UniORV, a New Multi-Unit Dosage Form, Improved Biopharmaceutical Properties of Tacrolimus in Rats and Humans

2020 ◽  
Vol 37 (3) ◽  
Author(s):  
Wataru Hirasawa ◽  
Shunsuke Sei ◽  
Misuzu Mineda ◽  
Norimasa Endo ◽  
Yoshiharu Matahira ◽  
...  
2020 ◽  
Vol 9 (4) ◽  
pp. 88-92
Author(s):  
A. G. Palvinskiy ◽  
E. O. Bakhrushina ◽  
Z. M. Kozlova ◽  
A. A. Sinitsyna ◽  
I. I. Krasnyuk

Introduction. Dental gel is one of the modern dosage forms with optimal biopharmaceutical properties for the treatment and prevention of oral diseases An isoquinoline alkaloid berberine is the promising active substance with antibacterial and anti-inflammatory effect, capable of forming stable dispersed systems with gel-forming components. It is noteworthy that, despite the pronounced antimicrobial activity of the alkaloid berberine, there is currently no dental dosage form with this component on the pharmaceutical market, and therefore research in this direction is of great interest.Aim. Selection of the optimal technology for obtaining dental gel with berberine for the treatment of oral diseases.Materials and methods. Berberine bisulfate (manufactured by CJSC «Vifitech», Obolensk, Moscow region, RF), poloxamers P407 and P338 (EP, USP/N; BASF, Germany), propylene glycol (USP; BASF, Germany), sodium chloride (Sigma-Aldrich, Germany, Cat. No. S9888), mucin type II from a pig stomach (Sigma-Aldrich, Germany, Cat. No. M2378). In the development of the composition and technology for the preparation of gels, a magnetic stirrer with a temperature control function (C-MAG HS 7 from IKA, Germany) was used. Gels were prepared by the «hot method» and «cold method».Results and discussion. The production of the gel by the «hot method» provided a uniform dosage form. The obtained pH value is within the range of optimal diapason. Measurement of the specific peel force of the model gel sample showed pronounced mucoadhesive properties, which indicates that there is no need to adjust this parameter by introducing additional components into the formulation. The spectroscopic method is applicable for the analysis of berberine gel. It has been found that a significant dilution of the reference substance sample is required to develop an identification procedure.Conclusion. The production of a sample of the dosage form by the «hot method» is optimal, which is probably due to the effect of solubilization and better distribution of the active substance in the base.


Author(s):  
IYAN SOPYAN ◽  
ALVIN B. ◽  
INSAN SUNAN K. S. ◽  
CIKRA IKHDA N. H. S.

Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability.


Author(s):  
B. S. Burlaka ◽  
I. F. Belenichev ◽  
V. V. Gladyshev

Recently, in the world, there is a negative dynamics of increasing diseases of the central nervous system. Creation of neuropeptide-based dosage forms with high pharmacological activity, neuroavailability and improved biopharmaceutical properties is an urgent problem today. The development of a novel intranasal dosage form with noopept that has high neuroavailability and therapeutic efficacy deserves attention. The purpose of the work is to conduct thermogravimetric studies to substantiate the possibility of combining active and auxiliary substances in a new intranasal gel with noopept and to characterize its temperature mode of manufacture. The following were used as objects of thermogravimetric studies: separate nasal gel ingredients: noopept (CAS No. 157115-85-0, obtained from Shijiazhuang Prosperity Import and Export Co., Ltd., China. Purity: ≥ 98%), Bischofite Poltava (standardized solution at ZDMU medicine technology department), polysorbate-80 (obtained from Sinbias LLC in Kyiv), sodium CMC (obtained from Sinbias LLC in Kyiv), glycerol (obtained from Sinbias LLC in Kyiv), benzalkonium chloride (obtained from LLC East-plus in Zaporizhzhya), as well as a ready-made intranasal gel without noopept, and a gel with noopept. Thermographic analysis was performed on a Shimadzu DTG-60 (Japan) derivative with a platinum-platinum thermocouple while heating specimens in aluminum crucibles (15 to 250 °C). As the reference substance used α-Al2O3. The heating rate was 10 ºC per minute. The weight of the samples was from 19.22 mg to 57.21 mg. As a result of thermogravimetric studies of the active and auxiliary substances of intranasal gel with noopept it is found that the technological process of making a gel with noopept is advisable to take into account thermolabile compounds, namely, a preservative, it is advisable to enter the formulation at a temperature not higher than 40 ºC. It has been found that the developed formulation of noopept gel is a mixture of active and auxiliary substances, the ingredients of which do not interact and can be combined in one dosage form.


2018 ◽  
Vol 4 (4) ◽  
pp. 523-531
Author(s):  
Hina Mumtaz ◽  
Muhammad Asim Farooq ◽  
Zainab Batool ◽  
Anam Ahsan ◽  
Ashikujaman Syed

The main purpose of development pharmaceutical dosage form is to find out the in vivo and in vitro behavior of dosage form. This challenge is overcome by implementation of in-vivo and in-vitro correlation. Application of this technique is economical and time saving in dosage form development. It shortens the period of development dosage form as well as improves product quality. IVIVC reduce the experimental study on human because IVIVC involves the in vivo relevant media utilization in vitro specifications. The key goal of IVIVC is to serve as alternate for in vivo bioavailability studies and serve as justification for bio waivers. IVIVC follows the specifications and relevant quality control parameters that lead to improvement in pharmaceutical dosage form development in short period of time. Recently in-vivo in-vitro correlation (IVIVC) has found application to predict the pharmacokinetic behaviour of pharmaceutical preparations. It has emerged as a reliable tool to find the mode of absorption of several dosage forms. It is used to correlate the in-vitro dissolution with in vivo pharmacokinetic profile. IVIVC made use to predict the bioavailability of the drug of particular dosage form. IVIVC is satisfactory for the therapeutic release profile specifications of the formulation. IVIVC model has capability to predict plasma drug concentration from in vitro dissolution media.


2017 ◽  
Vol 3 (3) ◽  
pp. 350-353
Author(s):  
Sabeeha Kausar ◽  
Muhammad Imran

Objective: This study was conducted to analyze and evaluate the prevalence of prescription errors, to optimize the medication effectiveness and patient safety and to encourage the rational prescribing practices. Method: sample of 250 prescriptions was randomly collected from outdoor hospital pharmacy (n=157) and from community pharmacy (n=93) and analyzed manually to estimate the prevalence of prescription errors. Results: Results calculated by using SPPS Version 23 and MS Excel 2013 are as follow; 41.4% prescription collected from outdoor hospital pharmacy presented significant prescribing errors while 54.7% in sample collected from community pharmacy. The prescriptions were segregated and errors were estimated using following parameters; dose, dosage form, dosing frequency, drug-drug interactions, spelling, and duplication of generic, therapy duration and unnecessary drugs. Conclusion: The prevalence of prescribing errors in sample of community pharmacy was 12.37% greater than found in prescriptions of hospital pharmacy. The prevalence of prescription errors can be reduced by physician education, using automated prescribing systems and immediate review of prescription by pharmacist before dispensing of prescription items to patients.


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