Formulation design and pharmaceutical development of a novel controlled release form of azithromycin for single-dose therapy

Lo, Julian B.; Appel, Leah E.; Herbig, Scott M.; McCray, Scott B.; Thombre, Avinash G.

doi:10.3109/03639040903037223

Cited by 37 publications

(18 citation statements)

References 20 publications

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“…The drugs which are prescribed with the causes like unpalatible formulations of the drug, administration of the drug through difficult routes, administration of unsuitable dosage forms (especially for the paediatric and the geriatric populations), the appearance of side effects at therapeutic doses and the designing of difficult medicine containers, can also be included among the drug related factors which lead to noncompliance to the treatment [26][27][28].…”

Section: Patient Related Factorsmentioning

confidence: 99%

Adherence and Non-Adherence to Treatments: Focus on Pharmacy Practice in Nepal

Bastakoti¹

2013

JCDR

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Nepal is one of the developing countries having many limitations in providing the quality health services to its population. In many countries, improvement in patients' adherence to the pharmacotherapy had been one of major outcome of quality pharmaceutical services. Till date, very less thing has been done in this area in Nepal; so it seems mandatory to improve the patient adherence to the treatment plans. Adherence to the medical therapy can be explained by the extent of the behavioral coincidence to the medication and non-medication regimen by a patient whereas compliance and concordance are two different models of patient adherence to the therapy. Compliance model suggests that patients have been brought responsible for being unable to follow 'doctor's order and concordance tempts to measure the degree of agreement between patient and his or her clinician about the nature of illness and the best possible therapy for the welfare of the patient. Non-adherence to the therapy may lead to different problems as consequences of non-adherence in four different level-individual, institutional, societal and national levels. Although some programs like, "Direct Observation Treatment, Short-course (DOTS) for tuberculosis, implementation of antiretroviral treatment schedules for HIV patients and pediatric vaccination models," are the examples of attention towards the cases of noncompliance in Nepal. It has long been faced its limitations in the forms of either untrained manpower or lack of good documentation of patients' adherence to therapy or high illiteracy rate or unaffordibility of patients to their treatment or lack of pharmaceutical care services. BACkgRoundNepal is a developing country which has major limitations in providing quality healthcare services to its population [1][2][3][4]. Most of the technical aspects of the socio-community pharmacy practice have not been addressed as yet, due to various reasons [3]. The access of people to the essential medicines and their affordability, is still a major problem in the country [5]. Hence, many aspects of the pharmaceutical care are still not major concerns for the policy makers and other relevant stakeholders. A majority of the pharmacies which are inside the country are being operated by manpower who are trained only for a few hours [6]. The prevailing primordial pharmacy practice, the absence of well qualified and trained pharmacists in the community settings, and the absence of hospital pharmacy practices inside a majority of the hospitals are some major barriers in the way of providing better pharmaceutical services to the people [6][7][8].In many developed countries, an improvement in the patients' adherence to the pharmacotherapy is one of major outcomes of the quality pharmaceutical services [9][10][11][12][13]. However, only few things had been achieved in this area in Nepal. So, it is necessary to promote the role of pharmacists to increase the patients' adherence towards the treatment in the Nepalese context. Therefore, in this article, the authors...

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Section: Patient Related Factorsmentioning

confidence: 99%

Adherence and Non-Adherence to Treatments: Focus on Pharmacy Practice in Nepal

Bastakoti¹

2013

JCDR

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“…This was followed by a collaboration between Pfizer and the drug delivery company Bend Research Inc. (Bend, OR), resulting in a dosage form which met the difficult physiological and practical constraints (35). This review will not cover the history of failed formulations, but will describe the progress to the successful formulation which has been approved by FDA and other regulatory bodies.…”

Section: Azithromycin Cr Dosage Formmentioning

confidence: 96%

“…Release of a high solubility drug like azithromycin is expected to be very rapid from such small beads (∼200 μm), and the effects of porosigen content and dissolution medium pH were studied. Figure 3 presents dissolution at pH 6.0 of microspheres containing three different levels of the poloxamer porosogen (35). It is clear that the azithromycin release rate is rapid and increases with increasing poloxamer content.…”

Section: Cr Microspheresmentioning

confidence: 97%

“…Because azithromycin exhibits pH-dependent solubility, the effect of pH was determined, and Fig. 4 presents the effect of pH on in vitro release of azithromycin from microspheres containing 4% poloxamer (35). It is clear that drug release from these small microspheres would be variable as they transit the varying pH environments of the GI tract and that release would be particularly rapid at pH 6 and below.…”

Section: Cr Microspheresmentioning

confidence: 99%

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Interdisciplinary Science and the Design of a Single-Dose Antibiotic Therapy

Curatolo¹

2011

Pharm Res

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Azithromycin is a unique antibiotic due to its serum half-life of 69 h. This half-life is long enough to permit administration of an entire course of therapy in a single dose, if the gastrointestinal (GI) side effects of such a high dose can be minimized. A series of exploratory clinical pharmacology studies were carried out to understand the site-specific absorption and toleration constraints involved in delivering a 2 g oral single-dose regimen. These studies demonstrated that (a) GI side effects were locally mediated in the GI tract, (b) the duodenum was more sensitive than the ileocecal region, and (c) colonic absorption was limited. A novel controlled release suspension dosage form was designed to meet these constraints, and was shown to deliver the desired systemic dose with acceptable toleration. This dosage form, Zmax®, is an oral powder-for-constitution which possesses two major features: (a) 200 μm controlled release microspheres which release the drug as they transit down the small intestine, and (b) alkalizing agents which raise the pH of the gastric milieu for ~20 min to minimize gastric release of the drug (which has high solubility at low pH), in order to minimize exposure of the drug to the sensitive duodenal region. The ability to provide a high single dose of azithromycin results in "front-loading" the mononuclear and polymorphonuclear leukocytes which concentrate the drug and carry it to sites of infection. This provides high drug concentrations early on at infection sites, when the bacterial burden is greatest, potentially improving efficacy and potentially overcoming resistant bacterial strains. Finally, this revolutionary single dose formulation gives 100% compliance, which maximizes the likelihood of therapeutic success.

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“…The formulation were evaluated clinically and provided complete release within 3 h, good tolerability without decreased bioavailability. 41 A similar formulation could be developed with Pheroid vesicles that could prove successful for malaria treatment.…”

Section: Characterization Of Formulationsmentioning

confidence: 99%

In vitro activity of Pheroid vesicles containing antibiotics against Plasmodium falciparum

et al. 2012

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The macrolide antibiotics, erythromycin and azithromycin, have been studied for their potential antimalarial activity, but only modest activity has been demonstrated. In this study, we investigated the enhancement of the efficacy of these antibiotics in combination with a patented lipid-based drug delivery system, Pheroid technology. A chloroquine resistant strain of Plasmodium falciparum (RSA11) was incubated with the formulations for a prolonged incubation time (144 h). Drug efficacy assays were conducted by analyzing the histidine-rich protein II levels of the parasites. The effects of azithromycin and erythromycin were compared with other antibiotics and standard antimalarial drugs. The poor water soluble nature of the drugs led to the formation of micro scale Pheroid vesicles with average particle sizes of 72.76±10.73 lm for azithromycin and 100.62±29.27 lm for erythromycin. The IC 50 values of erythromycin and azithromycin alone and entrapped in Pheroid vesicles decreased statistically significant (Pp0.05). Prolonged exposure was also statistically meaningful (Pp0.05), although it seems that exposure need not exceed 96 h. Pheroid vesicles also proved successful in decreasing the IC 50 values of doxycycline, tetracycline and triclosan. Pheroid vesicles containing antibiotics could prove successful as a malaria treatment option.

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Formulation design and pharmaceutical development of a novel controlled release form of azithromycin for single-dose therapy

Cited by 37 publications

References 20 publications

Adherence and Non-Adherence to Treatments: Focus on Pharmacy Practice in Nepal

Adherence and Non-Adherence to Treatments: Focus on Pharmacy Practice in Nepal

Interdisciplinary Science and the Design of a Single-Dose Antibiotic Therapy

In vitro activity of Pheroid vesicles containing antibiotics against Plasmodium falciparum

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