scholarly journals Thermogravimetric investigation of a new intranasal gel with noopept

2019 ◽  
pp. 54-61
Author(s):  
B. S. Burlaka ◽  
I. F. Belenichev ◽  
V. V. Gladyshev
Keyword(s):  
Dosage Form ◽  
Temperature Mode ◽  
The Central Nervous System ◽  
Thermographic Analysis ◽  
Import And Export ◽  
Thermogravimetric Investigation ◽  
Thermogravimetric Studies ◽  
Α Al2o3 ◽  
Biopharmaceutical Properties ◽  
Platinum Thermocouple

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.

scholarly journals Development of Thermoreversible Dental Gel with Berberine

2020 ◽  
Vol 9 (4) ◽  
pp. 88-92
Author(s):  
A. G. Palvinskiy ◽  
E. O. Bakhrushina ◽  
Z. M. Kozlova ◽  
A. A. Sinitsyna ◽  
I. I. Krasnyuk
Keyword(s):  
Active Substance ◽  
Dosage Form ◽  
Ph Value ◽  
Control Function ◽  
Spectroscopic Method ◽  
Isoquinoline Alkaloid ◽  
Oral Diseases ◽  
Treatment And Prevention ◽  
Optimal Technology ◽  
Biopharmaceutical Properties

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.

scholarly journals SYSTEMATIC REVIEW: COCRYSTAL AS EFFORTS TO IMPROVE PHYSICOCHEMICAL AND BIOAVAILABILITY PROPERTIES OF ORAL SOLID DOSAGE FORM

2021 ◽  
pp. 43-52
Author(s):  
IYAN SOPYAN ◽  
ALVIN B. ◽  
INSAN SUNAN K. S. ◽  
CIKRA IKHDA N. H. S.
Keyword(s):  
Physicochemical Properties ◽  
Dosage Form ◽  
Water Solubility ◽  
Drug Stability ◽  
Water Soluble ◽  
New Drugs ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Water Soluble Drug ◽  
Biopharmaceutical Properties

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.

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 ◽  
...  
Keyword(s):  
Dosage Form ◽  
Biopharmaceutical Properties

scholarly journals Analysis of patients’ request to switch from a generic drug to the original drug in external prescriptions

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Yuhei Hamada ◽  
Masashi Uchida ◽  
Sayaka Arai ◽  
Kaori Yamazaki ◽  
Mariko Takeda ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Generic Drug ◽  
Dosage Form ◽  
Generic Drugs ◽  
Median Number ◽  
Dosage Forms ◽  
Median Frequency ◽  
Therapeutic Category ◽  
The Central Nervous System

Abstract Background Generic drugs are heavily promoted in Japan. The aim of this retrospective single-center study was to clarify whether the frequency and reason that patients request a switch from a generic drug to the original drug differ according to therapeutic category and dosage form. Methods This study was performed at Chiba University Hospital. Prescription inquiries about 121 generic drugs from community pharmacies over a 3-year period (from July 2014 to June 2017) were analyzed. Results Approximately 30% of the requests were related to the efficacy, safety, and comfort of the generic drug. The most cited motive was “patient’s desire with no reason given” at 44.5%. According to multiple logistic regression analysis, therapeutic categories and dosage forms were associated with the requests. The median request frequency differed according to therapeutic category and dosage form. The frequency was highest for “agents affecting the central nervous system” and “tablets and capsules”, respectively. Among the therapeutic categories, “agents affecting the central nervous system” had the highest median number of requests related to “decreased effectiveness”; “cardiovascular agents” had the highest median number of requests related to “physician’s instruction”; and “agents for the epidermis” had the highest median number of requests related to “uncomfortable to use”. Among dosage forms, the odds ratio for patients’ original drug request for “liniment and patch” was about 1.5 times that for “tablets and capsules”. “Liniment and patch” had the highest median frequency of requests related to “decreased effectiveness”, “uncomfortable to use”, and “patient’s desire with no reason given”. Conclusions The request frequency and reason differed according to therapeutic category and dosage form. Pharmacists should advise each patient properly about the choice and switching of drug brands, taking into account the therapeutic category and dosage form, especially liniments and patches.

scholarly journals Development of a mafedine lyophilizate for parenteral use

2021 ◽  
Vol 10 (4) ◽  
pp. 88-94
Author(s):  
O. A. Terenteva ◽  
V. A. Vainshtein ◽  
V. V. Tikhonova ◽  
A. K. Whaley ◽  
M. A. Trofimov ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Particle Size ◽  
Nervous System ◽  
Zeta Potential ◽  
Dosage Form ◽  
Methylene Chloride ◽  
Ministry Of Health ◽  
Residual Solvent ◽  
The Central Nervous System ◽  
State Chemical

Introduction. Cerebrovascular disease (CVD) is the most important medical and social problem of modern neurology because they have the highest rates of morbidity, mortality and disablement in the population. The growing incidence of CVD as a result of an aging population worldwide requires the emergent development of therapeutics, diagnostic and preventive tools. However, the development of drugs for the treatment of brain diseases has limitations due to the presence of the blood-brain barrier, which protects the brain against most molecules from the bloodstream entering the central nervous system. At the St. Petersburg State Chemical Pharmaceutical University of the Ministry of Health of Russia the alpha-2 adrenergic agonist mafedine was synthesized, which has mild psychostimulant and anxiogenic effects and which may be used in the treatment of traumatic brain injury as a neuroprotective agent.Aim. The development of a dosage form of mafedine in order to improve its penetration into the central nervous system.Materials and methods. Mafedine (pharmaceutical substance) [6-oxo-1-phenyl-2-(phenylamino)-1,6-dihydropyrimidin-4-olate sodium] (St. Petersburg State Chemical-Pharmaceutical University of the Ministry of Health of Russia); lecithin, span-60, Tween-80, Poloxamer 188, mannitol, vitamin E, ascorbic acid, methylene chloride, dimethyl sulfoxide, acetonitrile, trifluoroacetic acid. The fine emulsion of mafedine was obtained by ultrasound. The dosage form of mafedine was obtained by freeze drying. Residual solvents were determined by gas chromatography. Quantitative analysis of mafedine was performed by high-performance liquid chromatography. Particle size and zeta potential of emulsion were determined on a Zetasizer Nano ZS.Results and discussion. Lyophilizate of mafedine was obtained and presenting as a light yellow porous, odorless tablet. The average mass of dry tablet was (0,17 ± 0,01) g with mafedine content is (26 ± 1) mg. The water content in the lyophilizate was 3,85 %. The quantity of methylene chloride in the lyophilizate correspond to the requirements for residual solvent content. The reconstitution time of lyophilizate into a primary emulsion was 3–5 seconds. The reconstituted dispersion was yellow, odorless, and did not break within 2 days during storage. The pH of the reconstituted emulsion was 7,34. The average particle size was (164,7 ± 6,4) nm, the zeta potential was –32 mV.Conclusion. The developed dosage form is stable according to its physicochemical and pharmaceutical characteristics and is suitable for experimental study on models as a neuroprotective and neurorehabilitation agent.

scholarly journals Thermogravimetric studies of a nasal preparation with an interleukin-1β (IL-1Ra) antagonist

2021 ◽  
Vol 14 (1) ◽  
pp. 56-63
Author(s):  
B. S. Burlaka
Keyword(s):  
Active Substance ◽  
Phosphate Buffer ◽  
Benzalkonium Chloride ◽  
Dosage Form ◽  
Interleukin 1 ◽  
Phosphate Buffer Solution ◽  
Tween 80 ◽  
Sodium Carboxymethylcellulose ◽  
Buffer Solution ◽  
Thermogravimetric Studies

Interleukin-1 receptor antagonist (IL-1Ra) is an active pharmaceutical ingredient obtained by the method of gene transformation of Escherichia coli, provides a neuroprotective effect, namely – inhibition of oxidative modification of proteins, normalization of functional activity of mitochondrial energy, mitochondrial energy. Early complex physical-chemical, microbiological, and biopharmaceutical studies have developed a new intranasal formulation, the formulation of which contains: IL-1Ra, sodium carboxymethyl cellulose, D-panthenol, benzalkonium chloride, trilon B, Tween-80, phosphate buffer solution. Given the peculiarities of the technological process, when creating a new gel dosage form, it is necessary to justify the temperature of the carrier base, the introduction of the active substance into the base, as well as to predict the possible chemical interaction of individual components in the dosage form. Therefore, the application of thermogravimetric analysis in pharmaceutical technology is relevant. The aim of the work is to conduct thermogravimetric studies of a new nasal form with an antagonist of interleukin-1β (IL-1Ra). Materials and methods. The objects of thermogravimetric studies were: semi-finished product-solution of the receptor antagonist of interleukin-1 (IL-1Ra). Excipients were: sodium carboxymethylcellulose, tween-80, D-panthenol, trilon B, benzalkonium chloride. To ensure the appropriate pH value used phosphate buffer solution (pH 6.0), according to the recipe to State Pharmacopoeia 2 ed. In addition to the individual components of the finished nasal gel, also prepared nasal gel without IL-1Ra, as well as gel with IL-1Ra. The thermographic analysis was performed on a derivatograph – Shimadzu DTG-60 (Japan) with a platinum-platinum-rhodium thermocouple when heating the samples in aluminum crucibles (from 15 °C to 250 °C). Al2O3 was used as a reference substance. The heating rate was 10 °C per minute. The weight of the test samples ranged from 19.22 mg to 52.91 mg. The derivatograph graphically recorded the obtained data in the form of curves T, DTA, TGA. The T curve on the derivatogram shows the change in temperature, and the TGA curve shows the change in mass of the sample during the study period. The DTA curve reflects the differentiation of thermal effects, contains information about endothermic and exothermic maxima, can be used for qualitative evaluation of the derivatogram. Results. The study consisted of two stages. At the first stage, we studied the derivatograms of experimental samples – individual ingredients of the finished nasal gel - active and excipients, namely: IL-1Ra, sodium carboxymethylcellulose, tween-80, D-panthenol, trilon B, benzalkonium chloride, phosphate buffer solution 6.0. In the second stage, samples of nasal gels were prepared: nasal gel with the required amount of excipients, in addition to the active substance – IL-1Ra, as well as a nasal gel containing IL-1Ra and the required amount of excipients. As a result, we obtained some parameters of thermogravimetric analysis in the form of a graphical image – derivatograms, which were then analyzed. Conclusions. Thermogravimetric studies of individual components of nasal gel with IL-1Ra, as well as nasal gels with active substance and without active substance, were found that the manufacturing process of gel with IL-1Ra should be carried out taking into account thermolabile compounds. First, you need to prepare the base without preservative and IL-1Ra. Then at a temperature not exceeding 40 °C dissolve the preservative, and then when cooled to 20 °C add IL-1Ra. It was found that the developed dosage form of the gel with IL-1Ra is a mixture of active and excipients, the ingredients of which do not interact with each other and can be combined in one dosage form.

Evidence for a Blood Ganglion Barrier in the Superior Cervical Ganglion of the Rat

1982 ◽  
Vol 40 ◽  
pp. 204-204
Author(s):  
D. M. DePace
Keyword(s):  
Blood Vessels ◽  
Superior Cervical Ganglion ◽  
Peripheral Nerves ◽  
Time Schedule ◽  
Transmission Electron ◽  
Cervical Ganglion ◽  
The Central Nervous System ◽  
Cervical Ganglia ◽  
Capillary Circulation ◽  
And Control

The majority of blood vessels in the superior cervical ganglion possess a continuous endothelium with tight junctions. These same features have been associated with the blood brain barrier of the central nervous system and peripheral nerves. These vessels may perform a barrier function between the capillary circulation and the superior cervical ganglion. The permeability of the blood vessels in the superior cervical ganglion of the rat was tested by intravenous injection of horseradish peroxidase (HRP). Three experimental groups of four animals each were given intravenous HRP (Sigma Type II) in a dosage of.08 to.15 mg/gm body weight in.5 ml of.85% saline. The animals were sacrificed at five, ten or 15 minutes following administration of the tracer. Superior cervical ganglia were quickly removed and fixed by immersion in 2.5% glutaraldehyde in Sorenson's.1M phosphate buffer, pH 7.4. Three control animals received,5ml of saline without HRP. These were sacrificed on the same time schedule. Tissues from experimental and control animals were reacted for peroxidase activity and then processed for routine transmission electron microscopy.

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