scholarly journals New Technology of Thermoplastic Coating for Osmotic Pump Tablets: Study on in vivo Drug Release

2020 ◽  
Vol 02 (01) ◽  
pp. e1-e10
Author(s):  
Chun Ping Yuan ◽  
Hui Min Hou ◽  
Zhi Hong Cheng ◽  
Qing Hua Ge ◽  
Ding Zhong Song ◽  
...  
Keyword(s):  
Drug Release ◽  
New Technology ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Metformin Hydrochloride ◽  
Beagle Dogs ◽  
Coating Technology ◽  
Vitro Release

Abstract Aim The in vivo pharmacokinetics of thermoplastic-coated tablets prepared by a new technology of thermoplastic coating in Beagle dogs were studied, and the correlation between in vitro release and in vivo absorption was analyzed. Methods The in vitro release profiles of metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets were investigated. The single-dose pharmacokinetic study of these tablets in Beagle dogs was performed, and the obtained results were separately compared with the data of conventional osmotic pump tablets reported in the literature. Results Metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets displayed controlled drug-release characteristics and had a good in vivo–in vitro correlation in Beagle dogs, respectively. The literature-compared results further demonstrated that both thermoplastic-coated tablets had release characteristics of osmotic pump tablets in vivo. Conclusion The thermoplastic-coated tablets could control drug release in vivo and it was further confirmed that the new thermoplastic coating technology could replace the spray coating of osmotic pump controlled-release tablets. This study provides a theoretical basis and practical support for the industrialization and clinical application of the new thermoplastic coating technology.

scholarly journals Design and evaluation of a novel floating osmotic pump system

2009 ◽  
Vol 12 (1) ◽  
pp. 129 ◽  
Author(s):  
Zhihong Zhang ◽  
Bo Peng ◽  
Xinggang Yang ◽  
Chao Wang ◽  
Guangmei Sun ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Administration ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
Pump System ◽  
Conventional Tablet

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.

Development of Mucoadhesive Patches for Buccal Administration of Prochlorperazine: Evaluation of In Vitro Release and Mechanical Properties

1970 ◽  
Vol 1 (1) ◽  
pp. 64-70
Author(s):  
Chandra Sekhar Kolli ◽  
Ramesh Gannu ◽  
Vamshi Vishnu Yamsani ◽  
Kishan V ◽  
Madhsudan Rao Yamsani
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Moisture Absorption ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Work Of Adhesion ◽  
Casting Technique ◽  
Vitro Release

The aim of this investigation was to develop and evaluate mucoadhesive buccal patches of prochlorperazine (PCPZ). Permeation of PCPZ was calculated in vitro using porcine buccal membrane. Buccal formulations were developed by solvent-casting technique using hydroxy propylmethyl cellulose (HPMC) as mucoadhesive polymer. The patches were evaluated for in vitro release, moisture absorption and mechanical properties. The optimized formulation, based on in vitro release and moisture absorption studies, was subjected for bioadhesion studies using porcine buccal membrane. In vitro flux of PCPZ was calculated to be 2.14 ± 0.01 µg. h–1.cm–2 and buccal absorption was also demonstrated in vivo in human volunteers.             In vitro drug release and moisture absorbed was governed by HPMC content. Increasing concentration of HPMC delayed the drug release. All formulations followed Zero order release kinetics whereas the release pattern was non-Fickian. The mechanical properties, tensile strength (10.28 ± 2.27 kg mm–2 for formulation P3) and elongation at break reveal that the formulations were found to be strong but not brittle. The peak detachment force and work of adhesion for formulation P3 were 0.68 ± 0.15 N and 0.14 ± 0.08 mJ, respectively. The results indicate that suitable bioadhesive buccal patches of PCPZ with desired permeability and suitable mechanical properties could be prepared

Fig. 12 Scanning electron micrograph of D.L-PLA nanoparticles loaded with CGP 57813. (Ref. 51.) scanning force microscopy (also called atomic force microscopy), enable the visualiza-tion of nanoparticles at atmospheric pressure without gold coating [12,64]. Neverthe-less, the resolution obtained with these new tools is still lower than that with SEM. For size determination, transmission electron microscopy is not as widely used as PCS and SEM, but it is still a powerful method for determining the morphology of particles. With this technique, Fessi et al. [42] estimated the wall thickness of PLA nanocapsules. Krause et al. [18] described the highly porous structure of PLA nano-spheres prepared by the emulsion-evaporation procedure. VIII. IN VITRO RELEASE STUDIES In vitro release studies should in principle be useful for quality control as well as for the prediction of in vivo kinetics. Unfortunately, due to the very small size of the par-ticles, the release rate observed in vivo can differ greatly from the release obtained in a buffer solution. However, in vitro release studies remain very useful for quality control as well as for evaluation of the influence of process parameters on the release rate of active compounds. In vitro drug release from microdispersed systems has been exten-sively reviewed by Washington [65]. Depending on the type of polyester, drug release from nanoparticles can take place through several processes, of which the following appear to be the most important: (1) The drug may diffuse out of the carrier through the solid matrix; to allow complete release from the carriers, (the concentration of drug in the release medium should re-main infinitely low, which condition is known as sink condition); (2) The solvent may penetrate the nanoparticles and dissolve the drug, which then diffuses out into the re-lease medium. Depending on the physico-chemical characteristics of the particles, wa-ter can enter the particles through narrow pores or by hydration. Once the drug is dis-solved, the drug diffuses out of the particles. Here again, since diffusion is driving the

1998 ◽  
pp. 204-216
Keyword(s):  
Quality Control ◽  
Drug Release ◽  
Release Rate ◽  
In Vitro Release ◽  
Scanning Force Microscopy ◽  
Force Microscopy ◽  
Release Studies ◽  
Vitro Release

In vitro release and in vivo absorption in beagle dogs of meloxicam from Eudragit® FS 30 D-coated pellets

2006 ◽  
Vol 322 (1-2) ◽  
pp. 104-112 ◽  
Author(s):  
Chunsheng Gao ◽  
Jian Huang ◽  
Yan Jiao ◽  
Li Shan ◽  
Yan Liu ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Beagle Dogs ◽  
In Vivo Absorption ◽  
Vitro Release

DEVELOPMENT OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM BASED ON A NOVEL EXCIPIENT FOR METFORMIN HYDROCHLORIDE USING MIXTURE DESIGN

2020 ◽  
pp. 62-71
Author(s):  
R. PAWAR ◽  
S. JAGDALE ◽  
D. RANDIVE
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Mixture Design ◽  
Release Profile ◽  
Metformin Hydrochloride ◽  
Matrix Tablet ◽  
Vitro Release

Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus. Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release. Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared. Conclusion: A sustained-release (GFT) of MH tablets using PEO-, HPMC K100M, and an effervescent system was successfully prepared. AGFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.

scholarly journals Evaluation of the Correlation between in Vivo and in Vitro Release. Effect of the Force of Contraction and Food on Drug Release.

1994 ◽  
Vol 17 (2) ◽  
pp. 291-295 ◽  
Author(s):  
Shigeru AOKI ◽  
Hidenobu ANDO ◽  
Masaaki ISHII ◽  
Katsumi IDA ◽  
Sumio WATANABE ◽  
...  
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Force Of Contraction ◽  
Vitro Release

scholarly journals In Situ-Forming Microparticles for Controlled Release of Rivastigmine: In Vitro Optimization and In Vivo Evaluation

2021 ◽  
Vol 14 (1) ◽  
pp. 66
Author(s):  
Mohamed Haider ◽  
Ibrahim Elsayed ◽  
Iman S. Ahmed ◽  
Ahmed R. Fares
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Flip Flop ◽  
In Situ Forming ◽  
Internal Phase ◽  
The Matrix ◽  
Vitro Release

In this work, sucrose acetate isobutyrate (SAIB) and polylactic co-glycolic acid (PLGA) were used alone or in combination as a matrix-former (MF) to prepare long-acting injectable rivastigmine (RV) in situ-forming microparticles (ISM). RV-ISM were prepared by the emulsification of an internal phase, containing the drug and the matrix former(s), into an external oily phase containing a stabilizer. The statistical design, Central Composite Design (CCD), was adopted as a quality by design (QbD) approach to optimize the formulation of RV-ISM systems. The fabricated RV-ISM systems was designed to minimize the initial burst drug release and maximize the sustainment of RV release from the ISM and ease of injection. The influence of critical formulation variables such as the matrix-former to drug (MF/D) ratio and SAIB to PLGA (S/P) ratio in the internal phase with respect to critical quality attributes (CQAs), such as the percentage drug release within the first day (Q1), the time required for 50% drug release (T50%) and the rate of injection, were studied using the CCD. The optimal RV-ISM system with the highest desirability value (0.74) was predicted to have an MF/D ratio of 11.7:1 (w/w) and an S/P ratio of 1.64:1 (w/w). The optimal RV-ISM system was assessed for its release profile, injectability, rheological properties, morphology, effect on cell viability, tolerance to γ-sterilization and in vivo performance in male albino rabbits. In vitro release studies revealed that the optimal RV-ISM system released 100% of its drug content throughout a release period of 30 days with only 15.5% drug release within the first day (Q1) and T50% of 13.09 days. Moreover, the optimal system showed a high injection rate of 1.012 mL/min, pseudoplastic flow, uniform spherical globules with homogenous particle size, minimal cytotoxicity and high tolerability to γ-sterilization. In vivo pharmacokinetic (PK) studies revealed that the rate of absorption of RV from the optimal RV-ISM system was controlled compared to a drug solution following either intramuscular (IM) or subcutaneous (SC) injection. Furthermore, the optimal RV-ISM was found to follow flip-flop PK with poor correlation between in vitro release and in vivo findings. These findings suggest that the optimal RV-ISM is a promising tool to achieve a sustained release therapy for RV; however, further investigation is still required to optimize the in vivo performance of RV-ISM.

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