Design and evaluation of sustained-release and buccal adhesive propranolol hydrochloride tablets

Taylan, B.; Çapan, Yılmaz; Güven, Olgun; Kes, Sırrı; Hıncal, A. A.

doi:10.1016/0168-3659(95)00094-1

Cited by 74 publications

(31 citation statements)

References 16 publications

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“…Its elimination half-life is also relatively short (about 2-6 h). [6][7][8] Therefore, it was chosen as a model drug for preparation of the once-daily extended-release dosage form.…”

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confidence: 99%

Optimization of Sustained-Release Propranolol Dosage form Using Factorial Design and Response Surface Methodology

Huang

Tsai

Yang

et al. 2004

Biological & Pharmaceutical Bulletin

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Hydrophilic gel-forming matrix tablets are extensively used for oral extended release dosage forms due to their simplicity, cost effectiveness, and reduction of the risk of systemic toxicity due to dose dumping.1,2) Furthermore, pHindependent drug release is preferable for oral extended release formulations, so drug release in the GI tracts is not affected by intra-and inter-subject variations in both gastric pH and GI transit time. Hydroxypropylmethylcellulose (HPMC) is a pH-independent material and the drug release rates from HPMC matrix formulations are generally independent of processing variables such as compaction pressure, drug particle size, and the incorporation of a lubricant. 3)Therefore, HPMC is widely used to prepare the extended release dosage forms of water-insoluble drugs such as promethazine and water-soluble drugs such as acetaminophen. [3][4][5] Propranolol, a non-selective beta-adrenergic blocking agent, has been widely used in the treatment of hypertension, angina pectoris, and many other cardiovascular disorders. It is highly lipophilic and is almost completely absorbed after oral administration. However, much of the drug is metabolized by the liver during its first passage through the portal circulation; on average, only about 30% reaches the systemic circulation. Its elimination half-life is also relatively short (about 2-6 h).6-8) Therefore, it was chosen as a model drug for preparation of the once-daily extended-release dosage form.In the development of an extended release dosage form, an important issue was to design an optimized pharmaceutical formulation with an appropriate dissolution rate in a short time period and minimum trials. For this purpose, a computer optimization technique, based on a response surface methodology (RSM) utilizing a polynomial equation and artificial neural networks (ANN) has been widely used. [9][10][11][12] The optimization procedure involved systematic formulation designs to minimize the number of trials and analyze the response surfaces in order to realize the effect of causal factors and to obtain the appropriate formulations with target goals and the acceptable component region as process control conditions in practical preparation. Therefore, the primary purpose of this study was to develop and optimize the propranolol extended release formulations with target release profiles using RSM and multiple response optimization utilizing a quadratic polynomial equation. The second aim of the study was to evaluate and demonstrate the usefulness of RSM with multiple response optimization technology in the development of extended-release dosage forms containing water-soluble drug. MATERIALS AND METHODS MaterialsPropranolol hydrochloride and p-hydroxybenzoate-butyl ester were purchased from TCI Co. (Japan). Hydroxypropylmethylcellulose (HPMC, viscosity 4000 grade) was obtained from Shin Etsu (Japan). Microcrystalline cellulose (Avicel) was purchased from Asahi Co. (Japan). All other chemicals and solvents were of analytical reagent grade.Preparation of Propranol...

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“…Its elimination half-life is also relatively short (about 2-6 h). [6][7][8] Therefore, it was chosen as a model drug for preparation of the once-daily extended-release dosage form.…”

mentioning

confidence: 99%

Optimization of Sustained-Release Propranolol Dosage form Using Factorial Design and Response Surface Methodology

Huang

Tsai

Yang

et al. 2004

Biological & Pharmaceutical Bulletin

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“…The polymer chains start gyrating and the matrix swells. Drug release is controlled by diffusion through such swollen gel layers (34). The true challenge is to control drug release from the formulation in the initial stages due to matrix swelling in the presence of dissolution fluid(s).…”

Section: Resultsmentioning

confidence: 99%

Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery

et al. 2009

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“…Buccoadhesive nifedipine tablets based on CMC and carbopol (Varshosaz & Dehghan 2002) adhered to the upper gums of humans for over 8 h. Other examples are the delivery of morphine sulfate, from tablets based on HPMC and PAA, in healthy subjects (Anlar et al 1994) and the delivery of thiocolchicoside from mucoadhesive tablet based on CMC and gelatin (Artusi et al 2003). Although the buccal mucosa is considered to be more resistant to damage than other mucosal membranes, serious irritation and ulceration can occur as a result of local toxicity, as in the case of buccal delivery of propranolol hydrochloride (Taylan et al 1996). One disadvantage of the single-layer tablet for systemic delivery is that the drug will also be released into the saliva and swallowed.…”

Section: The Buccal Routementioning

confidence: 99%

Pharmaceutical applications of mucoadhesion for the non-oral routes

Edsman

Hägerström

2005

Journal of Pharmacy and Pharmacology

154

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The adhesion of pharmaceutical formulations to the mucosal tissue offers the possibility of creating an intimate and prolonged contact at the site of administration. This prolonged residence time can result in enhanced absorption and, in combination with a controlled release of the drug, also improved patient compliance by reducing the frequency of administration. During the almost 30 years over which mucoadhesion has been studied, a considerable amount of knowledge has been gained, and much has been learned about the different mechanisms occurring at the formulationmucus interface and the properties that affect these mechanisms. The in-vivo performance of a dosage form not only depends on the mechanisms occurring at the interface, but also on the properties of the total mucoadhesive complex: the dosage form, the mucosa and the interface between them. A wide variety of methods are used for studying mucoadhesion; some rather similar to the in-vivo situation and some mimicking the interface alone. In this review, the mucus surface, the methods used for the study of mucoadhesion, the different mechanisms involved in mucoadhesion and theories underpinning them have been described. The complexity of mucoadhesion when trying to systemize the subject will also be discussed. The last part of the review describes the buccal, nasal, ocular, vaginal and rectal routes and provides examples of what can be achieved in-vivo when using mucoadhesive formulations.

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Design and evaluation of sustained-release and buccal adhesive propranolol hydrochloride tablets

Cited by 74 publications

References 16 publications

Optimization of Sustained-Release Propranolol Dosage form Using Factorial Design and Response Surface Methodology

Optimization of Sustained-Release Propranolol Dosage form Using Factorial Design and Response Surface Methodology

Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery

Pharmaceutical applications of mucoadhesion for the non-oral routes

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