Design, Development, and Biopharmaceutical Properties of Buccoadhesive Compacts of Pentazocine

Buccal delivery of drugs provides an attractive alternative to the oral route of drug administration, particularly in overcoming deficiencies associated with the latter mode of administration. Problems such as high first-pass metabolism and drug degradation in the harsh gastrointestinal environment can be circumvented by administering the drug via the buccal route (1-3). Moreover, buccal drug absorption can be promptly terminated in case of toxicity by removing the dosage form from the buccal cavity. It is also possible to administer drugs to patients who cannot be dosed orally to prevent accidental swallowing. Therefore adhesive mucosal dosage forms were suggested for oral delivery, which included adhesive tablets (4-6), adhesive gels (7, 8) and adhesive patches (9, 10). Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 ± 0.4%) with the Higuchi model release profile and permeated 21.5 ± 2.9% of the drug (flux 8.35 ± 0.291 µg h -1 cm -2 ) permeation coefficient 1.34 ± 0.05 cm h -1 ) through porcine buccal membrane. BC3 formulation showed 1.62 ± 0.15 N of peak detachment force and 0.24 ± 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.

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“…Moisture absorption study was performed according to the modified procedure reported earlier (16). Agar (5%, m/V) was dissolved in hot water.…”

Section: Moisture Absorptionmentioning

confidence: 99%

Development and in vitro evaluation of buccoadhesive carvedilol tablets

Yamsani¹,

Gannu²,

Kolli³

et al. 2007

Acta Pharmaceutica

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“…These results are in agreement with the findings reported earlier (21,22). Upon statistical evaluation (two-way ANOVA), a significant difference was observed between the test products (p < 0.01) but not within the test products for AUC (0)(1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12) , AUC (0-24) , AUC (0-∞) , t 1/2, K el and MRT values. Spearman rank correlation, a non-parametric statistical test, demonstrated a high degree of positive correlation, showing complete agreement in the order of ranks between the percentage of drug absorbed from patches and C max (p < 0.02; two tails), AUC (0-24) (p < 0.02; two tails) and AUC (0-∞) (p < 0.02; two tails).…”

Section: In Vivo Studies In Rabbitsmentioning

confidence: 99%

“…Pentazocine is used for relief of moderate to severe pain. Oral administration of PTZ has the disadvantage of low bioavailability (about 18-22 %) due to extensive first-pass metabolism (5)(6)(7). In addition, PTZ has a short half-life of 2-4 h and requires frequent dosing in order to maintain the optimal therapeutic concentration.…”

mentioning

confidence: 99%

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Verma

Chandak²

2009

Acta Pharmaceutica

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Transdermal drug delivery system is being extensively investigated as a viable alternative to drug delivery with improved bioavailability. It offers many advantages over conventional administration such as enhanced efficacy, increased safety, and greater convenience and improved patient compliance. Transdermal route permits the use of a relatively potent drug with minimal risk of systemic toxicity and avoids gastrointestinal degradation and hepatic first-pass metabolism (1-3). A number of therapeutic agents, including antihypertensive, antianginal, antihistaminic, anti-inflammatory, analgesic, The present study aimed to develop hydroxypropyl methylcellulose based transdermal delivery of pentazocine.In formulations containing lower proportions of polymer, the drug released followed the Higuchi kinetics while, with an increase in polymer content, it followed the zero-order release kinetics. Release exponent (n) values imply that the release of pentazocine from matrices was non-Fickian. FT-IR, DSC and XRD studies indicated no interaction between drug and polymer. The in vitro dissolution rate constant, dissolution half-life and pharmacokinetic parameters (C max , t max , AUC (s) , t 1/2, K el , and MRT) were evaluated statistically by two-way ANOVA. A significant difference was observed between but not within the tested products. Statistically, a good correlation was found between per cent of drug absorbed from patches vs. C max and AUC (s) . A good correlation was also observed when per cent drug released was correlated with the blood drug concentration obtained at the same time point. The results of this study indicate that the polymeric matrix films of pentazocine hold potential for transdermal drug delivery.Keywords: pentazocine, transdermal drug delivery, Cygnus' sandwich patch holder, in vitro characterization, in vivo evaluation * Correspondence; e-mail: prpverma275730@yahoo.com Unauthenticated Download Date | 8/28/18 7:56 PM and anti-arthritic drugs, are being investigated and developed for the transdermal therapeutic system either for academic research or for commercial purposes (3, 4). The present work is aimed at developing a matrix-dispersion type transdermal drug delivery of pentazocine.Pentazocine (PTZ), a benzomorphan derivative, is an opioid analgesic that has mixed opioid agonist and antagonist actions. It is considered to be a partial agonist or weak antagonist at the m-receptor and a k-receptor agonist. Pentazocine is used for relief of moderate to severe pain. Oral administration of PTZ has the disadvantage of low bioavailability (about 18-22 %) due to extensive first-pass metabolism (5-7). In addition, PTZ has a short half-life of 2-4 h and requires frequent dosing in order to maintain the optimal therapeutic concentration. Repeated injections over long periods may cause fibrotic changes in the skin and muscular tissue. Low molecular mass (285.4), suitable pK a values of 8.5 and 10, log P (octanol/phosphate buffer pH 7.4) of 2.0 and low oral bioavailability provide a rationale for developing a...

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“…This high mucoadhesive strength of CP may be due to formation of secondary mucoadhesive bonds with mucin because of rapid swelling and interpenetration of the polymer chains in the interfacial region, while other polymers undergo only superficial bioadhesion. 21 Formulation F4 showed good mucoadhesive strength (22.30 ± 0.99 g) for 5 minutes of contact time. The mucoadhesive time on sheep buccal mucosa ranged from 8 to 20 hours ( Table 2).…”

Section: E4mentioning

confidence: 99%

Mucoadhesive bilayer tablets of propranolol hydrochloride

Patel¹,

Prajapati

Patel

et al. 2007

AAPS PharmSciTech

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The purpose of this research was to study mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive polymers sodium alginate (Na-alginate) and Carbopol 934P (CP) along with ethyl cellulose as an impermeable backing layer. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling index, in vitro drug release, ex vivo drug permeation, ex vivo mucoadhesion, and in vivo pharmacodynamics in rabbits. Tablets containing Na-alginate and CP in the ratio of 5:1 (F2) had the maximum percentage of in vitro drug release without disintegration in 12 hours. The swelling index was proportional to Na-alginate content and inversely proportional to CP content. The surface pH of all tablets was found to be satisfactory (7.0 ± 1.5), close to neutral pH; hence, buccal cavity irritation should not occur with these tablets. The mechanism of drug release was found to be non-Fickian diffusion and followed zero-order kinetics. The formulation F4 was optimized based on good bioadhesive strength (28.9 ± 0.99 g) and sustained in vitro drug permeation (68.65% ± 3.69% for 12 hours). The behavior of formulation F4 was examined in human saliva, and both the drug and the buccal tablet were found to be stable. The formulation F4 was applied to rabbit oral mucosa for in vivo studies. The formulation inhibited isoprenaline-induced tachycardia. The studies conducted in rabbits confirmed the sustained release as compared with intravenous administration.

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Design, Development, and Biopharmaceutical Properties of Buccoadhesive Compacts of Pentazocine

Cited by 79 publications

References 9 publications

Development and in vitro evaluation of buccoadhesive carvedilol tablets

Development and in vitro evaluation of buccoadhesive carvedilol tablets

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Mucoadhesive bilayer tablets of propranolol hydrochloride

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