽

Enteric Coated

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Metformin and Diammonium Glycyrrhizinate Enteric-Coated Capsule versus Metformin Alone versus Diammonium Glycyrrhizinate Enteric-Coated Capsule Alone in Patients with Nonalcoholic Fatty Liver Disease and Type 2 Diabetes Mellitus

Gastroenterology Research and Practice ◽

10.1155/2017/8491742 ◽

2017 ◽

Vol 2017 ◽

pp. 1-11 ◽

Cited By ~ 1

Author(s):

Rong Zhang ◽

Keran Cheng ◽

Shizan Xu ◽

Sainan Li ◽

Yuqing Zhou ◽

...

Keyword(s):

Diabetes Mellitus ◽

Fatty Liver Disease ◽

Metabolic Parameters ◽

Nonalcoholic Fatty Liver ◽

Enteric Coated Capsule ◽

Group 3 ◽

Group 2 ◽

Enteric Coated ◽

Group 1

Objective. The present study was conducted to compare the efficacy of metformin combined with diammonium glycyrrhizinate enteric-coated capsule (DGEC) versus metformin alone versus DGEC alone for the treatment of nonalcoholic fatty liver disease (NAFLD) in patients with type 2 diabetes mellitus (T2DM). Subjects and Methods. 163 patients with NAFLD and T2DM were enrolled in this 24-week study and were randomized to one of three groups: group 1 was treated with metformin alone; group 2 was treated with DGEC alone; group 3 received metformin plus DGEC combination therapy. Anthropometric parameters, liver function, lipid profile, serum ferritin (SF), metabolic parameters, liver/spleen computed tomography (CT) ratio, and fibroscan value were evaluated at baseline and after 8, 16, and 24 weeks of treatment. Results. After 24 weeks, significant improvements in all measured parameters were observed in three groups (P<0.05) except for the improvements in low density lipoprotein cholesterol (LDL-C) and metabolic parameters in group 2 which did not reach statistical significance (P>0.05). Compared with group 1 and group 2, the patients in group 3 had greater reductions in observed parameters apart from CB and TB (P<0.05). Conclusions. This study showed that metformin plus DGEC was more effective than metformin alone or DGEC alone in reducing liver enzymes, lipid levels, and metabolic parameters and ameliorating the degree of hepatic fibrosis in patients with NAFLD and T2DM.

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