Design and Study of Rifampicin Oral Controlled Release Formulations

Hiremath, S. P.; Saha, Ranendra N.

doi:10.1080/10717540490494087

Cited by 15 publications

(5 citation statements)

References 16 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…10,11 Furthermore, repeated oral administration of high RIF doses yields autoinduction of RIF's own metabolism leading to a decrease in its bioavailability. 12 An alternative, a more effective approach to treat pulmonary TB is to deliver drugs directly to the lungs to achieve high local drug concentration for extended duration. Also, depending on the physicochemical characteristics of the particular drug and the formulation, pulmonary delivery could also result in systemic bioavailability of the drug, if treatment of extrapulmonary TB is desired.…”

Section: Introductionmentioning

confidence: 99%

“…This is a potentially easy solution since RIF is an inexpensive drug and well-known among physicians worldwide . However, this approach has the potential to increase unwanted side effects such as hepatotoxicity. , Furthermore, repeated oral administration of high RIF doses yields autoinduction of RIF’s own metabolism leading to a decrease in its bioavailability …”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs

et al. 2015

View full text Add to dashboard Cite

Tuberculosis (TB) is a life-threatening infection that requires a lengthy treatment process that is often associated with adverse effects. Pulmonary delivery of anti-TB drugs has the potential to increase efficacy of treatment by increasing drug concentrations at the lungs, the primary site of infection. The aim of the present study is to evaluate the disposition of rifampicin (RIF) after its pulmonary administration as porous particles (PPs) to guinea pigs and contrast it to that after oral administration. RIF microparticles were prepared by spray drying a solution of RIF and L-leucine (9:1), and the resulting particles were characterized for their physicochemical properties. Animals received RIF either as intravenous solution (iv), as oral suspension of micronized RIF (ORS) and RIF-PPs (ORPP), or by insufflation of the PPs (IRPP). Plasma samples were collected at preselected time points, and bronchoalveolar lavage (BAL) was performed at the end of the study. RIF concentrations in biological samples were analyzed by HPLC. Plasma concentration versus time data was analyzed by compartmental and noncompartmental methods. RIF PPs were thin walled porous particles with mass median aerodynamic diameter (MMAD) of 4.8±0.1 μm, GSD=1.29±0.03, and fine particle fraction below 5.8 μm of 52.9±2.0%. RIF content in the resulting particles was 91.8±0.1%. Plasma concentration vs time profiles revealed that the terminal slope of the iv group was different from that of the oral or pulmonary groups, indicating the possibility of flip-flop kinetics. RIF from IRPP appeared to be absorbed faster than that of ORPP or ORS as evidenced by higher RIF plasma concentrations up until 2 h. Notably, similar AUC (when corrected by dose), similar CL, λ, and half-life were obtained after oral administration of RIF at 40 mg/kg and pulmonary administration of RIF at 20 mg/kg. However, RIF in the IRPP group had a shorter Tmax and higher bioavailability than orally dosed groups. In addition, RIF concentrations in the BAL of animals in the IRPP group were 3-4-fold larger than those in the orally dosed groups. The disposition in ORS and ORPP were best described by a model with two sequential compartments, whereas the disposition of IRPP was best described by a two parallel compartment model. The advantages of delivering RIF by the pulmonary route are demonstrated in the present study. These include achieving higher RIF concentrations in the lungs and similar systemic levels after pulmonary delivery of one-half of the oral nominal dose. This is expected to result in a more effective treatment of pulmonary TB, as shown previously in published efficacy studies.

show abstract

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs

et al. 2015

View full text Add to dashboard Cite

show abstract

“…This is a part of research efforts from author's lab on the development of oral controlled release formulations of anti-tubercular drugs rifampicin and isoniazid. In this regard, authors have reported the oral CR formulations of rifampicin (20)(21) and rifampicin and isoniazid combination (22). In light of the above discussion, the objective of this study was to formulate controlled release oral tablet formulations of isoniazid by matrix embedding technique using HPMC polymer of different viscosity grades as a retardant material.…”

Section: Introductionmentioning

confidence: 99%

Controlled Release Hydrophilic Matrix Tablet Formulations of Isoniazid: Design and In Vitro Studies

Hiremath

Saha

2008

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. The aim of the present investigation was to develop oral controlled release matrix tablet formulations of isoniazid using hydroxypropyl methylcellulose (HPMC) as a hydrophilic release retardant polymer and to study the influence of various formulation factors like proportion of the polymer, polymer viscosity grade, compression force, and release media on the in vitro release characteristics of the drug. The formulations were developed using wet granulation technology. The in vitro release studies were performed using US Pharmacopoeia type 1 apparatus (basket method) in 900 ml of pH 7.4 phosphate buffer at 100 rpm. The release kinetics was analyzed using KorsmeyerPeppas model. The release profiles were also analyzed using statistical method (one-way analysis of variance) and f 2 metric values. The release profiles found to follow Higuchi's square root kinetics model irrespective of the polymer ratio and the viscosity grade used. The results in the present investigation confirm that the release rate of the drug from the HPMC matrices is highly influenced by the drug/ HPMC ratio and viscosity grade of the HPMC. Also, the effect of compression force and release media was found to be significant on the release profiles of isoniazid from HPMC matrix tablets. The release mechanism was found to be anomalous non-Fickian diffusion in all the cases. In the present investigation, a series of controlled release formulations of isoniazid were developed with different release rates and duration so that these formulations could further be assessed from the in vivo bioavailability studies. The formulations were found to be stable and reproducible.

show abstract

“…In this study, four different sustained release tablet formulations with same weighted tablets were developed to determine optimum formulation using different polymers which are Carbopol 974P, HPMC K100M, PEO (Polyox WSR303), guar gum (Supercol NF) and alginate (Protanal LF240). The polymer concentration was fixed to 40 % (w/w) according to previous studies (22). Because of the commercial tablet contains 75 mg venlafaxine, our tablet formulations contain 84.85 mg (VH) which is equivalent to 75 mg venlafaxine free base.…”

Section: Preparation Of Formulationsmentioning

confidence: 99%

Venlafaksin Hidroklorürün Uzatılmış Salım Yapan Tablet Formülasyonlarının Geliştirilmesi ve Değerlendirilmesi

Tort

AKÇA

Olgac

et al. 2022

Sağlık Bilimlerinde Değer

View full text Add to dashboard Cite

Aim: Depression is a mental disorder which affects more than 250 million people independently of their age. Venlafaxine is an antidepressant drug and used also for the treatment of panic attack and anxiety with fewer side effects than older antidepressant therapeutics. However, venlafaxine hydrochloride (VH) has a short half-life which requires three times dosing daily to maintain sufficient plasma drug concentration. The aim of this study is to develop sustained release VH tablets to be given once a day. Material and Methods: Polyethylene oxide, sodium alginate, hydroxypropyl methyl cellulose, guar gum and polyacrylic acid were used as controlled release agent. Tablets were prepared by direct compression method. Powder (angle of repose, flow rate, Carr index and Hausner ratio) and tablet (weight uniformity, hardness, friability,) characterizations were evaluated. In vitro release studies were carried out for 24 h and drug release kinetics were evaluated using different models. Results: All formulations showed suitable Carr index and Hausner ratio except the formulation prepared with guar gum. The tablets which had been manufactured via direct compression method were compared to the commercial tablet. Sustained release of VH was observed for all formulations. Based on the in-vitro dissolution studies, the drug release from F1 formulation which comprising HPMC and Carbopol polymers was found similar as compared to the commercial tablets. Conclusion: Directly compressed VH tablets could be a preferable alternative to the commercial tablets on behalf of patient compliance and fewer manufacturing steps compared to other production methods.

show abstract

Design and Study of Rifampicin Oral Controlled Release Formulations

Cited by 15 publications

References 16 publications

Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs

Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs

Controlled Release Hydrophilic Matrix Tablet Formulations of Isoniazid: Design and In Vitro Studies

Venlafaksin Hidroklorürün Uzatılmış Salım Yapan Tablet Formülasyonlarının Geliştirilmesi ve Değerlendirilmesi

Contact Info

Product

Resources

About