Features, applications, and sustainability of lipid nanoparticles in cosmeceuticals.

Cosmeceuticals are a branch of cosmetic products that forms a bridge between cosmetic and drug products. It is a fast-growing branch of the cosmetic industry, especially after the introduction of novel formulation and manufacturing techniques such as lipid nanoparticles (LNPs). These LNPs-based cosmeceutical products offer several advantages such as enhanced bioavailability of cosmeceutical active ingredients (CAIs), improved aesthetic appeal, and stability of the final products. However, the use of these LNPs may raise some concerns about possible side effects of these LNPs and potential hazards to the customer's health. Accordingly, an update that focuses on the use of this important branch of nanoparticles is necessary since most review papers are dealing with all types of nanocarriers in the same review with little focus on LNPs. Therefore, in the current review, a detailed analysis of the advantages and disadvantages of LNPs in this field was highlighted, to emphasize the LNPs-based cosmeceuticals on the market, as well as the potential risk posed by LNPs on exposure and recently introduced regulatory guidelines to address them. In addition, if these products can be a candidate as products that meet the sustainable development goals raised by the UN are discussed.

Knowledge, Perceptions and Attitudes among Sharia Practitioners in Palestine Regarding Halal Pharmaceuticals: An Exploratory Study.

The purpose of this questionnaire-based cross-sectional study was to investigate the knowledge, perceptions, and attitudes regarding halal pharmaceuticals among sharia practitioners in Palestine. A total of 420 sharia practitioners with different educational levels were included. This was a cross-sectional study conducted between March and July 2021 with the use of a standardized, self-administered questionnaire. Volunteers were selected throughout Palestine using a systematic random selection approach. The data were summarized using descriptive statistics (mean, standard deviation, frequency, percentage, median, and interquartile range). The Chi-square and Fisher's exact tests were used to examine the relationship between demographic factors and the knowledge, attitude, and perception scores, respectively. The results revealed that sharia practitioners have relatively good and positive knowledge toward halal pharmaceuticals. The main knowledge of most halal pharmaceuticals was about 50.2%, yet there is still significant latitude in their knowledge of a few issues. The main attitude and perception score was about 96.4%. The results showed a positive and fair correlation between knowledge and attitude (r = 0.153, P < 0.001) and also between knowledge and perception (r = 0.341, P < 0.001). In addition, there is a good correlation between attitude and perception (r = 0.681, P < 0.001). The study concluded that better knowledge of halal pharmaceuticals is associated with positive perceptions and behaviors. The government, pharmaceutical manufacturers, religious scholars, and health care professionals should collaborate to achieve the goal of using halal medications.

Herbal remedies used for the treatment of infertility in males and females by traditional healers in the rural areas of the West Bank/Palestine.

BACKGROUND: Infertility is considered one of the global public health problems and during human history, it is also considered one of the unsolved problems of the continuous human race. This study aimed to collect and document the ethnopharmacological data on herbal remedies, which traditionally used by Palestinian healers in the rural areas of the West Bank area for the treatment of infertility in males and females. METHODS: Using a semi-structured questionnaire, an ethnopharmacological survey of medicinal plants used for the treatment of infertility in the West Bank area of Palestine was investigated. This survey involved 51 traditional healers which were interviewed in rural areas from 9 Palestinian regions. RESULTS: Information about 31 plants used in the treatment of infertility in females and 24 plants used in the treatment of infertility in males were collected. This information including names of plants, parts used, mode and methods of preparation which were obtained from 51 traditional healers interviewed in rural areas of 9 regions of the West Bank/Palestine. This investigation is the first scientific work in the Middle East area which collected information about herbal remedies used by local Palestinian traditional healers for the treatments of infertility in males and females. The highest Frequency of Citation (FC) of herbal remedies used in case of infertility in females, were 98.04% for pollen grains from Ceratonia siliqua, 88.24% for Anastatica hierochuntica fruits and 84.31% for Parietaria judaica leaves, while the highest Frequency of Citation (FC) of herbal remedies used in case of infertility in males were 96.08% for Ferula hermonis roots, 88.24% for Phlomis brachyodon leaves and 86.27% for Phoenix dactylifera pollen grains. CONCLUSION: Herbal healers in the West Bank area of Palestine have a wide range of herbal remedies used in case of infertility in males and in females. Unfortunately, most of them lack scientific evidence of pharmacological or toxicological nature. Therefore, the information obtained in this study can serve as a scientific base for further investigations to determine their efficacy and safety which might contribute to better integration of Palestinian traditional medicine into the global health system in the future.

Evaluation of food effect on the oral absorption of clarithromycin from immediate release tablet using physiological modelling.

BACKGROUND: Food may affect the oral absorption of drugs. PURPOSE: The aim of the present study was to investigate the influence of food on the oral absorption of clarithromycin by evaluating the effect of media parameters, such as pH, bile secretions and food composition, on the release of the drug from immediate release tablets, using in vitro and in silico assessments. METHOD: The solubility, disintegration and dissolution profiles of clarithromycin 500 mg immediate release tablets in compendial media with/without the addition of a homogenized FDA meal as well as in biorelevant simulated intestinal media mimicking fasting and fed conditions were determined. These in vitro data were input to GastroPlus™, which was used for developing a physiological absorption model capable of anticipating the effect of food on clarithromycin absorption. Level A in vitro-in vivo linear correlations were established using a mechanistic absorption modelling based deconvolution approach. RESULTS: The pH of the media has a profound effect on clarithromycin solubility, tablet disintegration and drug release. Clarithromycin has lower solubility in biorelevant media compared with other media, due to complex formation with bile salts. Clarithromycin tablets exhibited prolonged disintegration times and reduced dissolution rates in the presence of the standard FDA meal. The simulation model predicted no significant food effect on the oral bioavailability of clarithromycin. The developed IVIVC model considered SIF, acetate buffer and FaSSIF media to be the most relevant from the physiological standpoint. CONCLUSION: The intake of a standard FDA meal may have no significant effect on the oral bioavailability of clarithromycin immediate release tablet.

Rapid, cost-effective and organic solvent-free production of biologically active essential oil from Mediterranean wild Origanum syriacum.

BACKGROUND: Origanum syriacum (O. syriacum) is a very popular edible and medicinal plant in the East Mediterranean countries. The aims of the current study were to use microwave-ultrasonic assisted hydrodistillation (MUAHD) method to produce essential oils (EOs) from wild O. syriacum samples collected from four different geographical areas in The West Bank using water as a solvent, determine the phytochemical profile using GC-MS analysis and assess their antioxidant and antibacterial potential. METHODS: Essential oils were produced using MUAHD method. Gas chromatography coupled with mass spectrometer detector (GC-MS) was employed for phytochemical analysis. In vitro antibacterial and antioxidant potentials were carried out. RESULTS: Differences in the EOs yield among the four Origanum samples were observed. GC-MS analysis of EOs revealed terpenes as the major constituents; monoterpenes (22-56%) and oxygenated monoterpenes (28-57%). Thymol, α-terpinene and carvacrol represent the bulk of all phytochemicals detected by GC-MS analysis. γ-Terpinene-rich EOs, exhibited the highest antioxidant capacity. Thymol-rich EOs were found to be most effective against Staphylococcus aureus and Methicillin-Resistant Staphylococcus aureus (MRSA) (MIC 390 µg/mL). Alpha-terpinene-rich chemotype EOs exhibited the highest inhibitory effect of Pseudomonas aeruginosa (MIC of 1560 µg/mL). Interestingly, γ-terpinene-rich EO showed promising antibacterial properties against Enterococcus faecium (MIC 97 µg/mL) and a powerful anti-oxidant effect (91.45% ±2.30). CONCLUSION: The current study supports the use of MUAHD as a time-saving, cost-effective, environment-friendly method for production of high quality O. syriacum EO for potential use as a natural complementary treatment and in the prevention of bacterial infections as well as oxidation by free radicals without compromising the quantity.

Impact of formulation variables on weight uniformity of scored tablets using factorial design.

Maintaining safety and efficacy is an important task when splitting a tablet. This Pharmacy practice affords the patient with unavailable required dose, easy swallowing, and cost-saving measure. To access the role of formulation variables on the weight uniformity test of halves tablets. Uncoated and coated placebo tablets were prepared using wet granulation technique. After compression, hardness, disintegration time, friability and weight variation were evaluated according to the USP test. Both coated and uncoated tablets were dived and the obtained halves were weighed and the uniformity of halves was assessed for each kind of tablets. Despite the hardness, size, tablet shape (oval, disc, capsule), all of them passed the splitting test except for the disc shape which showed %RSD higher than 6%. However, hardness and the coating had a generally positive trend on tablet breaking since they gave low% RSD. These findings suggest that the disc shape particle is not suitable for breaking. In addition, film coating, as well as high hardness may give better uniformity of the obtained halves, since a decrease in the calculated %RSD was observed.

Covalent functionalization of SWCNT with combretastatin A4 for cancer therapy.

Single walled carbon nanotubes (SWCNT) are currently under intensive investigation by many labs all over the world for being promising candidates for cancer chemotherapy delivery. On the other hand, combretastatin A4 (CA4) is an anticancer drug that induces cell apoptosis by inhibiting tubulin polymerization. However, it has the disadvantage of low water solubility and the non-selective targeting. Therefore, we aim to create nano-drug from the functionalization of SWCNT covalently with CA4 through click reaction in the presence of tetraethylene glycol linker in order to improve its dispersibility. Scanning electron microscopy and transmission electron microscopy showed good dispersibility of the functionalized SWCNT with diameters of 5-15 nm. Moreover, thermogravometric analysis showed that the efficiency of SWCNT functionalization was around 45%. The in vitro release profile of CA4 at physiological conditions showed that approximately 90% of the loaded drug was released over 50 h. After that MTS test was used to determine the suitable concentration range for the in vitro investigation of the SWCNT-CA4. After that the cytotoxic activity of the SWCNT-CA4 was evaluated by flow cytometry using annexin V/propidium iodide (PI) test. In comparison with free CA4, SWCNT-CA4 treatment demonstrated a significant increase in necrotic cells (around 50%) at the expense of the proportion of the apoptotic cells. Moreover, cell cycle PI test demonstrated that free CA4 and SWCNT-CA4 caused G2/M arrest. However with CA4 treatment higher proportion of cells were in the S-phase while with SWCNT-CA4 treatment greater proportion of cells appeared to be in the G1-phase. Taken together, the provided data suggest that the novel SWCNT-CA4 has a significant anticancer activity that might be superior to that of free CA4.

The Taste of Commercially Available Clarithromycin Oral Pharmaceutical Suspensions in the Palestinian Market: Electronic Tongue and In Vivo Evaluation.

Background: The taste of oral liquid dosage forms is a crucial factor that impacts paediatric patient compliance. The electronic tongue (ET) is an emerging tool that could be useful in taste assessment in order to minimize the involvement of humans in such evaluations. Purpose: The aim of this study is to evaluate the taste of commercially available clarithromycin (CM) oral pharmaceutical suspensions in the Palestinian market. Method: Commercially available CM suspensions (the brand Klacid® and two generic K1 and K2) were assayed using the high performance liquid chromatography (HPLC) method. Then, the taste of these products was assessed using alpha-astree ET. In addition, an in vivo taste assessment was conducted on paediatric patients by a hedonic panel test. Moreover, volunteering community pharmacists were asked to rank the taste of these three products according to their experience from the best to the worst. Results: All suspension products had a CM concentration not less than 98% of the label amount. The ET results coupled with the principal component analysis (PCA) showed a very clear discrimination of the samples with different distances between groups (p-values < 0.001). Suspensions were in the following order in terms of taste: Klacid® > K1 > K2. Moreover, The pattern discrimination index between (K1 and Klacid®), (K1 and K2) and (Klacid® and K2) were 8.81%, 65.75%, and71.94%, respectively which suggests that K1 and Klacid® are the most similar preparations in terms of taste. Interestingly, these results were in excellent agreement with the pharmacist ranking and patient acceptance test. Conclusions: The evaluated preparations showed significantly different taste within the order of Klacid® > K1 > K2, as suggested by both the ET and in vivo results. Moreover, our results confirm the capability of alpha-astree ET in the taste assessment of oral suspensions and in predicting volunteer responses, which highlights its beneficial use as an in vitro taste assessment tool and as an alternative to human-based taste evaluations.

Ethnopharmacological survey of home remedies used for treatment of hair and scalp and their methods of preparation in the West Bank-Palestine.

BACKGROUND: Natural products have many uses and purposes, including those linked to pharmaceutics and cosmetics. The aim of this study was to investigate the use of natural remedies for the treatment of hair and scalp disorders in the West Bank, Palestine. METHODS: An ethnopharmacological survey of herbal remedies and other natural products used in cosmetics and cosmeceuticals was carried out in the West Bank, Palestine. A questionnaire was distributed to 267 herbalists, traditional healers, hairdressers and rural dwellers. Collected information included: the names of plants and other natural products, the parts used, hair conditions, diseases and problems for which these products were used and also their methods of preparation. To identify the most important species used, the factor of informant's consensus (Fic), fidelity level (Fl) and the use-value (UV) were calculated. RESULTS: Collected data showed that 41 plants are utilized for the treatment of hair and scalp disorders, belonging to 27 families; among them Lamiaceae and Rosaceae, which were the most commonly used. Plant oils and their fruits are the most commonly used parts. Hair loss, dandruff, split hair endings and lice treatment, are reported as the most treated disorders. The number of plant species used consisted of 19, 14, 13, and again 13 with a factor of informant's consensus (Fic) for these disorders corresponding to 0.93, 0.94, 0.95 and 0.92, respectively. Fl was 100% for many plants; the highest UV value (0.84) was registered for Lawsonia inermis, which belongs to the Lythraceae family. CONCLUSIONS: This study showed that many natural remedies are still used in Palestine for the treatment of scalp and hair disorders as well as for cosmeceutical purposes. This study is of great importance as it allows us to have a greater perspective on our folkloric use of these natural products. A combined scientific effort between informants and the scientific community, working in this field, may help in the discovery of new cosmetics, cosmeceutical and nutraceutical products.

Ethnopharmacological survey of medicinal plants practiced by traditional healers and herbalists for treatment of some urological diseases in the West Bank/Palestine.

BACKGROUND: Throughout history, every civilization in the world used plants or their derivatives for treatment or prevention of diseases. In Palestine as in many other countries, herbal medicines are broadly used in the treatment of wide range of diseases including urological diseases. The main objective of this research is to study the use of herbal remedies by herbalists and traditional healers for treatment of various urological diseases in the West Bank regions of Palestine and to assess their efficacy and safety through the literature review of the most cited plants. METHOD: The study included a survey part, plant identification and a review study. The first part was a cross-sectional descriptive study. Face to face questionnaires were distributed to 150 traditional healers and herbalist in all regions of the West Bank of Palestine. The literature review part was to assess the most cited plants for their efficacy and toxicity. RESULTS: One hundred forty four herbalists and traditional healers accepted to participate in this study which was conducted between March and April, 2016. The results showed that 57 plant species belonging to 30 families were used by herbalists and traditional healers for treatment of various urinary tract diseases in Palestine. Of these, Apiaceae family was the most prevalent. Paronychia argentea, Plantago ovata, Punica granatum, Taraxacum syriacum, Morus alba and Foeniculum vulgare were the most commonly used plant species in the treatment of kidney stones, while Capsella bursa-pastoris, Ammi visnaga and Ammi majus were the most recommended species for treatment of urinary tract infections and Portulaca oleracea used for renal failure. In addition Curcuma longa and Crocus sativus were used for enuresis while Juglans regia, Quercus infectoria, Sambucus ebulus and Zea mays were used for treatment symptoms of benign prostate hyperplasia. Fruits were the most common parts used, and a decoction was the most commonly used method of preparation. Through literature review, it was found that Paronychia argentea has a low hemolytic effect and contains oxalic acid and nitrate. Therefore, it could be harmful to renal failure patients, also Juglans regia, Quercus infectoria and, Sambucus ebulus are harmful plants and cannot be used for treatment of any disease. CONCLUSIONS: Our data provided that ethnopharmacological flora in the West Bank regions of Palestine can be quite wealthy and diverse in the treatments of urinary tract diseases. Clinical trials and pharmacological tests are required evaluate safety and efficacy of these herbal remedies.

Topical aqueous extract of Ephedra alata can improve wound healing in an animal model.

PURPOSE: Ephedra alata (E. alata) is perennial tough shrub plant that grows in Palestine and other regions. It is used often in folk's medicine for the treatment of various diseases. In this project, E. alata extract was tested for its ability to improve wound and burn healing. METHODS: An aqueous extract of E. alata was prepared and underwent several phytochemical analyses for the presence of the major classes of phytochemical compounds. After that, a polyethylene glycol-based ointment containing the extract of E. alata was prepared and its wound and burn healing activities were tested in-vivo using an animal model for deep wound and full thickness skin burn. The effect was compared against a placebo ointment. Skin biopsies were evaluated by a blinded clinical histopathologist, in addition to digital analysis. RESULTS: Phytochemical analysis demonstrated the presence of the major classes of phytochemical compounds in the prepared extract including flavonoids, alkaloids, phytosteroids, phenolic compounds, volatile oils and tannins. As compared to placebo ointment, E. alata ointment significantly improved the healing of the wound ulcers, whereas it showed no advantage on the quality of the healing of burn ulcers. CONCLUSION: E. alata extract is rich in phytochemical compounds and can improve wound healing when applied topically.

Bioequivalence assessment of two pregabalin capsules in healthy Mediterranean Arab volunteers.

BACKGROUND: Treatment of neuropathic pain has always been challenging, not only from the pharmaco-therapeutic/toxicological point of view, but also due to the unpredictable pharmacokinetic (PK) variations among different generic formulations of the same drug, which require further dose optimization. OBJECTIVES: This progressive work aims to evaluate the bioequivalence (BE) of a generic product of 150 mg pregabalin capsule (antineuropathic drug) vs. the reference brand drug Lyrica^®. METHOD: An LC-MS/MS bioanalytical method was developed and validated according to the International Conference on Harmonization (ICH) guidelines in order to be used for the analysis of pregabalin in plasma. BE of capsules was tested by comparison against the reference brand capsules in accordance with the requirements of the declarations of Helsinki, the current Good Clinical Practice (GCP) Guidelines and the ICH. The resulting data were compared against corresponding pregabalin data published on other human races. RESULTS: The relationship between concentration and peak area ratio was found to be linear within the range 0.096 - 6.068 µg/mL for pregabalin. The correlation coefficient (r) was equal to 0.9983. Statistical comparison of the main PK parameters showed no significant difference between test and reference. The mean Cmax values for test and reference were 4.290 and 4.164 µg/mL, and the mean AUC0-last values were 24.275 h×µg/mL and 23.674 h×µg/mL, respectively. The 90% CIs of geometric mean ratios (test/reference) for pregabalin were 100.34 - 104.78%, 100.34 - 104.70%, and 95.65 - 110.96% for AUC0-last, AUC0-∞, and Cmax, respectively, thus fall within the international specified BE limit (80 - 125%). Both products were well tolerated by all the volunteers and there were no significant differences on physical examination or in vital signs and laboratory tests between groups. All volunteers completed the study and were discharged in good health. CONCLUSION: The tested generic capsules appear to be bioequivalent to the reference brand and are expected to have a similar efficacy and safety profile.

Chemical composition, anthelmintic, antibacterial and antioxidant effects of Thymus bovei essential oil.

BACKGROUND: It has been recently recognized that oxidative stress, helminth and microbial infections are the cause of much illness found in the underdeveloped, developing and developed countries. The present study was undertaken to identify the chemical composition, and to assess anthelmintic, antimicrobial and antioxidant effects of Thymus bovei essential oil. METHODS: The chemical composition of the essential oil was analyzed using gas chromatography mass spectrometry (GC-MS). Antimicrobial activity was tested against the selected strains from American Type Culture Collection (ATCC) and clinical isolates such as Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Methicillin Resistant Staphylococcus aureus, Candida albicans using MIC assay. The anthelmintic assay was carried out on adult earthworm (Pheretima posthuma), while antioxidant activity was analyzed using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging method. RESULTS: Trans-geraniol (35.38 %), α-citral (20.37 %) and ß-citral (14.76 %) were the major compounds comprising 70.51 % of the essential oil. Our results showed that T. bovei essential oil exhibited strong anthelmintic activity, even higher than piperazine citrate, the used reference standard, with potential antioxidant activity almost equal to the Trolox standard. Furthermore, T. bovei essential oil had powerful antibacterial and antifungal activities against the studied pathogens. CONCLUSION: Essential oil of T. bovei exerted excellent antioxidant, antimicrobial, and anthelmintic activities. Moreover, this study found that T. bovei volatile oil contains active substances that could potentially be used as natural preservatives in food and pharmaceutical industries, these substances could also be employed for developing new anthelmintic, antimicrobial and antioxidant agents.

Ethnopharmacological survey of herbal remedies used for treatment of various types of cancer and their methods of preparations in the West Bank-Palestine.

BACKGROUND: Plants have been the primary source of medicines since life on earth; more than 50 % of existing cancer treatments are derived from plants. METHODS: An ethnopharmacological survey of herbal remedies used in cancer treatment was carried out in the West Bank/ Palestine. A questionnaire was distributed to one hundred and fifty herbalists, traditional healers and rural dwellers. Collected information included the names of plants, the used parts, types of cancers for which these plants were used and also their methods of preparation. To identify the most important species used, Factor of informant's consensus (F(ic)), Fidelity level (Fl) and the Use-value (UV) were calculated. RESULTS: Collected data has shown that 72 plants are utilized for treatment of cancer, belonging to 44 families; from them Compositae and Lamiaceae were the most common. Leaves and fruits were the most commonly used parts, while decoctions, infusions and syrups were the main methods of preparation. Lung cancer was the most common type of cancer treated with these plants and Ephedra alata was the most commonly used plant for treatment of cancer in Palestine. The Fic was high for all the plants; Fl was 100% for many plants, the highest UV (0.72) was for Ephedra alata. CONCLUSIONS: This study showed that many herbal remedies are still used by herbalists in Palestine for treatment of cancer; some of them have been approved scientifically while others are not. A combined effort between informants and scientific institutions working in this field can help in the discovery of new anticancer agents. Moreover, scientists must explore the most suitable method of extraction, formulation and dose determination in order to achieve the best benefits from these herbals.

PHARMACEUTICAL QUALITY OF GENERIC ATORVASTATIN PRODUCTS COMPARED WITH THE INNOVATOR PRODUCT: A NEED FOR REVISING PRICING POLICY IN PALESTINE.

Atorvastatin reduces morbidity and mortality due to cardiovascular events. This study was conducted to assess the prices and pharmaceutical quality of innovator atorvastatin 20 mg with its locally available generics in Palestine and to assess the suitability of their interchangeability. The prices of innovator and generic atorvastatin 20 mg were determined and compared. Innovator atorvastatin and four generic products were tested for their pharmaceutical quality. Tablets were tested for their drug contents, weight uniformity, hardness, disintegration and dissolution. Three out of four generics were less expensive than the innovator. Pharmaceutical quality assessments were satisfactory and within limits for all atorvastatin tested products. The average weight ranged from 206.6 ± 8.40 to 330 ± 3.92 mg and the %RSDs were within the permitted limits as per USP. Tablet hardness ranged from 102 ± 1.41 to 197.4 ± 6.88 kg and drug contents ranged from 92.2% to 105.3%. All products disintegrated within permitted time limits and showed very rapid dissolution. Products released more than 85% of their drug contents in less than 15 min. Our results showed that all tested innovator and generic atorvastatin products were of good pharmaceutical quality. Despite the lack of in vivo evaluation, our results indicate that these products are equivalent in vitro. Considering the in vitro release characteristics, these products might be used interchangeably. However, regulatory authorities permit the use of in vitro data in establishing similarity between immediate release oral dosage forms containing biopharmaceutical classification system class I and III drugs only.

Formulation and bioequivalence of two sildenafil 50 mg film-coated tablets after a single oral administration.

OBJECTIVE: The aims of this study were to establish a bioanalytical method and to evaluate the bioequivalence of two drug products; a generic sildenafil 50 mg film-coated vs. the brand drug Viagra® 50 mg film-coated tablets. METHOD: Bioequivalence of tablets was tested by comparisons against the reference brand product in accordance with the requirements of the Declaration of Helsinki, the current Good Clinical Practice (GCP) Guidelines and the International Conference Harmonization (ICH). RESULTS: The relationship between concentration and peak area ratio was found to be linear within the range of 1.435 - 410.023 ng/mL for sildenafil. The correlation coefficient (r) was always greater than 0.99 during the course of the validation Statistical comparison of the main pharmacokinetic parameters showed no significant difference between test and reference. The 90% CIs of geometric mean ratios (test to reference ratios) were 99.656%, 99.806%, and 109.227% for AUC(0-last), AUC(0-∞), and C(max), respectively. These pharmacokinetic parameter values lie within the FDA and European Medicines Agency specified bioequivalence limit (80 - 125%). Both formulations were well tolerated by all subjects and they were discharged in good health. CONCLUSION: The tested drug product was bioequivalent to the reference drug and had the same safety profile.

Formulation and bioequivalence of two Valsartan/Amlodipine immediate release tablets after a single oral administration.

The aim of this study was to formulate a film-coated Valsartan/Amlodipine (VS/AM) immediate release tablets and to evaluate their in vivo release profile. VS/AM core tablets were manufactured using dry granulation method. Opadry aqueous coating dispersion was used as film coating material. Dissolution of the film coated tablets was tested in 900 ml of 0.5% SLS media, bioequivalence of tablets was tested by comparisons against the reference brand product. The ICH guidelines were used to evaluate the stability of the obtained tablets. The coated tablets were subjected to gastric pH, and drug release was analyzed using HPLC system to evaluate the efficiency of the film coat. The coated tablets had no defects. VS/AM release met the FDA guidelines for bioequivalence studies. Statistical comparison of the main pharmacokinetic parameters showed no significant difference between test and reference. These findings suggest that aqueous film coating with Opadry system is an easy and economical approach for preparing stable film coated VS/AM tablets without compromising their in vivo drugs release.

Weight and content uniformity of lorazepam half-tablets: A study of correlation of a low drug content product.

The aim of this study was to investigate the degree of correlation between the weight and the content of spilt-halves of lorazepam 2.5 mg tablets. Weight variation and drug content of lorazepam half-tablets were evaluated according to the European Pharmacopoeia tests. Only one individual mass of the 30 half tablets was outside the limits of 85-115% of the average mass, but since it was within 75-125% of the average mass, the product passed the test. Each individual content was between 85% and 115% of the average content (99.8% expressed as a percent to label claim) and within the limits of 75-125%, so the product passed the uniformity of content test. The correlation coefficient (r) between the weight and the content of split halves was found to be 0.994. The weights of split tablet halves appear to be directly correlated with their drug content even for a medication with a low drug content, thus it is recommended that pharmacists who split tablets into two halves, assure the weight uniformity of the resultant halves. Manufacturers should develop formulation and manufacturing procedures that ensure high degree of correlation between weight and content not only among the whole tablet but also among the obtained tablet halves.

Current iodine nutrition status and progress toward elimination of iodine deficiency disorders in Jazan, Saudi Arabia.

BACKGROUND: The term iodine deficiency disorders (IDD) refers to all the effects of iodine deficiency on growth and development in human and animal populations that can be prevented by correction of the iodine deficiency. The objective of this paper was to determine the iodine nutrition status among schoolchildren in the Jazan Region of the Kingdom of Saudi Arabia (KSA), by measuring urinary iodine concentrations and by clinical assessments of goiter rate. METHODS: A school-based cross-sectional survey was conducted in the Jazan region of southwestern KSA from May to November 2010. A total of 311 children, aged 6-13 years, drawn from 12 schools, were selected by a three-stage cluster random sampling method. Data on sociodemographic characteristics were collected using a structured questionnaire. Urine samples were collected and physical examinations were conducted to determine the presence or absence of goiter. Data were analyzed using SPSS version 17.0. Chi square and independent t-tests were used for proportions and mean comparisons between groups. RESULTS: Out of 360 selected children, 311 were examined. There were 131 males (42%) and 180 females (58%). The median urinary iodine concentration (UIC) of the study group was 421 µg/L. The study population proportion with UIC > 300 µg/L was 74% with a higher proportion among males and urban populations. The proportion of children with UIC of 100-300 µg/L was only 21% and was significantly higher among females compared with males (p < 0.001). Only about 3% of the children had a median UIC less than 50 µg/L. The prevalence of total goiter rate (TGR) among the sample of schoolchildren in Jazan was 11%, with significant variations between rural and urban populations and by gender. CONCLUSIONS: The present study demonstrates a remarkable achievement in Universal Salt Iodization (USI) and IDD elimination goals in the Jazan area. However, UIC levels reflect excessive iodine intake and may put the population at risk of adverse health consequences like iodine-induced hyperthyroidism and autoimmune thyroid diseases.

Development and stability evaluation of enteric coated Diclofenac sodium tablets using Sureteric.

This study was aimed to develop a stable enteric coated diclofenac sodium tablets using Sureteic without a subcoating layer. Diclofenac uncoated tablets were developed and manufactured through the non direct compression process. Sureteric white aqueous coating dispersion was used as enteric coating material. Sureteric is a special mixture of Polyvinyl Acetate Phthalate (Phthalavin (R), PVAP), plasticizers and other ingredients in a suitable optimized dry powder formulation. The obtained enteric coated tablets were subjected to disintegration and no sign of cracking was observed when they placed in a hydrochloric solution at pH 1.2, but they were completely disintegrated within 10 minutes when they putted in buffered solution at pH6.8. Dissolution test was also conducted by placing tablets in 0.1 M HCl for 2 hours and then 1 hour in phosphate buffer at pH 6.8. Less than 0.9% of drug was released in the acidic phase and up to 97% in the basic medium. These results show that Sureteric can be successfully used to produce diclofenac sodium enteric coated tablets in order to prevent its release in the stomach and facilitate immediate release of the drug in the duodenum. These findings suggest that aqueous enteric coating with Sureteric system is an easy and economical approach for preparing stable diclofenac sodium enteric coat without the use of a subcoating layer.