Dataset Information

In Vitro Evaluation of Enteric-Coated HPMC Capsules-Effect of Formulation Factors on Product Performance.

ABSTRACT: A comparative study on different enteric-coated hard capsules was performed. The influence of different formulation factors like choice of enteric polymer, triethyl citrate (TEC) concentration (plasticizer), talc concentrations (anti-tacking agent), and different coating process parameters on the sealing performance of the capsule and the disintegration time were investigated. Furthermore, the influence of different disintegration test methods (with disc vs. without disc and 50 mM U.S. Pharmacopoeia (USP) buffer pH 6.8 vs. biopredictive 15 mM phosphate buffer pH 6.5) was evaluated. All formulations showed sufficient but not equivalent acid resistance when tested. Polymer type was the main factor influencing the capsule sealing and disintegration time. In addition, TEC and talc could affect the performance of the formulation. Regarding the choice of the disintegration test method, the presence of a disc had for the most part only limited influence on the results. The choice of disintegration buffer was found to be important in identifying differences between the formulations.

SUBMITTER: Fu M

PROVIDER: S-EPMC7465055 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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In Vitro Evaluation of Enteric-Coated HPMC Capsules-Effect of Formulation Factors on Product Performance.

Fu Maoqi M Blechar Johannes Andreas JA Sauer Andreas A Al-Gousous Jozef J Langguth Peter P

Pharmaceutics 20200723 8

A comparative study on different enteric-coated hard capsules was performed. The influence of different formulation factors like choice of enteric polymer, triethyl citrate (TEC) concentration (plasticizer), talc concentrations (anti-tacking agent), and different coating process parameters on the sealing performance of the capsule and the disintegration time were investigated. Furthermore, the influence of different disintegration test methods (with disc vs. without disc and 50 mM U.S. Pharmacop ...[more]

PMID: 32717908

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Project description:BackgroundTo investigate the biosynthesis and pharmacokinetic course of enteric-coated soft capsules of Panax notoginseng saponins (PNS) in a beagle dog model.MethodsTo satisfy the enteric properties of soft capsules, the PNS enteric soft gelatin capsules were prepared by formaldehyde impregnation and orthogonal experimental design. The fluidity of gelatin and the disintegration time were selected as evaluation indexes; the soft gelatin capsule content was self-emulsifying, and the Km value and the optimal prescription were determined by making three-phase diagrams; in vivo pharmacokinetics studies were performed on six beagle dogs with 3 dogs in each group. Beagle dogs were divided into two groups randomly. One group was given PNS self-emulsifying enteric capsule and the other was given market conventional capsules. Plasma samples were collected at different times. After 1 week, the crossover experiment was carried out. The plasma concentration was detected by HPLC-MS (high performance liquid chromatography-mass spectrometry). Then the pharmacokinetic parameters were calculated by non-compartment model analysis.ResultsThe range and variance analysis of the orthogonal test determined that the best prescription of total saponins of Panax notoginseng enteric soft capsule was:gelatin:glycerol:water =1:1:2, Soak the films in 1% formaldehyde for 1 hour. The contents of the soft capsule self-microemulsion are prescribed as: IPM (isopropyl myristate):Cremophor RH40:PEG400 (polyethylene glycol 400) =1:4.5:4.5 (with suitable PNS); the pharmacokinetic parameters of PNS self-emulsified enteric capsules and conventional capsules in the market are as follows: Rb1:Cmax is (18.05±0.26) and (15.50±0.51) ng/mL, Tmax is (2.00±0) and (3.00±0) h, AUC0→t is 98.49±1.16 and 34.46±2.02 (ng/mL)·h, relative bioavailability is 196.2%; Rg1: Cmax is 4.16±0.25 and 3.88±0.28 ng/mL, Tmax is 2.00±0 and 1.50±0 h, area under drug time curve (AUC)0→t is 11.80±2.93 and 10.45±2.29 (ng/mL)·h, relative bioavailability is 77.2%; R1:Cmax is 1.84±0.25 and 1.48±0.21 ng/mL, Tmax is 2.08±0.49 and 1.92±0.20 h, AUC0→t is 7.06±2.07 and 7.16±2.59 (ng/mL)·h, relative bioavailability is 117.7%.ConclusionsThe experiment in vivo showed the higher relative bioavailability of PNS self-emulsifying enteric capsule compared with market conventional capsules. This will provide a potential application prospect for the clinical research and applications of PNS.

Project description:BackgroundUlcerative colitis (UC), a chronic inflammatory bowel disease, is characterized by abdominal pain, diarrhea, and mucopurulent bloody stool. In recent years, the incidence and prevalence of UC have been increasing consistently. Five-flavor Sophora falvescens enteric-coated capsule (FSEC), a licensed Chinese patent medicine, was specifically used to treat UC. This review was aimed to assess the effectiveness and safety of FSEC for the treatment of UC.MethodsSix electronic databases were searched from inception to March 2021. Randomized clinical trials (RCTs) comparing FSEC or FSEC plus conventional Western medicine with conventional Western medicine in participants with UC were included. Two authors screened all references, assessed the risk of bias, and extracted data independently. Binary data were presented as risk ratios (RRs) with 95% confidence intervals (CIs) and metric data as mean difference (MD) with 95% CI. The overall certainty of the evidence was assessed by GRADE.ResultsWe included 15 RCTs (1194 participants, 763 in the FSEC group and 431 in the control group). The treatment duration ranged from 42 to 64 days. Twelve trials compared FSEC with conventional Western medicine, and two trials compared FSEC plus conventional medicine with conventional medicine. Another trial compared FSEC plus mesalazine with compound glutamine enteric capsules plus mesalazine. FSEC showed a higher clinical effective rate (improved clinical symptoms, colonoscopy results, and stools) (RR 1.12, 95% CI 1.05 to 1.20; 729 participants; 8 trials; low-quality evidence) as well as the effective rate of traditional Chinese medicine (TCM) syndromes (RR 1.10, 95% CI 1.01 to 1.20; 452 participants; 5 trials; low-quality evidence) compared to mesalazine. There was no significant difference in the adverse events between FSEC and control groups.ConclusionsFSEC may show effectiveness in UC treatment compared to conventional medicine, and the use of FSEC may not increase the risk of adverse events. Due to the limited number of clinical trials and low methodological quality of the included trials, our findings must be interpreted with discretion.

Dataset Information

In Vitro Evaluation of Enteric-Coated HPMC Capsules-Effect of Formulation Factors on Product Performance.

Publications

In Vitro Evaluation of Enteric-Coated HPMC Capsules-Effect of Formulation Factors on Product Performance.

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