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1.
Gels ; 9(12)2023 Nov 28.
Article in English | MEDLINE | ID: mdl-38131920

ABSTRACT

BACKGROUND: The aim of this study was to evaluate the moisturizing efficacy of quince fruit, used in folk medicine. For this purpose, the phytoconstituents of Cydonia oblonga fruit extract, like phenolics and flavonoids, were determined. A stable cosmetic emulgel containing 4% Cydonia oblonga fresh fruit extract was formulated and subjected to in vivo evaluation compared with a control. MATERIALS AND METHODS: Cydonia oblonga fresh fruit extract was evaluated for tyrosinase activity and phenolic and flavonoid content. A stable emulgel containing 4% Cydonia oblonga fresh fruit extract was formulated and tested in a skin irritation test. After this, in vivo tests of erythema, moisture, sebum, and skin elasticity were conducted. The in vivo evaluation was a randomized and single-blind study. Thirteen healthy female volunteers were selected for a three-month study period. RESULTS: Cydonia oblonga fruit extract showed good phenolic and flavonoid content, which was associated with its good antioxidant and tyrosinase-inhibiting activity. Cydonia oblonga containing the emulgel showed a reduction in sebum and erythema, while the elasticity and moisture content showed increments in their levels after the three-month application of the formulation. The fruit contains chlorogenic acid and many sugars, which might account for its anti-inflammatory and sebum reduction effects; it is also capable of enhancing the skin's hydration level and decreasing skin sagging by enhancing its elasticity. CONCLUSION: The emulgel loaded with Cydonia oblonga fresh fruit extract is verified regarding its folklore status as a moisturizing agent that enhances the facial skin cells' resilience potential.

2.
Pak J Pharm Sci ; 35(4(Special)): 1173-1179, 2022 Jul.
Article in English | MEDLINE | ID: mdl-36218095

ABSTRACT

Current study was designed to determine the skin elasticity potential of tested emulgel formulations. One emulgel containing Pyrus communis fruit extract and the other had Cydonia oblonga fruit extract. For this purpose 26 female subjects were selected and divided into two batches. Each batch has 13 volunteers, who used tested formulations and their base for 90 days. Skin elasticity were observed by using Cutometer MPA 580. From Cutometer skin mechanical parameters were calculated. From the results it was noted that emulgel formulations containing extracts of Pyrus Communis and Cydonia oblonga showed marked effect on the facial skin mechanical properties during 90 days study period. Statistically observed skin mechanical parameters of tested formulations had significant difference from base. After distention from Cutometer both formulations enhance the retraction ability of the skin as compared to base. Moreover it was also noted that Cydonia oblonga had more pronounced results than Pyrus communis loaded emulgel. From the results it has been interpreted that although both formulations has good potential to hydrate the skin resulting in intensification of its elasticity. As both fruits are rich source of phytonutrients like Vitamin C, Sugar, organic acids which might be the reason of their enhancement potential of skin pliancy.


Subject(s)
Pyrus , Rosaceae , Ascorbic Acid , Female , Fruit , Humans , Phytochemicals , Plant Extracts , Sugars
3.
Med Chem ; 18(7): 791-809, 2022.
Article in English | MEDLINE | ID: mdl-34931968

ABSTRACT

BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are the commonly used therapeutic interventions of inflammation and pain that competitively inhibit the cyclooxygenase (COX) enzymes. Several side effects like gastrointestinal and renal toxicities are associated with the use of these drugs. The therapeutic anti-inflammatory benefits of NSAIDs are produced by the inhibition of COX-2 enzymes, while undesirable side effects arise from the inhibition of COX-1 enzymes. OBJECTIVE: In the present study, a new series of 2-substituted benzoxazole derivatives 2(a-f) and 3(ae) were synthesized in our lab as potent anti-inflammatory agents with outstanding gastro-protective potential. The new analogs 2(a-f) and 3(a-e) were designed depending upon the literature review to serve as ligands for the development of selective COX-2 inhibitors. METHODS: The synthesized analogs were characterized using different spectroscopic techniques (FTIR, 1HNMR, 13CNMR) and elemental analysis. All synthesized compounds were screened for their binding potential in the protein pocket of COX-2 and evaluated for their anti-inflammatory potential in animals using the carrageenan-induced paw edema method. Further 5 compounds were selected to assess the in vivo anti-ulcerogenic activity in an ethanol-induced anti-ulcer rat model. RESULTS: Five compounds (2a, 2b, 3a, 3b and 3c) exhibited potent anti-inflammatory activity and significant binding potential in the COX-2 protein pocket. Similarly, these five compounds demonstrated a significant gastro-protective effect (**p<0.01) in comparison to the standard drug, Omeprazole. CONCLUSION: Depending upon our results, we hypothesize that 2-substituted benzoxazole derivatives have excellent potential to serve as candidates for the development of selective anti-inflammatory agents (COX-2 inhibitors). However, further assessments are required to delineate their underlying mechanisms.


Subject(s)
Benzoxazoles , Cyclooxygenase 2 Inhibitors , Animals , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Benzoxazoles/chemistry , Benzoxazoles/pharmacology , Benzoxazoles/therapeutic use , Carrageenan/adverse effects , Cyclooxygenase 1/metabolism , Cyclooxygenase 2/metabolism , Cyclooxygenase 2 Inhibitors/chemistry , Cyclooxygenase 2 Inhibitors/pharmacology , Edema/chemically induced , Edema/drug therapy , Molecular Docking Simulation , Rats , Structure-Activity Relationship , Ulcer
4.
Pak J Pharm Sci ; 30(1): 11-16, 2017 Jan.
Article in English | MEDLINE | ID: mdl-28603106

ABSTRACT

180 million people are affected by chronic Hepatitis C Virus infection globally and more than 50 million in South East Asia. Combination of Interferon and Ribavirin is the current anti-HCV therapy in practice and is associated with certain hematologic adverse effects. In this concurrent observational study the incidence rate of major hematologic adverse effects and efficacy outcomes of Interferon and Ribavirin combination therapy was evaluated in 288 chronic hepatitis C patients at Lahore General Hospital. Levels of Hb, TLC, and Platelets counts were monitored for hematologic adverse effects monitoring, whereas, ALT, AST and bilirubin levels were monitored for efficacy. PCR was done at week 4, 12 &36 for therapeutic success evaluation. A significant reduction in Hb levels (p<0.05) was observed after week 4, 8 and 12 of therapy. Frequency of anemia increased in both genders with body weight <65kg and platelet count <150,000/mm3. End Treatment Response (ETR) was achieved in 64.5%. Anemia was the major side effect of the combination therapy particularly in the males. Higher ETR was observed in patients who achieved RVR and were <50 years of age.


Subject(s)
Anemia/chemically induced , Antiviral Agents/adverse effects , Hepatitis C, Chronic/drug therapy , Interferons/adverse effects , Ribavirin/adverse effects , Adult , Age Factors , Anemia/blood , Anemia/diagnosis , Anemia/epidemiology , Biomarkers/blood , Drug Therapy, Combination , Female , Hemoglobins/metabolism , Hepatitis C, Chronic/blood , Hepatitis C, Chronic/diagnosis , Hepatitis C, Chronic/epidemiology , Humans , Incidence , Male , Middle Aged , Pakistan/epidemiology , Risk Factors , Sex Factors , Sustained Virologic Response , Time Factors , Treatment Outcome
5.
Pak J Pharm Sci ; 29(2): 603-7, 2016 Mar.
Article in English | MEDLINE | ID: mdl-27087082

ABSTRACT

This study was conducted to evaluate the availability of antidotes/key emergency drugs in tertiary care hospitals of the Punjab province, and to assess the knowledge of health care professionals in the stocking and administration of antidotes in the proper management of poisoning cases. Seventeen (n=17) tertiary care hospitals of Punjab Pakistan were selected. Two performas (A and B) were designed for 26 antidotes/key emergency drugs and given to the hospital pharmacists and physicians respectively. It was observed that Activated Charcoal, being the universal antidote was found only in 6 hospitals (41%). Digoxin Immune Fab, Edentate Calcium disodium and Glucagon were not available in emergency department of any hospital and even not included in the formulary of any hospital. About 80% pharmacists were aware of the method of preparation of Activated Charcoal and 85% physicians were familiar with its route of administration. Data showed that tertiary care hospitals of Punjab do not stock antidotes according to national drug policy. Moreover the study strongly suggests the development of health care centers and professional by organizing antidote awareness programs, continuous education and record keeping of poisonous cases and availability of emergency drugs around the clock.


Subject(s)
Antidotes/supply & distribution , Attitude of Health Personnel , Clinical Competence , Emergency Medical Services , Health Knowledge, Attitudes, Practice , Health Services Accessibility , Poisoning/drug therapy , Tertiary Care Centers , Antidotes/administration & dosage , Clinical Competence/standards , Emergencies , Emergency Medical Services/standards , Guideline Adherence , Health Care Surveys , Health Services Accessibility/standards , Humans , Pakistan/epidemiology , Poisoning/diagnosis , Poisoning/epidemiology , Practice Guidelines as Topic , Tertiary Care Centers/standards
6.
Pak J Pharm Sci ; 28(6): 2001-7, 2015 Nov.
Article in English | MEDLINE | ID: mdl-26639477

ABSTRACT

Eczema is characterized by itching, lichenification, scaling, oedema and erythema. Current management strategies include corticosteroids, which are limited due to side effects. Many herbal remedies are used traditionally but unfortunately have not been validated in controlled clinical trials. Three popular traditional treatments of eczema include Indian pennywort, Walnut and Turmeric. In this study three topical formulations (micro emulsion, gel and ointment) were prepared from extracts of Indian pennywort, Walnut and Turmeric. These formulations were monitored for stability for a period of three months. Controlled clinical trials were conducted on 360 eczema patients. Clinical parameters observed were degree of erythema, oedema, scaling, itching and lichenification. Effects of each formulation on these clinical parameters were compared with placebo formulations. Micro emulsion formulations in all cases proved to be more effective in reducing semi quantitative scores of erythema and oedema. Itching was relieved more by gel formulation. The ointment showed more efficacy towards scaling and lichenification. Comparison of the effects of placebo and the specific formulations was performed by chi-square statistics and found to be highly significant. In summary it is concluded that all the formulations could be used as promising source for treatment of eczema.


Subject(s)
Centella , Curcuma , Dermatologic Agents/administration & dosage , Eczema/drug therapy , Juglans , Plant Extracts/administration & dosage , Administration, Cutaneous , Centella/chemistry , Chemistry, Pharmaceutical , Chi-Square Distribution , Curcuma/chemistry , Dermatologic Agents/chemistry , Double-Blind Method , Eczema/diagnosis , Emulsions , Female , Gels , Humans , Juglans/chemistry , Male , Ointments , Pakistan , Phytotherapy , Plant Extracts/chemistry , Plant Leaves , Plant Stems , Plants, Medicinal , Rhizome , Severity of Illness Index , Time Factors , Treatment Outcome
7.
Acta Pol Pharm ; 70(5): 873-5, 2013.
Article in English | MEDLINE | ID: mdl-24147366

ABSTRACT

The aim of this article was to assess and apply the in vitro to in vivo profiling (IVIVP), a new biowaiver approach, in designing a product with specific release pattern. The IVIVP was established by plotting the observed and predicted plasma drug concentrations. For IVIVP, convolution approach was employed to estimate plasma drug concentrations from in vitro dissolution profiles. The IVIVP for T1S exhibited a good correlation coefficient (R2 = 0.963) followed by the T2 (R2 = 0.682), T3 (R2 = 0.665), T1 (R2 = 0.616), and Mepresso (R2 = 0.345). Establishing an IVIVP, based on the convolution approach, can be more useful and practicable in the biowaiver studies, rather than present not useful practice of IVIVC estimated via deconvolution approach. This paper also elaborates that there is good correlation between the in vitro and in vivo profiles of the developed metoprolol tartrate formulations, particularly for T1S.


Subject(s)
Pharmaceutical Preparations/chemistry , Pharmacokinetics , Solubility , Adrenergic beta-Antagonists/chemistry , Adrenergic beta-Antagonists/pharmacokinetics , Algorithms , Computer Simulation , Drug Compounding , Excipients , Forecasting , Metoprolol/chemistry , Metoprolol/pharmacokinetics , Nanoparticles , Polymethacrylic Acids , Tablets
8.
Acta Pol Pharm ; 70(4): 597-600, 2013.
Article in English | MEDLINE | ID: mdl-23923383

ABSTRACT

Albumin is one of the most extensively studied endogenous proteins which are used in the fabrication of drug delivery and diagnostic technologies during last 10 years. This review provides a summary of products involving the use of albumin as a drug delivery tool for getting better the pharmacokinetics of a drug by developing the targetted drug delivery systems and diagnosing the pathologies. Using albumin, following market approved products have been developed: Levemir and Victoza (antidiabetic product), Abraxane (antimetastatic breast cancer product), and Nanocoll and Albures (for lymphoscintigraphy and diagnosis of cancer and rheumatoid arthritis).


Subject(s)
Albumins/administration & dosage , Drug Carriers , Albumin-Bound Paclitaxel , Albumins/chemistry , Animals , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/chemistry , Chemistry, Pharmaceutical , Glucagon-Like Peptide 1/administration & dosage , Glucagon-Like Peptide 1/analogs & derivatives , Glucagon-Like Peptide 1/chemistry , Humans , Hypoglycemic Agents/administration & dosage , Hypoglycemic Agents/chemistry , Insulin Detemir , Insulin, Long-Acting/administration & dosage , Insulin, Long-Acting/chemistry , Liraglutide , Paclitaxel/administration & dosage , Paclitaxel/chemistry , Predictive Value of Tests , Radiopharmaceuticals , Technetium Tc 99m Aggregated Albumin
9.
Pak J Pharm Sci ; 24(4): 421-6, 2011 Oct.
Article in English | MEDLINE | ID: mdl-21959800

ABSTRACT

Present study was designed to establish in-vitro and in-vivo correlation (IVIVC) of two immediate release tablet formulations of 400mg Norfloxacin [Drug A as test and Drug B as reference]. Dissolution study was conducted in 0.1 N HCl using USP apparatus II. In-vivo evaluation was carried out in 18 healthy humans according to a single dose, two-sequence, and cross-over randomized with a wash-out period of one week. After dosing, serial blood samples were collected for a period of 10 hours. Plasma harvested from blood, was analyzed for norfloxacin by a sensitive, reproducible and accurate HPLC method. Various pharmacokinetic parameters were determined from plasma concentrations for both the formulations. Non-significant difference was found for test/reference ratio of these parameters and the value of F was found to be 0.99 which is in good agreement with the limits given in FDA and WHO guidelines for such parameters. Difference factor (f(1)), similarity factor (f(2)) and level A IVIVC were evaluated showing that drug A is bioequivalent to drug B.


Subject(s)
Norfloxacin/administration & dosage , Norfloxacin/pharmacokinetics , Adolescent , Adult , Area Under Curve , Biological Availability , Chromatography, High Pressure Liquid , Cross-Over Studies , Humans , Male , Norfloxacin/blood , Tablets , Therapeutic Equivalency , Young Adult
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